Journal
CURRENT TOPICS IN MEDICINAL CHEMISTRY
Volume 9, Issue 5, Pages 428-435Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/156802609788340814
Keywords
HM74a; GPR109a; PUMA-G; Nicotinic Acid; HDL-Cholesterol
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The discovery of HM74a as a high affinity receptor for nicotinic acid has opened up new areas for investigation. Since its discovery, several new chemical entities have been reported as HM74a agonists. One of them, MK-0354, has been tested in phase II studies, but despite significant decreases in Free Fatty Acid levels with absence of flushing events in clinical studies, it failed to demonstrate effects on LDL-Cholesterol, Triglycerides and HDL-Cholesterol. These surprising results lead to questions about the reality of HM74a as the unique receptor responsible for the lipid modulating effects of nicotinic acid. This review summarizes these recent developments, and the novel HM74a antagonist structures recently published.
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