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Page 1
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: lucas scc. 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
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. 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
Design of a Lead-Like Cysteine-Targeting Covalent Library and the Identification of Hits to Cys55 of Bfl-1.
Lucas SCC, Milbradt AG, Blackwell JH, Bonomo S, Brierley A, Cassar DJ, Freeman J, Hadfield TE, Morrill LA, Riemens R, Sarda S, Schiesser S, Wiktelius D, Ahmed S, Bostock MJ, Börjesson U, De Fusco C, Guerot C, Hargreaves D, Hewitt S, Lamb ML, Su N, Whatling R, Wheeler M, Kettle JG. Lucas SCC, et al. J Med Chem. 2024 Jul 11;67(13):11209-11225. doi: 10.1021/acs.jmedchem.4c00781. Epub 2024 Jun 25. J Med Chem. 2024. PMID: 38916990
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. 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
Optimization of Potent Ligands for the E3 Ligase DCAF15 and Evaluation of Their Use in Heterobifunctional Degraders.
Lucas SCC, Ahmed A, Ashraf SN, Argyrou A, Bauer MR, De Donatis GM, Demanze S, Eisele F, Fusani L, Hock A, Kadamur G, Li S, Macmillan-Jones A, Michaelides IN, Phillips C, Rehnström M, Richter M, Rodrigo-Brenni MC, Shilliday F, Wang P, Storer RI. Lucas SCC, et al. J Med Chem. 2024 Apr 11;67(7):5538-5566. doi: 10.1021/acs.jmedchem.3c02136. Epub 2024 Mar 21. J Med Chem. 2024. PMID: 38513086
Covalent hits and where to find them.
Lucas SCC, Blackwell JH, Hewitt SH, Semple H, Whitehurst BC, Xu H. Lucas SCC, et al. SLAS Discov. 2024 Apr;29(3):100142. doi: 10.1016/j.slasd.2024.01.003. Epub 2024 Jan 24. SLAS Discov. 2024. PMID: 38278484 Free article. Review.
Exploration of piperidine 3D fragment chemical space: synthesis and 3D shape analysis of fragments derived from 20 regio- and diastereoisomers of methyl substituted pipecolinates.
Jones SP, Firth JD, Wheldon MC, Atobe M, Hubbard RE, Blakemore DC, De Fusco C, Lucas SCC, Roughley SD, Vidler LR, Whatton MA, Woolford AJ, Wrigley GL, O'Brien P. Jones SP, et al. Among authors: lucas scc. RSC Med Chem. 2022 Oct 11;13(12):1614-1620. doi: 10.1039/d2md00239f. eCollection 2022 Dec 14. RSC Med Chem. 2022. PMID: 36545433 Free PMC article.
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. 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.
Optimization of a Series of 2,3-Dihydrobenzofurans as Highly Potent, Second Bromodomain (BD2)-Selective, Bromo and Extra-Terminal Domain (BET) Inhibitors.
Lucas SCC, Atkinson SJ, Chung CW, Davis R, Gordon L, Grandi P, Gray JJR, Grimes T, Phillipou A, Preston AG, Prinjha RK, Rioja I, Taylor S, Tomkinson NCO, Wall I, Watson RJ, Woolven J, Demont EH. Lucas SCC, et al. J Med Chem. 2021 Aug 12;64(15):10711-10741. doi: 10.1021/acs.jmedchem.1c00344. Epub 2021 Jul 14. J Med Chem. 2021. PMID: 34260229 Free article.
25 results