Article
Molecular Basis for Redox Activation of Epidermal Growth Factor Receptor Kinase.
Cell chemical biology - 21 Jul 2016
Truong Thu H, Ung Peter Man-Un, Palde Prakash B, Paulsen Candice E, Schlessinger Avner, Carroll Kate S
Abstract excerpt
Epidermal growth factor receptor (EGFR) is a target of signal-derived H2O2, and oxidation of active-site cysteine 797 to sulfenic acid enhances kinase activity. Although a major class of covalent drugs targets C797, nothing is known about its catalytic importance or how S-sulfenylation leads to activation. Here, we report the first detailed functional analysis of C797. In contrast to prior assumptions, mutation...
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