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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: santoro j. 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.
Discovery and Preclinical Characterization of BIIB091, a Reversible, Selective BTK Inhibitor for the Treatment of Multiple Sclerosis.
Hopkins BT, Bame E, Bajrami B, Black C, Bohnert T, Boiselle C, Burdette D, Burns JC, Delva L, Donaldson D, Grater R, Gu C, Hoemberger M, Johnson J, Kapadnis S, King K, Lulla M, Ma B, Marx I, Magee T, Meissner R, Metrick CM, Mingueneau M, Murugan P, Otipoby KL, Polack E, Poreci U, Prince R, Roach AM, Rowbottom C, Santoro JC, Schroeder P, Tang H, Tien E, Zhang F, Lyssikatos J. Hopkins BT, et al. Among authors: santoro jc. J Med Chem. 2022 Jan 27;65(2):1206-1224. doi: 10.1021/acs.jmedchem.1c00926. Epub 2021 Nov 4. J Med Chem. 2022. PMID: 34734694
Corrigendum to "Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors" [Bioorg. Med. Chem. Lett. 60 (2022) 128549].
Ma B, Metrick CM, Gu C, Hoemberger M, Bajrami B, Bame E, Huang J, Mingueneau M, Murugan P, Nevalainen M, Santoro JC, Tang H, Wang T, Hopkins BT. Ma B, et al. Among authors: santoro jc. Bioorg Med Chem Lett. 2022 Sep 15;72:128856. doi: 10.1016/j.bmcl.2022.128856. Epub 2022 Jun 18. Bioorg Med Chem Lett. 2022. PMID: 35728998 No abstract available.
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: santoro jc. 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
Novel glucocorticoids containing a 6,5-bicyclic core fused to a pyrazole ring: synthesis, in vitro profile, molecular modeling studies, and in vivo experiments.
Thompson CF, Quraishi N, Ali A, Mosley RT, Tata JR, Hammond ML, Balkovec JM, Einstein M, Ge L, Harris G, Kelly TM, Mazur P, Pandit S, Santoro J, Sitlani A, Wang C, Williamson J, Miller DK, Yamin TT, Thompson CM, O'Neill EA, Zaller D, Forrest MJ, Carballo-Jane E, Luell S. Thompson CF, et al. Among authors: santoro j. Bioorg Med Chem Lett. 2007 Jun 15;17(12):3354-61. doi: 10.1016/j.bmcl.2007.03.103. Epub 2007 Apr 5. Bioorg Med Chem Lett. 2007. PMID: 17467988
Novel N-arylpyrazolo[3,2-c]-based ligands for the glucocorticoid receptor: receptor binding and in vivo activity.
Ali A, Thompson CF, Balkovec JM, Graham DW, Hammond ML, Quraishi N, Tata JR, Einstein M, Ge L, Harris G, Kelly TM, Mazur P, Pandit S, Santoro J, Sitlani A, Wang C, Williamson J, Miller DK, Thompson CM, Zaller DM, Forrest MJ, Carballo-Jane E, Luell S. Ali A, et al. Among authors: santoro j. J Med Chem. 2004 May 6;47(10):2441-52. doi: 10.1021/jm030585i. J Med Chem. 2004. PMID: 15115388
Novel heterocyclic glucocorticoids: in vitro profile and in vivo efficacy.
Thompson CF, Quraishi N, Ali A, Tata JR, Hammond ML, Balkovec JM, Einstein M, Ge L, Harris G, Kelly TM, Mazur P, Pandit S, Santoro J, Sitlani A, Wang C, Williamson J, Miller DK, Yamin TT, Thompson CM, O'Neill EA, Zaller D, Forrest MJ, Carballo-Jane E, Luell S. Thompson CF, et al. Among authors: santoro j. Bioorg Med Chem Lett. 2005 Apr 15;15(8):2163-7. doi: 10.1016/j.bmcl.2005.02.009. Bioorg Med Chem Lett. 2005. PMID: 15808489
Discovery of Potent, Selective, and Brain-Penetrant Apoptosis Signal-Regulating Kinase 1 (ASK1) Inhibitors that Modulate Brain Inflammation In Vivo.
Jones JH, Xin Z, Himmelbauer M, Dechantsreiter M, Enyedy I, Hedde J, Fang T, Coomaraswamy J, King KW, Murugan P, Santoro JC, Hesson T, Walther DM, Wei R, Zheng F, Marcotte DJ, Spilker K, Kumar PR, Liu Y, Gilfillan R, Gonzalez-Lopez de Turiso F. Jones JH, et al. Among authors: santoro jc. J Med Chem. 2021 Oct 28;64(20):15402-15419. doi: 10.1021/acs.jmedchem.1c01458. Epub 2021 Oct 15. J Med Chem. 2021. PMID: 34653340
Discovery of CNS-Penetrant Apoptosis Signal-Regulating Kinase 1 (ASK1) Inhibitors.
Xin Z, Himmelbauer MK, Jones JH, Enyedy I, Gilfillan R, Hesson T, King K, Marcotte DJ, Murugan P, Santoro JC, Gonzalez-Lopez de Turiso F. Xin Z, et al. Among authors: santoro jc. ACS Med Chem Lett. 2020 Feb 12;11(4):485-490. doi: 10.1021/acsmedchemlett.9b00611. eCollection 2020 Apr 9. ACS Med Chem Lett. 2020. PMID: 32292554 Free PMC article.
384 results