Inhibitors of Hedgehog acyltransferase block Sonic Hedgehog signaling Journal Article
| Authors: | Petrova, E.; Rios Esteves, J.; Ouerfelli, O.; Glickman, J. F.; Resh, M. D. |
| Article Title: | Inhibitors of Hedgehog acyltransferase block Sonic Hedgehog signaling |
| 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. © 2013 Nature America, Inc. All rights reserved. |
| Keywords: | signal transduction; controlled study; protein expression; unclassified drug; nonhuman; animal cell; mouse; enzyme inhibition; sonic hedgehog protein; animal experiment; animal model; drug structure; high throughput screening; in vitro study; autocrine effect; paracrine signaling; drug labeling; erinaceidae; chemical modification; palmitoylation; palmitic acid; acyltransferase inhibitor; renilla; hedgehog acyltransferase inhibitor; ru ski 39; ru ski 41; ru ski 43; ru ski 50 |
| Journal Title: | Nature Chemical Biology |
| Volume: | 9 |
| Issue: | 4 |
| ISSN: | 1552-4450 |
| Publisher: | Nature Publishing Group |
| Date Published: | 2013-04-01 |
| Start Page: | 247 |
| End Page: | 249 |
| Language: | English |
| PROVIDER: | scopus |
| PMCID: | PMC3604071 |
| PUBMED: | 23416332 |
| DOI: | 10.1038/nchembio.1184 |
| DOI/URL: | |
| Notes: | --- - Cited By (since 1996):1 - "Export Date: 1 May 2013" - "CODEN: NCBAB" - ":doi 10.1038/nchembio.1184" - ": Chemicals/CASpalmitic acid, 57-10-3" - "Source: Scopus" |
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