Fairlie Group - Medicinal Chemistry and Pharmacology Research at Institute for Molecular Bioscience, The University of Queensland, Brisbane, Australia

Pharmacology

CHEMISTRY, BIOCHEMISTRY, PHARMACOLOGY, PROTEIN SURFACE MIMETICS, GPCR REGULATION, ENZYME REGULATION, ANTI-INFLAMMATORY RESEARCH, ANTI-INFECTIVES RESEARCH, ANTI-CANCER RESEARCH, NEURODEGENERATIVE RESEARCH, CARDIOVASCULAR RESEARCH FAIRLIE GROUP LABS, UNIVERSITY OF QUEENSLAND, BRISBANE, AUSTRALIA.

Our research on diseases involves basic, strategic and applied research in biochemistry and pharmacology directed at: (1) understanding how the immune system resolves infection (by parasites, viruses, bacteria) and tissue injury; (2) how prolonged inflammatory responses can cause debilitating chronic inflammatory diseases, including onset of cancers, metabolic diseases (obesity, type 2 diabetes, atherosclerosis, cardiovascular diseases), chronic inflammatory pain, and neurodegenerative diseases (e.g. Alzheimer's disease); and (3) how our novel compounds can act on human proteins, human and rodent cells and tissues, and rat or mouse models of human diseases. See links for our publications in all of these disease areas and allied chemical, biochemical and pharmacological research. Our interests include molecular pharmacology (studies of novel ligand interactions with cellular receptors, modulation of intracellular signalling pathways using experimental new drugs discovered in our labs, mechanisms of physiological responses and disease induction/progression) and experimental pharmacology (studies of drug-induced effects in rodent models of human diseases, interrogating molecular mechanisms in vivo, examining human tissues from the clinic). Our goal is to discover new drugs, mechanisms of drug action and understanding disease development and how to treat it.

Recent Publications (Pharmacology)

2023

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.

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.

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.

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, 11, e0046523.

2022

Landscaping macrocyclic peptides: stapling hDM2-binding peptides for helicity, protein affinity, proteolytic stability and cell uptake. de Araujo AD, Lim J, Wu KC, Hoang HN, Nguyen HT, Fairlie DP. RSC Chem Biol 2022, 3, 895-904.

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 Engl 2022, 61, e202203995.

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.

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 SR, Simpson F, Barnett TC, Johansson J, Dankers W, Harris J, Wells TJ, Kapetanovic R, Sweet MJ, Latomanski EA, Newton HJ, Guérillot RJR, Hachani A, Stinear TP, Ong SY, Chandran Y, Hartland EL, Kobe B, Stow JL, Sauer-Eriksson AE, Begun J, Kling JC, Blumenthal A. PLoS Pathog 2022, 18, e1010166.

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.

2021

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.

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.

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.

Activation of protease‐activated receptor 2 is associated with blood pressure regulation and proteinuria reduction in metabolic syndromeMaruyama‐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.

2020

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.

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.

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.

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.

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.

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. Sci Rep 2020, 10, 13579.

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.

2019

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.

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. Chem Commun (Camb) 2019, 55, 13362-13365.

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.

Protease-activated receptor 2 does not contribute to renal inflammation or fibrosis in the obstructed kidney. Ma FY, Han Y, Ozols E, Chew P, Vesey DA, Gobe GC, Morais C, Lohman RJ, Suen JY, Johnson DW, Fairlie DP, Nikolic-Paterson DJ. Nephrology (Carlton) 2019, 24, 983-991.

Diverse MR1-restricted T cells in mice and humans. Koay HF, Gherardin NA, Xu C, Seneviratna R, Zhao Z, Chen Z, Fairlie DP, McCluskey J, Pellicci DG, Uldrich AP, Godfrey DI. Nature Commun 2019, 10(1), 2243.

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 Immunol 2019, 4(41), eaaw0402.

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.

2018

A potent antagonist of protease-activated receptor 2 that inhibits multiple signaling 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.

Chemical approaches to modulating complement-mediated diseases. Iyer A, Xu W, Reid RC, Fairlie DP. J Med Chem 2018, 61, 3253-3276.

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 JYW, 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, 3(24), pii: 121697.

Enumeration, functional responses and cytotoxic capacity of MAIT cells in newly diagnosed and relapsed multiple myeloma. Gherardin NA, Loh L, Admojo L, Davenport AJ, Richardson K, Rogers A, Darcy PK, Jenkins MR, Prince HM, Harrison SJ, Quach H, Fairlie DP, Kedzierska K, McCluskey J, Uldrich AP, Neeson PJ, Ritchie DS, Godfrey DI. Sci Rep 2018, 8, 4159.

Mucosal-associated invariant T Cells augment immunopathology and gastritis 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.

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.

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 TSC, Chen Z. Nat Commun 2018, 9, 3350.

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.

2017

Exploiting a novel conformational switch to control innate immunity mediated by complement protein C3a. Lohman R-J, Hamidon JK, Reid RC, Rowley JA, Yau M-K, Halili MA, Nielsen DS, Lim J, Wu K-C, Loh Z, Do A, Suen JY, Iyer A, Fairlie DP. Nature Commun 2017, 8, 351.

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.

Biased signaling by agonists of protease activated receptor 2. Jiang Y, Yau M-K, Kok WM, Lim J, Wu K-C, 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 A, He Y, Yau MK, Hooper JD, Fairlie DP. Pharmacol Res 2017, 117, 328-342.

Orally Absorbed Cyclic Peptides. Nielsen DS, Shepherd NE, Xu W, Lucke AJ, Stoermer MJ, Fairlie DP. Chem Rev. 2017, 117, 8094-8128.

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.

Histone deacetylases (HDAC) in physiological and pathological bone remodelling. Cantley MD, Zannettino AC, Bartold PM, Fairlie DP, Haynes DR. Bone 2017, 95, 162-174.

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.

Drugs and drug-like molecules can modulate the function of mucosal-associated invariant T cells. Keller AN, Eckle SBG, Xu W, Liu L, Hughes VA, Mak JYW, Meehan B, Pediongco T, Birkinshaw RW, Chen Z, Wang H, D’Souza C, Kjer-Nielsen L, Gheradin NA, Godfrey DI, Kostenko L, Corbett AJ, Purcell AW, Fairlie DP*, McCluskey J*, Rossjohn J*. Nat Immunol 2017, 18, 402-411.

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 SBG, Meehan BS, Jackson DC, Strugnell RA, Cao H, Wang N, Fairlie DP, Liu L, Godfrey DI, Rossjohn J, McCluskey J, Corbett AJ. Mucosal Immunology 2017, 10, 58-68.

2016

Differential anti-inflammatory activity of low versus high dose HDAC inhibitors in human macrophages and collagen induced arthritis in rats. Lohman RJ, Iyer A, Fairlie TJ, Cotterell A, Gupta P, Reid RC, Vesey DA, Sweet MJ, 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.

Inhibition of membrane-anchored serine protease matriptase reduces experimental pulmonary fibrosis. Bardou O, François C, Menou A, Jvon der Thüsen J, Borie R, Castier Y, Sage E, Liu L, Fairlie DP, Königshoff M, Crestani B, Borensztajn K. American Journal of Respiratory and Critical Care Medicine, 2016, 193, 847-860.

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. Science Reports 2016, 6, 24575.

Truncated Glucagon-like Peptide-1 and Exendin-4 α-Conotoxin pl14a Peptide Chimeras Maintain Potency and α-Helicity and Reveal Interactions Vital for cAMP Signaling in Vitro. Swedberg JE, Schroeder CI, Mitchell JM, 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.

Histone deacetylase inhibitors promote mitochondrial reactive oxygen species production and bacterial clearance by human macrophages. Ariffin JK, das Gupta K, Kapetanovic R, Iyer A, Reid RC, Fairlie DP, Sweet MJ. Antimicrob Agents Chemother 2016, 60, 1521-1529.

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, Fairlie DP. ACS Med Chem Lett 2016, 7, 105–110.

PAR2 modulators derived from GB88. Yau MK, Liu L, Suen JY, Lim J, Lohman RJ, Cotterell AJ, Barry GD, Mak JYC, Vesey DA, Reid RC, Fairlie DP. ACS Med Chem Lett 2016, 7, 1179-1184.

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. [special issue on cyclic peptides]

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 Med Chem Lett 2016, 26, 986-991.

Helix nucleation by the smallest known alpha helix in water. Hoang HN, Driver RW, Beyer RL, Hill TA, de Araujo AD, Plisson F, Harrison RS, Goedecke L, Shepherd NE, Fairlie DP. Angew Chem Int Edit 2016, 55, 8275-8279.

Protease activated receptor 2 (PAR2) modulators: a patent review (2010-2015). Yau MK, Lim J, Liu L, Fairlie DP. Expert Opinion on Therapeutic Patents 2016, 26, 471-483.

Histone deacetylase inhibitors promote mitochondrial reactive oxygen species production and bacterial clearance by human macrophages. Ariffin JK, Iyer A, Reid RC, Fairlie DP, Sweet MJ. Antimicrobial Agents and Chemotherapy 2016, 60, 1521-1529.

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, 853-863.

2015

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.

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.

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.

Helix-constrained nociceptin peptides are potent agonists and antagonists of ORL-1 and nociception. Lohman RJ, Harrison RS, Ruiz-Gomez G, Hoang HN, Shepherd NE, Chow S, Hill TA, Madala PK, Fairlie DP. Vitamins and Hormones 2015, 97, 1-55.

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.

Functional heterogeneity and anti-mycobacterial effects of mouse mucosal associated invariant T (MAIT) cells specific for riboflavin metabolites. Sakala IG, Kjer-Nielsen L, Eickhoff CS, Wang X, Blazevic A, Liu L, Fairlie DP, Rossjohn J, McCluskey J, Hansen TH, Hoft DF. J Immunol 2015, 195, 587-601.

Identification of phenotypically and functionally heterogeneous mouse Mucosal Associated Invariant T cells using MR1 tetramers. Rahimpour A, Koay HF, Enders A, Clanchy R, Eckle SB, Meehan B, Chen Z, Whittle B, Liu L, Fairlie DP, Goodnow C, McCluskey J, Rossjohn J, Uldrich AP, Pellicci DG, Godfrey DI. J Exp Med 2015, 212, 1095-1108.

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.

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.

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.

2014

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.

Pathway Selective Antagonism Of Proteinase Activated Receptor 2. Suen JY, Cotterell A, Lohman RJ, Han A, Yau MK, Liu L, Cooper MA, Vesey DA, Fairlie DP. Br J Pharmacol 2014, 171, 4112-4124.

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.

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.

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.

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

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 [special issue on cyclic peptides].

Cyclic Penta- and Hexa- Leucine Peptides Without N-Methylation Are Orally Absorbed. Hill TA, 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.

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.

2013

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.

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.

Diet-Induced Obesity, Adipose Tissue Inflammation And Metabolic Dysfunction Correlating With PAR2 Expression Are Attenuated By A PAR2 Antagonist. Lim J, Iyer A, Suen JY, Liu L, Lohman RJ, Seow V, Yau MK, Brown L, Fairlie DP. FASEB J 2013, 27, 4757-4767.

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.

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, 25362-25372.

PAR2-induced inflammatory responses in human kidney tubular epithelial cells. Vesey DA, Suen JY, Seow V, Lohman RJ, Liu L, Gobe GC, Johnson DW, Fairlie DP. Am J Physiol Renal Physiol. 2013, 304, F737-F750.

Towards Drugs for Protease-Activated Receptor 2 (PAR2). Yau MK, Liu L, Fairlie DP. J Med Chem 2013, 56, 7477–7497.

An mRNA atlas of G protein-coupled receptor expression during primary human monocyte/macrophage differentiation and lipopolysaccharide-mediated activation identifies targetable candidate regulators of inflammation. Hohenhaus DM, Schaale K, Le Cao KA, Seow V, Iyer A, Fairlie DP, Sweet MJ. Immunobiology. 2013, 218, 1345-1353.

C5a, but not C5a-des Arg, induces upregulation of heteromer formation between complement C5a receptors C5aR and C5L2Croker DE, Halai R, Fairlie DP, Cooper MA. Immunol Cell Biol 2013, 91, 625-633.

The Future of Peptide-Based DrugsCraik DJ, Fairlie DP, Liras S, Price D. Chem Biol Drug Des 2013, 81, 136-147. ISI Highly Cited [>100 citations]

Recognition of vitamin B metabolites by mucosal-associated invariant T cellsPatel O, Kjer-Nielsen L, Le Nours J, Eckle SBG, Birkinshaw R, Beddoe T, Corbett AJ, Liu L, Miles JJ, Meehan B, Reantragoon R, Sandoval-Romero ML, Sullivan LC, Brooks AG, Chen Z, Fairlie DP, McCluskey J, Rossjohn J. Nature Communications 2013, 4, 2142. doi: 10.1038/ncomms3142.

2012

MR1 presents microbial vitamin 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(7426), 717-723. Faculty1000Prime Recommendation. ISI Highly Cited. [>100 citations]

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.

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.

Antagonism of protease-activated receptor 2 protects against experimental colitis. Lohman RJ, Cotterell AJ, Suen J, Liu L, Do AT, 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.

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.

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.

Lysine acetylation in obesity, diabetes and metabolic disease. Iyer A, Fairlie DP, Brown L. Immunol Cell Biol 2012, 90, 39-46.

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. [>100 citations]

Histone deacetylases as regulators of inflammation and immunity. Shakespear MR, Halili MA, Irvine KM, Fairlie DP, Sweet MJ. Trends Immunol. 2011, 32, 335-343. [>100 citations]

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.

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.

Inflammatory lipid mediators in adipocyte function and obesity. Iyer, A.; Fairlie, D. P.; Prins J.; Hammock B. D.; Brown, L. Nature Reviews Endocrinology 2010, 6, 71-82. [>100 citations]

Downsizing human, bacterial, and viral proteins to short water-stable alpha helices that maintain biological potency. Harrison RS, Shepherd NE, Hoang HN, Ruiz-Gómez G, Hill TA, Driver RW, Desai VS, Young PR, Abbenante G, Fairlie DP. Proc Natl Acad Sci U S A. 2010, 107, 11686-11691.

Novel Helix-Constrained Nociceptin Derivatives 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 RJ, Abbenante G, Hoang HN, Fairlie DP. J Med Chem 2010, 53, 8400-8408.

Selective hexapeptide agonists and antagonists for human complement C3a receptor. Scully CC, Blakeney JS, Singh R, Hoang HN, Abbenante G, Reid RC, Fairlie DP. J Med Chem 2010, 53, 4938-4948.

Novel agonists and antagonists for human protease activated receptor 2. Barry GD, Suen JY, Le GT, Cotterell A, Reid RC, Fairlie DP. J Med Chem 2010, 53, 7428-7440.

Over one hundred peptide-activated G protein-coupled receptors recognize ligands with turn structure. Ruiz-Gómez G, Tyndall JD, Pfeiffer B, Abbenante G, Fairlie DP. Chem Rev 2010, 110(4), PR1-41.

Histone deacetylase inhibitors in inflammatory disease. Halili MA, Andrews MR, Sweet MJ, Fairlie DP. Curr Top Med Chem 2009, 9, 309-319.[>100 citations]

Intravenous immunoglobulin (IVIG) protects the brain against experimental stroke by preventing complement-mediated neuronal cell death. Arumugam TV, Tang SC, Lathia JD, Cheng A, Mughal MR, Chigurupati S, Magnus T, Chan SL, Jo DG, Ouyang X,Fairlie DP, Granger DN, Vortmeyer A, Basta M, Mattson MP. Proc Natl Acad Sci USA 2007, 104, 14104-14109. [>100 citations]

Function, structure and therapeutic potential of complement C5a receptors. Monk PN, Scola AM, Madala P, Fairlie DP. Br J Pharmacol 2007, 152, 429-448. [>100 citations]

Protease-activated receptor-2 peptides activate neurokinin-1 receptors in the mouse isolated trachea. Abey HT, Fairlie DP, Moffatt JD, Balzary RW, Cocks TM. J Pharmacol Exp Ther 2006, 317, 598-605.

Therapeutic targets in inflammatory disease. Hume DA, Fairlie DP. Curr. Med. Chem. 2005, 12, 2925-2929.