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

new page under reconstruction

We discover and develop new experimental drugs for treatment of cancers and investigate new targets and mechanisms of action.

Publications on Cancer

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.

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.

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, Pizzolla A, Mak JYW, McCulloch TR, Souza-Fonseca-Guimaraes F, Kearney CJ, Millen R, Ramsay RG, Huntington ND, McCluskey J, Oliaro1 J, Fairlie DP, Neeson PJ, Godfrey DI, Beavis PA, Darcy PK. MAIT cells regulate NK cell mediated tumor immunity.

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, Politisc P, kid AR, Kokotos G. Synthesis of benzoxazole-based vorinostat analogs and their antiproliferative activity. Bioorg Chem 2021, in press.

Liu L, Dong L, Fairlie DP. Targeting class IIa HDACs: insights from phenotypes and inhibitors. Curr Med Chem 2021, in press.

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.