Publications
List Publications
A novel inhibitor of class IIa histone deacetylases attenuates collagen-induced arthritis
Poon EK, Liu L, Wu KC, Lim J, Sweet MJ, Lohman RJ, Iyer A, Fairlie DP.
Br J Pharmacol. 2024 Sep 2. doi: 10.1111/bph.17306.
Varicella Zoster Virus disrupts MAIT cell polyfunctional effector responses
Purohit SK, Stern L, Corbett AJ, Mak JYW, Fairlie DP, Slobedman B, Abendroth A.
PLOS Pathogens 2024 Aug 7;20(8):e1012372.
MAIT cell activation and recruitment in inflammation and tissue damage in acute appendicitis
Zheng Y, Han F, Wu Z, Wang B, Chen X, Boulouis C, Jiang Y, Ho A, He D, Si WR, Mak JYW, Fairlie DP, Wang L-F, Sandberg JK, Lobie PE, Ma S, Leeansyah E.
Sci Adv. 2024 Jun 14;10(24):eadn6331.
Potent immunomodulators developed from an unstable bacterial metabolite of vitamin B2 biosynthesis
Mak JWY, Rivero RJD, Hoang HN, Lim XY, Deng J, McWilliam HEG,
Villadangos JA, McCluskey J, Corbett AJ, Fairlie DP.
Angew Chem Int Ed Engl 2024 Apr 28:e202400632.
doi: 10.1002/anie.202400632. Online ahead of print.
Sulfated bile acid is a host-derived ligand for MAIT cells.
Ito E, Inuki S, Izumi Y, Takahashi M, Dambayashi Y, Ciacchi L, Awad W, Takeyama A, Shibata K, Mori S, Mak JYW, Fairlie DP, Bamba T, Ishikawa E, Nagae M, Rossjohn J, Yamasaki S.
Science Immunol 2024, 9, eade6924.
Mouse mucosal-associated invariant T cell receptor recognition of MR1 presenting the vitamin B metabolite, 5-(2-oxopropylideneamino)-6-d-ribitylaminouracil.
Ciacchi L, Mak JWY, Le JP, Fairlie DP, McCluskey J, Corbett AJ, Rossjohn J, Awad W.
J Biol Chem 2024 Mar 25;300(5):107229.
doi: 10.1016/j.jbc.2024.107229. Online ahead of print.
Protease-activated receptor 2: a promising therapeutic target for women's cancers
Shah H, Fairlie DP, Lim J.
J Pharmacol Exp Ther, 2024, May 6, JPET-MR-2024-002176. doi: 10.1124/jpet.124.002176. Online ahead of print.
MAIT cell-MR1 reactivity is highly conserved across multiple divergent species.
Edmans MD, Connelley TK, Morgan S, Pediongco TJ, Jayaraman S, Juno JA, Meehan BS, Dewar PM, Maze EA, Roos EO, Paudyal B, Mak JYW, Liu L, Fairlie DP, Wang H, Corbett AJ, McCluskey J, Benedictus L, Tchilian E, Klenerman P, Eckle SBG.
J Biol Chem 2024 May 3:107338.
doi: 10.1016/j.jbc.2024.107338. Online ahead of print.
Wnt dose escalation during the exit from pluripotency identifies tranilast as a regulator of cardiac mesoderm.
Wu Z, Shen S, Mizikovsky D, Cao Y, Naval-Sanchez M, Tan SZ, Alvarez YD, Sun Y, Chen X, Zhao Q, Kim D, Yang P, Hill TA, Jones A, Fairlie DP, Pébay A, Hewitt AW, Tam PPL, White MD, Nefzger CM, Palpant NJ.
Dev Cell. 2024 Feb 9:S1534-5807(24)00039-X. doi: 10.1016/j.devcel.2024.01.019. Online ahead of print.PMID: 38354738
Dynamic MAIT cell recovery after severe COVID-19 is transient with signs of heterogeneous functional anomalies.
Kammann T, Gorin JB, Parrot T, Gao Y, Ponzetta A, Emgård J, Maleki KT, Sekine T, Rivera-Ballesteros O; Karolinska COVID-19 Study Group; Gredmark-Russ S, Rooyackers O, Skagerberg M, Eriksson LI, Norrby-Teglund A, Mak JYW, Fairlie DP, Björkström NK, Klin
J Immunol 2024, 212, 389-396.
N-(2-Aminophenyl)-benzamide inhibitors of class I HDAC enzymes with antiproliferative and antifibrotic activity.
Gerokonstantis DT, Mantzourani C, Gkikas D, Wu KC, Hoang HN, Triandafillidi I, Barbayianni I, Kanellopoulou P, Kokotos AC, Moutevelis-Minakakis P, Aidinis V, Politis PK, Fairlie DP, Kokotos G.
J Med Chem 2023, 66, 14357-14376.
HDAC7 is an immunometabolic switch triaging danger signals for engagement of antimicrobial versus inflammatory responses in macrophages.
Das Gupta K, Ramnath D, ....Kapetanovic R, Reid RC, Iyer A, ...Shakespear MR, Schembri MA, Fairlie DP, Sweet MJ.
Proc Natl Acad Sci U S A 2023, 120, e2212813120.
Talarolides revisited: Cyclic heptapeptides from an Australian marine tunicate-associated fungus, Talaromyces sp. CMB-TU011.
Salim AA, Hussein WM, Dewapriya P, Hoang HN, Zhou Y, Samarasekera K, Khalil ZG, Fairlie DP, Capon RJ.
Marine Drugs 2023, 21, 487.
Protease-activated receptor 2 attenuates doxorubicin-induced apoptosis in colon cancer cells.
Shah H, Hill TA, Lim J, Fairlie DP.
J Cell Commun Signal 2023, 17, 1293-1307.
Synthetic 5-amino-6-D-ribitylaminouracil paired with inflammatory stimuli facilitates MAIT cell expansion in vivo.
Nelson AG, Wang H, Dewar PM, Eddy EM, Li S, Lim XY, Patton T, Zhou Y, Pediongco TJ, Meehan LJ, Meehan BS, Mak JYW, Fairlie DP, Stent AW, Kjer-Nielsen L, McCluskey J, Eckle SBG, Corbett AJ, Souter MNT, Chen Z.
Front Immunol 2023, 14, 1109759.
Molecular insights into metabolite antigen recognition by mucosal-associated invariant T cells.
Awad W, Ciacchi L, McCluskey J, Fairlie DP, Rossjohn J.
Curr Opin Immunol 2023, 83, 102351.
Venom composition and bioactive RF-amide peptide toxins of the saddleback caterpillar, Acharia stimulea (Lepidoptera: Limacodidae).
Goudarzi MH, Eagles DA, Lim J, Biggs KA, Kotze AC, Ruffell AP, Fairlie DP, King GF, Walker AA.
Biochem Pharmacol 2023, 213, 115598.
Ras-related protein Rab5a regulates complement C5a receptor trafficking, chemotaxis, and chemokine secretion in human macrophages.
Wu KC, Condon ND, Hill TA, Reid RC, Fairlie DP, Lim J.
J Innate Immun 2023, 15, 468-484.
Suppression of MR1 by human cytomegalovirus inhibits MAIT cell activation.
Ashley CL, McSharry BP, McWilliam HEG, Stanton RJ, Fielding CA, Mathias RA, Fairlie DP, McCluskey J, Villadangos JA, Rossjohn J, Abendroth A, Slobedman B.
Front Immunol 2023, 14, 1107497.
Molecular insights into metabolite antigen recognition by mucosal-associated invariant T cells.
Awad W, Ciacchi L, McCluskey J, Fairlie DP, Rossjohn J.
Curr Opin Immunol 2023, 83, 102351.
Wollamide cyclic hexapeptides synergize with established and new tuberculosis antibiotics in targeting mycobacterium tuberculosis.
Rollo RF, Mori G, Hill TA, Hillemann D, Niemann S, Homolka S, Fairlie DP, Blumenthal A.
Microbiol Spectr 2023, 8, e0046523.
Effect of a protease-activated receptor-2 antagonist (GB88) on inflammation-related loss of alveolar bone in periodontal disease.
Francis N, Sanaei R, Ayodele BA, O'Brien-Simpson NM, Fairlie DP, Wijeyewickrema LC, Pike RN, Mackie EJ, Pagel CN.
J Periodontal Res 2023, 58, 544-552.
Histone deacetylase 7: a signalling hub controlling development, inflammation, metabolism and disease.
Wang Y, Abrol R, Mak JYW, Das Gupta K, Ramnath D, Karunakaran D, Fairlie DP, Sweet MJ.
FEBS J 2023, 290, 2805-2832.
Tuning electrostatic and hydrophobic surfaces of aromatic rings to enhance membrane association and cell uptake of peptides.
de Araujo AD, Hoang HN, Lim J, Mak JYW, Fairlie DP.
Angew Chem Int Ed 2022 61, e202203995.
Landscaping macrocyclic peptides: stapling hDM2-binding peptides for helicity, protein affinity, proteolytic stability and cell uptake.
de Aruajo AD, Lim J, Wu KC, Hoang HN, Nguyen HT, Fairlie DP.
RSC Chem Biol 2022 3, 895-904.
Helical structure in cyclic peptides: effect of N-methyl amides versus esters.
Wu C, Hoang HN, Hill TA, Lim J, Kok WM, Akondi K, Liu L, Fairlie DP.
Chem Commun 2022, 58, 12475-12478.
Modifying a hydroxyl patch in glucagon-like peptide 1 produces biased agonists with unique signaling profiles.
Wang P, Hill TA, Mitchell J, Fitzsimmons RL, Xu W, Loh Z, Suen JY, Lim J, Iyer A, Fairlie DP.
J Med Chem 2022, 65, 11759-11775.
Temporal perturbation of histone deacetylase activity reveals a requirement for HDAC1-3 in mesendoderm cell differentiation.
Sinniah E, Wu Z, Shen S, Naval-Sanchez M, Chen X, Lim J, Helfer A, Iyer A, Tng J, Lucke AJ, Reid RC, Redd MA, Nefzger CM, Fairlie DP, Palpant NJ.
Cell Rep 2022 39, 110818.
CD8 coreceptor engagement of MR1 enhances antigen responsiveness by human MAIT and other MR1-reactive T cells
Souter MNT, Awad W, Li S, Pediongco T, Meehan BS, Meehan L, Tian Z, Zhao Z, Wang H, Nelson A, Le Nours J, Khandokar Y, Pravena T, Wubben J, Lin J, Sullivan LC, Lovrecz G, Mak JYW, Liu L, Kostenko L, Kedzierska K, Corbett AJ, Kjer-Nielsen L, Fairlie DP, Br
J Exp Med 2022, 219, e20210828.
A specialized tyrosine-based endocytosis signal in MR1 controls antigen presentation to MAIT cells.
Lim HJ, Wubben JM, Garcia CP, Cruz-Gomez S, Deng J, Mak JYW, Hachani A, Anderson RJ, Painter GF, Goyette J, Amarasinghe SL, Ritchie ME, Roquilly A, Fairlie DP, Gaus K, Rossjohn J, Villadangos JA, McWilliam HEG.
J Cell Biol 2022, 221, e202110125.
Quantitative affinity measurement of small molecule ligand binding to Major Histocompatibility Complex class-I related protein 1 MR1.
Wang CJH, Awad W, Liu L, Mak JYW, Veerapen N, Illing PT, Purcell AW, Eckle SBG, McCluskey J, Besra GS, Fairlie DP, Rossjohn J, Le Nours J.
J Biol Chem 2022, 102714. doi: 10.1016/j.jbc.2022.102714.
Inhibition of the master regulator of Listeria monocytogenes virulence enables bacterial clearance from spacious replication vacuoles in infected macrophages.
Tran TT, Mathmann CD, Gatica-Andrades M, Rollo RF, Oelker M, Ljungberg JK, Nguyen TTK, Zamoshnikova A, Kummari LK, Wyer OJK, Irvine KM, Melo-Bolívar J, Gross A, Brown D, Mak JYW, Fairlie DP, Hansford KA, Cooper MA, Giri R, Schreiber V, Joseph S, Simpson
PloS Pathog 2022, 18, e1010166.
The balance of IL-12 and IL-23 determines the bias of MAIT1 versus MAIT17 responses during bacterial infection.
Wang H, Nelson AG, Wang B, Zhao Z, Lim XY, Shi M, Meehan LJ, Jia X, Kedzierska K, Meehan BS, Eckle SB, Souter MN, Pediongco TJ, Mak JY, Fairlie DP, McCluskey J, Wang Z, Corbett AJ, Chen Z.
Immunol Cell Biol 2022, 100, 547-561.
The histone deacetylase Hdac7 supports LPS-inducible glycolysis and Il-1β production in murine macrophages via distinct mechanisms.
Ramnath D, Das Gupta K, Wang Y, Abrol R, Curson JEB, Lim J, Reid RC, Mansell A, Blumenthal A, Karunakaran D, Fairlie DP, Sweet MJ.
J Leukoc Biol. 2022 111, 327-336.
Histone deacetylase 7: a signalling hub controlling development, inflammation, metabolism and disease
Wang Y, Abrol R, Mak, JYW, Das Gupta K, Ramnath D, Karunakaran D, Fairlie DP, and Sweet, MJ.
FEBS J 2022 doi:10.1111/febs.16437
QSAR classification models for prediction of hydroxamate histone deacetylase inhibitor activity against malaria parasites.
Hesping E, Chua MJ, Pflieger M, Qian Y, Dong L, Bachu P, Liu L, Kurz T, Fisher GM, Skinner-Adams TS, Reid RC, Fairlie DP.
ACS Infect Dis. 2022 8, 106-117.
Differential location of NKT and MAIT cells within lymphoid tissue.
Johnson DN, Ruan Z, Petley EV, Devi S, Holz LE, Uldrich AP, Mak JYW, Hor JL, Mueller SN, McCluskey J, Fairlie DP, Darcy PK, Beavis PA, Heath WR, Godfrey DI.
Chemical modulators of mucosal associated invariant T cells.
Mak JYW, Liu L, Fairlie DP.
Accounts of Chemical Research 2021, 54, 3462-3475.
Taking the Myc out of cancer: Toward therapeutic strategies to directly inhibit c-Myc.
S Madden, AD de Araujo, M Gerhardt, DP Fairlie, JM Mason
Molecular Cancer 2021, 20, 3.
Connecting hydrophobic surfaces in cyclic peptides increases membrane permeability.
Hoang HN, Hill TA, Fairlie DP.
Angew Chem Int Edit 2021, 60, 8385-8390.
Fortified coiled coils: enhancing mechanical stability with lactam or metal staples.
López-García P, de Araujo AD, Bergues-Pupo AE, Tunn I, Fairlie DP*, Blank KG*.
Angew Chem Int Edit 2021, 60, 232-236.
PAR2 induces ovarian cancer cell motility by merging three signalling pathways to transactivate EGFR.
Jiang Y, Lim J, Wu KC, Xu W, Suen JY, Fairlie DP.
Br J Pharmacol 2021, 178, 913-932.
HDAC7 inhibition by phenacetyl and phenylbenzoyl hydroxamates.
Mak JYW, Wu KC, Gupta PK, Barbero S, McLaughlin MG, Lucke AJ, Tng J, Lim J, Loh Z, Sweet MJ, Reid RC, Liu L, Fairlie DP.
J Med Chem 2021, 64, 2186-2204.
De novo macrocyclic peptides for inhibiting, stabilizing, and probing the function of the retromer endosomal trafficking complex.
Kai-En Chen, Qian Guo, Timothy A Hill, Yi Cui, Amy K Kendall, Zhe Yang, Ryan J Hall, Michael D Healy, Joanna Sacharz, Suzanne J Norwood, Sachini Fonseka, Boyang Xie, Robert C Reid, Natalya Leneva, Robert G Parton, Rajesh Ghai, David A Stroud, David P Fair
Science Advances 2021, 79, eabg4007.
MAIT cells regulate NK cell-mediated tumor immunity.
Petley EV, Koay HF, Henderson MA, Sek K, Todd KL, Keam SK, Lai J, House IG, Li J, Zehoven M, Chen AXY, Oliver AJ, Michie J, Freeman AJ, Giuffrida L, Chan JD, et al.
Nature Communications 2021,12, 4746.
Francisella tularensis induces Th1 like MAIT cells conferring protection against systemic and local infection.
Zhao Z, Wang H, Shi M, Zhu T, Pediongco T, Lim XY, Meehan BS, Nelson AG, Fairlie DP, Mak JYW, Eckle SBG, Moreira MdL, Tumpach C, Bramhall M, Williams CG, Lee HJ, Haque A, Evrard M, Rossjohn J, McCluskey J, Corbett AJ, Chen Z.
Nature Communications 2021,12, 4355.
Histone deacetylase inhibitor AR-42 and achiral analogues kill malaria parasites in vitro and in mice.
Chua MJ, Tng J, Hesping E, Fisher GM, Goodman CD, Skinner-Adams T, Do D, Lucke AJ, Reid RC, Fairlie DP, Andrews KT.
Int J Parasiol Drugs Drug Resist 2021, 17, 118-127.
Human MAIT cells respond to and suppress HIV-1.
Phetsouphanh C, Phalora P, Hackstein CP, ... Mak JY, Fairlie DP, Fidler S, Kelleher AD, Frater J, Klenerman P.
Targeting Class IIa HDACs: Insights from Phenotypes and Inhibitors.
Liu L, Dong L, Bourguet E, Fairlie DP.
Curr Med Chem 2021, 28, 8628-8672.
PAR2-induced tissue factor synthesis by primary cultures of human kidney tubular epithelial cells is modified by glucose availability.
Humphries TLR, Shen K, Iyer A, Johnson DW, Gobe GC, Nikolic-Paterson D, Fairlie DP, Vesey DA.
Int J Mol Sci 2021, 22, 7532.
Identification and phenotype of MAIT cells in cattle and their response to bacterial infections
Edmans MD, Connelley TK, Jayaraman S, Vrettou C, Vordermeier M, Mak JYW, Liu L, Fairlie DP, Maze EA, Chrun T, Klenerman P, Eckle SBG, Tchilian E, Benedictus L.
Front Immunol 2021, 12, 627173.
Synthesis of benzoxazole-based vorinostat analogs and their antiproliferative activity.
Mantzourania C, Gkikasc D, Kokotosc A, Nummelad P, Theodoropouloua M, Wu KC, Fairlie DP, Politisc P, Kid AR, Kokotos G.
Bioorg Chem 2021, 114, 105132.
Late-stage hydrocarbon conjugation and cyclization in synthetic peptides and proteins.
de Araujo AD, Nguyen HT, Fairlie DP.
ChemBioChem 2021, 22, 1784-1789.
Mechanotransduction activates RhoA in the neighbors of apoptotic epithelial cells to engage apical extrusion.
Duszyc K, Gomez GA, Lagendijk AK, Yau MK, Nanavati BN, Gliddon BN, Hall TE, Verma S, Hogan BM, Pitson SM, Fairlie DP, Parton RG, Yap AS.
Curr Biol 2021, 31, 1326-1336.e5.
Mucosal-associated invariant T cells effector function is an intrinsic cell property that can be augmented by the metabolic cofactor α-ketoglutarate.
Howson L, Li J, von Borstel A, Barugahare A, Mak J, Fairlie D, McCluskey J, Turner SJ, Davey M, Rossjohn J.
J Immunol 2021, 206, 1425-1435.
A nucleotide analog prevents colitis associated cancer via Β-catenin independently of inflammation and autophagy.
Sheng YH, Giri R, Davies J, Schreiber V, Alabbas S, Movva R, He Y, Wu A, Hooper J, McWhinney B, Oancea I, Kijanka G, Hasnain S, Lucke AJ, Fairlie DP, McGuckin MA, Florin TH, Begun J.
Cell Mol Gastroenterol Hepatol, 2021,11, 33-53.
Activation of protease‐activated receptor 2 is associated with blood pressure regulation and proteinuria reduction in metabolic syndrome
Maruyama‐Fumoto K, McGuire JJ, Fairlie DP, Shinozuka K, Kagota S.
Clin Exp Pharmacol Physiol 2021, 48, 211-220.
PAR2 activation on human kidney tubular epithelial cells induces tissue factor synthesis that enhances blood clotting.
Iyer A, Humphries TLR, Owens EP, Zhao K, Masci P, Johnson DW, Nikolic-Paterson D, Gobe G, Fairlie DP, Vesey DA.
Frontiers in Physiology, Renal and Epithelial Physiology 2021, 12, 615428.
Expression of protease activated receptor-2 is reduced in renal cell carcinoma biopsies and cell lines.
Morais C, Rajandram R, Blakeney JS, Iyer A, Suen JY, Johnson DW, Gobe GC, Fairlie DP, Vesey DA.
PLoS One 2021, 16, e0248983.
MAIT cells promote tumor initiation, growth, and metastases via tumor MR1.
Yan J, Allen S, McDonald E, Das I, Mak JYW, Liu L, Fairlie DP, Meehan BS, Chen Z, Corbett AJ, Varelias A, Smyth MJ, Teng MWL.
Cancer Discov 2020, 10, 124-141.
The molecular basis underpinning the potency and specificity of MAIT cell antigens.
Awad W, Ler G, Xu W, Keller AN, Mak JYW, Yi X, Lim J, Liu L, Eckle SBG, Le Nours J, McCluskey J, Corbett AJ, Fairlie DP*, Rossjohn J*.
Nat Immunol 2020, 21, 400-411.
Endoplasmic reticulum chaperones stabilize ligand-receptive MR1 molecules for efficient presentation of metabolite antigens.
McWilliam HEG, Mak JYW, Awad W, Zorkau M, Cruz-Gomez S, Lim HL, Yan Y, Wormald S, Dagley LF, Eckle SBG, Corbett AJ, Liu H, Li S, Reddiex SJJ, Mintern JD, Liu L, McCluskey J, Rossjohn J, Fairlie DP*, Villadangos JA*.
Proc Natl Acad Sci USA 2020, 117, 24974-24985.
Achiral derivatives of hydroxamate AR-42 potently inhibit class I HDAC enzymes and cancer cell proliferation.
Tng J, Lim J, Wu KC, Lucke AJ, Xu W, Reid RC, Fairlie DP.
J Med Chem 2020, 63, 5956-5971.
Potent thiophene antagonists of human complement C3a receptor with anti-inflammatory activity.
Rowley JA, Reid RC, Poon EKY, Wu KC, Lim J, Lohman RJ, Hamidon JK, Yau MK, Halili MA, Durek T, Iyer A, Fairlie DP.
J Med Chem 2020, 63, 529-541.
Protease-activated receptor-2 ligands reveal orthosteric and allosteric mechanisms of receptor inhibition.
Kennedy AJ, Sundström L, Geschwindner S, Poon EKY, Jiang Y, Chen R, Cooke R, Johnstone S, Madin A, Lim J, Liu Q, Lohman RJ, Nordqvist A, Fridén-Saxin M, Yang W, Brown DG, Fairlie DP, Dekker N.
Commun Biol 2020, 3(1), 782.
MR1-restricted T cells with MAIT-like characteristics are functionally conserved in the pteropid bat Pteropus alecto.
Leeansyah E, Hey YY, Sia WR, Ng JHJ, Gulam MY, Boulouis C, Zhu F, Ahn M, Mak JYW, Fairlie DP, Kwa ALH, Sandberg JK, Wang L-F.
iScience 2020, 23, 101876.
Systemic delivery of peptides by the oral route: Formulation and medicinal chemistry approaches.
Brayden DJ, Hill TA, Fairlie DP, Maher S, Mrsny RJ.
Adv Drug Deliv Rev, 2020, 157, 2-36.
Absence of mucosal-associated invariant T cells in a person with a homozygous point mutation in MR1
Howson LJ, Awadl W, von Borstell A,
Lim HJ, McWilliam HEG,Sandoval-Romero1 ML, Majumdar S, Hamzeh AR,
Andrews TD, McDermott DH, Murphy PM, LeNours J, Mak JYW, Liu L, Fairlie DP, McCluskey J, Villadangos JA, Cook MC, Turner SJ, Davey MS, Ojaimill S,
Science Immunology, 2020, 5(49), eabc9492.
Human MAIT cell cytolytic effector proteins synergize to overcome carbapenem resistance in Escherichia coli.
Boulouis C, Sia WR, Gulam MY, Teo JQM, Phan TK, Mak JYW, Fairlie DP, Poon IKH, Koh TH, Bergman P, Wang LF, Kwa ALH, Sandberg JK, Leeansyah E.
PLoS Biol 2020,18(6), e3000644.
Class IIa histone deacetylases drive toll-like receptor-inducible glycolysis and macrophage inflammatory responses via pyruvate kinase M2.
Das Gupta K, Shakespear MR, Curson JEB, Murthy AMV, Iyer A, Hodson MP, Ramnath D, Tillu VA, von Pein JB, Reid RC,..... Fairlie DP, Sweet MJ.
Cell Rep 2020, 30, 2712-2728.
Virus-mediated suppression of the antigen presentation molecule MR1.
McSharry BP, Samer C, McWilliam HEG, Ashley CL, Yee MB, Steain M, Liu L, Fairlie DP, Kinchington PR, McCluskey J, Abendroth A, Villadangos JA, Rossjohn J, Barry Slobedman B.
Cell Rep 2020, 30, 2948–2962.
High cell permeability does not predict oral bioavailability for analogues of cyclic heptapeptide sanguinamide A.
Nielsen DS, Lohman RJ, Hoang HN, Fairlie DP, Hill TA.
Aust J Chem, 2020, 73, 344-451
Atypical TRAV1-2- T cell receptor recognition of the antigen-presenting molecule MR1.
Awad W, Meermeier EW, Sandoval-Romero ML, Le Nours J, Worley AH, Null MD, Liu L, McCluskey J, Fairlie DP, Lewinsohn DM, Rossjohn J.
J Biol Chem 2020, 295, 14445-14457.
Artificially induced MAIT cells inhibit M. bovis BCG but not M. tuberculosis during in vivo pulmonary infection.
Yu H, Yang A, Derrick S, Mak JYW, Liu L, Fairlie DP, Cowley S.
Lipopolysaccharide promotes Drp1-dependent mitochondrial fission and associated inflammatory responses in macrophages.
Kapetanovic R, Afroz SF, Ramnath D, Lawrence G, Okada T, Curson J, de Bruin J, Fairlie DP, Schroder K, St John J, Blumenthal A, Sweet MJ.
Immunol Cell Biology 2020, 98, 528-539.
CXCL16 stimulates antigen-induced MAIT cell accumulation but trafficking during lung infection is CXCR6-independent.
Yu H, Yang A, Liu L, Mak JYW, Fairlie DP, Cowley S.
Front Immunol 2020, 11, 1773.
HDAC 1 and 2 inhibition suppresses cytokine production and osteoclast bone resorption in vitro.
Algate K, Haynes D, Fitzsimmons T, Romeo O, Wagner F, Holson E, Reid R, Fairlie DP, Bartold P, Cantley M.
J Cell Biochem, 2020, 121, 244-258.
Crystal structures of protein-bound cyclic peptides.
Malde A, Hill TA, Iyer A, Fairlie DP.
Chemical Reviews 2019,119, 9861−9914.
A novel long-range n to π* interaction secures the smallest known α-helix in water.
Hoang HN, Wu C, Hill TA, de Araujo AD, Bernhardt PV, Liu L, Fairlie DP.
Angew Chem Int Ed Engl 2019, 58, 18873-18877.
Twists or Turns: stabilising alpha vs beta turns in tetrapeptides.
Hoang HN, Hill TA, Ruiz-Gómez G, Diness F, Mason JM, Wu C, Abbenante G, Shepherd NE, Fairlie DP.
Chemical Science 2019, 10, 10595-10600.
Mirror image pairs of cyclic hexapeptides have different
oral bioavailabilities and metabolic stabilities.
Lohman RJ, Nielsen DS, Kok WM, Hoang HN, Hill TA, Fairlie DP.
Chemical Communications 2019, 55, 13362-13365.
A class of γδ T cell receptors recognize the underside of the antigen-presenting molecule MR1.
J Le Nours, NA Gherardin, SH Ramarathinam, W Awad, F Wiede, BS Gully, Y Khandokar, T Praveena, JM Wubben, JJ Sandow, Webb AI, A von Borstel, MT Rice, SJ Redmond, R Seneviratna, ML Sandoval-Romero, S Li, MN Souter, SBG Eckle, AJ Corbett, HH Reid, L Liu, DP
Science 2019, 366 (6472), 1522-1527.
IL-23 costimulates antigen-specific MAIT cell activation and enables vaccination against bacterial infection.
Wang H, Kjer-Nielsen L, Shi M, D'Souza C, Pediongco TJ, Cao H, Kostenko L, Lim XY, Eckle SBG, Meehan BS, Zhu T, Wang B, Zhao Z, Mak JYW, Fairlie DP, Teng MWL, Rossjohn J, Yu D, de St Groth BF, Lovrecz G, Lu L, McCluskey J, Strugnell RA, Corbett AJ, Chen Z
Science Immunology 2019, 4(41). pii: eaaw0402.
A divergent transcriptional landscape underpins the development and functional branching of MAIT cells.
Koay HF, Su S, Amann-Zalcenstein D, Daley SR, Comerford I, Miosge L, Whyte CE, Konstantinov IE, d'Udekem Y, Baldwin T, Hickey PF, Berzins SP, Mak JYW, Sontani Y, Roots CM, Sidwell T, Kallies A, Chen Z, Nüssing S, Kedzierska K, Mackay LK, McColl SR, Deeni
Science Immunology 2019, 4(41). pii: eaay6039.
Computer modelling and synthesis of deoxy and monohydroxy analogues of a ribitylaminouracil bacterial metabolite that potently activates human T cells.
Ler GJM, Xu W, Mak JYW, Liu L, Bernhardt PV, Fairlie DP.
Chemistry 2019, 25, 15594-15608.
Diverse MR1-restricted T cells in mice and humans.
Koay H-F, Gherardin NA, Xu C, Seneviratna R, Zhao Z, Chen Z, Fairlie DP, McCluskey J, Pellicci DG, Uldrich AP, Godfrey DI.
Nature Communications 2019, 10, 2243.
MAIT cells upregulate α4β7 in response to acute Simian Immunodeficiency Virus/Simian HIV infection but are resistant to peripheral depletion in pigtail macaques.
Juno JA, Wragg KM, Amarasena T, Meehan BS, Mak JYW, Liu L, Fairlie DP, McCluskey J, Eckle SBG, Kent SJ.
J Immunol. 2019, 202, 2105-2120.
Picture: ©JoshKellogPhotography
Inhibitors of class I histone deacetylases attenuate thioacetamide-induced liver fibrosis in mice by suppressing hepatic type 2 inflammation.
Loh Z, Fitzsimmons RL, Reid RC, Ramnath D, Clouston A, Gupta PK, Irvine KM, Powell EE, Schroder K, Stow JL, Sweet MJ, Fairlie DP,* Iyer A.*
Br J Pharmacol 2019,176, 3775-3790.
Pharmacological inhibition of protease-activated receptor-2 reduces crescent formation in rat nephrotoxic serum nephritis.
Han Y, Tian L, Ma F, Tesch G, Vesey DA, Gobe GC, Lohman RJ, Morais C, Suen JY, Fairlie DP, Nikolic-Paterson DJ.
Clin Exp Pharmacol Physiol 2019, 46, 456-464.
Oxazole-benzenesulfonamide derivatives inhibit HIV-1 reverse transcriptase interaction with cellular eEF1A and reduce viral replication.
Rawle DJ, Li D, Wu Z, Wang L, Choong M, Lor M, Reid RC, Fairlie DP, Harris J, Tachedjian G, Poulsen SA, Harrich D.
J Virol 2019, 93(12). e00239-19.
Alpha synuclein structure and Parkinson’s disease - lessons and emerging principles.
Meade RM, Fairlie DP, Mason JM.
Molecular Neurodegeneration 2019, 14, 29.
Structure-activity relationships of wollamide cyclic hexapeptides with activity against drug-resistant and Intracellular Mycobacterium tuberculosis.
Khalil ZG, Hill TA, De Leon Rodriguez LM, Lohman RJ, Hoang HN, Reiling N, Hillemann D, Brimble MA, Fairlie DP, Blumenthal A, Capon RJ.
Antimicrob Agents Chemother 2019, 63(3), e01773-18. doi: 10.1128/AAC.01773-18
Histone deacetylases 1 and 2 inhibition suppresses cytokine production and osteoclast bone resorption in vitro.
Algate K, Haynes D, Fitzsimmons T, Romeo O, Wagner F, Holson E, Reid R, Fairlie D, Bartold P, Cantley M.
J Cell Biochem 2019, doi: 10.1002/jcb.29137.
Recipient mucosal-associated invariant T cells control GVHD within the colon.
Varelias A, Bunting MD, Ormerod KL, Koyama M, Olver SD, Straube J, Kuns RD, Robb RJ, Henden AS, Cooper L, Lachner N, Gartlan KH, Lantz O, Kjer-Nielsen L, Mak JY, Fairlie DP, Clouston AD, McCluskey J, Rossjohn J, Lane SW, Hugenholtz P, Hill GR.
J Clin Invest 2018, 128, 1919-1936.
Complement C3a and C5a receptors promote GVHD by suppressing mitophagy in recipient dendritic cells.
Nguyen H, Kuril S, Bastian D, Kim J, Zhang M, Vaena SG, Dany M, Dai M, Heinrichs JL, Daenthanasanmak A, Iamsawat S, Schutt S, Fu J, Wu Y, Fairlie DP, Atkinson C, Ogretmen B, Tomlinson S, Yu XZ.
JCI Insight 2018, Dec 20;3(24). pii: 121697.
Chemical Approaches To Modulating Complement-Mediated Diseases.
Iyer A, Xu W, Reid RC, Fairlie DP.
J Med Chem 2018, 61, 3253-3276.
Bicyclic helical peptides as dual inhibitors selective for Bcl2A1 and Mcl-1 proteins.
de Araujo AD, Lim J, Wu KC, Xiang Y, Good AC, Skerlj R, Fairlie DP.
J Med Chem 2018, 61, 2962-2972.
MAIT cells protect against pulmonary Legionella longbeachae infection.
Wang H, D'Souza C, Lim XY, Kostenko L, Pediongco TJ, Eckle SBG, Meehan BS, Shi M, Wang N, Li S, Liu L, Mak JYW, Fairlie DP, Iwakura Y, Gunnersen JM, Stent AW, Godfrey DI, Rossjohn J, Westall GP, Kjer-Nielsen L, Strugnell RA, McCluskey J, Corbett AJ, Hinks
Nature Communications 2018, 9, 3350.
Hepatic expression profiling identifies steatosis-independent and steatosis-driven advanced fibrosis genes.
Ramnath D, Irvine KM, Lukowski SW, Horsfall LU, Loh Z, Clouston AD, Patel PJ, Fagan KJ, Iyer A, Lampe G, Stow JL, Schroder K, Fairlie DP, Powell JE, Powell EE, Sweet MJ.
JCI Insight 2018, 3(14), pii: 120274.
Lysine deacetylases and regulated glycolysis in macrophages.
Shakespear MR, Iyer A, Cheng CY, Das Gupta K, Singhal A, Fairlie DP, Sweet MJ.
Trends Immunol 2018, 39, 473-488.
Chemically diverse helix-constrained peptides using selenocysteine crosslinking.
Dantas de Araujo A, Perry SR, Fairlie DP.
Org Lett 2018, 20, 1453-1456.
Mucosal-associated invariant T cells augment immunopathology and gastritis in chronic Helicobacter pylori Infection.
D'Souza C, Pediongco T, Wang H, Scheerlinck JY, Kostenko L, Esterbauer R, Stent AW, Eckle SBG, Meehan BS, Strugnell RA, Cao H, Liu L, Mak JYW, Lovrecz G, Lu L, Fairlie DP, Rossjohn J, McCluskey J, Every AL, Chen Z, Corbett AJ.
J Immunol 2018, 200, 1901-1916.
Glucuronic acid as a helix-inducing linker in short peptides.
Wu C, Hoang HN, Liu L, Fairlie DP.
Chemical Communications 2018, 54, 2162-2165.
A potent antagonist of protease-activated receptor 2 that inhibits multiple signalling functions in human cancer cells.
Jiang Y, Yau MK, Lim J, Wu KC, Xu W, Suen JY, Fairlie DP.
J Pharmacol Exp Ther 2018, 364, 246-257.
Contiguous hydrophobic and charged surface patches in short helix-constrained peptides drive cell permeability.
Perry SR, Hill TA, de Araujo AD, Hoang HN, Fairlie DP.
Org Biomol Chem 2018, 16, 367-371.
Orally Absorbed Cyclic Peptides
Nielsen DS, Shepherd NE, Xu W, Lucke AJ, Stoermer MJ, Fairlie DP
Chemical Reviews 2017, 117, 8094-8128.
Exploiting a novel conformational switch to control innate immunity mediated by complement protein C3a.
Lohman RJ, Hamidon JK, Reid RC, Rowley JA, Yau MK, Halili MA, Nielsen DS, Lim J, Wu KC, Loh Z, Do A, Suen JY, Iyer A, Fairlie DP.
Nature Communications 2017, 8, 351.
Stabilising short-lived Schiff base derivatives of 5-aminouracils that activate mucosal-associated invariant T cells.
Mak JYW, Xu W, Reid RC, Corbett AJ, Meehan B, Wang H, Chen Z, Rossjohn J, McCluskey J, Liu L, Fairlie DP.
Nature Communications 2017, 8, 14599.
Drugs and drug-like molecules can modulate the function of mucosal-associated invariant T cells.
Keller AN, Eckle SB, Xu W, Liu L, Hughes VA, Mak JY, Meehan BS, Pediongco T, Birkinshaw RW, Chen Z, Wang H, D'Souza C, Kjer-Nielsen L, Gherardin NA, Godfrey DI, Kostenko L, Corbett AJ, Purcell AW, Fairlie DP*, McCluskey J*, Rossjohn J*.
Nature Immunology 2017, 18, 402-411.
Protease activated receptor 2 controls myelin development, resiliency and repair.
Yoon H, Radulovic M, Walters G, Paulsen AR, Drucker K, Starski P, Wu J, Fairlie DP, Scarisbrick IA.
Glia 2017, 65, 2070-2086.
Quinazolinone derivatives as inhibitors of homologous recombinase RAD51.
Ward A, Dong L, Harris JM, Khanna KK, Al-Ejeh F, Fairlie DP, Wiegmans AP, Liu L.
Bioorg Med Chem Lett 2017, 27, 3096-3100.
Europium-Labeled Synthetic C3a Protein as a Novel Fluorescent Probe for Human Complement C3a Receptor
Dantas de Araujo A, Wu C, Wu KC, Reid RC, Durek T, Lim J, Fairlie DP.
Bioconjug Chem 2017, 28, 1669-1676.
The Ribosomal Protein S19 Suppresses Antitumor Immune Responses via the Complement C5a Receptor 1.
Markiewski MM, Vadrevu SK, Sharma SK, Chintala NK, Ghouse S, Cho JH, Fairlie DP, Paterson Y, Astrinidis A, Karbowniczek M.
J Immunol 2017, 198, 2989-2999.
Biased signaling by agonists of protease activated receptor 2.
Jiang Y, Yau MK, Kok WM, Lim J, Wu KC, Liu L, Hill TA, Suen JY, Fairlie DP.
ACS Chem Biol 2017, 12, 1217-1226.
Mapping transmembrane residues of proteinase activated receptor 2 (PAR2) that influence ligand-modulated calcium signaling.
Suen JY, Adams MN, Lim J, Madala PK, Xu W, Cotterell AJ, He Y, Yau MK, Hooper JD, Fairlie DP.
Pharmacol Research 2017, 117, 328-342.
Total Synthesis of Mycobacterium tuberculosis Dideoxymycobactin-838 and Stereoisomers: Diverse CD1a-Restricted T Cells Display a Common Hierarchy of Lipopeptide Recognition.
Cheng JM, Liu L, Pellicci DG, Reddiex SJ, Cotton RN, Cheng TY, Young DC, Van Rhijn I, Moody DB, Rossjohn J, Fairlie DP*, Godfrey DI*, Williams SJ*.
Chemistry 2017, 23, 1694-1701.
Stereoelectronic effects on dienophile separation influence the Diels-Alder synthesis of molecular clefts.
Stoermer MJ, Wickramasinghe WA, Byriel KA, Hockless DCR, Skelton BW, Sobolev AN, White AH, Mak JYW, Fairlie DP.
Eur J Org Chem 2017, 6793–6796.
Downsizing Proto-oncogene cFos to short helix-constrained peptides that bind Jun.
Baxter D, Perry SR, Hill TA, Kok WM, Zaccai NR, Brady RI, Fairlie DP,* Mason JM*
ACS Chem Biol 2017, 12, 2051-2061.
Tolyporphin Macrocycles from the Cyanobacterium Tolypothrix nodosa Selectively Bind Copper and Silver and Reverse Multidrug Resistance.
Prinsep MR, Appleton TG, Hanson GR, Lane I, Smith CD, Puddick J, Fairlie DP.
Inorg Chem 2017, 56, 5577-5585.
Histone deacetylases (HDAC) in physiological and pathological bone remodelling.
Cantley MD, Zannettino AC, Bartold PM, Fairlie DP, Haynes DR.
Alpha Helix Nucleation by a Simple Cyclic Tetrapeptide
Hoang HN, Wu C, Beyer RL, Hill TA, Fairlie DP.
Aust J Chem 2017, 70, 213–219.
Mucosal-associated invariant T-cell activation and accumulation after in vivo infection depends on microbial riboflavin synthesis and co-stimulatory signals.
Chen Z, Wang H, D'Souza C, Sun S, Kostenko L, Eckle SB, Meehan BS, Jackson DC, Strugnell RA, Cao H, Wang N, Fairlie DP, Liu L, Godfrey DI, Rossjohn J, McCluskey J, Corbett AJ.
Mucosal Immunol 2017, 10, 58-68.
Receptor residence time trumps drug-likeness and oral bioavailability in determining efficacy of complement C5a antagonists.
Seow V, Lim J, Cotterell AJ, Yau MK, Xu W, Lohman RJ, Kok WM, Stoermer MJ, Sweet MJ, Reid RC, Suen JY, Fairlie DP.
Scientific Reports 2016, 6, 24575.
Electrophilic helical peptides that bond covalently, irreversibly and selectively in a protein-protein interaction site.
Dantas de Araujo A, Lim J, Good AC, Skerlj RT, Fairlie DP.
ACS Med Chem Lett 2017, 8, 22−26. [Featured Article]
An HDAC6 inhibitor confers protection and selectively inhibits B-cell infiltration in DSS-induced colitis in mice.
Do A, Reid RC, Lohman RJ, Sweet MJ, Fairlie DP*, Iyer A*.
J Pharmacol Exp Ther 2017, 360, 140-151.
Helix-constraints and amino acid substitution in GLP-1 increase cAMP and insulin secretion but not beta arrestin 2 signalling.
Plisson F, Hill TA, Mitchell JM, Hoang HN, de Araujo AD, Xu W, Cotterell A, Edmonds DJ, Stanton RV, Derksen DR, Loria PM, Griffith DA, Price DA, Liras S, Fairlie DP.
Eur J Med Chem 2017, 127, 703-714.
Helix Nucleation by the Smallest Known α-Helix in Water.
Hoang HN, Driver RW, Beyer RL, Hill TA, D de Araujo A, Plisson F, Harrison RS, Goedecke L, Shepherd NE, Fairlie DP.
Angew Chem Int Ed Engl 2016, 55, 8275-8279.
Downsizing the BAD BH3 peptide to small constrained α-helices with improved ligand efficiency.
Shepherd NE, Harrison RS, Ruiz-Gomez G, Abbenante G, Mason JM, Fairlie DP.
Org Biomol Chem 2016, 14, 10939–10945.
Potent Small Agonists of Protease Activated Receptor 2.
Yau MK, Suen JY, Xu W, Lim J, Liu L, Adams MN, He Y,
Hooper JD, Reid RC. and Fairlie DP.
ACS Med Chem Lett 2016, 7, 105-110.
PAR2 modulators derived from GB88
Yau MK, Liu L, Suen JY, Lim J, Lohman R-J, Jiang Y, Cotterel AJ, Barry GD, Mak JYW, Vesey DA, Reid RC. and Fairlie DP.
ACS Med Chem Lett 2016, 7, 1179–1184.
Benzylamide antagonists of protease activated receptor 2 with anti-inflammatory activity.
Yau MK, Liu L, Lim J, Lohman RJ, Cotterell AJ, Suen JY, Vesey DA, Reid RC, Fairlie DP.
Bioorg Chem Med Lett 2016, 26, 986-991.
The intracellular pathway for the presentation of vitamin B-related antigens by the antigen-presenting molecule MR1.
McWilliam HE, Eckle SB1, Theodossis A, Liu L, Chen Z, Wubben J, Fairlie DP, Strugnell RA, Mintern JD, McCluskey J, Rossjohn J, Villadangos JA.
Nature Immunology 2016, 17, 531-537.
A three-stage intrathymic development pathway for the mucosal-associated invariant T cell lineage.
Koay HF, Gherardin NA, Enders A, Loh L, Mackay LK, Almeida CF, Russ BE, Nold-Petry CA, Nold MF, Bedoui S, Chen Z, Corbett AJ, Eckle SB, Meehan B, d'Udekem Y, Konstantinov IE, Lappas M, Liu L, Goodnow CC, Fairlie DP, et al
Nature Immunology 2016, 17, 1300-1311.
Membrane-anchored Serine Protease Matriptase is a Trigger of Pulmonary Fibrogenesis.
Bardou O, Menou A, François C, Duitman JW, von der Thüsen JH, Borie R, Sales KU, Mutze K, Castier Y, Sage E, Liu L, Bugge TH, Fairlie DP, Königshoff M, Crestani B, Borensztajn KS.
Am J Respir Crit Care Med 2016, 193, 847-860.
Human mucosal-associated invariant T cells contribute
to antiviral influenza immunity via IL-18- dependent activation.
Loha L, Wanga Z, Santa S, Koutsakosa M, Jegaskandaa S, Corbetta AJ, Liu L, Fairlie DP, Crowed J, Rossjohn J, Xuh J, Doherty PC, McCluskey J, Kedzierska K.
Proc Natl Acad Sci 2016, 113, 10133-10138.
Differential Anti-inflammatory Activity of HDAC Inhibitors in Human Macrophages and Rat Arthritis
Lohman R-J, Iyer A, Fairlie TJ, Cotterell A, Gupta P, Reid RC, Vesey DA, Sweet MJ, and Fairlie DP.
J Pharmacol Exp Ther 2016, 356, 387-396.
Antagonism of the proinflammatory and pronociceptive actions of canonical and biased agonists of protease-activated receptor-2.
Lieu T, Savage E, Zhao P, Edgington-Mitchell L, Barlow N, Bron R, Poole DP, McLean P, Lohman RJ, Fairlie DP, Bunnett NW.
Br J Pharmacol 2016, 173, 2752-2765.
Product release is rate-limiting for catalytic processing by Dengue virus protease.
Shannon, AE, Pedroso MM, Chappell KJ, Watterson D, Liebscher S, Kok WM, Fairlie DP, Schenk G, Young PR.
Scientific Reports 2016, 6, 37539; doi: 10.1038/srep37539.
Development of cell-penetrating peptide-based drug leads to inhibit MDMX:p53 and MDM2:p53 interactions.
Philippe G, Huang YH, Cheneval O, Lawrence N, Zhang Z, Fairlie DP, Craik DJ, de Araujo AD, Henriques ST.
Biopolymers 2016, 106(6), 853-863. doi: 10.1002/bip.22893.
Simultaneous uncoupled expression and purification of the Dengue virus NS3 protease and NS2B co-factor domain.
Shannon AE, Chappell KJ, Stoermer MJ, Chow SY, Kok WM, Fairlie DP, Young PR.
Protein Exp Purif 2016, 119, 124-129.
Truncated glucagon-like peptide-1 and exendin-4 α-conotoxin pl14a peptide chimeras maintain potency, α-helicity and reveal interactions vital for cAMP signaling in vitro.
Swedberg JE, Schroeder CI, Mitchell J, Fairlie DP, Edmonds DJ, Griffith DA, Ruggeri RB, Derksen DR, Loria PM, Price DA, Liras S, Craik DJ.
J Biol Chem 2016, 291, 15778-15787.
Stapling peptides using cysteine crosslinking.
Fairlie DP, de Araujo AD.
Biopolymers 2016, 106(6), 843-852. doi: 10.1002/bip.22877.
Histone Deacetylase Inhibitors Promote Mitochondrial Reactive Oxygen Species Production and Bacterial Clearance by Human Macrophages
Ariffin JK, Gupta KD, Kapetanovic R, Iyer A, Reid RC, Fairlie DP. and Sweet MJ.
Antimicrobial Agents and Chemotherapy 2016, 60, 1521-1529.
Diversity of T Cells Restricted by the MHC Class I-Related Molecule MR1 Facilitates Differential Antigen Recognition
Gherardin NA, Keller AN, Woolley RE, Le Nours J, Ritchie DS, Neeson PJ, Birkinshaw RW, Eckle SBG, Waddington JN, Liu L, Fairlie DP, Uldrich AP, Pellicci DG, McCluskey J, Godfrey DI, Rossjohn J.
Immunity 2016, 44, 32-45. [ISI Highly Cited]
Protease activated receptor 2 (PAR2) modulators: a
patent review (2010-2015)
Yau M-K, Lim J, Liu L. & Fairlie DP.
Expert Opinion on Therapeutic Patents 2016, 471-483.
Histone deacetylases in monocyte/macrophage
development, activation and metabolism: refining
HDAC targets for inflammatory and infectious diseases
Gupta KD, Shakespear MR, Iyer A, Fairlie DP. and
Sweet MJ.
Clinical and Translational Immunology 2016, 5, e62.
Nutrient and immune sensing are obligate pathways in
metabolism, immunity, and disease.
Iyer A, Brown L, Whitehead JP, Prins JB, Fairlie DP.
FASEB J 2015, 29, 3612-3625.
Short hydrophobic peptides with cyclic constraints are potent glucagon-like peptide-1 receptor (GLP-1R) agonists.
Hoang HN, Song K, Hill TA, Derksen DR, Edmonds DJ, Kok WM, Limberakis C, Liras S, Loria PM, Mascitti V, Mathiowetz AM, Mitchell JM, Piotrowski DW, Price DA, Stanton RV, Suen JY, Withka JM, Griffith DA, Fairlie DP.
J Med Chem 2015, 58, 4080-4085.
Flexibility versus Rigidity for Orally Bioavailable Cyclic Hexapeptides
Nielsen DS, Lohman RJ, Hoang HN, Hill TA, Jones A, Lucke AJ, Fairlie DP.
ChemBioChem 2015, 16, 2289-2293.
Identification of phenotypically and functionally heterogeneous mouse mucosal-associated invariant T cells using MR1 tetramers
Rahimpour A, Koay HF, Enders A, Clanchy R,
Eckle SBG, Meehan B, Chen Z, Whittle B,
Liu L, Fairlie DP, Goodnow CC, McCluskey J,
Rossjohn J, Uldrich AP, Pellicci DG.
and Godfrey DI.
J Exp Med 2015, 212, 1095-1108.
Small Molecule Inhibitors of Disulfide Bond Formation by the Bacterial DsbA-DsbB Dual Enzyme System.
Halili MA, Bachu P, Lindahl F, Bechara C, Mohanty B, Reid RC, Scanlon MJ, Robinson CV, Fairlie DP, Martin JL.
ACS Chem Biol 2015, 10, 957–964.
Helix-Constrained Nociceptin Peptides Are Potent Agonists and Antagonists of ORL-1 and Nociception, in Nociceptin Opioid.
Lohman RJ, Harrison RS, Ruiz-Gómez GG, Hoang HN, Shepherd NE, Chow S, Hill TA, Madala PK, Fairlie DP.
Vitamins and Hormones 2015, 97, 1–55.
Functional Heterogeneity and Antimycobacterial Effects of Mouse Mucosal-Associated Invariant T Cells Specific for Riboflavin Metabolites.
Sakala IG, Kjer-Nielsen L, Eickhoff CS, Wang X, Blazevic A, Liu L, Fairlie DP,Rossjohn J, McCluskey J, Fremont DH, Hansen TH, Hoft DF.
J Immunol 2015, 195, 587-601.
Downsizing Proteins Without Losing Potency or Function
Fairlie DP, Yau MK, Hamidon JK, Singh R, Lim J, Suen JY, Rowley JA, Lohman RJ, Stoermer MJ, Iyer A, Reid RC.
Proc 24th Amer Peptide Symp (June 2015); Srivastava V, Yudin A, Lebl M (Eds); American Peptide Society 2015, 16-19. http://dx.doi.org/10.17952/24APS.2015.016
Potent complement C3a receptor agonists derived from oxazole amino acids: Structure-activity relationships.
Singh R, Reed AN, Chu P, Scully CC, Yau MK, Suen JY, Durek T, Reid RC, Fairlie DP.
Bioorg Med Chem Lett 2015, 25, 5604-5608.
Recognition of Vitamin B precursors and byproducts by Mucosal Associated Invariant T cells.
Eckle SB, Corbett AJ, Keller A, Chen Z, Godfrey DI, Liu L, Mak JY, Fairlie DP, Rossjohn J, McCluskey J.
J Biol Chem 2015, 290, 30204-30211.
Cyclic alpha-conotoxin peptidomimetic chimeras as potent GLP-1R agonists.
Swedberg JE, Schroeder CI, Mitchell JM, Durek T, Fairlie DP, Edmonds DJ, Griffith DA, Ruggeri RB, Derksen DR, Loria PM, Liras S, Price DA, Craik DJ.
Eur J Med Chem 2015, 103, 175-184.
Thiazoles in Peptides and Peptidomimetics
Mak JYW, Xu W, Fairlie DP
Topics in Heterocyclic Chemistry: “Heterocyclic Peptidomimetics” Chapter 1, 2015, 1-32. DOI: 10.1007/7081_2015_176.
Towards peptide-based inhibitors as therapies for Parkinson's disease
Mason JM, Fairlie DP
Future Medicinal Chemistry 2015, 7, 2103-2105.
Comparing Sixteen Scoring Functions for Predicting Biological Activities of Ligands for Protein Targets.
Xu W, Lucke AJ, Fairlie DP.
J Mol Graphics Modelling 2015, 57, 76-88.
Three homology models of PAR2 derived from different templates: application to antagonist discovery.
Perry SR, Xu W, Wirija A, Lim J, Yau MK, Stoermer MJ, Lucke AJ, Fairlie DP.
J Chem Info Model 2015, 55, 1181−1191.
Inhibiting Histone Deacetylase 1 (HDAC 1) Suppresses both Inflammation and Bone Loss in Arthritis.
Cantley MD, Fairlie DP, Bartold PM, Marino V, Gupta PK, Haynes DR.
Rheumatology 2015, 54, 1713-1723.
Peptide Inhibitors of the Escherichia coli DsbA Oxidative Machinery Essential for Bacterial Virulence.
Duprez W, Premkumar L, Halili MA, Lindahl F, Reid RC, Fairlie DP, Martin JL.
J Med Chem 2015, 58, 577-587.
Facile synthesis of mono- and bis-methylated Fmoc-Dap, -Dab and -Orn amino acids
Lindahl F, Hoang HN, Fairlie DP, Cooper MA.
Chem Commun 2015, 51, 4496-4498.
Virtual Screening of Peptide and Peptidomimetic Fragments Targeted to Inhibit Bacterial Dithiol Oxidase DsbA.
Duprez W, Bachu P, Stoermer MJ, Tay S, McMahon RM, Fairlie DP, Martin JL.
PLoS One 2015, 10(7), e0133805.
Profiling the anti-protozoal activity of anti-cancer HDAC inhibitors against Plasmodium and Trypanosoma parasites
Engel JA, Jones AJ, Avery VM, Sumanadasa SD, Ng SS, Fairlie DP, Adams TS, Andrews KT.
Int J Parasitol Drugs: Drug Resist 2015, 5, 117-126.
T cell activation by transitory neo-antigens derived from distinct microbial pathways.
Corbett AJ, Eckle SBG, Birkinshaw RW, Liu L, Patel O, Mahony J, Chen Z, Reantra-goon R, Meehan B, Cao H, Williamson NA, Strugnell RA, Sinderen DV, Mak JYW, Fairlie DP*, Lars Kjer-Nielsen*, Rossjohn J*, McCluskey J*.
Nature 2014, 509, 361-365. [ISI: Highly Cited Article]
Constraining Cyclic Peptides To Mimic Protein Structure Motifs.
Hill TA, Shepherd NE, Diness F, Fairlie DP.
Angew Chem Int Edit 2014, 53, 13020-13041.
Improving on Nature: Making a Cyclic Heptapeptide Orally Bioavailable.
Nielsen DS, Hoang HN, Lohman RJ, Hill TA, Lucke AJ, Craik DJ, Edmonds DJ, Griffith DA, Rotter CJ, Ruggeri RB, Price DA, Liras S, Fairlie DP.
Angew Chem Int Edit 2014, 53, 12059-12063.
Comparative α-Helicity of Cyclic Pentapeptides in Water.
de Araujo AD, Hoang HN, Kok WM, Diness F, Gupta G, Hill TA, Driver RW, Price DA, Liras S, Fairlie DP.
Angew Chem Int Edit 2014, 53, 6965-6969.
Stereoelectronic effects dictate molecular conformation and biological function of heterocyclic amides.
Reid RC, Yau MK; Singh R, Lim J, Fairlie DP.
J Am Chem Soc 2014, 136, 11914-11917. [Faculty1000Prime recommendation]
Rational design and synthesis of an orally bioavailable peptide guided by NMR amide temperature coefficients.
Wang CK, Northfield SE, Colless B, Chaousis D, Hamernig I, Lohman RJ, Nielsen DS, Schroeder CI, Liras S, Price DA, Fairlie DP, Craik DJ.
Proc Natl Acad Sci 2014, 111, 17504-17509.
A Molecular Basis Underpinning the T Cell Heterogeneity of Mucosal Associated Invariant T Cells.
Eckle SBG, Birkinshaw RW, Kostenko L, Corbett AJ, McWilliam HEG, Reantragoon R, Chen Z, Gherardin NA, Beddoe T, Liu L, Patel O, Meehan B, Fairlie DP, Villadangos JA, Godfrey DI, Kjer-Nielsen L, McCluskey J, Rossjohn J.
J Exp Med 2014, 211, 1585-1600.
Cyclic Penta- and Hexa- Leucine Peptides Without N-Methylation Are Orally Absorbed.
Hill T, Lohman RJ, Hoang HN, Nielsen DS, Scully CCG, Kok WM, Liu L, Lucke AJ, Stoermer MJ, Schroeder CI, Chaousis S, Colless B, Bernhardt PV, Edmonds DJ, Griffith DA, Rotter CJ, Ruggeri RB, Price DA, Liras S, Craik DJ, Fairlie DP.
ACS Med Chem Lett 2014, 5, 1148–1151. [Faculty1000Prime recommendation]
Potent Heterocyclic Ligands for Human Complement C3a Receptor.
Reid RC, Yau M-K, Singh R, Hamidon JK, Lim J, Stoermer MJ, Fairlie DP.
J Med Chem 2014, 57, 8459−8470.
Complement C5a receptor facilitates cancer metastasis by altering T cell responses in the metastatic niche
Vadrevu SK, Chintala NK, Sharma SK, Sharma P, Cleveland C, Riediger L, Manne S, Fairlie DP, Gorczyca W, Almanza O, Karbowniczek M, Markiewski MM
Cancer Research 2014, 74, 3454-3465.
Pathway Selective Antagonism Of Proteinase Activated Receptor 2.
Suen JY, Cotterell A, Lohman RJ, Lim J, Han A, Yau MK, Liu L, Cooper MA, Vesey DA, Fairlie DP.
Br J Pharmacol 2014, 171, 4112-4124.
Biased Signalling and Proteinase-Activated Receptors (PARs): Targeting Inflammatory Disease.
Hollenberg MD, Mihara K, Polley D, Suen JY, Han A, Fairlie DP, Ramachandran R.
Br J Pharmacol 2014, 171, 1180-1194. [ISI Highly Cited]
Crystal Structure of the Dithiol Oxidase DsbA Enzyme from Proteus Mirabilis Bound Non-Covalently to an Active Site Peptide Ligand.
Kurth F, Duprez W, Premkumar L, Schembri M, Fairlie DP, Martin JL.
J Biol Chem 2014, 289, 19810-19822.
Helical cyclic pentapeptides constrain HIV-1 Rev peptide for enhanced RNA binding.
Harrison RS, Shepherd NE, Hoang HN, Beyer RL, Ruiz-Gómez G, Kelso MJ, WM Kok, TA Hill, Abbenante G, Fairlie DP.
Tetrahedron 2014, 70, 7645-7650.
Lysine acetylation in sexual stage malaria parasites is a target for antimalarial small molecules.
Trenholme K, Marek L, Duffy S, Pradel G, Fisher G, Hansen FK, Skinner-Adams TS, Butterworth A, Julius Ngwa C, Moecking J, Goodman CD, McFadden GI, Sumanadasa SD, Fairlie DP, Avery VM, Kurz T, Andrews KT.
Antimicrob Agents Chemother 2014, 58, 3666-3678.
C5aR and C5L2 act in concert to balance immunometabolism in adipose tissue.
Poursharifi P, Lapointe M, Fisette A, Lu H, Roy C, Munkonda MN, Fairlie DP, Cianflone K.
Molecular and Cellular Endocrinology 2014, 382, 325-333.
C5aR and C3aR antagonists each inhibit diet-induced obesity, metabolic dysfunction, and adipocyte and macrophage signaling.
Lim J, Iyer A, Suen JY, Seow V, Reid RC, Brown L, Fairlie DP.
FASEB J 2013, 27, 822-831.
Diet-induced obesity, adipose inflammation, and metabolic dysfunction correlating with PAR2 expression are attenuated by PAR2 antagonism.
Lim J, Iyer A, Liu L, Suen JY, Lohman RJ, Seow V, Yau MK, Brown L, Fairlie DP.
FASEB J 2013, 27, 4757-4767.
Downsizing a Human Inflammatory Protein to a Small Molecule with Equal Potency and Functionality.
Reid RC, Yau M-K, Singh R, Hamidon JK, Reed AN, Chu P, Suen JY, Stoermer MJ, Blakeney JS, Lim J, Faber JM, Fairlie DP.
Nature Communications 2013, 4, 2802. doi: 10.1038/ncomms3802.
The Future of Peptide-Based Drugs.
David J. Craik, David P. Fairlie, Spiros Liras and David Price.
Chem Biol Drug Des 2013, 81, 136-147. [ISI Highly Cited] [ISI Hot Paper]
Inflammatory responses induced by lipopolysaccharide are amplified in primary human monocytes but suppressed in macrophages by complement protein C5a.
Seow V, Lim J, Iyer A, Suen JY, Ariffin JK, Hohenhaus DM, Sweet MJ, Fairlie DP.
J Immunol 2013, 191, 4308-4316.
Towards Drugs for Protease-Activated Receptor 2 (PAR2).
Yau MK, Liu L, Fairlie DP.
J Med Chem 2013, 56, 7477–7497.
Histone deacetylase 7 promotes Toll-like Receptor 4-dependent pro-inflammatory gene expression in macrophages.
Shakespear MR, Hohenhaus DM, Kelly GM, Kamal NA, Gupta P, Labzin LI, Schroder K, Garceau V, Barbero S, Iyer A, Hume DA, Reid RC, Irvine KM, Fairlie DP, Sweet MJ.
J Biol Chem 2013, 288, 25362-25374.
Antigen-loaded MR1 tetramers define T cell receptor heterogeneity in Mucosal-Associated Invariant T-cells.
Reantragoon R, Corbett AJ, Sakala IG, Gherardin NA, Furness JB, Birkinshaw R, Chen Z, Patel O, Kostenko L, Meehan B, Eckle SBG, Kedzierska K, Pellicci D, Liu L, Fairlie DP, Godfrey DI, Hansen TH, Kjer-Nielsen L, Rossjohn J, McCluskey J.
J Exp Med 2013, 210, 2305-2320. [ISI Highly Cited]
Recognition of vitamin B metabolites by mucosal-associated invariant T cells.
Patel O, Kjer-Nielsen L, Nours JL, Eckle SBG, Bikinshaw R, Beddoe T, Corbett AJ, Liu L, Miles JJ, Mehan B, Reantragoon R, Sandoval-Romero ML, Sullivan LC, Brooks AG, Chen Z, Fairlie DP, McCluskey J, Rossjohn J.
Nature Commun 2013, 4, 2142. doi: 10.1038/ncomms3142.
Efficient chemical synthesis of human complement protein C3a.
Artin Ghassemian,zy Ching-I Anderson Wang,y Mei-Kwan Yau, Robert C. Reid, Richard J. Lewis, David P. Fairlie, Paul F. Alewood and Thomas Durek.
Chem Commun 2013, 49, 2356-2358.
Rv2969c, essential for optimal growth in Mycobacterium tuberculosis, is a DsbA-like enzyme that interacts with VKOR-derived peptides and has atypical features of DsbA-like disulfide oxidases.
Premkumar L, Heras B, Duprez W, Walden P,
Halili M, Kurth F, Fairlie DP, Martin JL.
Acta Crystallogr D Biol Crystallogr 2013, D69, 1981–1994.
An interaction between the methyltransferase and RNA dependent RNA polymerase domains of the West Nile virus NS5 protein.
Tan CS, Hobson-Peters JM, Stoermer MJ, Fairlie DP, Khromykh AA, Hall RA.
J Gen Virol 2013, 94, 1961-1971.
Truncated and helix-constrained peptides with high affinity and specificity for the cFos coiled-coil of AP-1.
Rao T, Ruiz-Gómez G, Hill TA, Hoang HN, Fairlie DP, Mason JM.
PLoS One 2013, 8(3), e59415.
Identification and characterization of bi-thiazole-2,2′-diamines as kinase inhibitory scaffolds.
Kevin R.W. Ngoei, Dominic C.H. Ng, Paul R. Gooley, David P. Fairlie, Martin J. Stoermer, Marie A. Bogoyevitch.
Biochimica et Biophysica Acta, 2013, 1834, 1077-1088.
C5a, but not C5a-des Arg, induces upregulation of heteromer formation between complement C5a receptors C5aR and C5L2.
Croker DE, Halai R, Fairlie DP, Cooper MA.
Immunol Cell Biol. 2013, 91, 625-633.
The α-Proteobacteria Wolbachia pipientis Protein Disulfide Machinery Has a Regulatory Mechanism Absent in γ-Proteobacteria
Walden PM, Halili MA, Archbold JK, Lindahl F, Fairlie DP, Inaba K, Martin JL
PLOS One 2013, 8 (11), e81440.
PAR2-induced inflammatory responses in human kidney tubular epithelial cells.
David A. Vesey, Jacky Y. Suen, Vernon Seow, Rink-Jan Lohman, Ligong Liu, Glenda C. Gobe, David W. Johnson, and David P. Fairlie.
Am J Physiol Renal Physiol, 2013, 304, F737-F750.
MR1 presents microbial vitamin B metabolites to MAIT cells.
Kjer-Nielsen L, Patel O, Nours JL, Meehan B, Corbett AJ, Liu L, Bhati M, Chen Z, Kostenko L, Reantragoon R, Williamson NA, Purcell AW, Dudek NL, McConville MJ, O’Hair RAJ, Khairallah GN, Godfrey DI, Fairlie DP, Rossjohn J, McCluskey J.
Nature 2012, 491, 717-723. [Faculty1000Prime recommendation] [ISI Highly Cited]
Catalyst-Free N-arylation Using Unactivated Fluorobenzenes.
Diness F, Fairlie DP.
Angew. Chem. Int. Edit. 2012, 51, 8012-8016.
Total Synthesis, Structure, and Oral Absorption of a Thiazole Cyclic Peptide, Sanguinamide A.
Nielsen DS, Hoang HN, Lohman RJ, Diness F, Fairlie DP.
Org Lett. 2012, 14, 5720–5723.
An antagonist of human protease activated receptor-2 attenuates PAR2 signaling, macrophage activation, mast cell degranulation, and collagen-induced arthritis in rats.
Lohman RJ, Cotterell AJ, Barry GD, Liu L, Suen JY, Vesey DA, Fairlie DP.
FASEB J. 2012, 26, 2877-2887.
An inhibitor of pla2g2a modulates adipocyte signaling and protects against diet-induced metabolic syndrome in rats.
Iyer A, Lim J, Poudyal H, Reid RC, Suen JY, Webster J, Prins JB, Whitehead JP, Fairlie DP*, Brown L*.
Diabetes 2012, 61(9), 2320-2329.
Towards Histone Deacetylase Inhibitors as New Antimalarial Drugs.
Andrews KT, Tran TN, Fairlie DP.
Current Pharmaceutical Design 2012, 18, 3467-79.
Antagonism of protease activated receptor 2 protects against experimental colitis.
Lohman RJ, Cotterell AJ, Suen JY, Liu L, Do TA, Vesey DA, Fairlie DP.
J Pharmacol Exp Ther. 2012, 340, 256-265.
Modulating Human Proteinase Activated Receptor 2 With A Novel Antagonist (GB88) and Agonist (GB110)
Suen JY, Barry GD, Lohman RJ, Halili MA, Cotterell AJ, Le GT, Fairlie DP.
Br J Pharmacol. 2012, 165, 1413-1423.
Targeting quorum sensing and competence stimulation for antimicrobial chemotherapy.
Shepherd NE, Harrison RS, Fairlie DP.
Current Drug Targets 2012, 13(11), 1348-1359.
Anti-malarial activity of the anti-cancer HDAC inhibitor SB939.
Sumanadasa SD, Goodman CD, Lucke AJ, Skinner-Adams T, Sahama I, Haque A, Do TA, McFadden GI, Fairlie DP, Andrews KT.
Antimicrob Agents Chemother. 2012, 56, 3849-3856.
Matching cavities in G protein-coupled receptors to infer ligand-binding sites.
Madala PK, Fairlie DP, Boden M.
J. Chem. Inf. Model. 2012, 52, 1401-1410.
Comparative Gene Expression Profiling of P. falciparum Malaria Parasites Exposed to Three Different Histone Deacetylase Inhibitors.
Andrews KT, Gupta AP, Tran TN, Fairlie DP, Gobert GN, Bozdech Z.
PLoS One, 2012, 7, e31847
Folding pentapeptides into left and right handed alpha helices
Hoang, HN, Abbenante G, Hill TA, Ruiz-Gomez G, Fairlie DP
Tetrahedron, 2012, 68, 4513–4516.
C5a Receptor (CD88) Inhibition Improves Hypothermia-induced Neuroprotection in an In Vitro Ischemic Model
Thundyil J, Pavlovski D, Hsieh YH, Gelderblom M, Magnus T, Fairlie DP, Arumugam, TV.
Neuromolecular Med. 2012, 14, 30-39.
HDACs and their Inhibitors in Immunology: Teaching Anticancer Drugs New Tricks.
Fairlie DP, Sweet MJ.
Immunol Cell Biol, 2012, 90, 3-5.
Lysine Acetylation in Obesity, Diabetes and Metabolic Disease.
Iyer A, Fairlie DP, Brown L.
Immunol Cell Biol. 2012, 90, 39-46.
HDAC inhibitors: modulating leukocyte differentiation, survival, proliferation and inflammation.
Sweet MJ, Shakespear MR, Kamal NA, Fairlie DP.
Immunol Cell Biol. 2012, 90, 14-22.
Structures of Peptide Agonists for Human Protease Activated Receptor 2
Stoermer MJ, Flanagan B, Beyer RL , Madala PK, Fairlie DP.
Chemical Biology Down Under.
Fairlie DP.
Current Topics in Medicinal Chemistry 2012, 12(14), 1469-1470.
Towards Isozyme-Selective HDAC Inhibitors For Interrogating Disease.
Gupta P, Reid RC, Iyer A, Sweet MJ, Fairlie DP.
Current Topics in Medicinal Chemistry 2012, 12(14), 1479-1499.
Histone deacetylase inhibitors as suppressors of bone destruction in inflammatory diseases.
Cantley MD, Bartold PM, Fairlie DP, Rainsford KD, Haynes DR.
J. Pharm. Pharmacol. 2012, 64, 763-774.
Protein α-Turns Recreated in Structurally Stable Small Molecules.
Hoang HN, Driver RW, Beyer RL, Malde AK, Le GT, Abbenante G, Mark AE, Fairlie DP.
Angew. Chem. Int. Ed. Engl. 2011, 50, 11107-11111.
Synthesis of the Thiazole-Thiazoline Fragment of Largazole Analogues.
Diness F, Nielsen DS, Fairlie DP.
J. Org. Chem. 2011, 76, 9845-9851.
Inhibitors of Histone
Deacetylases in Class I and Class II
Suppress Human Osteoclasts
In Vitro
Cantley MD, Fairlie DP, Bartold PM, Rainsford KD, Le GT, Lucke AJ, Holding CA, Haynes DR
J. Cellular Physiology, 2011, 226, 3233-3241.
Ex Vivo Activity of Histone Deacetylase Inhibitors against Multidrug-Resistant Clinical Isolates of Plasmodium falciparum and P. vivax.
Marfurt J, Chalfein F, Prayoga P, Wabiser F, Kenangalem E, Piera KA, Fairlie DP, Tjitra E, Anstey NM, Andrews KT, Price RN.
Antimicrob Agents Chemother. 2011, 55, 961-966.
Histone deacetylase inhibitors and periodontal bone loss
Cantley MD, Bartold PM, Marino V, Fairlie DP, Le GT, Lucke AJ, Haynes DR.
Journal of Periodontal Research 2011, 46, 697–703.
Structure, function and pathophysiology of protease activated receptors.
Adams MN, Ramachandran R, Yau MK, Suen JY, Fairlie DP, Hollenberg MD, Hooper JD.
Pharmacol Ther 2011, 130, 248-282. [ISI Highly Cited]
Amyloid Formation from an α-Helix Peptide Bundle Is Seeded by 310-Helix Aggregates.
Singh Y, Sharpe PC, Hoang HN, Lucke AJ, McDowall AW, Bottomley SP, Fairlie DP.
Chemistry Eur. J. 2011, 17, 151-160. ["Very Important Paper" Category]
Inflammatory lipid mediators in adipocyte function and obesity.
Abishek Iyer, David P. Fairlie, Johannes B. Prins, Bruce D. Hammock and Lindsay Brown.
Nature Reviews Endocrinology 2010, 6, 71-82.
Downsizing human, bacterial, and viral proteins to short water-stable alpha helices that maintain biological potency.
Harrison RS, Shepherd NE, Hoang HN, Ruiz-Gomez G, Hill TA, Driver RW, Desai VS, Young PR, Abbenante G, Fairlie DP.
Proc. Natl. Acad. Sci 2010, 107, 11686-11691.
Novel Helix-Constrained Nociceptin Derivates Are Potent Agonists and Antagonists of ERK Phosphorylation and Thermal Analgesia in Mice.
Harrison RS, Ruiz-Gómez G, Hill TA, Chow SY, Shepherd NE, Lohman R-J, Abbenante G, Hoang HN, Fairlie DP.
J. Med. Chem. 2010, 53, 8400–8408.
Novel Agonists and Antagonists for Human Protease Activated Receptor 2 (PAR2).
Barry GD, Suen JY, Le GT, Cotterell A, Reid RC, Fairlie DP.
J. Med. Chem. 2010, 53, 7428-7440.
Non-covalent tripeptidylbenzyl and cyclohexyl amine inhibitors of the cysteine protease caspase-1.
Löser R, Abbenante G, Madala PK, Halili M, Le GT, Fairlie DP.
J. Med. Chem. 2010, 53, 2651-2655.
Selective Hexapeptide Agonists and Antagonists for Human Complement C3a Receptor.
Scully CCG, Blakeney JS, Singh R, Hoang, HN, Abbenante G, Reid RC, Fairlie DP.
J. Med. Chem. 2010, 53, 4938-4948.
Inhibitors Selective For HDAC6 In Enzymes and Cells.
Gupta PK, Reid RC, Liu L, Lucke AJ, Broomfield SA, Andrews MR, Sweet MJ, Fairlie DP.
Bioorg. Med. Chem. Lett. 2010, 20, 7067-7070.
Antimalarial Histone Deacetylase Inhibitors Containing Cinnamate or NSAID Components.
Wheatley NC, Andrews KT, Tran TL, Lucke AJ, Reid RC, Fairlie DP.
Bioorg. Med. Chem. Lett. 2010, 20, 7080-7084.
Update 1 of: Over One Hundred Peptide-Activated G Protein-Coupled Receptors Recognize Ligands with Turn Structure.
Gloria Ruiz-Gómez, Joel D. A. Tyndall, Bernhard Pfeiffer, Giovanni Abbenante and David P. Fairlie.
Chemical Reviews, 2010, 110(4), PR1-PR41.
Update 1 of: Beta-Strand Mimetics.
Loughlin WA, Tyndall JD, Glenn MP, Hill TA, Fairlie DP.
Chemical Reviews 2010, 110(6), PR32-PR69.
Update 1 of: Proteases Universally Recognize Beta Strands in their active sites.
Madala PK, Tyndall JD, Nall T, Fairlie DP.
Chemical Reviews 2010, 110(6), PR1-PR31.
Profiling gene expression induced by protease-activated receptor 2 (PAR2) activation in human kidney cells.
Suen JY, Gardiner B, Grimmond S, Fairlie DP.
PLoS One 2010, 5, e13809.
Differential effects of selective HDAC inhibitors on macrophage inflammatory responses to the Toll-like receptor 4 agonist LPS.
Halili MA, Andrews MR, Labzin LI, Schroder K, Matthias G, Cao C, Lovelace E, Reid RC, Le GT, Hume DA, Irvine KM, Mathias P, Fairlie DP, Sweet MJ.
J Leukoc Biol. 2010, 87, 1103-1114.
Antifibrotic activity of an inhibitor of histone deacetylases in DOCA-salt hypertensive rats.
Iyer A, Fenning A, Lim J, Le GT, Reid RC, Halili MA, Fairlie DP, Brown L.
Br J Pharmacol. 2010, 159, 1408-1417.
