Target Information

Target General Infomation
Target ID
T88185
Former ID
TTDC00317
Target Name
Nicotinic acid receptor
Synonyms
G-protein coupled receptor 109A; G-protein coupled receptor HM74A; GPR109A; HM74A; NIACR1; Niacin receptor 1
Target Type
Successful
Disease Lipid disorder; Cardiovascular disease [ICD9: 272, 390-459; ICD10: E78, I00-I99]
Function
Acts as a high affinity receptor for both nicotinic acid (also known as niacin) and (d)-beta-hydroxybutyrate and mediates increased adiponectin secretion and decreased lipolysis through g(i)-protein-mediated inhibition of adenylyl cyclase. This pharmacological effect requires nicotinic acid doses that are much higher than those provided by a normal diet. Mediates nicotinic acid-induced apoptosis in mature neutrophils.
Target Validation
T88185
Drugs and Mode of Action
Drug(s) Vitamin B3 Drug Info Approved Lipid disorder; Cardiovascular disease [526373]
MK-0354 Drug Info Phase 2 Discovery agent [521843], [541103]
Inhibitor 1H-Pyrazole-3-carboxylic acid Drug Info [526698]
2-(2-(4-tert-butylphenoxy)acetamido)benzoic acid Drug Info [529664]
2-(3-(naphthalen-2-yl)propanamido)benzoic acid Drug Info [529664]
2-(3-biphenyl-4-yl-propionylamino)-benzoic acid Drug Info [529144]
2-(4-phenylbutyl)pyrido[2,3-d]pyrimidin-4(3H)-one Drug Info [531113]
2-(6-phenylhexyl)pyrido[2,3-d]pyrimidin-4(3H)-one Drug Info [531113]
2-(cinnamyloxy)pyrido[2,3-d]pyrimidin-4(3H)-one Drug Info [531113]
4,5,6,7-Tetrahydro-1H-indazole-3-carboxylic acid Drug Info [526698]
5-(3-Chloro-benzyl)-1H-pyrazole-3-carboxylic acid Drug Info [526698]
5-(3-Phenyl-propyl)-1H-pyrazole-3-carboxylic acid Drug Info [526698]
5-(4-Chloro-benzyl)-1H-pyrazole-3-carboxylic acid Drug Info [526698]
5-Benzyl-1H-pyrazole-3-carboxylic acid Drug Info [526698]
5-Butyl-1H-pyrazole-3-carboxylic acid Drug Info [526698]
5-Isopropyl-1H-pyrazole-3-carboxylic acid Drug Info [526698]
5-Phenethyl-1H-pyrazole-3-carboxylic acid Drug Info [526698]
5-Propyl-1H-pyrazole-3-carboxylic acid Drug Info [526698]
ISONICOTINIC ACID Drug Info [526698]
MK-0354 Drug Info [531020]
Agonist Vitamin B3 Drug Info [526373]
References
Ref 521843ClinicalTrials.gov (NCT00337415) MK0354 Clinical Efficacy and Tolerability Study (0354-004). U.S. National Institutes of Health.
Ref 526373Hakozaki T, Minwalla L, Zhuang J, Chhoa M, Matsubara A, Miyamoto K, Greatens A, Hillebrand GG, Bissett DL, Boissy RE: The effect of niacinamide on reducing cutaneous pigmentation and suppression of melanosome transfer. Br J Dermatol. 2002 Jul;147(1):20-31.
Ref 541103(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5784).
Ref 526373Hakozaki T, Minwalla L, Zhuang J, Chhoa M, Matsubara A, Miyamoto K, Greatens A, Hillebrand GG, Bissett DL, Boissy RE: The effect of niacinamide on reducing cutaneous pigmentation and suppression of melanosome transfer. Br J Dermatol. 2002 Jul;147(1):20-31.
Ref 526698J Med Chem. 2003 Aug 28;46(18):3945-51.Pyrazole derivatives as partial agonists for the nicotinic acid receptor.
Ref 529144J Med Chem. 2007 Dec 13;50(25):6303-6. Epub 2007 Nov 10.Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptor.
Ref 529664Bioorg Med Chem Lett. 2008 Sep 15;18(18):4963-7. Epub 2008 Aug 14.Molecular modeling aided design of nicotinic acid receptor GPR109A agonists.
Ref 531020Bioorg Med Chem Lett. 2010 Aug 1;20(15):4472-4. Epub 2010 Jun 10.GPR109a agonists. Part 2: pyrazole-acids as agonists of the human orphan G-protein coupled receptor GPR109a.
Ref 531113Bioorg Med Chem Lett. 2010 Sep 15;20(18):5426-30. Epub 2010 Jul 29.Pyrido pyrimidinones as selective agonists of the high affinity niacin receptor GPR109A: optimization of in vitro activity.
Ref 1587926URL: https://www.ebi.ac.uk/chembl/ The ChEMBL database in 2017

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