Since the identification of the membrane-bound O-acyltransferase (MBOATs) protein family in the early 2000s, three distinct members [porcupine (PORCN), hedgehog (Hh) acyltransferase (HHAT) and ghrelin O-acyltransferase (GOAT)] have been shown to acylate specific proteins or peptides. In this review, topology determination, development of assays to measure enzymatic activities and discovery of small molecule inhibitors are compared and discussed for each of these enzymes.
- ghrelin O-acyltransferase (GOAT)
- hedgehog acyltransferase (HHAT)
- membrane-bound O-acyltransferases (MBOATs)
- porcupine (PORCN)
Protein Acylation: from Mechanism to Drug Discovery: Held at the University of Edinburgh, U.K., 10–12 September 2014.
Abbreviations: ACAT, acyl–coA:cholesterol acyltransferase; ER, endoplasmic reticulum; GOAT, ghrelin O-acyltransferase; Hh, hedgehog; HHAT, hedgehog acyltransferase; IWP, inhibitors of Wnt production; MBOAT, membrane-bound O-acyltransferase; Panc-1, pancreatic cancer; PORCN, porcupine; RL, re-entrant loop; Shh, sonic hedgehog; SOAT, sterol O-acyltransferase; TMD, transmembrane domain; UAG, unacylated ghrelin
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