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Discovery and Preclinical Characterization of BIIB129, a Covalent, Selective, and Brain-Penetrant BTK Inhibitor for the Treatment of Multiple Sclerosis.
Himmelbauer MK, Bajrami B, Basile R, Capacci A, Chen T, Choi CK, Gilfillan R, Gonzalez-Lopez de Turiso F, Gu C, Hoemberger M, Johnson DS, Jones JH, Kadakia E, Kirkland M, Lin EY, Liu Y, Ma B, Magee T, Mantena S, Marx IE, Metrick CM, Mingueneau M, Murugan P, Muste CA, Nadella P, Nevalainen M, Parker Harp CR, Pattaropong V, Pietrasiewicz A, Prince RJ, Purgett TJ, Santoro JC, Schulz J, Sciabola S, Tang H, Vandeveer HG, Wang T, Yousaf Z, Helal CJ, Hopkins BT. Himmelbauer MK, et al. Among authors: tang h. J Med Chem. 2024 May 23;67(10):8122-8140. doi: 10.1021/acs.jmedchem.4c00220. Epub 2024 May 7. J Med Chem. 2024. PMID: 38712838 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: tang h. 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: tang h. 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.
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: tang h. 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.
BTK inhibition limits B-cell-T-cell interaction through modulation of B-cell metabolism: implications for multiple sclerosis therapy.
Li R, Tang H, Burns JC, Hopkins BT, Le Coz C, Zhang B, de Barcelos IP, Romberg N, Goldstein AC, Banwell BL, Luning Prak ET, Mingueneau M, Bar-Or A. Li R, et al. Among authors: tang h. Acta Neuropathol. 2022 Apr;143(4):505-521. doi: 10.1007/s00401-022-02411-w. Epub 2022 Mar 18. Acta Neuropathol. 2022. PMID: 35303161 Free PMC article.
MOG autoantibodies trigger a tightly-controlled FcR and BTK-driven microglia proliferative response.
Pellerin K, Rubino SJ, Burns JC, Smith BA, McCarl CA, Zhu J, Jandreski L, Cullen P, Carlile TM, Li A, Rebollar JV, Sybulski J, Reynolds TL, Zhang B, Basile R, Tang H, Harp CP, Pellerin A, Silbereis J, Franchimont N, Cahir-McFarland E, Ransohoff RM, Cameron TO, Mingueneau M. Pellerin K, et al. Among authors: tang h. Brain. 2021 Sep 4;144(8):2361-2374. doi: 10.1093/brain/awab231. Brain. 2021. PMID: 34145876
Oxidative phosphorylation regulates B cell effector cytokines and promotes inflammation in multiple sclerosis.
Li R, Lei Y, Rezk A, Diego A Espinoza, Wang J, Feng H, Zhang B, Barcelos IP, Zhang H, Yu J, Huo X, Zhu F, Yang C, Tang H, Goldstein AC, Banwell BL, Hakonarson H, Xu H, Mingueneau M, Sun B, Li H, Bar-Or A. Li R, et al. Among authors: tang h. Sci Immunol. 2024 May 3;9(95):eadk0865. doi: 10.1126/sciimmunol.adk0865. Epub 2024 May 3. Sci Immunol. 2024. PMID: 38701189
Toxicological and pharmacological assessment of AGEN1884, a novel human IgG1 anti-CTLA-4 antibody.
Gombos RB, Gonzalez A, Manrique M, Chand D, Savitsky D, Morin B, Breous-Nystrom E, Dupont C, Ward RA, Mundt C, Duckless B, Tang H, Findeis MA, Schuster A, Waight JD, Underwood D, Clarke C, Ritter G, Merghoub T, Schaer D, Wolchok JD, van Dijk M, Buell JS, Cuillerot JM, Stein R, Drouin EE, Wilson NS. Gombos RB, et al. Among authors: tang h. PLoS One. 2018 Apr 4;13(4):e0191926. doi: 10.1371/journal.pone.0191926. eCollection 2018. PLoS One. 2018. PMID: 29617360 Free PMC article.
Evaluation of JAK3 Biology in Autoimmune Disease Using a Highly Selective, Irreversible JAK3 Inhibitor.
Elwood F, Witter DJ, Piesvaux J, Kraybill B, Bays N, Alpert C, Goldenblatt P, Qu Y, Ivanovska I, Lee HH, Chiu CS, Tang H, Scott ME, Deshmukh SV, Zielstorff M, Byford A, Chakravarthy K, Dorosh L, Rivkin A, Klappenbach J, Pan BS, Kariv I, Dinsmore C, Slipetz D, Dandliker PJ. Elwood F, et al. Among authors: tang h. J Pharmacol Exp Ther. 2017 May;361(2):229-244. doi: 10.1124/jpet.116.239723. Epub 2017 Feb 13. J Pharmacol Exp Ther. 2017. PMID: 28193636
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