Btk SH2-kinase interface is critical for allosteric kinase activation and its targeting inhibits B-cell neoplasms

Btk SH2-kinase interface is critical for allosteric kinase activation and its targeting inhibits B-cell neoplasms

Constitutive Btk signaling drives several B-cell cancers. Here the authors demonstrate key allosteric intramolecular interactions between the SH2 domain and the kinase domain of Btk, and propose an alternative approach for inhibition of both wild-type and tyrosine kinase inhibitor-resistant Btk.

Bibliographic Details
Main Authors: Daniel P. Duarte, Allan J. Lamontanara, Giuseppina La Sala, Sukyo Jeong, Yoo-Kyoung Sohn, Alejandro Panjkovich, Sandrine Georgeon, Tim Kükenshöner, Maria J. Marcaida, Florence Pojer, Marco De Vivo, Dmitri Svergun, Hak-Sung Kim, Matteo Dal Peraro, Oliver Hantschel
Format: Article
Language:English
Published: Nature Publishing Group 2020-05-01
Series:Nature Communications
Online Access:https://doi.org/10.1038/s41467-020-16128-5

Internet

https://doi.org/10.1038/s41467-020-16128-5

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