Article
Btk SH2-kinase interface is critical for allosteric kinase activation and its targeting inhibits B-cell neoplasms.
Nature communications - 8 May 2020
Duarte Daniel P, Lamontanara Allan J, La Sala Giuseppina, Jeong Sukyo, Sohn Yoo-Kyoung, Panjkovich Alejandro, Georgeon Sandrine, Kükenshöner Tim, Marcaida Maria J, Pojer Florence, De Vivo Marco, Svergun Dmitri, Kim Hak-Sung, Dal Peraro Matteo, Hantschel Oliver
Abstract excerpt
Bruton's tyrosine kinase (Btk) is critical for B-cell maturation and activation. Btk loss-of-function mutations cause human X-linked agammaglobulinemia (XLA). In contrast, Btk signaling sustains growth of several B-cell neoplasms which may be treated with tyrosine kinase inhibitors (TKIs). Here, we uncovered the structural mechanism by which certain XLA mutations in the SH2 domain strongly perturb Btk activation....
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