Acyltransferase inhibitors: a patent review (2010–present)

Abstract

Introduction: Acyltransferase (AT) catalyzes the transfer of an acyl moiety from acyl-coenzyme A (acyl-CoA) to an acceptor. ATs play important roles in the maintenance of homeostasis in the human body and have been linked to various diseases; therefore, several ATs have been proposed as potential targets for the treatment or prevention of such diseases. The AT family includes acyl-CoA:cholesterol AT (ACAT), diacylglycerol AT (DGAT), and monoacylglycerol AT (MGAT) for the metabolism of lipids. Furthermore, recent molecular biological studies revealed the existence of their isozymes with distinct functions in the body.

Areas covered: This review summarized patent filings published between 2010 and the present date that claimed isozyme-selective inhibitors of ACAT, DGAT and MGAT, which are involved in neutral lipid metabolism.

Expert opinion: Isozymes of ACAT, DGAT and MGAT play distinct functions in neutral lipid metabolism in the human body and have been considered as potential therapeutic targets. Accordingly, isozyme-selective inhibitors that could be used in the treatment or prevention of lipid metabolism disorders were searched for. Of these, pyripyropene A derivatives, ACAT2-selective inhibitors, may be potential therapeutics for the treatment of atherosclerosis, homozygous familial hypercholesterolemia and nonalcoholic fatty liver disease.

Keywords:

• acyl-CoA:cholesterol acyltransferase
• diacylglycerol acyltransferase
• inhibitor
• isozyme
• monoacylglycerol acyltransferase
• neutral lipid metabolism

Declaration of interest

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Notes

This box summarizes key points contained in the article.