A natural product-like inhibitor of NEDD8-activating enzyme

Chem Commun (Camb). 2011 Mar 7;47(9):2511-3. doi: 10.1039/c0cc04927a. Epub 2011 Jan 14.

Abstract

The natural product-like 6,6″-biapigenin has been identified as only the second inhibitor of NEDD8-activating enzyme using virtual screening. This compound was active in enzyme and cell-based assays, with potency in the micromolar range.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Apigenin / chemistry*
  • Biflavonoids / chemistry*
  • Binding Sites
  • Cell Line, Tumor
  • Computer Simulation
  • Cyclopentanes / chemistry
  • Drug Design
  • Humans
  • NEDD8 Protein
  • Pyrimidines / chemistry
  • Ubiquitins / antagonists & inhibitors*
  • Ubiquitins / metabolism

Substances

  • Biflavonoids
  • Cyclopentanes
  • NEDD8 Protein
  • NEDD8 protein, human
  • Pyrimidines
  • Ubiquitins
  • biapigenin
  • Apigenin
  • pevonedistat