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Discovery of neuroprotective agents that inhibit human prolyl hydroxylase PHD2
Bioorg Med Chem. 2021 Mar 24;38:116115. doi: 10.1016/j.bmc.2021.116115. Online ahead of print.ABSTRACTProlyl hydroxylase (PHD) enzymes play a critical role in the cellular responses to hypoxia through their regulation of the hypoxia inducible factor α (HIF-α) transcription factors. PHD inhibitors show promise for the treatment of diseases including anaemia, cardiovascular disease and stroke. In this work, a pharmacophore-based virtual high throughput screen was used to identify novel potential inhibitors of human PHD2. Two moderately potent new inhibitors were discovered, with IC50 values of 4 μM and 23 μM respectively...
Source: Bioorganic and Medicinal Chemistry - April 16, 2021 Category: Chemistry Authors: Nicole L Richardson Laura J O'Malley Daniel Weissberger Anthony Tumber Christopher J Schofield Renate Griffith Nicole M Jones Luke Hunter Source Type: research