In Search of Selective 11β-HSD 1 Inhibitors without Nephrotoxicity

By Rakesh Jagtap

Over expression of 11β-HSD 1 in key metabolic tissues is related to the development of type 2 diabetes, obesity, hypertension and metabolic syndrome. Nephrotoxicity of corosolic acid (selective inhibitor of 11β-HSD 1) is recently reported, which is one of the major drawback. Therefore, it is of great interest to find out the selective 11β-HSD 1 inhibitors without nephrotoxicity. Using crystal structures of 11β-HSD 1 in complex with inhibitors as a source of structural information, a combined structure-based virtual screening approach followed by PASS toxicity prediction, Lipinski's rule and ADME prediction implemented to find out the potent and selective 11 β-HSD 1 analog of corosolic acid without nephrotoxicity.

• Format: Paperback
• Language: English
• ISBN: 365979001X
• ISBN13: 9783659790010
• Release Date: October 2015
• Publisher: LAP Lambert Academic Publishing
• Length: 56 Pages
• Weight: 0.21 lbs.
• Dimensions: 0.1" x 6.0" x 9.0"