108 research outputs found
Structure-guided design and optimization of small molecules targeting the protein-protein interaction between the von hippel-lindau (VHL) E3 ubiquitin ligase and the hypoxia inducible factor (HIF) alpha subunit with in vitro nanomolar affinities
E3 ubiquitin ligases are attractive targets in the ubiquitin-proteasome system, however, the development of small-molecule ligands has been rewarded with limited success. The von Hippel-Lindau protein (pVHL) is the substrate recognition subunit of the VHL E3 ligase that targets HIF-1α for degradation. We recently reported inhibitors of the pVHL:HIF-1α interaction, however they exhibited moderate potency. Herein, we report the design and optimization, guided by X-ray crystal structures, of a ligand series with nanomolar binding affinities
Regulation of Erythropoietin Expression in the Nervous System: The Hypoxia Inducible Factor
Oxidation by 2-oxoglutarate oxygenases: non-haem iron systems in catalysis and signalling
The pattern of the expression of hypoxia-inducible factor (HIF-1α) in the neocortex and hippocampus of rats after the presentation of different modes of hypobaric hypoxia
Role of hypoxia-inducible factor-1α in formation of multidrug resistance induced by microenvironment in hepatocellular carcinoma
Transcription Association of VHL and SDH Mutations Link Hypoxia and Oxidoreductase Signals in Pheochromocytomas
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