Article
A regulatory SH2 domain-targeting protein binder effectively inhibits the activity of Bruton's tyrosine kinase and its drug-resistant variants.
Biochemical and biophysical research communications - 21 May 2020
Jeong Sukyo, Sohn Yoo-Kyoung, Choi Yoonjoo, Park Jinho, Kim Hak-Sung
Abstract excerpt
Human Bruton's tyrosine kinase (hBtk) plays a key role in growth and metabolism of B cells, but its dysfunctions cause various B-cell malignancies. Inhibitors targeting the ATP-binding pocket of hBtk have been developed, but they have several drawbacks such as adverse side effects and occurrence of drug-resistant mutations. Here, we present a protein binder which specifically binds to an allosteric regulatory SH2...
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