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Version 2.5
Creation Date 2005-06-13 13:24:05
Update Date 2009-04-16 16:47:51
Primary Accession Number DB00627
Secondary Accession Number
  • APRD00536
  • NUTR00042
Name Niacin
Drug Type
  • Approved
  • Investigational
  • Nutraceutical
  • Small Molecule
Description A water-soluble vitamin of the B complex occurring in various animal and plant tissues. It is required by the body for the formation of coenzymes NAD and NADP. It has pellagra-curative, vasodilating, and antilipemic properties. [PubChem]
Synonyms
  1. 3-Pyridinecarboxylic acid
  2. Acide Nicotinique
  3. Acidum Nicotinicum
  4. M-Pyridinecarboxylic Acid
  5. NAH
  6. Nicotine Acid
  7. Nicotinic Acid
  8. Pyridinecarboxylic Acid
  9. Pyridylcarboxylic Acid
  10. Vitamin B3
  11. niacin
Brand Names
  1. Akotin
  2. Anti-Pellagra Vitamin
  3. Apelagrin
  4. Bionic
  5. Daskil
  6. Davitamon PP
  7. Diacin
  8. Direktan
  9. Efacin
  10. Kyselina Nikotinova
  11. Linic
  12. NICO
  13. Naotin
  14. Niac
  15. Niaspan
  16. Nicacid
  17. Nicangin
  18. Nico-Span
  19. Nicocidin
  20. Nicocrisina
  21. Nicodan
  22. Nicodelmine
  23. Nicodon
  24. Niconacid
  25. Niconat
  26. Niconazid
  27. Nicorol
  28. Nicosan 3
  29. Nicoside
  30. Nicosyl
  31. Nicotamin
  32. Nicotene
  33. Nicotil
  34. Nicotinipca
  35. Nicotinsaure
  36. Nicovasan
  37. Nicovasen
  38. Nicovel
  39. Nicyl
  40. Nipellen
  41. Nyclin
  42. P.P. Factor
  43. PP Factor
  44. Pellagra Preventive Factor
  45. Pellagramin
  46. Pellagrin
  47. Pelonin
  48. Peviton
  49. Simcor
  50. Sk-Niacin
  51. Tega-Span
  52. Tinic
  53. Vitaplex N
Brand Mixtures
  1. Chromium with Niacin and Niacinamide-Liq (Chromium (Chromic Chloride) + Nicotinamide + Nicotinic Acid)
  2. Ff Formula Niacin & Inositol (Inositol + Nicotinic Acid)
  3. Flush Free Niacin with Inositol (Inositol (Inositol Hexanicotinate) + Nicotinic Acid)
  4. Lipofactors & Niacin (Choline (Choline Bitartrate) + Inositol + Nicotinic Acid)
  5. My Favorite Niacin and Inositol Tab (Inositol + Nicotinic Acid)
  6. Niacin 500 Mg and Inositol (Inositol + Nicotinic Acid)
  7. Niacin Capsules with Chromium (Chromium + Nicotinic Acid)
  8. Niacin and Inositol (Inositol + Nicotinic Acid)
  9. Niacin-Niacinamide Tab (Nicotinamide + Nicotinic Acid)
  10. No Flush Niacin with Inositol (Inositol (Inositol Hexanicotinate) + Nicotinic Acid)
  11. One Tablet Daily High Potency B Complex and C (Beta-Carotene + Copper (Cupric Oxide) + D-Pantothenic Acid (Calcium D-Pantothenate) + Folic Acid + Iron (Ferrous Fumarate) + Nicotinamide (Niacin Ascorbate) + Vitamin a (Vitamin a Acetate) + Vitamin B1 (Thiamine Mononitrate) + Vitamin B12 + Vitamin B2 + Vitamin B6 + Vitamin C + Vitamin D + Vitamin E (Dl-Alpha Tocopheryl Acetate) + Zinc (Zinc Oxide))
  12. One a Day Advance High Pot.B Complex and C (Beta-Carotene + Copper (Cupric Oxide) + D-Pantothenic Acid (Calcium D-Pantothenate) + Dl-Alpha Tocopheryl Acetate + Folic Acid + Iron (Ferrous Fumarate) + Nicotinamide (Niacin Ascorbate) + Thiamine Mononitrate + Vitamin a Acetate + Vitamin B12 + Vitamin B2 + Vitamin B6 + Vitamin C + Vitamin D + Zinc (Zinc Oxide))
  13. Primanol-Borage with Niacin and Chromium Tab (Chromium (Chromium Hvp Chelate) + Gamma-Linolenic Acid (Borage Oil) + Nicotinic Acid)
  14. Vitamin C with Niacin and Niacinamide-Liq (Nicotinamide + Nicotinic Acid + Vitamin C)
Chemical IUPAC Name pyridine-3-carboxylic acid
Chemical Formula C6H5NO2
Chemical Structure Structure
CAS Registry Number 59-67-6
InChI Identifier InChI=1/C6H5NO2/c8-6(9)5-2-1-3-7-4-5/h1-4H,(H,8,9)/f/h8H
InChI Key PVNIIMVLHYAWGP-FZOZFQFYCF
KEGG Drug D00049 Link Image
KEGG Compound C00253 Link Image
PubChem Compound 938 Link Image
PubChem Substance 442239 Link Image
ChEBI ID 15940 Link Image
PharmGKB ID PA450617 Link Image
HET ID NIO Link Image
GenBank ID Not Available
Drug ID Number [DIN] 02245265 Link Image
RxList Link http://www.rxlist.com/cgi/generic3/niacor.htm Link Image
PDRhealth Link Not Available
Wikipedia Link http://en.wikipedia.org/wiki/Niacin Link Image
FDA Label
Material Safety Data Sheet (MSDS)
Synthesis Reference Not Available
Average Molecular Weight 123.1094
Monoisotopic Molecular Weight 123.0320
State Solid
Melting Point 237 oC
Experimental Water Solubility 18 mg/mL at 25 oC [YALKOWSKY,SH & DANNENFELSER,RM (1992)] Source: PhysProp
Predicted Water Solubility 8.31e+01 mg/mL Calculated using ALOGPS
Experimental LogP/Hydrophobicity 0.4 Source: PhysProp
Predicted LogP 0.29 Calculated using ALOGPS
Experimental LogS -0.84 [ADME Research, USCD]
Predicted LogS -0.17 Calculated using ALOGPS
Experimental Caco2 Permeability Not Available
pKa/Isoelectric Point 4.75
Mass Spectrum Not Available
MOL File Show Link Image | Download Link Image
SDF File Show Link Image | Download Link Image
PDB File Show Link Image | Download Link Image
2D Structure
3D Structure
Experimental PDB ID 1ICR Link Image
Experimental PDB File Show
Experimental PDB Structure
Isomeric SMILES OC(=O)C1=CN=CC=C1
Canonical SMILES OC(=O)C1=CN=CC=C1
Drug Category
  • Antilipemic Agents
  • Vasodilator Agents
  • Vitamin B Complex
  • Vitamins (Vitamin B Complex)
ATC Codes
AHFS Codes
  • 24:06.92
  • 88:08.00
Indication For the treatment of type IV and V hyperlipidemia. It is indicated as ajunctive therapy.
Pharmacology Niacin and niacinamide are indicated for prevention and treatment of vitamin B3 deficiency states. Vitamin B3 (Niacin) also acts to reduce LDL cholesterol, triglycerides, and HDL cholesterol. The magnitude of individual lipid and lipoprotein responses may be influenced by the severity and type of underlying lipid abnormality. The increase in total HDL is associated with a shift in the distribution of HDL subfractions (as defined by ultra-centrifugation) with an increase in the HDL2:HDL3 ratio and an increase in apolipoprotein A-I content. Vitamin B3 (Niacin) treatment also decreases the serum levels of apolipoprotein B-100 (apo B), the major protein component of the VLDL (very low-density lipoprotein) and LDL fractions, and of lipoprotein-a, a variant form of LDL independently associated with coronary risk.
Mechanism of Action Niacin binds to Nicotinate D-ribonucleotide phyrophsopate phosphoribosyltransferase, Nicotinic acid phosphoribosyltransferase, Nicotinate N-methyltransferase and the Niacin receptor. Niacin is the precursor to nicotinamide adenine dinucleotide (NAD) and nicotinamide adenine dinucleotide phosphate (NADP), which are vital cofactors for dozens of enzymes. The mechanism by which niacin exerts its lipid lowering effects is not entirely understood, but may involve several actions, including a decrease in esterification of hepatic triglycerides. Niacin treatment also decreases the serum levels of apolipoprotein B-100 (apo B), the major protein component of the VLDL (very low-density lipoprotein) and LDL fractions.
Absorption Both nicotinic acid and nicotinamide are efficiently absorbed from the stomach and small intestine.
Toxicity Nicotinic acid can cause vasodilation of cutaneous blood vessels resulting in increased blood flow, principally in the face, neck and chest. This produces the niacin- or nicotinic acid-flush. The niacin-flush is thought to be mediated via the prostaglandin prostacyclin. Histamine may also play a role in the niacin-flush. Flushing is the adverse reaction first observed after intake of a large dose of nicotinic acid, and the most bothersome one. LD50 7000 mg/kg (Rat)
Protein Binding Not Available
Biotransformation Hepatic
Half Life 20-45 minutes.
Dosage Forms
Form Route
Capsule Oral
Capsule, extended release Oral
Powder Oral
Solution Intramuscular
Tablet Oral
Tablet, extended release Oral
Patient Information Show Link Image
Contraindications Show Link Image
Interactions Show Link Image
Drug Interactions
Drug Interaction
Lovastatin Risk of severe myopathy/rhabdomyolysis with this combination
Food Interactions
  • Avoid alcohol.
  • Take with food.
Pathways Not Available
General References
  1. Drugs.com Link Image
  2. Wikipedia Link Image
  3. RxList Link Image
Organisms Affected
  • Humans and other mammals
Targets
  1. Nicotinate-nucleotide pyrophosphorylase [carboxylating]
  2. Nicotinic acid receptor 1
  3. Nicotinamide N-methyltransferase
  4. Nicotinic acid receptor 2
Drug Target 1 [top]
Target 1 ID 583
Target 1 Name Nicotinate-nucleotide pyrophosphorylase [carboxylating]
Target 1 Synonyms
  1. EC 2.4.2.19
  2. QAPRTase
  3. QPRTase
  4. Quinolinate phosphoribosyltransferase [decarboxylating]
Target 1 Gene Name QPRT
Target 1 Protein Sequence >Nicotinate-nucleotide pyrophosphorylase [carboxylating] 
MDAEGLALLLPPVTLAALVDSWLREDCPGLNYAALVSGAGPSQAALWAKSPGVLAGQPFF
DAIFTQLNCQVSWFLPEGSKLVPVARVAEVRGPAHCLLLGERVALNTLARCSGIASAAAA
AVEAARGAGWTGHVAGTRKTTPGFRLVEKYGLLVGGAASHRYDLGGLVMVKDNHVVAAGG
VEKAVRAARQAADFALKVEVECSSLQEAVQAAEAGADLVLLDNFKPEELHPTATVLKAQF
PSVAVEASGGITLDNLPQFCGPHIDVISMGMLTQAAPALDFSLKLFAKEVAPVPKIH
Target 1 Number of Residues 301
Target 1 Molecular Weight 30816
Target 1 Theoretical pI 6.15
Target 1 GO Classification
Function
nicotinate-nucleotide diphosphorylase (carboxylating) activity
catalytic activity
transferase activity
transferase activity, transferring glycosyl groups
transferase activity, transferring pentosyl groups
nicotinate-nucleotide diphosphorylase (carboxylating) activity
Process
NAD biosynthesis
physiological process
metabolism
cellular metabolism
cofactor metabolism
coenzyme metabolism
coenzyme biosynthesis
pyridine nucleotide biosynthesis
Component
Not Available
Target 1 General Function Coenzyme transport and metabolism
Target 1 Specific Function Not Available
Target 1 Pathways
Name SMPDB Link KEGG Link
Nicotinate and nicotinamide metabolism SMP00048 Link Image map00760 Link Image
Target 1 Reactions
  • nicotinate D-ribonucleotide + diphosphate + CO2 = pyridine-2,3-dicarboxylate + 5-phospho-alpha-D-ribose 1-diphosphate
Target 1 Pfam Domain Function
Target 1 Signals
  • None
Target 1 Transmembrane Regions
  • None
Target 1 Essentiality Non-Essential
Target 1 GenBank ID Protein 1060907 Link Image
Target 1 UniProtKB/Swiss-Prot ID Q15274 Link Image
Target 1 UniProtKB/Swiss-Prot Entry Name NADC_HUMAN Link Image
Target 1 PDB ID Not Available
Target 1 Cellular Location Not Available
Target 1 Gene Sequence >894 bp 
ATGGACGCTGAAGGCCTGGCGCTGCTGCTGCCGCCCGTCACCCTGGCAGCCCTGGTGGAC
AGCTGGCTCCGAGAGGACTGCCCAGGGCTCAACTACGCAGCCTTGGTCAGCGGGGCAGGC
CCCTCGCAGGCGGCGCTGTGGGCCAAATCCCCTGGGGTACTGGCAGGGCAGCCTTTCTTC
GATGCCATATTTACCCAACTCAACTGCCAAGTCTCCTGGTTCCTCCCCGAGGGATCGAAG
CTGGTGCCGGTGGCCAGAGTGGCCGAGGTCCGGGGCCCTGCCCACTGCCTGCTGCTGGGG
GAACGGGTGGCCCTCAACACGCTGGCCCGCTGCAGTGGCATTGCCAGTGCTGCCGCCGCT
GCAGTGGAGGCCGCCAGGGGGGCCGGCTGGACTGGGCACGTGGCAGGCACGAGGAAGACC
ACGCCAGGCTTCCGGCTGGTGGAGAAGTATGGGCTCCTGGTGGGCGGGGCCGCCTCGCAC
CGCTACGACCTGGGAGGGCTGGTGATGTTGAAGGATAACCATGTGGTGCCCCCCGGTGGC
GTGGAGAAGGCGGTGCGGGCGGCCAGACAGGCGGCTGACTTCGCTCTGAAGGTGGAAGTG
GAATGCAGCAGCCTGCAGGAGGTCGTCCAGGCAGCTGAGGCTGGCGCCGACCTTGTCCTG
CTGGACAACTTCAAGCCAGAGGAGCTGCACCCCACGGCCACCGCGCTGAAGGCCCAGTTC
CCGAGTGTGGCTGTGGAAGCCAGTGGGGGCATCACCCTGGACAACCTCCCCCAGTTCTGC
GGGCCGCACATAGACGTCATCTCCATGGGGATGCTGACCCAGGCGGTCCCAGCCCTTGAT
TTCTCCCTCAAGCTGTTTGCCAAAGAGGTGGCTCCAGTGCCCAAAATCCACTAG
Target 1 GenBank Gene ID
Target 1 GeneCard ID QPRT Link Image
Target 1 GenAtlas ID QPRT Link Image
Target 1 HGNC ID HGNC:9755 Link Image
Target 1 Chromosome Location 16
Target 1 Locus 16p11.2
Target 1 SNPs SNPJam Report Link Image
Target 1 General References
  1. Fukuoka SI, Nyaruhucha CM, Shibata K: Characterization and functional expression of the cDNA encoding human brain quinolinate phosphoribosyltransferase. Biochim Biophys Acta. 1998 Jan 21;1395(2):192-201. [PubMed Link Image]
Target 1 Drug References
  1. Fukuwatari T, Morikawa Y, Hayakawa F, Sugimoto E, Shibata K: Influence of adenine-induced renal failure on tryptophan-niacin metabolism in rats. Biosci Biotechnol Biochem. 2001 Oct;65(10):2154-61. [PubMed Link Image]
  2. Shin DH, Oganesyan N, Jancarik J, Yokota H, Kim R, Kim SH: Crystal structure of a nicotinate phosphoribosyltransferase from Thermoplasma acidophilum. J Biol Chem. 2005 May 6;280(18):18326-35. Epub 2005 Mar 6. [PubMed Link Image]
  3. Zheng XQ, Hayashibe E, Ashihara H: Changes in trigonelline (N-methylnicotinic acid) content and nicotinic acid metabolism during germination of mungbean (Phaseolus aureus) seeds. J Exp Bot. 2005 Jun;56(416):1615-23. Epub 2005 Apr 18. [PubMed Link Image]
Drug Target 2 [top]
Target 2 ID 699
Target 2 Name Nicotinic acid receptor 1
Target 2 Synonyms
  1. G-protein coupled receptor 109A
  2. G-protein coupled receptor HM74A
Target 2 Gene Name GPR109A
Target 2 Protein Sequence >Nicotinic acid receptor 1 
MNRHHLQDHFLEIDKKNCCVFRDDFIVKVLPPVLGLEFIFGLLGNGLALWIFCFHLKSWK
SSRIFLFNLAVADFLLIICLPFLMDNYVRRWDWKFGDIPCRLMLFMLAMNRQGSIIFLTV
VAVDRYFRVVHPHHALNKISNRTAAIISCLLWGITIGLTVHLLKKKMPIQNGGANLCSSF
SICHTFQWHEAMFLLEFFLPLGIILFCSARIIWSLRQRQMDRHAKIKRAITFIMVVAIVF
VICFLPSVVVRIRIFWLLHTSGTQNCEVYRSVDLAFFITLSFTYMNSMLDPVVYYFSSPS
FPNFFSTLINRCLQRKMTGEPDNNRSTSVELTGDPNKTRGAPEALMANSGEPWSPSYLGP
TSP
Target 2 Number of Residues 369
Target 2 Molecular Weight 41850
Target 2 Theoretical pI 9.37
Target 2 GO Classification
Function
nucleotide receptor activity, G-protein coupled
purinergic nucleotide receptor activity, G-protein coupled
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 2 General Function Involved in rhodopsin-like receptor activity
Target 2 Specific Function Acts as a high affinity receptor for nicotinic acid and mediates its anti-lipolytic effect through a 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
Target 2 Pathways Not Available
Target 2 Reactions Not Available
Target 2 Pfam Domain Function
Target 2 Signals
  • None
Target 2 Transmembrane Regions
  • 34-54
  • 64-84
  • 103-123
  • 143-163
  • 193-213
  • 230-250
  • 274-294
Target 2 Essentiality Non-Essential
Target 2 GenBank ID Protein 28975188 Link Image
Target 2 UniProtKB/Swiss-Prot ID Q8TDS4 Link Image
Target 2 UniProtKB/Swiss-Prot Entry Name G109A_HUMAN Link Image
Target 2 PDB ID Not Available
Target 2 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 2 Gene Sequence >1092 bp 
ATGAATCGGCACCATCTGCAGGATCACTTTCTGGAAATAGACAAGAAGAACTGCTGTGTG
TTCCGAGATGACTTCATTGTCAAGGTGTTGCCGCCGGTGTTGGGGCTGGAGTTTATCTTC
GGGCTTCTGGGCAATGGCCTTGCCCTGTGGATTTTCTGTTTCCACCTCAAGTCCTGGAAA
TCCAGCCGGATTTTCCTGTTCAACCTGGCAGTGGCTGACTTTCTACTGATCATCTGCCTG
CCCTTCCTGATGGACAACTATGTGAGGCGTTGGGACTGGAAGTTTGGGGACATCCCTTGC
CGGCTGATGCTCTTCATGTTGGCTATGAACCGCCAGGGCAGCATCATCTTCCTCACGGTG
GTGGCGGTAGACAGGTATTTCCGGGTGGTCCATCCCCACCACGCCCTGAACAAGATCTCC
AATCGGACAGCAGCCATCATCTCTTGCCTTCTGTGGGGCATCACTATTGGCCTGACAGTC
CACCTCCTGAAGAAGAAGATGCCGATCCAGAATGGCGGTGCAAATTTGTGCAGCAGCTTC
AGCATCTGCCATACCTTCCAGTGGCACGAAGCCATGTTCCTCCTGGAGTTCTTCCTGCCC
CTGGGCATCATCCTGTTCTGCTCAGCCAGAATTATCTGGAGCCTGCGGCAGAGACAAATG
GACCGGCATGCCAAGATCAAGAGAGCCATCACCTTCATCATGGTGGTGGCCATCGTCTTT
GTCATCTGCTTCCTTCCCAGCGTGGTTGTGCGGATCCGCATCTTCTGGCTCCTGCACACT
TCGGGCACGCAGAATTGTGAAGTGTACCGCTCGGTGGACCTGGCGTTCTTTATCACTCTC
AGCTTCACCTACATGAACAGCATGCTGGACCCCGTGGTGTACTATTTTTCCAGCCCATCC
TTTCCCAACTTCTTCTCCACTTTGATCAACCGCTGCCTCCAGAGGAAGATGACAGGTGAG
CCAGATAATAACCGCAGCACGAGCGTCGAGCTCACAGGGGACCCCAACAAAACCAGAGGC
GCTCCAGAGGCGTTAATGGCCAACTCCGGTGAGCCATGGAGCCCCTCTTATCTGGGCCCA
ACCTCTCCTTAA
Target 2 GenBank Gene ID
Target 2 GeneCard ID GPR109A Link Image
Target 2 GenAtlas ID GPR109A Link Image
Target 2 HGNC ID HGNC:24827 Link Image
Target 2 Chromosome Location 12
Target 2 Locus 12q24.31
Target 2 SNPs SNPJam Report Link Image
Target 2 General References
  1. 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. [PubMed Link Image]
  2. 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. [PubMed Link Image]
Target 2 Drug 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. [PubMed Link Image]
  2. Soga T, Kamohara M, Takasaki J, Matsumoto S, Saito T, Ohishi T, Hiyama H, Matsuo A, Matsushime H, Furuichi K: Molecular identification of nicotinic acid receptor. Biochem Biophys Res Commun. 2003 Mar 28;303(1):364-9. [PubMed Link Image]
  3. Zellner C, Pullinger CR, Aouizerat BE, Frost PH, Kwok PY, Malloy MJ, Kane JP: Variations in human HM74 (GPR109B) and HM74A (GPR109A) niacin receptors. Hum Mutat. 2005 Jan;25(1):18-21. [PubMed Link Image]
  4. Zhang Y, Schmidt RJ, Foxworthy P, Emkey R, Oler JK, Large TH, Wang H, Su EW, Mosior MK, Eacho PI, Cao G: Niacin mediates lipolysis in adipose tissue through its G-protein coupled receptor HM74A. Biochem Biophys Res Commun. 2005 Aug 26;334(2):729-32. [PubMed Link Image]
  5. Tunaru S, Lattig J, Kero J, Krause G, Offermanns S: Characterization of determinants of ligand binding to the nicotinic acid receptor GPR109A (HM74A/PUMA-G). Mol Pharmacol. 2005 Nov;68(5):1271-80. Epub 2005 Aug 11. [PubMed Link Image]
Drug Target 3 [top]
Target 3 ID 860
Target 3 Name Nicotinamide N-methyltransferase
Target 3 Synonyms
  1. EC 2.1.1.1
Target 3 Gene Name NNMT
Target 3 Protein Sequence >Nicotinamide N-methyltransferase 
MESGFTSKDTYLSHFNPRDYLEKYYKFGSRHSAESQILKHLLKNLFKIFCLDGVKGDLLI
DIGSGPTIYQLLSACESFKEIVVTDYSDQNLQELEKWLKKEPEAFDWSPVVTYVCDLEGN
RVKGPEKEEKLRQAVKQVLKCDVTQSQPLGAVPLPPADCVLSTLCLDAACPDLPTYCRAL
RNLGSLLKPGGFLVIMDALKSSYYMIGEQKFSSLPLGREAVEAAVKEAGYTIEWFEVISQ
SYSSTMANNEGLFSLVARKLSRPL
Target 3 Number of Residues 268
Target 3 Molecular Weight 29574
Target 3 Theoretical pI 5.45
Target 3 GO Classification
Function
catalytic activity
transferase activity
transferase activity, transferring one-carbon groups
methyltransferase activity
Process
Not Available
Component
Not Available
Target 3 General Function Involved in methyltransferase activity
Target 3 Specific Function Catalyzes the N-methylation of nicotinamide and other pyridines to form pyridinium ions. This activity is important for biotransformation of many drugs and xenobiotic compounds
Target 3 Pathways
Name SMPDB Link KEGG Link
Nicotinate and nicotinamide metabolism SMP00048 Link Image map00760 Link Image
Target 3 Reactions
  • S-adenosyl-L-methionine + nicotinamide = S-adenosyl-L-homocysteine + 1-methylnicotinamide
Target 3 Pfam Domain Function
Target 3 Signals
  • None
Target 3 Transmembrane Regions
  • None
Target 3 Essentiality Non-Essential
Target 3 GenBank ID Protein 494989 Link Image
Target 3 UniProtKB/Swiss-Prot ID P40261 Link Image
Target 3 UniProtKB/Swiss-Prot Entry Name NNMT_HUMAN Link Image
Target 3 PDB ID Not Available
Target 3 Cellular Location
  • Cytoplasm
Target 3 Gene Sequence >795 bp 
ATGGAATCAGGCTTCACCTCCAAGGACACCTATCTAAGCCATTTTAACCCTCGGGATTAC
CTAGAAAAATATTACAAGTTTGGTTCTAGGCACTCTGCAGAAAGCCAGATTCTTAAGCAC
CTTCTGAAAAATCTTTTCAAGATATTCTGCCTAGACGGTGTGAAGGGAGACCTGCTGATT
GACATCGGCTCTGGCCCCACTATCTATCAGCTCCTCTCTGCTTGTGAATCCTTTAAGGAG
ATCGTCGTCACTGACTACTCAGACCAGAACCTGCAGGAGCTGGAGAAGTGGCTGAAGAAA
GAGCCAGAGGCCTTTGACTGGTCCCCAGTGGTGACCTATGTGTGTGATCTTGAAGGGAAC
AGAGTCAAGGGTCCAGAGAAGGAGGAGAAGTTGAGACAGGCGGTCAAGCAGGTGCTGAAG
TGTGATGTGACTCAGAGCCAGCCACTGGGGGCCGTCCCCTTACCCCCGGCTGACTGCGTG
CTCAGCACACTGTGTCTGGATGCCGCCTGCCCAGACCTCCCCACCTACTGCAGGGCGCTC
AGGAACCTCGGCAGCCTACTGAAGCCAGGGGGCTTCCTGGTGATCATGGATGCGCTCAAG
AGCAGCTACTACATGATTGGTGAGCAGAAGTTCTCCAGCCTCCCCCTGGGCCGGGAGGCA
GTAGAGGCTGCTGTGAAAGAGGCTGGCTACACAATCGAATGGTTTGAGGTGATCTCGCAA
AGTTATTCTTCCACCATGGCCAACAACGAAGGACTTTTCTCCCTGGTGGCGAGGAAGCTG
AGCAGACCCCTGTGA
Target 3 GenBank Gene ID
Target 3 GeneCard ID NNMT Link Image
Target 3 GenAtlas ID NNMT Link Image
Target 3 HGNC ID HGNC:7861 Link Image
Target 3 Chromosome Location 11
Target 3 Locus 11q23.1
Target 3 SNPs SNPJam Report Link Image
Target 3 General References
  1. Hubbard MJ, McHugh NJ: Human ERp29: isolation, primary structural characterisation and two-dimensional gel mapping. Electrophoresis. 2000 Nov;21(17):3785-96. [PubMed Link Image]
  2. Aksoy S, Szumlanski CL, Weinshilboum RM: Human liver nicotinamide N-methyltransferase. cDNA cloning, expression, and biochemical characterization. J Biol Chem. 1994 May 20;269(20):14835-40. [PubMed Link Image]
  3. Aksoy S, Brandriff BF, Ward A, Little PF, Weinshilboum RM: Human nicotinamide N-methyltransferase gene: molecular cloning, structural characterization and chromosomal localization. Genomics. 1995 Oct 10;29(3):555-61. [PubMed Link Image]
Target 3 Drug References
  1. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed Link Image]
  2. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Drug Target 4 [top]
Target 4 ID 928
Target 4 Name Nicotinic acid receptor 2
Target 4 Synonyms
  1. G-protein coupled receptor 109B
  2. G-protein coupled receptor HM74
  3. G-protein coupled receptor HM74B
Target 4 Gene Name GPR109B
Target 4 Protein Sequence >Nicotinic acid receptor 2 
MNRHHLQDHFLEIDKKNCCVFRDDFIAKVLPPVLGLEFIFGLLGNGLALWIFCFHLKSWK
SSRIFLFNLAVADFLLIICLPFVMDYYVRRSDWKFGDIPCRLVLFMFAMNRQGSIIFLTV
VAVDRYFRVVHPHHALNKISNWTAAIISCLLWGITVGLTVHLLKKKLLIQNGPANVCISF
SICHTFRWHEAMFLLEFLLPLGIILFCSARIIWSLRQRQMDRHAKIKRAITFIMVVAIVF
VICFLPSVVVRIRIFWLLHTSGTQNCEVYRSVDLAFFITLSFTYMNSMLDPVVYYFSSPS
FPNFFSTLINRCLQRKMTGEPDNNRSTSVELTGDPNKTRGAPEALMANSGEPWSPSYLGP
TSNNHSKKGHCHQEPASLEKQLGCCIE
Target 4 Number of Residues 393
Target 4 Molecular Weight 44496
Target 4 Theoretical pI 9.01
Target 4 GO Classification
Function
nucleotide receptor activity, G-protein coupled
purinergic nucleotide receptor activity, G-protein coupled
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 4 General Function Involved in rhodopsin-like receptor activity
Target 4 Specific Function Acts as a low affinity receptor for nicotinic acid and mediate its anti-lipolytic effect through a 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
Target 4 Pathways Not Available
Target 4 Reactions Not Available
Target 4 Pfam Domain Function
Target 4 Signals
  • None
Target 4 Transmembrane Regions
  • 29-50
  • 64-85
  • 103-123
  • 143-163
  • 195-209
  • 237-256
  • 274-298
Target 4 Essentiality Non-Essential
Target 4 GenBank ID Protein 219867 Link Image
Target 4 UniProtKB/Swiss-Prot ID P49019 Link Image
Target 4 UniProtKB/Swiss-Prot Entry Name G109B_HUMAN Link Image
Target 4 PDB ID Not Available
Target 4 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 4 Gene Sequence >1164 bp 
ATGAATCGGCACCATCTGCAGGATCACTTTCTGGAAATAGACAAGAAGAACTGCTGTGTG
TTCCGAGATGACTTCATTGCCAAGGTGTTGCCGCCGGTGTTGGGGCTGGAGTTTATCTTT
GGGCTTCTGGGCAATGGCCTTGCCCTGTGGATTTTCTGTTTCCACCTCAAGTCCTGGAAA
TCCAGCCGGATTTTCCTGTTCAACCTGGCAGTAGCTGACTTTCTACTGATCATCTGCCTG
CCGTTCGTGATGGACTACTATGTGCGGCGTTCAGACTGGAACTTTGGGGACATCCCTTGC
CGGCTGGTGCTCTTCATGTTTGCCATGAACCGCCAGGGCAGCATCATCTTCCTCACGGTG
GTGGCGGTAGACAGGTATTTCCGGGTGGTCCATCCCCACCACGCCCTGAACAAGATCTCC
AATTGGACAGCAGCCATCATCTCTTGCCTTCTGTGGGGCATCACTGTTGGCCTAACAGTC
CACCTCCTGAAGAAGAAGTTGCTGATCCAGAATGGCCCTGCAAATGTGTGCATCAGCTTC
AGCATCTGCCATACCTTCCGGTGGCACGAAGCTATGTTCCTCCTGGAGTTCCTCCTGCCC
CTGGGCATCATCCTGTTCTGCTCAGCCAGAATTATCTGGAGCCTGCGGCAGAGACAAATG
GACCGGCATGCCAAGATCAAGAGAGCCATCACCTTCATCATGGTGGTGGCCATCGTCTTT
GTCATCTGCTTCCTTCCCAGCGTGGTTGTGCGGATCCGCATCTTCTGGCTCCTGCACACT
TCGGGCACGCAGAATTGTGAAGTGTACCGCTCGGTGGACCTGGCGTTCTTTATCACTCTC
AGCTTCACCTACATGAACAGCATGCTGGACCCCGTGGTGTACTACTTCTCCAGCCCATCC
TTTCCCAACTTCTTCTCCACTTTGATCAACCGCTGCCTCCAGAGGAAGATGACAGGTGAG
CCAGATAATAACCGCAGCACGAGCGTCGAGCTCACAGGGGACCCCAACAAAACCAGAGGC
GCTCCAGAGGCGTTAATGGCCAACTCCGGTGAGCCATGGAGCCCCTCTTATCTGGGCCCA
ACCTCAAATAACCATTCCAAGAAGGGACATTGTCACCAAGAACCAGCATCTCTGGAGAAA
CAGTTGGGCTGTTGCATCGAGTAA
Target 4 GenBank Gene ID
Target 4 GeneCard ID GPR109B Link Image
Target 4 GenAtlas ID GPR109B Link Image
Target 4 HGNC ID HGNC:16824 Link Image
Target 4 Chromosome Location 12
Target 4 Locus 12q24.31
Target 4 SNPs SNPJam Report Link Image
Target 4 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. [PubMed Link Image]
  2. Nomura H, Nielsen BW, Matsushima K: Molecular cloning of cDNAs encoding a LD78 receptor and putative leukocyte chemotactic peptide receptors. Int Immunol. 1993 Oct;5(10):1239-49. [PubMed Link Image]
Target 4 Drug References
  1. Tunaru S, Kero J, Schaub A, Wufka C, Blaukat A, Pfeffer K, Offermanns S: PUMA-G and HM74 are receptors for nicotinic acid and mediate its anti-lipolytic effect. Nat Med. 2003 Mar;9(3):352-5. Epub 2003 Feb 3. [PubMed Link Image]
  2. Taggart AK, Kero J, Gan X, Cai TQ, Cheng K, Ippolito M, Ren N, Kaplan R, Wu K, Wu TJ, Jin L, Liaw C, Chen R, Richman J, Connolly D, Offermanns S, Wright SD, Waters MG: (D)-beta-Hydroxybutyrate inhibits adipocyte lipolysis via the nicotinic acid receptor PUMA-G. J Biol Chem. 2005 Jul 22;280(29):26649-52. Epub 2005 Jun 1. [PubMed Link Image]
  3. Zhang Y, Schmidt RJ, Foxworthy P, Emkey R, Oler JK, Large TH, Wang H, Su EW, Mosior MK, Eacho PI, Cao G: Niacin mediates lipolysis in adipose tissue through its G-protein coupled receptor HM74A. Biochem Biophys Res Commun. 2005 Aug 26;334(2):729-32. [PubMed Link Image]
  4. Tunaru S, Lattig J, Kero J, Krause G, Offermanns S: Characterization of determinants of ligand binding to the nicotinic acid receptor GPR109A (HM74A/PUMA-G). Mol Pharmacol. 2005 Nov;68(5):1271-80. Epub 2005 Aug 11. [PubMed Link Image]
  5. Benyo Z, Gille A, Kero J, Csiky M, Suchankova MC, Nusing RM, Moers A, Pfeffer K, Offermanns S: GPR109A (PUMA-G/HM74A) mediates nicotinic acid-induced flushing. J Clin Invest. 2005 Dec;115(12):3634-40. [PubMed Link Image]

This project is supported by Genome Alberta & Genome Canada, a not-for-profit organization that is leading Canada's national genomics strategy with $600 million in funding from the federal government. This project is also supported in part by GenomeQuest, Inc., an enterprise genomic information company serving the life science community.