Autoinhibition of Bruton's tyrosine kinase (Btk) and activation by soluble inositol hexakisphosphate

Wang, Qi; Vogan, Erik M.; Nocka, Laura M.; Rosen, Connor E.; Zorn, Julie A.; Harrison, Stephen C.; Kuriyan, John

doi:10.7554/elife.06074

Title: Autoinhibition of Bruton's tyrosine kinase (Btk) and activation by soluble inositol hexakisphosphate

Journal Article · Fri Feb 20 00:00:00 EST 2015 · eLife

DOI:https://doi.org/10.7554/elife.06074· OSTI ID:1628833

Wang, Qi ^[1]; Vogan, Erik M. ^[2]; Nocka, Laura M. ^[3]; Rosen, Connor E. ^[1]; Zorn, Julie A. ^[1]; Harrison, Stephen C. ^[4]; Kuriyan, John ^[5]

Department of Molecular and Cell Biology, Howard Hughes Medical Institute, University of California, Berkeley, Berkeley, United States; California Institute for Quantitative Biosciences, University of California, Berkeley, Berkeley, United States
Beryllium Inc, Boston, United States; Laboratory of Molecular Medicine, Harvard Medical School, Howard Hughes Medical Institute, Boston, United States
Department of Chemistry, University of California, Berkeley, Berkeley, United States
Laboratory of Molecular Medicine, Harvard Medical School, Howard Hughes Medical Institute, Boston, United States
Department of Molecular and Cell Biology, Howard Hughes Medical Institute, University of California, Berkeley, Berkeley, United States; California Institute for Quantitative Biosciences, University of California, Berkeley, Berkeley, United States; Department of Chemistry, University of California, Berkeley, Berkeley, United States; Physical Biosciences Division, Lawrence Berkeley National Laboratory, Berkeley, United States

Bruton's tyrosine kinase (Btk), a Tec-family tyrosine kinase, is essential for B-cell function. We present crystallographic and biochemical analyses of Btk, which together reveal molecular details of its autoinhibition and activation. Autoinhibited Btk adopts a compact conformation like that of inactive c-Src and c-Abl. A lipid-binding PH-TH module, unique to Tec kinases, acts in conjunction with the SH2 and SH3 domains to stabilize the inactive conformation. In addition to the expected activation of Btk by membranes containing phosphatidylinositol triphosphate (PIP₃), we found that inositol hexakisphosphate (IP₆₆₆

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Research Organization:: Lawrence Berkeley National Laboratory (LBNL), Berkeley, CA (United States)

Sponsoring Organization:: USDOE Office of Science (SC); National Institutes of Health (NIH); Cancer Research Institute-Irvington Institute Fellowship Program

Grant/Contract Number:: AC02-05CH11231; PO1 AI091580

OSTI ID:: 1628833

Journal Information:: eLife, Vol. 4; ISSN 2050-084X

Publisher:: eLife Sciences Publications, Ltd.Copyright Statement

Country of Publication:: United States

Language:: English

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