Galdeano, Carles published the artcileStructure-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, Application In Synthesis of 87150-13-8, the main research area is von Hippel Lindau protein ubiquitin ligase hypoxia inducible factor; crystal structure complex thiasole preparation.
E3 ubiquitin ligases are attractive targets in the ubiquitin-proteasome system, however, the development of small-mol. 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 The authors recently reported inhibitors of the pVHL:HIF-1α interaction, however they exhibited moderate potency. Herein, the authors report the design and optimization, guided by x-ray crystal structures, of a ligand series with nanomolar binding affinities.
Journal of Medicinal Chemistry published new progress about Crystal structure. 87150-13-8 belongs to class nitriles-buliding-blocks, name is 4-(5-Oxazolyl)benzonitrile, and the molecular formula is C10H6N2O, Application In Synthesis of 87150-13-8.
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts