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Page 1
A Qualified Success: Discovery of a New Series of ATAD2 Bromodomain Inhibitors with a Novel Binding Mode Using High-Throughput Screening and Hit Qualification.
Bamborough P, Chung CW, Demont EH, Bridges AM, Craggs PD, Dixon DP, Francis P, Furze RC, Grandi P, Jones EJ, Karamshi B, Locke K, Lucas SCC, Michon AM, Mitchell DJ, Pogány P, Prinjha RK, Rau C, Roa AM, Roberts AD, Sheppard RJ, Watson RJ. Bamborough P, et al. Among authors: lucas scc. J Med Chem. 2019 Aug 22;62(16):7506-7525. doi: 10.1021/acs.jmedchem.9b00673. Epub 2019 Aug 9. J Med Chem. 2019. PMID: 31398032
Cellular Target Engagement Approaches to Monitor Epigenetic Reader Domain Interactions.
Phillipou AN, Lay CS, Carver CE, Messenger C, Evans JP, Lewis AJ, Gordon LJ, Mahmood M, Greenhough LA, Sammon D, Cheng AT, Chakraborty S, Jones EJ, Lucas SCC, Gatfield KM, Brierley DJ, Craggs PD. Phillipou AN, et al. Among authors: lucas scc. SLAS Discov. 2020 Feb;25(2):163-175. doi: 10.1177/2472555219896278. Epub 2019 Dec 25. SLAS Discov. 2020. PMID: 31875412 Free 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.
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
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
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
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
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
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.
16 results