Hydroxycarboxylic acid receptor 2

Details

Name
Hydroxycarboxylic acid receptor 2
Synonyms
  • G-protein coupled receptor 109A
  • G-protein coupled receptor HM74A
  • GPR109A
  • HCA2
  • HM74A
  • Niacin receptor 1
  • NIACR1
  • Nicotinic acid receptor
Gene Name
HCAR2
Organism
Humans
Amino acid sequence
>lcl|BSEQ0010442|Hydroxycarboxylic acid receptor 2 MNRHHLQDHFLEIDKKNCCVFRDDFIVKVLPPVLGLEFIFGLLGNGLALWIFCFHLKSWK SSRIFLFNLAVADFLLIICLPFLMDNYVRRWDWKFGDIPCRLMLFMLAMNRQGSIIFLTV VAVDRYFRVVHPHHALNKISNRTAAIISCLLWGITIGLTVHLLKKKMPIQNGGANLCSSF SICHTFQWHEAMFLLEFFLPLGIILFCSARIIWSLRQRQMDRHAKIKRAITFIMVVAIVF VICFLPSVVVRIRIFWLLHTSGTQNCEVYRSVDLAFFITLSFTYMNSMLDPVVYYFSSPS FPNFFSTLINRCLQRKMTGEPDNNRSTSVELTGDPNKTRGAPEALMANSGEPWSPSYLGP TSP
Number of residues
363
分子量
41849.08
Theoretical pI
9.37
GO Classification
Functions
nicotinic acid receptor activity
Processes
negative regulation of lipid catabolic process/neutrophil apoptotic process/positive regulation of adiponectin secretion/positive regulation of neutrophil apoptotic process
Components
cell junction/integral component of membrane/plasma membrane
General Function
Nicotinic acid receptor activity
Specific 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. Receptor activation by nicotinic acid results in reduced cAMP levels which may affect activity of cAMP-dependent protein kinase A and phosphorylation of target proteins, leading to neutrophil apoptosis. The rank order of potency for the displacement of nicotinic acid binding is 5-methyl pyrazole-3-carboxylic acid = pyridine-3-acetic acid > acifran > 5-methyl nicotinic acid = acipimox >> nicotinuric acid = nicotinamide.
Pfam Domain Function
Transmembrane Regions
34-54 64-84 103-123 143-163 193-213 230-250 274-294
Cellular Location
细胞会员ane
Gene sequence
>lcl|BSEQ0010443|Hydroxycarboxylic acid receptor 2 (HCAR2) ATGAATCGGCACCATCTGCAGGATCACTTTCTGGAAATAGACAAGAAGAACTGCTGTGTG TTCCGAGATGACTTCATTGTCAAGGTGTTGCCGCCGGTGTTGGGGCTGGAGTTTATCTTC GGGCTTCTGGGCAATGGCCTTGCCCTGTGGATTTTCTGTTTCCACCTCAAGTCCTGGAAA TCCAGCCGGATTTTCCTGTTCAACCTGGCAGTGGCTGACTTTCTACTGATCATCTGCCTG CCCTTCCTGATGGACAACTATGTGAGGCGTTGGGACTGGAAGTTTGGGGACATCCCTTGC CGGCTGATGCTCTTCATGTTGGCTATGAACCGCCAGGGCAGCATCATCTTCCTCACGGTG GTGGCGGTAGACAGGTATTTCCGGGTGGTCCATCCCCACCACGCCCTGAACAAGATCTCC AATCGGACAGCAGCCATCATCTCTTGCCTTCTGTGGGGCATCACTATTGGCCTGACAGTC CACCTCCTGAAGAAGAAGATGCCGATCCAGAATGGCGGTGCAAATTTGTGCAGCAGCTTC AGCATCTGCCATACCTTCCAGTGGCACGAAGCCATGTTCCTCCTGGAGTTCTTCCTGCCC CTGGGCATCATCCTGTTCTGCTCAGCCAGAATTATCTGGAGCCTGCGGCAGAGACAAATG GACCGGCATGCCAAGATCAAGAGAGCCATCACCTTCATCATGGTGGTGGCCATCGTCTTT GTCATCTGCTTCCTTCCCAGCGTGGTTGTGCGGATCCGCATCTTCTGGCTCCTGCACACT TCGGGCACGCAGAATTGTGAAGTGTACCGCTCGGTGGACCTGGCGTTCTTTATCACTCTC AGCTTCACCTACATGAACAGCATGCTGGACCCCGTGGTGTACTACTTCTCCAGCCCATCC TTTCCCAACTTCTTCTCCACTTTGATCAACCGCTGCCTCCAGAGGAAGATGACAGGTGAG CCAGATAATAACCGCAGCACGAGCGTCGAGCTCACAGGGGACCCCAACAAAACCAGAGGC GCTCCAGAGGCGTTAATGGCCAACTCCGGTGAGCCATGGAGCCCCTCTTATCTGGGCCCA ACCTCTCCTTAA
Chromosome Location
12
Locus
12q24.31
External Identifiers
资源 Link
UniProtKB ID Q8TDS4
UniProtKB Entry Name HCAR2_HUMAN
GenBank Protein ID 28975188
GenBank Gene ID AY148884
GenAtlas ID GPR109A
HGNC ID HGNC:24827
General References
  1. Wise A, Foord SM, Fraser NJ, Barnes AA, Elshourbagy N, Eilert M, Ignar DM, Murdock PR, Steplewski K, Green A, Brown AJ, Dowell SJ, Szekeres PG, Hassall DG, Marshall FH, Wilson S, Pike NB: Molecular identification of high and low affinity receptors for nicotinic acid. J Biol Chem. 2003 Mar 14;278(11):9869-74. Epub 2003 Jan 9. [Article]
  2. Takeda S, Kadowaki S, Haga T, Takaesu H, Mitaku S: Identification of G protein-coupled receptor genes from the human genome sequence. FEBS Lett. 2002 Jun 5;520(1-3):97-101. [Article]
  3. Gerhard DS, Wagner L, Feingold EA, Shenmen CM, Grouse LH, Schuler G, Klein SL, Old S, Rasooly R, Good P, Guyer M, Peck AM, Derge JG, Lipman D, Collins FS, Jang W, Sherry S, Feolo M, Misquitta L, Lee E, Rotmistrovsky K, Greenhut SF, Schaefer CF, Buetow K, Bonner TI, Haussler D, Kent J, Kiekhaus M, Furey T, Brent M, Prange C, Schreiber K, Shapiro N, Bhat NK, Hopkins RF, Hsie F, Driscoll T, Soares MB, Casavant TL, Scheetz TE, Brown-stein MJ, Usdin TB, Toshiyuki S, Carninci P, Piao Y, Dudekula DB, Ko MS, Kawakami K, Suzuki Y, Sugano S, Gruber CE, Smith MR, Simmons B, Moore T, Waterman R, Johnson SL, Ruan Y, Wei CL, Mathavan S, Gunaratne PH, Wu J, Garcia AM, Hulyk SW, Fuh E, Yuan Y, Sneed A, Kowis C, Hodgson A, Muzny DM, McPherson J, Gibbs RA, Fahey J, Helton E, Ketteman M, Madan A, Rodrigues S, Sanchez A, Whiting M, Madari A, Young AC, Wetherby KD, Granite SJ, Kwong PN, Brinkley CP, Pearson RL, Bouffard GG, Blakesly RW, Green ED, Dickson MC, Rodriguez AC, Grimwood J, Schmutz J, Myers RM, Butterfield YS, Griffith M, Griffith OL, Krzywinski MI, Liao N, Morin R, Palmquist D, Petrescu AS, Skalska U, Smailus DE, Stott JM, Schnerch A, Schein JE, Jones SJ, Holt RA, Baross A, Marra MA, Clifton S, Makowski KA, Bosak S, Malek J: The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). Genome Res. 2004 Oct;14(10B):2121-7. [Article]
  4. Kostylina G, Simon D, Fey MF, Yousefi S, Simon HU: Neutrophil apoptosis mediated by nicotinic acid receptors (GPR109A). Cell Death Differ. 2008 Jan;15(1):134-42. Epub 2007 Oct 12. [Article]
  5. Offermanns S, Colletti SL, Lovenberg TW, Semple G, Wise A, IJzerman AP: International Union of Basic and Clinical Pharmacology. LXXXII: Nomenclature and Classification of Hydroxy-carboxylic Acid Receptors (GPR81, GPR109A, and GPR109B). Pharmacol Rev. 2011 Jun;63(2):269-90. doi: 10.1124/pr.110.003301. Epub 2011 Mar 31. [Article]

Drug Relations

Drug Relations
DrugBank ID Name Drug group Pharmacological action? Actions Details
DB00627 Niacin approved, investigational, nutraceutical yes agonist Details
DB08949 Inositol nicotinate approved, withdrawn yes agonist Details
DB00257 Clotrimazole approved, vet_approved unknown partial agonist Details