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Page 1
Small-molecule inhibition of METTL3 as a strategy against myeloid leukaemia.
Yankova E, Blackaby W, Albertella M, Rak J, De Braekeleer E, Tsagkogeorga G, Pilka ES, Aspris D, Leggate D, Hendrick AG, Webster NA, Andrews B, Fosbeary R, Guest P, Irigoyen N, Eleftheriou M, Gozdecka M, Dias JML, Bannister AJ, Vick B, Jeremias I, Vassiliou GS, Rausch O, Tzelepis K, Kouzarides T. Yankova E, et al. Among authors: blackaby w. Nature. 2021 May;593(7860):597-601. doi: 10.1038/s41586-021-03536-w. Epub 2021 Apr 26. Nature. 2021. PMID: 33902106 Free PMC article.
Targeting the m6A RNA modification pathway blocks SARS-CoV-2 and HCoV-OC43 replication.
Burgess HM, Depledge DP, Thompson L, Srinivas KP, Grande RC, Vink EI, Abebe JS, Blackaby WP, Hendrick A, Albertella MR, Kouzarides T, Stapleford KA, Wilson AC, Mohr I. Burgess HM, et al. Among authors: blackaby wp. Genes Dev. 2021 Jul 1;35(13-14):1005-1019. doi: 10.1101/gad.348320.121. Epub 2021 Jun 24. Genes Dev. 2021. PMID: 34168039 Free PMC article.
Inhibition of METTL3 Results in a Cell-Intrinsic Interferon Response That Enhances Antitumor Immunity.
Guirguis AA, Ofir-Rosenfeld Y, Knezevic K, Blackaby W, Hardick D, Chan YC, Motazedian A, Gillespie A, Vassiliadis D, Lam EYN, Tran K, Andrews B, Harbour ME, Vasiliauskaite L, Saunders CJ, Tsagkogeorga G, Azevedo A, Obacz J, Pilka ES, Carkill M, MacPherson L, Wainwright EN, Liddicoat B, Blyth BJ, Albertella MR, Rausch O, Dawson MA. Guirguis AA, et al. Among authors: blackaby w. Cancer Discov. 2023 Oct 5;13(10):2228-2247. doi: 10.1158/2159-8290.CD-23-0007. Cancer Discov. 2023. PMID: 37548590
Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma.
Wang X, Blackaby W, Allen V, Chan GKY, Chang JH, Chiang PC, Diène C, Drummond J, Do S, Fan E, Harstad EB, Hodges A, Hu H, Jia W, Kofie W, Kolesnikov A, Lyssikatos JP, Ly J, Matteucci M, Moffat JG, Munugalavadla V, Murray J, Nash D, Noland CL, Del Rosario G, Ross L, Rouse C, Sharpe A, Slaga D, Sun M, Tsui V, Wallweber H, Yu SF, Ebens AJ. Wang X, et al. Among authors: blackaby w. J Med Chem. 2019 Feb 28;62(4):2140-2153. doi: 10.1021/acs.jmedchem.8b01857. Epub 2019 Feb 20. J Med Chem. 2019. PMID: 30715878
Imidazo[1,2-a]pyrimidines as functionally selective and orally bioavailable GABA(A)alpha2/alpha3 binding site agonists for the treatment of anxiety disorders.
Goodacre SC, Street LJ, Hallett DJ, Crawforth JM, Kelly S, Owens AP, Blackaby WP, Lewis RT, Stanley J, Smith AJ, Ferris P, Sohal B, Cook SM, Pike A, Brown N, Wafford KA, Marshall G, Castro JL, Atack JR. Goodacre SC, et al. J Med Chem. 2006 Jan 12;49(1):35-8. doi: 10.1021/jm051065l. J Med Chem. 2006. PMID: 16392789
Probing Mechanisms of CYP3A Time-Dependent Inhibition Using a Truncated Model System.
Wang X, Sun M, New C, Nam S, Blackaby WP, Hodges AJ, Nash D, Matteucci M, Lyssikatos JP, Fan PW, Tay S, Chang JH. Wang X, et al. Among authors: blackaby wp. ACS Med Chem Lett. 2015 Jul 12;6(8):925-9. doi: 10.1021/acsmedchemlett.5b00191. eCollection 2015 Aug 13. ACS Med Chem Lett. 2015. PMID: 26288695 Free PMC article.
Optimization of Potent and Selective Ataxia Telangiectasia-Mutated Inhibitors Suitable for a Proof-of-Concept Study in Huntington's Disease Models.
Toledo-Sherman L, Breccia P, Cachope R, Bate JR, Angulo-Herrera I, Wishart G, Matthews KL, Martin SL, Cox HC, McAllister G, Penrose SD, Vater H, Esmieu W, Van de Poël A, Van de Bospoort R, Strijbosch A, Lamers M, Leonard P, Jarvis RE, Blackaby W, Barnes K, Eznarriaga M, Dowler S, Smith GD, Fischer DF, Lazari O, Yates D, Rose M, Jang SW, Muñoz-Sanjuan I, Dominguez C. Toledo-Sherman L, et al. Among authors: blackaby w. J Med Chem. 2019 Mar 28;62(6):2988-3008. doi: 10.1021/acs.jmedchem.8b01819. Epub 2019 Mar 19. J Med Chem. 2019. PMID: 30840447
Evaluation of 5-(Trifluoromethyl)-1,2,4-oxadiazole-Based Class IIa HDAC Inhibitors for Huntington's Disease.
Stott AJ, Maillard MC, Beaumont V, Allcock D, Aziz O, Borchers AH, Blackaby W, Breccia P, Creighton-Gutteridge G, Haughan AF, Jarvis RE, Luckhurst CA, Matthews KL, McAllister G, Pollack S, Saville-Stones E, Van de Poël AJ, Vater HD, Vann J, Williams R, Yates D, Muñoz-Sanjuán I, Dominguez C. Stott AJ, et al. Among authors: blackaby w. ACS Med Chem Lett. 2021 Feb 11;12(3):380-388. doi: 10.1021/acsmedchemlett.0c00532. eCollection 2021 Mar 11. ACS Med Chem Lett. 2021. PMID: 33738065 Free PMC article.
Discovery of a novel class of inhaled dual pharmacology muscarinic antagonist and β2 agonist (MABA) for the treatment of chronic obstructive pulmonary disease (COPD).
Rancati F, Linney ID, Rizzi A, Delcanale M, Knight CK, Schmidt W, Pastore F, Riccardi B, Mileo V, Carnini C, Cesari N, Blackaby WP, Patacchini R, Carzaniga L. Rancati F, et al. Among authors: blackaby wp. Bioorg Med Chem Lett. 2021 Jun 1;41:127975. doi: 10.1016/j.bmcl.2021.127975. Epub 2021 Mar 19. Bioorg Med Chem Lett. 2021. PMID: 33753262
26 results