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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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 |
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Format: | article |
Language: | EN |
Published: |
Nature Portfolio
2020
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Subjects: | |
Online Access: | https://doaj.org/article/35d89457e02f4b24aac8c29d22647799 |
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