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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
Clinical & Translational Immunology ( IF 4.6 ) Pub Date : 2021-06-14 , DOI: 10.1002/cti2.1295
Eris Bame 1 , Hao Tang 2 , Jeremy C Burns 2 , Million Arefayene 1 , Klaus Michelsen 3, 4 , Bin Ma 3 , Isaac Marx 3 , Robin Prince 3 , Allie M Roach 2, 5 , Urjana Poreci 1, 6 , Douglas Donaldson 1, 7 , Patrick Cullen 2 , Fergal Casey 2 , Jing Zhu 2 , Thomas M Carlile 2 , Dipen Sangurdekar 2, 8 , Baohong Zhang 2 , Patrick Trapa 3 , Joseph Santoro 3 , Param Muragan 3 , Alex Pellerin 2 , Stephen Rubino 2 , Davide Gianni 3 , Bekim Bajrami 3 , Xiaomei Peng 9 , Alex Coppell 10 , Katherine Riester 1 , Shibeshih Belachew 11 , Devangi Mehta 1, 12 , Mike Palte 13 , Brian T Hopkins 3 , Matthew Scaramozza 13 , Nathalie Franchimont 13 , Michael Mingueneau 2
Affiliation  

Bruton's tyrosine kinase (BTK) plays a non-redundant signaling role downstream of the B-cell receptor (BCR) in B cells and the receptors for the Fc region of immunoglobulins (FcR) in myeloid cells. Here, we characterise BIIB091, a novel, potent, selective and reversible small-molecule inhibitor of BTK.

中文翻译:

新一代 Bruton 酪氨酸激酶抑制剂 BIIB091 选择性且有效地抑制 B 细胞和 Fc 受体信号传导以及 B 细胞和骨髓细胞的下游功能

布鲁顿酪氨酸激酶 (BTK) 在 B 细胞中的 B 细胞受体 (BCR) 和骨髓细胞中免疫球蛋白 (FcR) 的 Fc 区受体下游发挥非冗余信号传导作用。在这里,我们描述了 BIIB091,一种新型、有效、选择性和可逆的 BTK 小分子抑制剂。
更新日期:2021-06-15
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