Volume 89 Issue 36 | pp. 19-26
Issue Date: September 5, 2011

Cover Story

Covalent Drugs Form Long-Lived Ties

Irreversible inhibitors may provide unique benefits in drug development
Department: Science & Technology
News Channels: Organic SCENE, Biological SCENE
Keywords: covalent drugs, irreversible inhibitors, drug discovery, drug design, Pfizer, Avila, Zafgen

When most small-molecule drugs meet a protein target, they nestle close to their intended. But the flirtatious relationship between drug and target is often fleeting, with the drug repeatedly drifting away and coming back. Like a teenager with no interest in settling down, the drug forms no permanent bond with its target.

Some small molecules, however, do forge lasting ties. Their irreversible covalent bonds with proteins link compound and protein for good.

The pharmaceutical industry . . .

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