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Page 1
Discovery, Optimization, and Biological Evaluation of Arylpyridones as Cbl-b Inhibitors.
Mfuh AM, Boerth JA, Bommakanti G, Chan C, Chinn AJ, Code E, Fricke PJ, Giblin KA, Gohlke A, Hansel C, Hariparsad N, Hughes SJ, Jin M, Kantae V, Kavanagh SL, Lamb ML, Lane J, Moore R, Puri T, Quinn TR, Reddy I, Robb GR, Robbins KJ, Gancedo Rodrigo M, Schimpl M, Singh B, Singh M, Tang H, Thomson C, Walsh JJ, Ware J, Watson IDG, Ye MW, Wrigley GL, Zhang AX, Zhang Y, Grimster NP. Mfuh AM, et al. Among authors: gohlke a. J Med Chem. 2024 Jan 25;67(2):1500-1512. doi: 10.1021/acs.jmedchem.3c02083. Epub 2024 Jan 16. J Med Chem. 2024. PMID: 38227216
Fragment screening at AstraZeneca: developing the next generation biophysics fragment set.
Lucas SCC, Börjesson U, Bostock MJ, Cuff J, Edfeldt F, Embrey KJ, Eriksson PO, Gohlke A, Gunnarson A, Lainchbury M, Milbradt AG, Moore R, Rawlins PB, Sinclair I, Stubbs C, Storer RI. Lucas SCC, et al. Among authors: gohlke a. RSC Med Chem. 2022 Jul 4;13(9):1052-1057. doi: 10.1039/d2md00154c. eCollection 2022 Sep 21. RSC Med Chem. 2022. PMID: 36324499 Free PMC article.
Discovery of a Novel Benzodiazepine Series of Cbl-b Inhibitors for the Enhancement of Antitumor Immunity.
Boerth JA, Chinn AJ, Schimpl M, Bommakanti G, Chan C, Code EL, Giblin KA, Gohlke A, Hansel CS, Jin M, Kavanagh SL, Lamb ML, Lane JS, Larner CJB, Mfuh AM, Moore RK, Puri T, Quinn TR, Ye M, Robbins KJ, Gancedo-Rodrigo M, Tang H, Walsh J, Ware J, Wrigley GL, Reddy IK, Zhang Y, Grimster NP. Boerth JA, et al. Among authors: gohlke a. ACS Med Chem Lett. 2023 Nov 17;14(12):1848-1856. doi: 10.1021/acsmedchemlett.3c00439. eCollection 2023 Dec 14. ACS Med Chem Lett. 2023. PMID: 38116444 Free PMC article.
Identification of Novel Potent NSD2-PWWP1 Ligands Using Structure-Based Design and Computational Approaches.
Carlino L, Astles PC, Ackroyd B, Ahmed A, Chan C, Collie GW, Dale IL, O'Donovan DH, Fawcett C, di Fruscia P, Gohlke A, Guo X, Hao-Ru Hsu J, Kaplan B, Milbradt AG, Northall S, Petrović D, Rivers EL, Underwood E, Webb A. Carlino L, et al. Among authors: gohlke a. J Med Chem. 2024 Jun 13;67(11):8962-8987. doi: 10.1021/acs.jmedchem.4c00215. Epub 2024 May 15. J Med Chem. 2024. PMID: 38748070
Identification and Evaluation of Reversible Covalent Binders to Cys55 of Bfl-1 from a DNA-Encoded Chemical Library Screen.
Lucas SCC, Blackwell JH, Börjesson U, Hargreaves D, Milbradt AG, Ahmed S, Bostock MJ, Guerot C, Gohlke A, Kinzel O, Lamb ML, Selmi N, Stubbs CJ, Su N, Su Q, Luo H, Xiong T, Zuo X, Bazzaz S, Bienstock C, Centrella PA, Denton KE, Gikunju D, Guié MA, Guilinger JP, Hupp C, Keefe AD, Satoh T, Zhang Y, Rivers EL. Lucas SCC, et al. Among authors: gohlke a. ACS Med Chem Lett. 2024 May 20;15(6):791-797. doi: 10.1021/acsmedchemlett.4c00113. eCollection 2024 Jun 13. ACS Med Chem Lett. 2024. PMID: 38894895
Fragment-Based Discovery of Novel MUS81 Inhibitors.
Collie GW, Börjesson U, Chen Y, Dong Z, Di Fruscia P, Gohlke A, Hoyle A, Hunt TA, Jesani MH, Luo H, Luptak J, Milbradt AG, Narasimhan P, Packer M, Patel S, Qiao J, Storer RI, Stubbs CJ, Tart J, Truman C, Wang AT, Wheeler MG, Winter-Holt J. Collie GW, et al. Among authors: gohlke a. ACS Med Chem Lett. 2024 Jun 7;15(7):1151-1158. doi: 10.1021/acsmedchemlett.3c00453. eCollection 2024 Jul 11. ACS Med Chem Lett. 2024. PMID: 39015284 Free PMC article.
Structure-Based Optimization of a Series of Covalent, Cell Active Bfl-1 Inhibitors.
Lucas SCC, Blackwell JH, Börjesson U, Hargreaves D, Milbradt AG, Bostock MJ, Ahmed S, Beaumont K, Cheung T, Demanze S, Gohlke A, Guerot C, Haider A, Kantae V, Kauffman GW, Kinzel O, Kupcova L, Lainchbury MD, Lamb ML, Leon L, Palisse A, Sacchetto C, Storer RI, Su N, Thomson C, Vales J, Chen Y, Hu X. Lucas SCC, et al. Among authors: gohlke a. J Med Chem. 2024 Sep 26;67(18):16455-16479. doi: 10.1021/acs.jmedchem.4c01288. Epub 2024 Sep 18. J Med Chem. 2024. PMID: 39291659
Structure-Based Discovery of a Series of Covalent, Orally Bioavailable, and Selective BFL1 Inhibitors.
Palisse A, Cheung T, Blokhuis A, Cogswell T, Martins BS, Riemens R, Schellekens R, Battocchio G, Jansen C, Cottee MA, Ornell K, Sacchetto C, Leon L, van Hoek-Emmelot M, Bostock M, Brauer BL, Beaumont K, Lucas SCC, Ahmed S, Blackwell JH, Börjesson U, Gohlke A, Gramatikov IMT, Hargreaves D, van Hoeven V, Kantae V, Kupcova L, Milbradt AG, Seneviratne U, Su N, Vales J, Wang H, White MJ, Kinzel O. Palisse A, et al. Among authors: gohlke a. J Med Chem. 2024 Dec 26;67(24):22055-22079. doi: 10.1021/acs.jmedchem.4c01995. Epub 2024 Dec 6. J Med Chem. 2024. PMID: 39641779
High throughput application of the NanoBiT Biochemical Assay for the discovery of selective inhibitors of the interaction of PI3K-p110α with KRAS.
Ismail M, Davies G, Sproat G, Monteverde T, Tart J, Acebrón-García-de-Eulate M, Gohlke A, Hancock D, Adhikari S, Stefanovic-Barrett S, Smith DM, Flemington V, Gleave-Hanford ES, Holdgate GA, Kettle JG, Downward J. Ismail M, et al. Among authors: gohlke a. SLAS Discov. 2024 Dec;29(8):100197. doi: 10.1016/j.slasd.2024.100197. Epub 2024 Nov 28. SLAS Discov. 2024. PMID: 39613028 Free article.
37 results