Article
Stabilization of warfarin-binding pocket of VKORC1 and VKORL1 by a peripheral region determines their different sensitivity to warfarin inhibition.
Journal of thrombosis and haemostasis : JTH - 1 Jun 2018
Shen G, Li S, Cui W, Liu S, Liu Q, Yang Y, Gross M, Li W
Abstract excerpt
Essentials VKORL1 and VKORC1 have a similar overall structure and warfarin-binding pocket. A peripheral region stabilizing this pocket controls warfarin sensitivity of the VKOR paralogs. A human single nucleotide polymorphism in this region renders VKORL1 sensitive to warfarin. A group of warfarin-resistant mutations in VKORC1 acts by disrupting peripheral interactions. SUMMARY: Background The human genome...
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