Distinctive molecular inhibition mechanisms for selective inhibitors of human 11β-hydroxysteroid dehydrogenase type 1

Hua Tu,Jay P. Powers,Jinsong Liu,Stefania Ursu,Athena Sudom,Xuelei Yan,Haoda Xu,David Meininger,Michael DeGraffenreid,Xiao He,Juan C. Jaen,Daqing Sun,Marc Labelle,Hiroshi Yamamoto,Bei Shan,Nigel P.C. Walker,Zhulun Wang

Bioorganic & Medicinal Chemistry（2008）

Cited 43|Views10

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Abstract

The synthesis, X-ray co-crystal structures and kinetic analysis of two novel and potent small molecule inhibitors of 11β-HSD1 are reported. Structural and kinetic analyses demonstrate two distinctive molecular inhibition mechanisms for the two classes of inhibitors.

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Key words

11β-Hydroxysteroid dehydrogenase (11β-HSD1),Small molecule inhibitor,Inhibition mechanism,Enzyme kinetics,Crystal structure,X-ray crystallography

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