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Biochemistry, Biophysics, and Structural Biology Commons

Open Access. Powered by Scholars. Published by Universities.®

Molecular Biology

Catalytic activity

Iowa State University

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Full-Text Articles in Biochemistry, Biophysics, and Structural Biology

A Conserved Isoleucine Maintains The Inactive State Of Bruton’S Tyrosine Kinase, Scott E. Boyken, Nikita Chopra, Qian Xie, Raji E. Joseph, Thomas E. Wales, D. Bruce Fulton, John R. Engen, Robert L. Jernigan, Amy H. Andreotti Oct 2014

A Conserved Isoleucine Maintains The Inactive State Of Bruton’S Tyrosine Kinase, Scott E. Boyken, Nikita Chopra, Qian Xie, Raji E. Joseph, Thomas E. Wales, D. Bruce Fulton, John R. Engen, Robert L. Jernigan, Amy H. Andreotti

Biochemistry, Biophysics and Molecular Biology Publications

Despite high homology among non-receptor tyrosine kinases, different kinase families employ a diverse array of regulatory mechanisms. For example, the catalytic kinase domains of the Tec family kinases are inactive without assembly of the adjacent regulatory domains, whereas the Src kinase domains are autoinhibited by the assembly of similar adjacent regulatory domains. Using molecular dynamic simulations, biochemical assays, and biophysical approaches, we have uncovered an isoleucine residue in the kinase domain of the Tec family member Btk that, when mutated to the closely related leucine, leads to a shift in the conformational equilibrium of the kinase domain toward the active ...