Structure-guided optimisation of <i>N</i>-hydroxythiazole-derived inhibitors of factor inhibiting hypoxia-inducible factor-α
Thomas P. Corner, Ryan Z. R. Teo, Yue Wu, E. Salah, Yu Nakashima, Giorgia Fiorini, Anthony Tumber, Amelia Brasnett, James P. Holt‐Martyn, William D. Figg, Xiaojin Zhang, Lennart Brewitz, Christopher J. Schofield
Abstract
Optimised N -hydroxythiazoles are efficient and selective inhibitors of the 2-oxoglutrate dependent oxygenase factor inhibiting HIF, which has a key role in the human hypoxic response; the inhibitors decrease lipid accumualtion in adipocytes.
Topics & Concepts
Factor (programming language)Hypoxia (environmental)Hypoxia-Inducible Factor 1Hypoxia-inducible factorsChemistryComputational biologyPharmacologyComputer scienceMedicineBiochemistryBiologyTranscription factorOxygenOrganic chemistryGeneProgramming languageCancer, Hypoxia, and MetabolismATP Synthase and ATPases ResearchHigh Altitude and Hypoxia