Abstract
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 HDLCholesterol. 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.
Keywords: HM74a, GPR109a, PUMA-G, Nicotinic Acid, HDL-Cholesterol
Current Topics in Medicinal Chemistry
Title: HM74a Agonists: Will they be the New Generation of Nicotinic Acid?
Volume: 9 Issue: 5
Author(s): Paul Martres
Affiliation:
Keywords: HM74a, GPR109a, PUMA-G, Nicotinic Acid, HDL-Cholesterol
Abstract: 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 HDLCholesterol. 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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Cite this article as:
Martres Paul, HM74a Agonists: Will they be the New Generation of Nicotinic Acid?, Current Topics in Medicinal Chemistry 2009; 9 (5) . https://dx.doi.org/10.2174/156802609788340814
DOI https://dx.doi.org/10.2174/156802609788340814 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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