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LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor.
Clark PG, Vieira LC, Tallant C, Fedorov O, Singleton DC, Rogers CM, Monteiro OP, Bennett JM, Baronio R, Müller S, Daniels DL, Méndez J, Knapp S, Brennan PE, Dixon DJ. Clark PG, et al. Among authors: bennett jm. Angew Chem Int Ed Engl. 2015 May 18;54(21):6217-21. doi: 10.1002/anie.201501394. Epub 2015 Apr 13. Angew Chem Int Ed Engl. 2015. PMID: 25864491 Free PMC article.
Discovery of a Chemical Tool Inhibitor Targeting the Bromodomains of TRIM24 and BRPF.
Bennett J, Fedorov O, Tallant C, Monteiro O, Meier J, Gamble V, Savitsky P, Nunez-Alonso GA, Haendler B, Rogers C, Brennan PE, Müller S, Knapp S. Bennett J, et al. J Med Chem. 2016 Feb 25;59(4):1642-7. doi: 10.1021/acs.jmedchem.5b00458. Epub 2015 May 20. J Med Chem. 2016. PMID: 25974391 Free PMC article.
8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors.
Bavetsias V, Lanigan RM, Ruda GF, Atrash B, McLaughlin MG, Tumber A, Mok NY, Le Bihan YV, Dempster S, Boxall KJ, Jeganathan F, Hatch SB, Savitsky P, Velupillai S, Krojer T, England KS, Sejberg J, Thai C, Donovan A, Pal A, Scozzafava G, Bennett JM, Kawamura A, Johansson C, Szykowska A, Gileadi C, Burgess-Brown NA, von Delft F, Oppermann U, Walters Z, Shipley J, Raynaud FI, Westaway SM, Prinjha RK, Fedorov O, Burke R, Schofield CJ, Westwood IM, Bountra C, Müller S, van Montfort RL, Brennan PE, Blagg J. Bavetsias V, et al. Among authors: bennett jm. J Med Chem. 2016 Feb 25;59(4):1388-409. doi: 10.1021/acs.jmedchem.5b01635. Epub 2016 Jan 7. J Med Chem. 2016. PMID: 26741168 Free PMC article.
Mapping the chemical chromatin reactivation landscape identifies BRD4-TAF1 cross-talk.
Sdelci S, Lardeau CH, Tallant C, Klepsch F, Klaiber B, Bennett J, Rathert P, Schuster M, Penz T, Fedorov O, Superti-Furga G, Bock C, Zuber J, Huber KV, Knapp S, Müller S, Kubicek S. Sdelci S, et al. Nat Chem Biol. 2016 Jul;12(7):504-10. doi: 10.1038/nchembio.2080. Epub 2016 May 9. Nat Chem Biol. 2016. PMID: 27159579
LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor.
Clark PG, Vieira LC, Tallant C, Fedorov O, Singleton DC, Rogers CM, Monteiro OP, Bennett JM, Baronio R, Müller S, Daniels DL, Méndez J, Knapp S, Brennan PE, Dixon DJ. Clark PG, et al. Among authors: bennett jm. Angew Chem Weinheim Bergstr Ger. 2015 May 18;127(21):6315-6319. doi: 10.1002/ange.201501394. Epub 2015 Apr 13. Angew Chem Weinheim Bergstr Ger. 2015. PMID: 27346896 Free PMC article.
Oxalyl Boronates Enable Modular Synthesis of Bioactive Imidazoles.
Lee CF, Holownia A, Bennett JM, Elkins JM, St Denis JD, Adachi S, Yudin AK. Lee CF, et al. Among authors: bennett jm. Angew Chem Int Ed Engl. 2017 May 22;56(22):6264-6267. doi: 10.1002/anie.201611006. Epub 2017 Mar 7. Angew Chem Int Ed Engl. 2017. PMID: 28267269
Benzoisoquinolinediones as Potent and Selective Inhibitors of BRPF2 and TAF1/TAF1L Bromodomains.
Bouché L, Christ CD, Siegel S, Fernández-Montalván AE, Holton SJ, Fedorov O, Ter Laak A, Sugawara T, Stöckigt D, Tallant C, Bennett J, Monteiro O, Díaz-Sáez L, Siejka P, Meier J, Pütter V, Weiske J, Müller S, Huber KVM, Hartung IV, Haendler B. Bouché L, et al. J Med Chem. 2017 May 11;60(9):4002-4022. doi: 10.1021/acs.jmedchem.7b00306. Epub 2017 May 1. J Med Chem. 2017. PMID: 28402630 Free PMC article.
Synthesis of kinase inhibitors containing a pentafluorosulfanyl moiety.
Sansook S, Ocasio CA, Day IJ, Tizzard GJ, Coles SJ, Fedorov O, Bennett JM, Elkins JM, Spencer J. Sansook S, et al. Among authors: bennett jm. Org Biomol Chem. 2017 Oct 18;15(40):8655-8660. doi: 10.1039/c7ob02289a. Org Biomol Chem. 2017. PMID: 28984325 Free PMC article.
711 results