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.

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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:EN
Published: Nature Portfolio 2020
Subjects:
Science
Q
Online Access:https://doaj.org/article/35d89457e02f4b24aac8c29d22647799
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Summary: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.

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