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Small-molecule inhibitors of the interaction between the E3 ligase VHL and HIF1α.

Buckley DL, Gustafson JL, Van Molle I, Roth AG, Tae HS, Gareiss PC, Jorgensen WL, Ciulli A, Crews CM
Angew Chem Int Ed Engl 51 11463-7 (2012)
Cited: 107 times
EuropePMC logo PMID: 23065727

Abstract

E3 ubiquitin ligases, such as the therapeutically relevant VHL, are challenging targets for traditional medicinal chemistry, as their modulation requires targeting protein-protein interactions. We report novel small-molecule inhibitors of the interaction between VHL and its molecular target HIF1α, a transcription factor involved in oxygen sensing.

Articles - 4b95 mentioned but not cited (2)

  1. Discovery of novel inhibitors disrupting HIF-1α/von Hippel-Lindau interaction through shape-based screening and cascade docking. Xue X, Zhao NY, Yu HT, Sun Y, Kang C, Huang QB, Sun HP, Wang XL, Li NG. PeerJ 4 e2757 (2016)
  2. Preparing a database of corrected protein structures important in cell signaling pathways. Hatami S, Sirous H, Mahnam K, Najafipour A, Fassihi A. Res Pharm Sci 18 67-77 (2023)


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