Article
Coupling of receptor conformation and ligand orientation determine graded activity.
Nature chemical biology - 1 Nov 2010
Bruning John B, Parent Alexander A, Gil German, Zhao Min, Nowak Jason, Pace Margaret C, Smith Carolyn L, Afonine Pavel V, Adams Paul D, Katzenellenbogen John A, Nettles Kendall W
Abstract excerpt
Small molecules stabilize specific protein conformations from a larger ensemble, enabling molecular switches that control diverse cellular functions. We show here that the converse also holds true: the conformational state of the estrogen receptor can direct distinct orientations of the bound ligand. 'Gain-of-allostery' mutations that mimic the effects of ligand in driving protein conformation allowed...
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