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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. 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 of BIIB068: A Selective, Potent, Reversible Bruton's Tyrosine Kinase Inhibitor as an Orally Efficacious Agent for Autoimmune Diseases.
Ma B, Bohnert T, Otipoby KL, Tien E, Arefayene M, Bai J, Bajrami B, Bame E, Chan TR, Humora M, MacPhee JM, Marcotte D, Mehta D, Metrick CM, Moniz G, Polack E, Poreci U, Prefontaine A, Sheikh S, Schroeder P, Smirnakis K, Zhang L, Zheng F, Hopkins BT. Ma B, et al. Among authors: bame e. J Med Chem. 2020 Nov 12;63(21):12526-12541. doi: 10.1021/acs.jmedchem.0c00702. Epub 2020 Aug 6. J Med Chem. 2020. PMID: 32696648
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: bame e. 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
Optimization of novel reversible Bruton's tyrosine kinase inhibitors identified using Tethering-fragment-based screens.
Hopkins BT, Bame E, Bell N, Bohnert T, Bowden-Verhoek JK, Bui M, Cancilla MT, Conlon P, Cullen P, Erlanson DA, Fan J, Fuchs-Knotts T, Hansen S, Heumann S, Jenkins TJ, Marcotte D, McDowell B, Mertsching E, Negrou E, Otipoby KL, Poreci U, Romanowski MJ, Scott D, Silvian L, Yang W, Zhong M. Hopkins BT, et al. Among authors: bame e. Bioorg Med Chem. 2019 Jul 1;27(13):2905-2913. doi: 10.1016/j.bmc.2019.05.021. Epub 2019 May 14. Bioorg Med Chem. 2019. PMID: 31138459
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: bame e. 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.
Utilizing structure based drug design and metabolic soft spot identification to optimize the in vitro potency and in vivo pharmacokinetic properties leading to the discovery of novel reversible Bruton's tyrosine kinase inhibitors.
Hopkins BT, Bame E, Bell N, Bohnert T, Bowden-Verhoek JK, Bui M, Cancilla MT, Conlon P, Cullen P, Erlanson DA, Fan J, Fuchs-Knotts T, Hansen S, Heumann S, Jenkins TJ, Gua C, Liu Y, Liu Y, Lulla M, Marcotte D, Marx I, McDowell B, Mertsching E, Negrou E, Romanowski MJ, Scott D, Silvian L, Yang W, Zhong M. Hopkins BT, et al. Among authors: bame e. Bioorg Med Chem. 2021 Aug 15;44:116275. doi: 10.1016/j.bmc.2021.116275. Epub 2021 Jun 15. Bioorg Med Chem. 2021. PMID: 34314938
Effect of dimethyl fumarate on lymphocytes in RRMS: Implications for clinical practice.
Mehta D, Miller C, Arnold DL, Bame E, Bar-Or A, Gold R, Hanna J, Kappos L, Liu S, Matta A, Phillips JT, Robertson D, von Hehn CA, Campbell J, Spach K, Yang L, Fox RJ. Mehta D, et al. Among authors: bame e. Neurology. 2019 Apr 9;92(15):e1724-e1738. doi: 10.1212/WNL.0000000000007262. Epub 2019 Mar 27. Neurology. 2019. PMID: 30918100 Free PMC article.
Dimethyl fumarate treatment shifts the immune environment toward an anti-inflammatory cell profile while maintaining protective humoral immunity.
Longbrake EE, Mao-Draayer Y, Cascione M, Zielinski T, Bame E, Brassat D, Chen C, Kapadia S, Mendoza JP, Miller C, Parks B, Xing D, Robertson D. Longbrake EE, et al. Among authors: bame e. Mult Scler. 2021 May;27(6):883-894. doi: 10.1177/1352458520937282. Epub 2020 Jul 27. Mult Scler. 2021. PMID: 32716690 Free PMC article. Clinical Trial.
2019 White Paper on Recent Issues in Bioanalysis: FDA Immunogenicity Guidance, Gene Therapy, Critical Reagents, Biomarkers and Flow Cytometry Validation (Part 3 - Recommendations on 2019 FDA Immunogenicity Guidance, Gene Therapy Bioanalytical Challenges, Strategies for Critical Reagent Management, Biomarker Assay Validation, Flow Cytometry Validation & CLSI H62).
Piccoli S, Mehta D, Vitaliti A, Allinson J, Amur S, Eck S, Green C, Hedrick M, Hopper S, Ji A, Joyce A, Litwin V, Maher K, Mathews J, Peng K, Safavi A, Wang YM, Zhang Y, Amaravadi L, Palackal N, Thankamony S, Beaver C, Bame E, Emrich T, Grimaldi C, Haulenbeek J, Joyce A, Kakkanaiah V, Lanham D, Maher K, Mayer A, Trampont PC, Vermet L, Dakappagari N, Fleener C, Garofolo F, Rogers C, Tangri S, Xu Y, Liang M, Rajadhyaksha M, Richards S, Schweighardt B, Purushothama S, Baltrukonis D, Brumm J, Cherry E, Delcarpini J, Gleason C, Kirshner S, Kubiak R, Pan L, Partridge M, Pedras-Vasconcelos J, Qu Q, Skibeli V, Saunders TS, Staack RF, Stubenrauch K, Torri A, Verthelyi D, Yan H, Gorovits B, Palmer R, Milton M, Long B, Corsaro B, Farrokhi V, Fiscella M, Henderson N, Jawa V, McNally J, Murphy R, Waldner H, Yang TY. Piccoli S, et al. Among authors: bame e. Bioanalysis. 2019 Dec;11(24):2207-2244. doi: 10.4155/bio-2019-0271. Epub 2019 Dec 10. Bioanalysis. 2019. PMID: 31820675 Free article.
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