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Potent, non-covalent reversible BTK inhibitors with 8-amino-imidazo[1,5-a]pyrazine core featuring 3-position bicyclic ring substitutes.
Liu J, Guiadeen D, Krikorian A, Gao X, Wang J, Babu Boga S, Alhassan AB, Yu W, Selyutin O, Yu Y, Anand R, Xu J, Kelly J, Duffy JL, Liu S, Yang C, Wu H, Cai J, Bennett C, Maloney KM, Tyagarajan S, Gao YD, Fischmann TO, Presland J, Mansueto M, Xu Z, Leccese E, Zhang-Hoover J, Knemeyer I, Garlisi CG, Stivers P, Brandish PE, Hicks A, Kim R, Kozlowski JA. Liu J, et al. Among authors: brandish pe. Bioorg Med Chem Lett. 2020 Sep 1;30(17):127390. doi: 10.1016/j.bmcl.2020.127390. Epub 2020 Jul 11. Bioorg Med Chem Lett. 2020. PMID: 32738973
Discovery of 8-Amino-imidazo[1,5-a]pyrazines as Reversible BTK Inhibitors for the Treatment of Rheumatoid Arthritis.
Liu J, Guiadeen D, Krikorian A, Gao X, Wang J, Boga SB, Alhassan AB, Yu Y, Vaccaro H, Liu S, Yang C, Wu H, Cooper A, de Man J, Kaptein A, Maloney K, Hornak V, Gao YD, Fischmann TO, Raaijmakers H, Vu-Pham D, Presland J, Mansueto M, Xu Z, Leccese E, Zhang-Hoover J, Knemeyer I, Garlisi CG, Bays N, Stivers P, Brandish PE, Hicks A, Kim R, Kozlowski JA. Liu J, et al. Among authors: brandish pe. ACS Med Chem Lett. 2015 Dec 19;7(2):198-203. doi: 10.1021/acsmedchemlett.5b00463. eCollection 2016 Feb 11. ACS Med Chem Lett. 2015. PMID: 26985298 Free PMC article.
Discovery of novel BTK inhibitors with carboxylic acids.
Gao X, Wang J, Liu J, Guiadeen D, Krikorian A, Boga SB, Alhassan AB, Selyutin O, Yu W, Yu Y, Anand R, Liu S, Yang C, Wu H, Cai J, Cooper A, Zhu H, Maloney K, Gao YD, Fischmann TO, Presland J, Mansueto M, Xu Z, Leccese E, Zhang-Hoover J, Knemeyer I, Garlisi CG, Bays N, Stivers P, Brandish PE, Hicks A, Kim R, Kozlowski JA. Gao X, et al. Among authors: brandish pe. Bioorg Med Chem Lett. 2017 Mar 15;27(6):1471-1477. doi: 10.1016/j.bmcl.2016.11.079. Epub 2016 Nov 25. Bioorg Med Chem Lett. 2017. PMID: 28254166
Discovery of 3-morpholino-imidazole[1,5-a]pyrazine BTK inhibitors for rheumatoid arthritis.
Boga SB, Alhassan AB, Liu J, Guiadeen D, Krikorian A, Gao X, Wang J, Yu Y, Anand R, Liu S, Yang C, Wu H, Cai J, Zhu H, Desai J, Maloney K, Gao YD, Fischmann TO, Presland J, Mansueto M, Xu Z, Leccese E, Knemeyer I, Garlisi CG, Bays N, Stivers P, Brandish PE, Hicks A, Cooper A, Kim RM, Kozlowski JA. Boga SB, et al. Among authors: brandish pe. Bioorg Med Chem Lett. 2017 Aug 15;27(16):3939-3943. doi: 10.1016/j.bmcl.2017.03.040. Epub 2017 Mar 18. Bioorg Med Chem Lett. 2017. PMID: 28720503
Discovery of selective glucocorticoid receptor modulator MK-5932.
Bungard CJ, Hartman GD, Manikowski JJ, Perkins JJ, Bai C, Brandish PE, Euler DH, Hershey JC, Schmidt A, Fang Y, Norcross RT, Rushmore TH, Thompson CD, Meissner RS. Bungard CJ, et al. Among authors: brandish pe. Bioorg Med Chem. 2011 Dec 15;19(24):7374-86. doi: 10.1016/j.bmc.2011.10.054. Epub 2011 Oct 24. Bioorg Med Chem. 2011. PMID: 22079253
Development of Anti-CD74 Antibody-Drug Conjugates to Target Glucocorticoids to Immune Cells.
Brandish PE, Palmieri A, Antonenko S, Beaumont M, Benso L, Cancilla M, Cheng M, Fayadat-Dilman L, Feng G, Figueroa I, Firdos J, Garbaccio R, Garvin-Queen L, Gately D, Geda P, Haines C, Hseih S, Hodges D, Kern J, Knudsen N, Kwasnjuk K, Liang L, Ma H, Manibusan A, Miller PL, Moy LY, Qu Y, Shah S, Shin JS, Stivers P, Sun Y, Tomazela D, Woo HC, Zaller D, Zhang S, Zhang Y, Zielstorff M. Brandish PE, et al. Bioconjug Chem. 2018 Jul 18;29(7):2357-2369. doi: 10.1021/acs.bioconjchem.8b00312. Epub 2018 Jul 2. Bioconjug Chem. 2018. PMID: 29923706
ILT3 (LILRB4) Promotes the Immunosuppressive Function of Tumor-Educated Human Monocytic Myeloid-Derived Suppressor Cells.
Singh L, Muise ES, Bhattacharya A, Grein J, Javaid S, Stivers P, Zhang J, Qu Y, Joyce-Shaikh B, Loboda A, Zhang C, Meehl M, Chiang DY, Ranganath SH, Rosenzweig M, Brandish PE. Singh L, et al. Among authors: brandish pe. Mol Cancer Res. 2021 Apr;19(4):702-716. doi: 10.1158/1541-7786.MCR-20-0622. Epub 2020 Dec 28. Mol Cancer Res. 2021. PMID: 33372059
The preclinical efficacy, selectivity and pharmacologic profile of MK-5932, an insulin-sparing selective glucocorticoid receptor modulator.
Brandish PE, Anderson K, Baltus GA, Bai C, Bungard CJ, Bunting P, Byford A, Chiu CS, Cicmil M, Corcoran H, Euler D, Fisher JE, Gambone C, Hasbun-Manning M, Kuklin N, Landis E, Lifsted TQ, McElwee-Witmer S, McIntosh IS, Meissner RS, Miao J, Mitchell HJ, Musselman A, Schmidt A, Shin J, Szczerba P, Thompson CD, Tribouley C, Vogel RL, Warrier S, Hershey JC. Brandish PE, et al. Eur J Pharmacol. 2014 Feb 5;724:102-11. doi: 10.1016/j.ejphar.2013.12.031. Epub 2013 Dec 27. Eur J Pharmacol. 2014. PMID: 24374007
31 results