11beta-HSD1 focused library from OTAVA

VAUGHAN, ON - Nov 14, 2014 - 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1, 11beta-HSD1) is an NADPH-dependent enzyme, which catalyses conversion of inactive glucocorticoids 11-dehydrocorticosterone and cortisone to active corticosterone and cortisol and vice versa. 11beta-HSD1 is also implicated in the regulation of glucocorticoid access to nuclear receptors.

Chronically increased levels of glucocorticoids are associated with the development of obesity, diabetes, cardiovascular disease (the metabolic syndrome) and impairments in memory. Dysregulation of 11beta-HSD1 has been reported to be involved in all of these human pathologies. It was demonstrated that the inhibition of 11beta-HSD1 activity decreased hypertension, insulin resistance, glucose intolerance, and hypertriglyceridemia. Therefore, 11beta-HSD1 is an attractive drug target for the treatment of the metabolic syndrome and cognitive impairment.

OTAVA Ltd. offers new 11beta-hydroxysteroid dehydrogenase type 1 target-focused library containing 1,060 compounds which has been designed with receptor-based approach that included docking of Drug-like Green Collection in the active site of human 11beta-HSD1 (PDB ID: 4C7K) and filtering by score values and hydrogen bonds formed between ligand and key residues of the 11beta-HSD1 active site. The library comprises drug-like compounds only.

The 11beta-HSD1 focused library from OTAVA is an excellent choice for drug discovery in endocrine and metabolic disorders treatment. More information about this library you can find at the web-site www.otavachemicals.com.