作者: Leanne E. Wybenga-Groot , Berivan Baskin , Siew Hwa Ong , Jiefei Tong , Tony Pawson
DOI: 10.1016/S0092-8674(01)00496-2
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摘要: The Eph receptor tyrosine kinase family is regulated by autophosphorylation within the juxtamembrane region and activation segment. We have solved X-ray crystal structure to 1.9 A resolution of an autoinhibited, unphosphorylated form EphB2 comprised domain. structure, supported mutagenesis data, reveals that segment adopts a helical conformation distorts small lobe domain, blocks from attaining activated conformation. Phosphorylation conserved tyrosines would relieve this autoinhibition disturbing association with while liberating phosphotyrosine sites for binding SH2 domains target proteins. propose autoinhibitory mechanism employed more general device through which kinases are controlled.