Extending the reach of covalent drugs | April 24, 2017 Issue - Vol. 95 Issue 17 | Chemical & Engineering News
Volume 95 Issue 17 | p. 6 | News of The Week
Issue Date: April 24, 2017

Extending the reach of covalent drugs

Inhibitors that bond covalently with oxidized protein residues could represent a new class of drugs
Department: Science & Technology
News Channels: Organic SCENE, JACS In C&EN
Keywords: drug discovery, cysteine, sulfenylation, electrophile, nucleophile, phosphatases

The ability of covalent drugs to form strong bonds to protein targets tends to give them the advantage of long-lasting action. So far, covalent drug discovery has almost exclusively involved electrophilic small molecules that react with cysteine thiol groups (–SH) on proteins. The approved anticancer drug afatinib, for instance, is an electrophile that bonds covalently to a cysteine in epidermal growth factor receptor. A new study could help expand the reach of covalent drugs to . . .

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