Design and Activity of Specific Hypoxia-Inducible Factor-2α (HIF-2α) Inhibitors for the Treatment of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate (S)-3-((2,2-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1H-inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385)
Author:
Affiliation:
1. Peloton Therapeutics, Inc., 2330 Inwood Road, Suite 226, Dallas, Texas 75235, United States
Funder
Cancer Prevention and Research Institute of Texas
Publisher
American Chemical Society (ACS)
Subject
Drug Discovery,Molecular Medicine
Link
https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.8b01196
Reference36 articles.
1. Hypoxia-inducible factor 1 is a basic-helix-loop-helix-PAS heterodimer regulated by cellular O2 tension.
2. Endothelial PAS domain protein 1 (EPAS1), a transcription factor selectively expressed in endothelial cells.
3. Targeting of HIF-α to the von Hippel-Lindau Ubiquitylation Complex by O 2 -Regulated Prolyl Hydroxylation
4. A Conserved Family of Prolyl-4-Hydroxylases That Modify HIF
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