Nicotinic acid receptor subtypes and their ligands

@article{Soudijn2007NicotinicAR,
  title={Nicotinic acid receptor subtypes and their ligands},
  author={Willem Soudijn and Ineke van Wijngaarden and Adriaan P. IJzerman},
  journal={Medicinal Research Reviews},
  year={2007},
  volume={27}
}
Half a century ago, nicotinic acid (niacin) was introduced into the clinic as the first orally available drug to treat high cholesterol levels and to improve the balance between (V)low density lipoproteins (LDL) and high density lipoproteins (HDL). Remarkably, its putative mechanism of action has only been recently elucidated, particularly because of the cloning of a G protein‐coupled receptor (HM74A or GPR109A). This receptor responds to both nicotinic acid and the ketone body… 
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TLDR
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TLDR
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Niacin in cardiovascular prevention: mechanisms, efficacy, and safety
  • J. Guyton
  • Biology, Medicine
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  • 2007
TLDR
Understanding of the mechanisms, efficacy, and safety of niacin, along with progress in reducing the chief side effect of flushing, should enhance the use of this valuable agent for cardiovascular prevention.
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TLDR
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TLDR
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TLDR
It is shown that the orphan G-protein-coupled receptor, 'protein upregulated in macrophages by interferon-γ' (mouse PUMA-G, human HM74), is highly expressed in adipose tissue and is a nicotinic acid receptor.
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TLDR
G protein activation in adipocyte membranes in the presence of maximally activating concentrations of the selective A(1) adenosine receptor agonist 2-chloro-N(6)-cyclopentyladenosine and nicotinic acid was almost additive, indicating that G proteins of mostly distinct pools were activated by these agonists.
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TLDR
The data suggest that the ligand binding pocket for nicotinic acid of GPR109A is distinct from that of most other group A receptors, which will facilitate the design of new antidyslipidemic drugs acting via GPR 109A.
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TLDR
The identification of this elusive receptor is described, and the evidence suggesting that this may be the molecular target for the clinical effects of nicotinic acid is outlined.
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TLDR
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