期刊
TRENDS IN BIOCHEMICAL SCIENCES
卷 39, 期 10, 页码 437-446出版社
ELSEVIER SCIENCE LONDON
DOI: 10.1016/j.tibs.2014.08.001
关键词
receptor tyrosine kinases; epidermal growth factor receptor; signal transduction; allostery
The activation of receptor tyrosine kinases in response to extracellular signals is a principal component of metazoan signaling. Structural analysis of the extracellular and intracellular domains of these receptors has shed substantial light on the mechanisms underlying their activation. A remaining challenge is to understand how these domains operate together in the context of the full-length receptors. With a focus on the epidermal growth factor (EGF) receptor, this review highlights recent advances towards this goal. Although receptor tyrosine kinases are divergent in terms of the details of how they operate, these studies reveal common mechanisms that ensure activation in the proper context. Understanding these mechanisms provides insights into the vulnerabilities of these receptors to disease-causing mutations.
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