Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 191, Issue -, Pages -Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2020.112134
Keywords
11 beta-HSD1 inhibitors; Metabolic syndrome; Obesity; Type 2 diabetes; Structure-activity relationships; Molecular modeling
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Funding
- National Key R&D Program of China [2018YFA0800804]
- Hong Kong General Research Fund [HKBU12136616, HKBU12103519]
- National Natural Science Foundation Council of China [81702189]
- National Natural Science Foundation of China [21602252]
- Hong Kong Scholars Program [XJ201713]
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11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1) is a key metabolic enzyme that catalyzing the intracellular conversion of inactive glucocorticoids to physiologically active ones. Work over the past decade has demonstrated the aberrant overexpression of 11 beta-HSD1 contributed to the pathophysiological process of metabolic diseases like obesity, type 2 diabetes mellitus, and metabolic syndromes. The inhibition of 11 beta-HSD1 represented an attractive therapeutic strategy for the treatment of metabolic diseases. Therefore, great efforts have been devoted to developing 11 beta-HSD1 inhibitors based on the diverse molecular scaffolds. This review focused on the structural features of the most important 11 beta-HSD1 inhibitors and categorized them into natural products derivatives and synthetic compounds. We also briefly discussed the optimization process, binding modes, structure-activity relationships (SAR) and biological evaluations of each inhibitor. Moreover, the challenges and directions for 11 beta-HSD1 inhibitors were discussed, which might provide some useful clues to guide the future discovery of novel 11 beta-HSD1 inhibitors. (c) 2020 Elsevier Masson SAS. All rights reserved.
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