2. Academic Validation
  3. Inhibitors of Hedgehog acyltransferase block Sonic Hedgehog signaling

Inhibitors of Hedgehog acyltransferase block Sonic Hedgehog signaling

  • Nat Chem Biol. 2013 Apr;9(4):247-9. doi: 10.1038/nchembio.1184.
Elissaveta Petrova 1,  Jessica Rios-Esteves,  Ouathek Ouerfelli,  J Fraser Glickman,  Marilyn D Resh
Affiliations

Affiliation

  • 1 Cell Biology Program, Memorial Sloan-Kettering Cancer Center, New York, New York, USA.
PMID: 23416332 DOI: 10.1038/nchembio.1184
Abstract

Inhibition of Sonic Hedgehog (Shh) signaling is of great clinical interest. Here we exploit Hedgehog Acyltransferase (Hhat)-mediated Shh palmitoylation, a modification critical for Shh signaling, as a new target for Shh pathway inhibition. A target-oriented high-throughput screen was used to identify small-molecule inhibitors of Hhat. In cells, these Hhat inhibitors specifically block Shh palmitoylation and inhibit autocrine and paracrine Shh signaling.

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