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Page 1
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.
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.
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
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
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
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
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.
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