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Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands.
Hewings DS, Fedorov O, Filippakopoulos P, Martin S, Picaud S, Tumber A, Wells C, Olcina MM, Freeman K, Gill A, Ritchie AJ, Sheppard DW, Russell AJ, Hammond EM, Knapp S, Brennan PE, Conway SJ. Hewings DS, et al. Among authors: conway sj. J Med Chem. 2013 Apr 25;56(8):3217-27. doi: 10.1021/jm301588r. Epub 2013 Apr 5. J Med Chem. 2013. PMID: 23517011 Free PMC article.
Bifunctional Molecules beyond PROTACs.
Conway SJ. Conway SJ. J Med Chem. 2020 Mar 26;63(6):2802-2806. doi: 10.1021/acs.jmedchem.0c00293. Epub 2020 Mar 11. J Med Chem. 2020. PMID: 32157887
Controlling Intramolecular Interactions in the Design of Selective, High-Affinity Ligands for the CREBBP Bromodomain.
Brand M, Clayton J, Moroglu M, Schiedel M, Picaud S, Bluck JP, Skwarska A, Bolland H, Chan AKN, Laurin CMC, Scorah AR, See L, Rooney TPC, Andrews KH, Fedorov O, Perell G, Kalra P, Vinh KB, Cortopassi WA, Heitel P, Christensen KE, Cooper RI, Paton RS, Pomerantz WCK, Biggin PC, Hammond EM, Filippakopoulos P, Conway SJ. Brand M, et al. Among authors: conway sj. J Med Chem. 2021 Jul 22;64(14):10102-10123. doi: 10.1021/acs.jmedchem.1c00348. Epub 2021 Jul 13. J Med Chem. 2021. PMID: 34255515 Free PMC article.
3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands.
Hewings DS, Wang M, Philpott M, Fedorov O, Uttarkar S, Filippakopoulos P, Picaud S, Vuppusetty C, Marsden B, Knapp S, Conway SJ, Heightman TD. Hewings DS, et al. Among authors: conway sj. J Med Chem. 2011 Oct 13;54(19):6761-70. doi: 10.1021/jm200640v. Epub 2011 Sep 6. J Med Chem. 2011. PMID: 21851057 Free PMC article.
Discovery and optimization of small-molecule ligands for the CBP/p300 bromodomains.
Hay DA, Fedorov O, Martin S, Singleton DC, Tallant C, Wells C, Picaud S, Philpott M, Monteiro OP, Rogers CM, Conway SJ, Rooney TP, Tumber A, Yapp C, Filippakopoulos P, Bunnage ME, Müller S, Knapp S, Schofield CJ, Brennan PE. Hay DA, et al. Among authors: conway sj. J Am Chem Soc. 2014 Jul 2;136(26):9308-19. doi: 10.1021/ja412434f. Epub 2014 Jun 19. J Am Chem Soc. 2014. PMID: 24946055 Free PMC article.
Epigenetics: novel therapeutics targeting epigenetics.
Conway SJ, Woster PM, Shen JK, Georg G, Wang S. Conway SJ, et al. J Med Chem. 2015 Jan 22;58(2):523-4. doi: 10.1021/jm501941q. Epub 2014 Dec 22. J Med Chem. 2015. PMID: 25532017 No abstract available.
Small molecule inhibitors of bromodomain-acetyl-lysine interactions.
Brand M, Measures AR, Wilson BG, Cortopassi WA, Alexander R, Höss M, Hewings DS, Rooney TP, Paton RS, Conway SJ. Brand M, et al. Among authors: conway sj. ACS Chem Biol. 2015 Jan 16;10(1):22-39. doi: 10.1021/cb500996u. ACS Chem Biol. 2015. PMID: 25549280 Review.
333 results