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Next-generation Bruton's tyrosine kinase inhibitor BIIB091 selectively and potently inhibits B cell and Fc receptor signaling and downstream functions in B cells and myeloid cells.
Bame E, Tang H, Burns JC, Arefayene M, Michelsen K, Ma B, Marx I, Prince R, Roach AM, Poreci U, Donaldson D, Cullen P, Casey F, Zhu J, Carlile TM, Sangurdekar D, Zhang B, Trapa P, Santoro J, Muragan P, Pellerin A, Rubino S, Gianni D, Bajrami B, Peng X, Coppell A, Riester K, Belachew S, Mehta D, Palte M, Hopkins BT, Scaramozza M, Franchimont N, Mingueneau M. Bame E, et al. Among authors: michelsen k. Clin Transl Immunology. 2021 Jun 14;10(6):e1295. doi: 10.1002/cti2.1295. eCollection 2021. Clin Transl Immunology. 2021. PMID: 34141433 Free PMC article.
ATP-Competitive MLKL Binders Have No Functional Impact on Necroptosis.
Ma B, Marcotte D, Paramasivam M, Michelsen K, Wang T, Bertolotti-Ciarlet A, Jones JH, Moree B, Butko M, Salafsky J, Sun X, McKee T, Silvian LF. Ma B, et al. Among authors: michelsen k. PLoS One. 2016 Nov 10;11(11):e0165983. doi: 10.1371/journal.pone.0165983. eCollection 2016. PLoS One. 2016. PMID: 27832137 Free PMC article.
Human PLD structures enable drug design and characterization of isoenzyme selectivity.
Metrick CM, Peterson EA, Santoro JC, Enyedy IJ, Murugan P, Chen T, Michelsen K, Cullivan M, Spilker KA, Kumar PR, May-Dracka TL, Chodaparambil JV. Metrick CM, et al. Among authors: michelsen k. Nat Chem Biol. 2020 Apr;16(4):391-399. doi: 10.1038/s41589-019-0458-4. Epub 2020 Feb 10. Nat Chem Biol. 2020. PMID: 32042197
Structure-based design of novel inhibitors of the MDM2-p53 interaction.
Rew Y, Sun D, Gonzalez-Lopez De Turiso F, Bartberger MD, Beck HP, Canon J, Chen A, Chow D, Deignan J, Fox BM, Gustin D, Huang X, Jiang M, Jiao X, Jin L, Kayser F, Kopecky DJ, Li Y, Lo MC, Long AM, Michelsen K, Oliner JD, Osgood T, Ragains M, Saiki AY, Schneider S, Toteva M, Yakowec P, Yan X, Ye Q, Yu D, Zhao X, Zhou J, Medina JC, Olson SH. Rew Y, et al. Among authors: michelsen k. J Med Chem. 2012 Jun 14;55(11):4936-54. doi: 10.1021/jm300354j. Epub 2012 May 9. J Med Chem. 2012. PMID: 22524527
Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept.
Ashton KS, Andrews KL, Bryan MC, Chen J, Chen K, Chen M, Chmait S, Croghan M, Cupples R, Fotsch C, Helmering J, Jordan SR, Kurzeja RJ, Michelsen K, Pennington LD, Poon SF, Sivits G, Van G, Vonderfecht SL, Wahl RC, Zhang J, Lloyd DJ, Hale C, St Jean DJ Jr. Ashton KS, et al. Among authors: michelsen k. J Med Chem. 2014 Jan 23;57(2):309-24. doi: 10.1021/jm4016735. Epub 2014 Jan 9. J Med Chem. 2014. PMID: 24405172
Antidiabetic effects of glucokinase regulatory protein small-molecule disruptors.
Lloyd DJ, St Jean DJ Jr, Kurzeja RJ, Wahl RC, Michelsen K, Cupples R, Chen M, Wu J, Sivits G, Helmering J, Komorowski R, Ashton KS, Pennington LD, Fotsch C, Vazir M, Chen K, Chmait S, Zhang J, Liu L, Norman MH, Andrews KL, Bartberger MD, Van G, Galbreath EJ, Vonderfecht SL, Wang M, Jordan SR, Véniant MM, Hale C. Lloyd DJ, et al. Among authors: michelsen k. Nature. 2013 Dec 19;504(7480):437-40. doi: 10.1038/nature12724. Epub 2013 Nov 13. Nature. 2013. PMID: 24226772
142 results