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388 results

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Page 1
Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia.
Pappalardi MB, Keenan K, Cockerill M, Kellner WA, Stowell A, Sherk C, Wong K, Pathuri S, Briand J, Steidel M, Chapman P, Groy A, Wiseman AK, McHugh CF, Campobasso N, Graves AP, Fairweather E, Werner T, Raoof A, Butlin RJ, Rueda L, Horton JR, Fosbenner DT, Zhang C, Handler JL, Muliaditan M, Mebrahtu M, Jaworski JP, McNulty DE, Burt C, Eberl HC, Taylor AN, Ho T, Merrihew S, Foley SW, Rutkowska A, Li M, Romeril SP, Goldberg K, Zhang X, Kershaw CS, Bantscheff M, Jurewicz AJ, Minthorn E, Grandi P, Patel M, Benowitz AB, Mohammad HP, Gilmartin AG, Prinjha RK, Ogilvie D, Carpenter C, Heerding D, Baylin SB, Jones PA, Cheng X, King BW, Luengo JI, Jordan AM, Waddell I, Kruger RG, McCabe MT. Pappalardi MB, et al. Among authors: briand j. Nat Cancer. 2021 Oct;2(10):1002-1017. Epub 2021 Sep 27. Nat Cancer. 2021. PMID: 34790902 Free PMC article.
Aminoindazole PDK1 Inhibitors: A Case Study in Fragment-Based Drug Discovery.
Medina JR, Blackledge CW, Heerding DA, Campobasso N, Ward P, Briand J, Wright L, Axten JM. Medina JR, et al. Among authors: briand j. ACS Med Chem Lett. 2010 Jul 22;1(8):439-42. doi: 10.1021/ml100136n. eCollection 2010 Nov 11. ACS Med Chem Lett. 2010. PMID: 24900229 Free PMC article.
Discovery of a Novel 2,6-Disubstituted Glucosamine Series of Potent and Selective Hexokinase 2 Inhibitors.
Lin H, Zeng J, Xie R, Schulz MJ, Tedesco R, Qu J, Erhard KF, Mack JF, Raha K, Rendina AR, Szewczuk LM, Kratz PM, Jurewicz AJ, Cecconie T, Martens S, McDevitt PJ, Martin JD, Chen SB, Jiang Y, Nickels L, Schwartz BJ, Smallwood A, Zhao B, Campobasso N, Qian Y, Briand J, Rominger CM, Oleykowski C, Hardwicke MA, Luengo JI. Lin H, et al. Among authors: briand j. ACS Med Chem Lett. 2015 Dec 28;7(3):217-22. doi: 10.1021/acsmedchemlett.5b00214. eCollection 2016 Mar 10. ACS Med Chem Lett. 2015. PMID: 26985301 Free PMC article.
Quinoline 3-sulfonamides inhibit lactate dehydrogenase A and reverse aerobic glycolysis in cancer cells.
Billiard J, Dennison JB, Briand J, Annan RS, Chai D, Colón M, Dodson CS, Gilbert SA, Greshock J, Jing J, Lu H, McSurdy-Freed JE, Orband-Miller LA, Mills GB, Quinn CJ, Schneck JL, Scott GF, Shaw AN, Waitt GM, Wooster RF, Duffy KJ. Billiard J, et al. Among authors: briand j. Cancer Metab. 2013 Sep 6;1(1):19. doi: 10.1186/2049-3002-1-19. Cancer Metab. 2013. PMID: 24280423 Free PMC article.
Kinetic mechanism and rate-limiting steps of focal adhesion kinase-1.
Schneck JL, Briand J, Chen S, Lehr R, McDevitt P, Zhao B, Smallwood A, Concha N, Oza K, Kirkpatrick R, Yan K, Villa JP, Meek TD, Thrall SH. Schneck JL, et al. Among authors: briand j. Biochemistry. 2010 Aug 24;49(33):7151-63. doi: 10.1021/bi100824v. Biochemistry. 2010. PMID: 20597513
CCR2 receptor antagonists: optimization of biaryl sulfonamides to increase activity in whole blood.
Wang GZ, Haile PA, Daniel T, Belot B, Viet AQ, Goodman KB, Sha D, Dowdell SE, Varga N, Hong X, Chakravorty S, Webb C, Cornejo C, Olzinski A, Bernard R, Evans C, Emmons A, Briand J, Chung CW, Quek R, Lee D, Gough PJ, Sehon CA. Wang GZ, et al. Among authors: briand j. Bioorg Med Chem Lett. 2011 Dec 15;21(24):7291-4. doi: 10.1016/j.bmcl.2011.10.038. Epub 2011 Oct 19. Bioorg Med Chem Lett. 2011. PMID: 22047688
Design of potent and selective human cathepsin K inhibitors that span the active site.
Thompson SK, Halbert SM, Bossard MJ, Tomaszek TA, Levy MA, Zhao B, Smith WW, Abdel-Meguid SS, Janson CA, D'Alessio KJ, McQueney MS, Amegadzie BY, Hanning CR, DesJarlais RL, Briand J, Sarkar SK, Huddleston MJ, Ijames CF, Carr SA, Garnes KT, Shu A, Heys JR, Bradbeer J, Zembryki D, Lee-Rykaczewski L, James IE, Lark MW, Drake FH, Gowen M, Gleason JG, Veber DF. Thompson SK, et al. Among authors: briand j. Proc Natl Acad Sci U S A. 1997 Dec 23;94(26):14249-54. doi: 10.1073/pnas.94.26.14249. Proc Natl Acad Sci U S A. 1997. PMID: 9405598 Free PMC article.
388 results