Basic Information
ID: ALA4819086
Journal: Bioorg Med Chem
Title: Discovery of neuroprotective agents that inhibit human prolyl hydroxylase PHD2.
Authors: Richardson NL, O'Malley LJ, Weissberger D, Tumber A, Schofield CJ, Griffith R, Jones NM, Hunter L.
Abstract: Prolyl 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. Cell-based studies demonstrate that these compounds exhibit protective activity in neuroblastoma cells, suggesting that they have the potential to be developed into clinically useful neuroprotective agents.
CiteXplore: 33862469
DOI: 10.1016/j.bmc.2021.116115
Patent ID: ┄
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