Niacin receptor 1

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niacin receptor 1
Identifiers
SymbolsNIACR1; GPR109A; PUMAG; Puma-g; HM74a; HM74b
External IDsOMIM: 609163 MGI: 1933383 HomoloGene: 4391 IUPHAR: GeneCards: NIACR1 Gene
Orthologs
SpeciesHumanMouse
Entrez33844280885
EnsemblENSG00000182782ENSMUSG00000045502
UniProtQ8TDS4Q0VBA6
RefSeq (mRNA)NM_177551NM_030701
RefSeq (protein)NP_808219NP_109626
Location (UCSC)Chr 12:
121.75 - 121.75 Mb		Chr 5:
124.12 - 124.13 Mb
PubMed search[1][2]

Niacin receptor 1, also known as NIACR1 or GPR109A, is a protein which in humans is encoded by the NIACR1 gene.[1][2][3][4]

Function

GPR109A is a high affinity receptor for nicotinic acid (niacin)[3][4] and is a member of the nicotinic acid receptor family of G protein-coupled receptors (the other identified member being GPR109B).

GPR109A is a Gi / Go protein-coupled receptor with high affinity for nicotinic acid.[3]

Clinical significance

GPR109A is believed to be an important biomolecular target of niacin which is a widely prescribed drug for the treatment of dyslipidemia and to increase HDL cholesterol but whose therapeutic use is limited by flushing.[5] In GPR109A knockout mice, the effects of niacin on both lipids[6] and flushing[7] is eliminated. Furthermore in arrestin beta 1 knockout mice, niacin's effect on flushing is greatly reduced while the lipid modifying effects are maintained.[8]

The precise mechanism of action of niacin therapeutic effects has not been fully elucidated but appears to work in part through activation of GPR109A which reduces the levels of intracellular cAMP thereby inhibiting lipolysis in adipocytes.[9] In contrast, the flushing effect is due to GPR109A activation of ERK 1/2 MAP kinase[10] mediated by arrestin beta 1.[8] Activation of MAP kinase in turn causes release of prostaglandin D2 from Langerhans cells in the skin.[11]

References

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External links

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Class A: Rhodopsin like
α1 (A, B, D) · α2 (A, B, C) · β1 · β2 · β3
Adenosine (A1, A2A, A2B, A3) · P2Y (1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14)
(all but 5-HT3) 5-HT1 (A, B, D, E, F) · 5-HT2 (A, B, C) · 5-HT (4, 5A, 6, 7)
Other
Acetylcholine (M1, M2, M3, M4, M5) · Dopamine (D1, D2, D3, D4, D5) · Histamine (H1, H2, H3, H4) · Melatonin (1A, 1B, 1C) · TAAR (1, 2, 3, 5, 6, 8, 9)
Metabolites and
signaling molecules
CysLT (1, 2) · LTB4 (1, 2) · FPRL1 · OXE · Prostaglandin (DP (1, 2), EP (1, 2, 3, 4), FP) · Prostacyclin · Thromboxane
Other
Bile acid · Cannabinoid (CB1, CB2, GPR (18, 55, 119)) · EBI2 · Estrogen · Free fatty acid (1, 2, 3, 4) · Lactate  · Lysophosphatidic acid (1, 2, 3, 4, 5, 6)  · Lysophospholipid (1, 2, 3, 4, 5, 6, 7, 8) · Niacin (1, 2) · Oxoglutarate · PAF · Sphingosine-1-phosphate (1, 2, 3, 4, 5) · Succinate
Peptide
B/W (1, 2) · FF (1, 2) · S · Y (1, 2, 4, 5) · Neuromedin (B, U (1, 2)) · Neurotensin (1, 2)
Other
Miscellaneous
GPR (1, 3, 4, 6, 12, 15, 17, 18, 19, 20, 21, 22, 23, 25, 26, 27, 31, 32, 33, 34, 35, 37, 39, 42, 44, 45, 50, 52, 55, 61, 62, 63, 65, 68, 75, 77, 78, 81, 82, 83, 84, 85, 87, 88, 92, 101, 103, 109A, 109B, 119, 120, 132, 135, 137B, 139, 141, 142, 146, 148, 149, 150, 151, 152, 153, 160, 161, 162, 171, 173, 174, 176, 177, 182, 183)
Other
Class B: Secretin like
GPR (56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 155, 157)
Other
Class C: Metabotropic
glutamate / pheromone
TAS1R (1, 2, 3) · TAS2R (1, 3, 4, 5, 8, 9, 10, 12, 13, 14, 16, 19, 20, 30, 31, 38, 39, 40, 41, 42, 43, 45, 46, 50)
Other
Class F:
Frizzled / Smoothened
Frizzled
Frizzled (1, 2, 3, 4, 5, 6, 7, 8, 9, 10)
Smoothened
  1. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  2. ↑ "Entrez Gene: GPR109A G protein-coupled receptor 109A". 
  3. ↑ 3.0 3.1 3.2 Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  4. ↑ 4.0 4.1 Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  5. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  6. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  7. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  8. ↑ 8.0 8.1 Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  9. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  10. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  11. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
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