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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: monteiro op. 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.
[1,2,4]triazolo[4,3-a]phthalazines: inhibitors of diverse bromodomains.
Fedorov O, Lingard H, Wells C, Monteiro OP, Picaud S, Keates T, Yapp C, Philpott M, Martin SJ, Felletar I, Marsden BD, Filippakopoulos P, Müller S, Knapp S, Brennan PE. Fedorov O, et al. Among authors: monteiro op. J Med Chem. 2014 Jan 23;57(2):462-76. doi: 10.1021/jm401568s. Epub 2013 Dec 30. J Med Chem. 2014. PMID: 24313754 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: monteiro op. 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.
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.
Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy.
Picaud S, Fedorov O, Thanasopoulou A, Leonards K, Jones K, Meier J, Olzscha H, Monteiro O, Martin S, Philpott M, Tumber A, Filippakopoulos P, Yapp C, Wells C, Che KH, Bannister A, Robson S, Kumar U, Parr N, Lee K, Lugo D, Jeffrey P, Taylor S, Vecellio ML, Bountra C, Brennan PE, O'Mahony A, Velichko S, Müller S, Hay D, Daniels DL, Urh M, La Thangue NB, Kouzarides T, Prinjha R, Schwaller J, Knapp S. Picaud S, et al. Cancer Res. 2015 Dec 1;75(23):5106-5119. doi: 10.1158/0008-5472.CAN-15-0236. Epub 2015 Nov 9. Cancer Res. 2015. PMID: 26552700 Free PMC article.
Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance.
Fedorov O, Castex J, Tallant C, Owen DR, Martin S, Aldeghi M, Monteiro O, Filippakopoulos P, Picaud S, Trzupek JD, Gerstenberger BS, Bountra C, Willmann D, Wells C, Philpott M, Rogers C, Biggin PC, Brennan PE, Bunnage ME, Schüle R, Günther T, Knapp S, Müller S. Fedorov O, et al. Sci Adv. 2015 Nov 13;1(10):e1500723. doi: 10.1126/sciadv.1500723. eCollection 2015 Nov. Sci Adv. 2015. PMID: 26702435 Free PMC article.
Identification and Development of 2,3-Dihydropyrrolo[1,2-a]quinazolin-5(1H)-one Inhibitors Targeting Bromodomains within the Switch/Sucrose Nonfermenting Complex.
Sutherell CL, Tallant C, Monteiro OP, Yapp C, Fuchs JE, Fedorov O, Siejka P, Müller S, Knapp S, Brenton JD, Brennan PE, Ley SV. Sutherell CL, et al. Among authors: monteiro op. J Med Chem. 2016 May 26;59(10):5095-101. doi: 10.1021/acs.jmedchem.5b01997. Epub 2016 May 11. J Med Chem. 2016. PMID: 27119626 Free PMC article.
BET inhibition as a new strategy for the treatment of gastric cancer.
Montenegro RC, Clark PG, Howarth A, Wan X, Ceroni A, Siejka P, Nunez-Alonso GA, Monteiro O, Rogers C, Gamble V, Burbano R, Brennan PE, Tallant C, Ebner D, Fedorov O, O'Neill E, Knapp S, Dixon D, Müller S. Montenegro RC, et al. Oncotarget. 2016 Jul 12;7(28):43997-44012. doi: 10.18632/oncotarget.9766. Oncotarget. 2016. PMID: 27259267 Free PMC article.
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: monteiro op. 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.
20 results