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Future of GPR109A agonists in the treatment of dyslipidaemia.
Diabetes Obes Metab. 2011 Aug; 13(8):685-91.DO

Abstract

Abnormal blood lipids are the major modifiable risk factor underlying the development of cardiovascular disease. Niacin has a profound ability to reduce low-density lipoprotein-C, very low-density lipoprotein-C and triglycerides and is the most effective pharmacological agent to increase high-density lipoprotein-C. Recently, the receptor for niacin, GPR109A, was discovered. GPR109A in the adipocyte mediates a niacin-induced inhibition of lipolysis, which could play a crucial part in its role as a lipid-modifying drug. GPR109A in epidermal Langerhans cells mediates flushing, an unwanted side effect of niacin therapy. For the past decade, the functions of GPR109A have been studied and full or partial agonists have been developed in an attempt to achieve the beneficial effects of niacin while avoiding the unwanted flushing side effect. This review presents what is known to date about GPR109A biology and function and the future of GPR109A as a pharmacological target.

Authors+Show Affiliations

Department of Anatomy, Physiology and Pharmacology, College of Veterinary Medicine, Auburn University, Auburn, AL 36849, USA.No affiliation info available

Pub Type(s)

Journal Article
Review

Language

eng

PubMed ID

21418500

Citation

Wanders, D, and R L. Judd. "Future of GPR109A Agonists in the Treatment of Dyslipidaemia." Diabetes, Obesity & Metabolism, vol. 13, no. 8, 2011, pp. 685-91.
Wanders D, Judd RL. Future of GPR109A agonists in the treatment of dyslipidaemia. Diabetes Obes Metab. 2011;13(8):685-91.
Wanders, D., & Judd, R. L. (2011). Future of GPR109A agonists in the treatment of dyslipidaemia. Diabetes, Obesity & Metabolism, 13(8), 685-91. https://doi.org/10.1111/j.1463-1326.2011.01400.x
Wanders D, Judd RL. Future of GPR109A Agonists in the Treatment of Dyslipidaemia. Diabetes Obes Metab. 2011;13(8):685-91. PubMed PMID: 21418500.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Future of GPR109A agonists in the treatment of dyslipidaemia. AU - Wanders,D, AU - Judd,R L, PY - 2011/3/23/entrez PY - 2011/3/23/pubmed PY - 2011/9/17/medline SP - 685 EP - 91 JF - Diabetes, obesity & metabolism JO - Diabetes Obes Metab VL - 13 IS - 8 N2 - Abnormal blood lipids are the major modifiable risk factor underlying the development of cardiovascular disease. Niacin has a profound ability to reduce low-density lipoprotein-C, very low-density lipoprotein-C and triglycerides and is the most effective pharmacological agent to increase high-density lipoprotein-C. Recently, the receptor for niacin, GPR109A, was discovered. GPR109A in the adipocyte mediates a niacin-induced inhibition of lipolysis, which could play a crucial part in its role as a lipid-modifying drug. GPR109A in epidermal Langerhans cells mediates flushing, an unwanted side effect of niacin therapy. For the past decade, the functions of GPR109A have been studied and full or partial agonists have been developed in an attempt to achieve the beneficial effects of niacin while avoiding the unwanted flushing side effect. This review presents what is known to date about GPR109A biology and function and the future of GPR109A as a pharmacological target. SN - 1463-1326 UR - https://www.unboundmedicine.com/medline/citation/21418500/Future_of_GPR109A_agonists_in_the_treatment_of_dyslipidaemia_ L2 - https://doi.org/10.1111/j.1463-1326.2011.01400.x DB - PRIME DP - Unbound Medicine ER -