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.
Export Options
About this article
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 |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Sunlight Vitamin D and Skin Cancer
Anti-Cancer Agents in Medicinal Chemistry Prostaglandin EP Receptor Subtypes Involved in Regulating HCO3- Secretion from Gastroduodenal Mucosa
Current Pharmaceutical Design Patenting Penicillium Strains
Recent Patents on Biotechnology Noncoding Variants Functional Prioritization Methods Based on Predicted Regulatory Factor Binding Sites
Current Genomics Chemokines and Chemokine Receptors Blockers as New Drugs for the Treatment of Chronic Obstructive Pulmonary Disease
Current Medicinal Chemistry Pre-eclampsia Versus Cardiovascular Disease Versus CRP
Current Hypertension Reviews Involvement of P-glycoprotein and Multidrug Resistance Associated Protein 1 in the Transport of Tanshinone IIB, a Primary Active Diterpenoid Quinone from the Roots of Salvia miltiorrhiza, Across the Blood-Brain Barrier
Drug Metabolism Letters Risk Factors and Potential Preventive Measures for Vascular Disease Progression in Hemodialysis Patients
Vascular Disease Prevention (Discontinued) Some Important Dietary Polyphenolic Compounds: An Anti-inflammatory and Immunoregulatory Perspective
Mini-Reviews in Medicinal Chemistry Editorial: Time for Earlier and More Intensive Preventive Therapy
Current Vascular Pharmacology Heart Failure Pharmacotherapy and Supports in the Elderly - A Short Review
Current Cardiology Reviews The Role of Amino Acids in the Modulation of Cardiac Metabolism During Ischemia and Heart Failure
Current Pharmaceutical Design One-Compound-Multi-Target: Combination Prospect of Natural Compounds with Thrombolytic Therapy in Acute Ischemic Stroke
Current Neuropharmacology Common Comorbidities that Alter Heart Failure Prognosis - Shaping New Thinking for Practice
Current Cardiology Reviews The Role of Vitamin D in Dyslipidemia and Cardiovascular Disease
Current Pharmaceutical Design Understanding and Avoiding Antiretroviral Adverse Events
Current Pharmaceutical Design ATP-Sensitive Potassium Channels
Current Pharmaceutical Design Vitamin D3, D2 and Arterial Wall Properties in Coronary Artery Disease
Current Pharmaceutical Design Pleiotropic Actions of PPARg Activators Thiazolidinediones in Cardiovascular Diseases
Current Pharmaceutical Design Highest Mortality During the Last Year Before and the First Year After Start of Dialysis Treatment in Type 2 Diabetic Patients with Nephropathy
Current Diabetes Reviews