Anti-Cancer Research
CHEMISTRY, BIOCHEMISTRY, PHARMACOLOGY, PROTEIN SURFACE MIMETICS, GPCR REGULATION, ENZYME REGULATION, ANTI-INFLAMMATORY RESEARCH, ANTI-INFECTIVES RESEARCH, ANTI-CANCER RESEARCH, NEURODEGENERATIVE RESEARCH, CARDIOVASCULAR RESEARCH
Under Reconstruction
We discover and develop new experimental drugs for treatment of cancers and investigate new targets and mechanisms of action.
Publications on Cancer
Shah H, Fairlie DP, Lim J. Protease-activated receptor 2: A promising therapeutic target for women's cancers. J Pharmacol Exp Ther 2025, 392, 100016.
Boulouis C, Mouchtaridi E, Müller TR, Mak JYW, Fairlie DP, Bergman P, Michaëlsson J, Halfvarson J, Mjösberg J, Buggert M, Sandberg JK. Human MAIT cell response profiles biased toward IL-17 or IL-10 are distinct effector states directed by the cytokine milieu. Proc Natl Acad Sci U S A 2025, 122, e2414230122.
Awad W, Mayall JR, Xu W, Johansen MD, Patton T, Lim XY, Galvao I, Howson LJ, Brown AC, Haw TJ, Donovan C, Das S, Albers GJ, Pai TY, Hortle E, Gillis CM, Hansbro NG, Horvat JC, Liu L, Mak JYW, McCluskey J, Fairlie DP, Corbett AJ, Hansbro PM, Rossjohn J.Cigarette smoke components modulate the MR1-MAIT axis. J Exp Med 2025, 222, e20240896.
McInerney MP, Awad W, Souter MNT, Kang Y, Wang CJH, Chan Yew Poa K, Abdelaal MR, Le NH, Shepherd CM, McNeice C, Meehan LJ, Nelson AG, Raynes JM, Mak JYW, McCluskey J, Chen Z, Ang CS, Fairlie DP, Le Nours J, Illing PT, Rossjohn J, Purcell AW. MR1 presents vitamin B6-related compounds for recognition by MR1-reactive T cells. Proc Natl Acad Sci U S A 2024, 121, e2414792121.
Xu C, Obers A, Qin M, Brandli A, Wong J, Huang X, Clatch A, Fayed A, Starkey G, D'Costa R, Gordon CL, Mak JYW, Fairlie DP, Beattie L, Mackay LK, Godfrey DI, Koay HF. Selective regulation of IFN-γ and IL-4 co-producing unconventional T cells by purinergic signaling. J Exp Med 2024, 221, e20240354.
Shah H, Hill TA, Lim J, Fairlie DP. Protease-activated receptor 2 attenuates doxorubicin-induced apoptosis in colon cancer cells. J Cell Commun Signal 2023, 17, 1293-1307.
Wang Y, Abrol R, Mak JYW, Das Gupta K, Ramnath D, Karunakaran D, Fairlie DP, Sweet MJ. Histone deacetylase 7: a signalling hub controlling development, inflammation, metabolism and disease. FEBS J 2023, 290, 2805-2832.
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. N-(2-Aminophenyl)-benzamide inhibitors of class I HDAC enzymes with antiproliferative and antifibrotic Activity. J Med Chem 2023, 66, 14357-14376.
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. Differential location of NKT and MAIT cells within lymphoid tissue. Sci Rep 2022, 12, 4034.
Madden S, de Araujo AD, Gerhardt M, Fairlie DP, Mason JM. Taking the Myc out of cancer: Toward therapeutic strategies to directly inhibit c-Myc. Molecular Cancer 2021, 20, 3.
Petley EV, Koay HF, Henderson MA, Sek K, Todd KL, Keam SP, Lai J, House IG, Li J, Zethoven M, Chen AXY, Oliver AJ, Michie J, Freeman AJ, Giuffrida L, Chan JD, Pizzolla A, Mak JYW, McCulloch TR, Souza-Fonseca-Guimaraes F, Kearney CJ, Millen R, Ramsay RG, Huntington ND, McCluskey J, Oliaro J, Fairlie DP, Neeson PJ, Godfrey DI, Beavis PA, Darcy PK. MAIT cells regulate NK cell-mediated tumor immunity. Nat Commun 2021, 12, 4746.
Mak JYW, Liu L, Fairlie DP. Chemical Modulators of Mucosal Associated Invariant T Cells. Acc Chem Res 2021, 54, 3462-3475.
Jiang Y, Lim J, Wu KC, Xu W, Suen JY, Fairlie DP. PAR2 induces ovarian cancer cell motility by merging three signalling pathways to transactivate EGFR. Br J Pharmacol 2021, 178, 913-932.
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. HDAC7 inhibition by phenacetyl and phenylbenzoyl hydroxamates. J Med Chem 2021, 64, 2186-2204.
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. A nucleotide analog prevents colitis associated cancer via Β-catenin independently of inflammation and autophagy. Cell Mol Gastroenterol Hepatol 2021, 11, 33-53.
Mantzourania C, Gkikasc D, Kokotosc A, Nummelad P, Theodoropouloua M, Wu KC, Fairlie DP, Politis PK, Ristimäki A, Kokotos G. Synthesis of benzoxazole-based vorinostat analogs and their antiproliferative activity. Bioorg Chem 2021, 114, 105132.
Liu L, Dong L, Fairlie DP. Targeting class IIa HDACs: insights from phenotypes and inhibitors. Curr Med Chem 2021, 28, 8628-8672.
Morais C, Rajandram R, Blakeney JS, Iyer A, Suen JY, Johnson DW, Gobe GC, Fairlie DP, Vesey DA. Expression of protease activated receptor-2 is reduced in renal cell carcinoma biopsies and cell lines. PLoS One 2021, 16, e0248983.
Yan J, Allen S, McDonald E, Das I, Mak JYW, Liu L, Fairlie DP, Meehan BS, Chen Z, Corbett A, Varelias A, Smyth M, Teng MWL. MAIT cells promote tumor intiation, growth, and metastasis via tumor MR1. Cancer Discovery 2020, 10, 124-141.
Tng J, Lim J, Wu K-C, Lucke AJ, Xu W, Reid RC, Fairlie DP. Achiral derivatives of hydroxamate AR-42 potently inhibit class I HDAC enzymes and cancer cell proliferation. J Med Chem 2020, 63, 5956-5971.
de Araujo AD, Lim J, Wu K-C, Xiang Y, Good AC, Skerlj R, Fairlie DP. Bicyclic helical peptides as dual inhibitors selective for Bcl2A1 and Mcl-1 proteins. J Med Chem 2018, 61, 2962-2972.
Jiang Y, Yau MK, Lim J, Wu KC, Xu W, Suen JY, Fairlie DP. A potent antagonist of protease-activated receptor 2 that inhibits multiple signalling functions in human cancer cells. J Pharmacol Exp Ther 2018, 364, 246-257.
Iyer A, Xu W, Reid RC, Fairlie DP. Chemical approaches to modulating complement-mediated disease. J Med Chem 2018, 61, 3253-327
Gherardin NA, Loh L, Admojo L, Davenport AJ, Richardson K, Rogers A, Darcy PK, Jenkins MR, Trapani JA, Prince HM, Harrison SJ, Quach H, Fairlie DP, Kedzierska K, McCluskey J, Uldrich AP, Neeson PJ, Ritchie DS, Godfrey DI. Enumeration, functional responses and cytotoxic capacity of MAIT cells in newly diagnosed and relapsed myeloma. Science Reports 2018, 8, 4159.
Kim SH, Redvers RP, Chi LH, Ling X, Lucke AJ, Reid RC, Fairlie DP, Baptista Moreno Martin AC, Anderson RL, Denoyer D, Pouliot N. Identification of brain metastasis genes and therapeutic evaluation of histone deacetylase inhibitors in a clinically relevant model of breast cancer brain metastasis. Dis Model Mech 2018, 11(7), pii: DMM034850.
Vadrevu SK, Sharma SK, Chintala NK, Cho J-H, Patel J, Patel B, Fairlie DP, Paterson Y, Astrinidis A, Karbowniczek M, Markiewski MM. The ribosomal protein S19 suppresses antitumor immune responses via the complement C5a receptor 1. J Immunol 2017, 198, 2989-2999.
Baxter D, Perry S, Hill TA, Kok WM, Zaccai N, Brady R, Fairlie DP*, Mason J*. Downsizing protooncogene cFos to short helix-constrained peptides that bind Jun. ACS Chem Biol 2017, 12, 2051-2061.
de Araujo AD, Lim J, Good AC, Skerlj RT, Fairlie DP. Electrophilic helical peptides that bind covalently, irreversibly and selectively in a protein-protein interaction site. ACS Med Chem Lett 2017, 8, 22−26.
Ward A, Dong L, Harris JM, Khanna KK, Al-Ejeh F, Fairlie DP, Wiegmans AP, Liu L. Quinazolinone derivatives as inhibitors of homologous recombinase RAD51. Bioorg Med Chem Lett 2017, 27, 3096-3100.
Shepherd NE, Harrison RS, Ruiz-Gomez G, Abbenante G, Mason JM, Fairlie DP. Downsizing BAD BH3 peptide to small constrained α-helices with improved ligand efficiency. Org Biomol Chem 2016, 14, 10939–10945.
Philippe G, Huang YH, Cheneval O, Lawrence N, Zhang Z, Fairlie DP, Craik DJ, de Araujo AD, Henriques ST. Development of cell-penetrating peptide-based drug leads to inhibit MDMX:p53 and MDM2:p53 interactions. Peptide Science 2016, 106, 853-863.
Vadrevu SK, Chintala NK, Sharma SK, Sharma P, Cleveland C, Riediger L, Manne S, Fairlie DP, Gorczyca W, Almanza O, Karbowniczek M, Markiewski MM. Complement C5a receptor facilitates cancer metastasis by altering T cell responses in the metastatic niche. Cancer Research 2014, 74, 3454-3465.
Rao T, Ruiz-Gómez G, Hill TA, Hoang HN, Fairlie DP, Mason JM. Truncated and helix-constrained peptides with high affinity and specificity for the cFos coiled-coil of AP-1. PLoS One 2013, 8(3), e59415.
Kahnberg P, Lucke AJ, Glenn MP, Boyle GM, Tyndall JDA, Parsons PG, Fairlie DP. Design, synthesis, potency and cytoselectivity of anticancer agents derived by parallel synthesis from alpha-aminosuberic acid. J Med Chem 2006, 49, 7611-7622.
