Target Information

Target General Infomation
Target ID
T30563
Former ID
TTDR00545
Target Name
Leukotriene B4 receptor 2
Gene Name
LTB4R2
Synonyms
LTB4 receptor JULF2; LTB4-R2; Leukotriene B(4) receptor BLT2; Leukotriene B4 receptor BLT2; Seven transmembrane receptor BLTR2; LTB4R2
Target Type
Discontinued
Disease Asthma [ICD10: J45]
Inflammatory bowel disease [ICD9: 555, 556; ICD10: K50, K51]
Function
Low-affinity receptor for leukotrienes including leukotriene B4. Mediates chemotaxis of granulocytes and macrophages. The response is mediated via G-proteins that activate a phosphatidylinositol-calcium second messenger system. The rank order of affinities for the leukotrienes is LTB4 > 12-epi-LTB4 > LTB5 > LTB3.
BioChemical Class
GPCR rhodopsin
Target Validation
T30563
UniProt ID
Q9NPC1
Sequence
MAPSHRASQVGFCPTPERPLWRLPPTCRPRRMSVCYRPPGNETLLSWKTSRATGTAFLLL
AALLGLPGNGFVVWSLAGWRPARGRPLAATLVLHLALADGAVLLLTPLFVAFLTRQAWPL
GQAGCKAVYYVCALSMYASVLLTGLLSLQRCLAVTRPFLAPRLRSPALARRLLLAVWLAA
LLLAVPAAVYRHLWRDRVCQLCHPSPVHAAAHLSLETLTAFVLPFGLMLGCYSVTLARLR
GARWGSGRHGARVGRLVSAIVLAFGLLWAPYHAVNLLQAVAALAPPEGALAKLGGAGQAA
RAGTTALAFFSSSVNPVLYVFTAGDLLPRAGPRFLTRLFEGSGEARGGGRSREGTMELRT
TPQLKVVGQGRGNGDPGGGMEKDGPEWDL
Drugs and Mode of Action
Drug(s) ONO-4057 Drug Info Discontinued in Phase 2 Inflammatory bowel disease [1], [2]
CP-105696 Drug Info Discontinued in Phase 1 Inflammatory bowel disease [3], [4]
LY-255283 Drug Info Terminated Asthma [5], [6]
LY-292728 Drug Info Terminated Discovery agent [7]
Inhibitor (3S,4R)-3-Benzyl-7-isopropyl-chroman-4-ol Drug Info [8]
CP-105696 Drug Info [8]
LEUKOTRIENE_B4 Drug Info [9]
LY-255283 Drug Info [10]
LY-282210 Drug Info [11]
LY-292728 Drug Info [11]
SC-41390 Drug Info [9]
Agonist 12-epi LTB4 Drug Info [12]
12-hydroxyheptadecatrienoic acid Drug Info [13]
12R-HETE Drug Info [14]
12S-HETE Drug Info [12]
20-hydroxy-LTB4 Drug Info [14]
CAY10583 Drug Info [15]
Antagonist BIIL 260 Drug Info [16]
RO5101576 Drug Info [17]
ZK-158252 Drug Info [12]
Modulator ONO-4057 Drug Info [18]
[3H]LTB4 Drug Info [19]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Calcium signaling pathway
Neuroactive ligand-receptor interaction
PANTHER Pathway Inflammation mediated by chemokine and cytokine signaling pathway
Reactome Leukotriene receptors
G alpha (q) signalling events
WikiPathways Gastrin-CREB signalling pathway via PKC and MAPK
GPCR ligand binding
GPCR downstream signaling
GPCRs, Other
References
REF 1(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: 6157).
REF 2Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003085)
REF 3(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: 3368).
REF 4Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005644)
REF 5(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: 3351).
REF 6Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001833)
REF 7Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007211)
REF 83-Substituted-4-hydroxy-7-chromanylacetic acid derivatives as antagonists of the leukotriene B4 (LTB4) receptor, Bioorg. Med. Chem. Lett. 7(17):2307-2312 (1997).
REF 9Diaryl ether/carboxylic acid derivatives of LY255283: Receptor antagonists of leukotriene B4, Bioorg. Med. Chem. Lett. 3(10):1985-1990 (1993).
REF 10J Med Chem. 1993 Nov 26;36(24):3978-81.o-phenylphenols: potent and orally active leukotriene B4 receptor antagonists.
REF 11J Med Chem. 1993 Nov 26;36(24):3982-4.Biphenylyl-substituted xanthones: highly potent leukotriene B4 receptor antagonists.
REF 12Hydroxyeicosanoids bind to and activate the low affinity leukotriene B4 receptor, BLT2. J Biol Chem. 2001 Apr 13;276(15):12454-9. Epub 2001 Jan 18.
REF 1312(S)-Hydroxyheptadeca-5Z, 8E, 10E-trienoic acid is a natural ligand for leukotriene B4 receptor 2. J Exp Med. 2008 Apr 14;205(4):759-66.
REF 14A G-protein-coupled receptor for leukotriene B4 that mediates chemotaxis. Nature. 1997 Jun 5;387(6633):620-4.
REF 15Characterization of a mouse second leukotriene B4 receptor, mBLT2: BLT2-dependent ERK activation and cell migration of primary mouse keratinocytes. J Biol Chem. 2005 Jul 1;280(26):24816-23. Epub 2005 May 2.
REF 16Clinical trial of a leucotriene B4 receptor antagonist, BIIL 284, in patients with rheumatoid arthritis. Ann Rheum Dis. 2007 May;66(5):628-32. Epub 2006 Dec 14.
REF 17Effects of LTB4 receptor antagonism on pulmonary inflammation in rodents and non-human primates. Prostaglandins Other Lipid Mediat. 2010 Jun;92(1-4):33-43.
REF 18ONO-4057, a novel, orally active leukotriene B4 antagonist: effects on LTB4-induced neutrophil functions. Prostaglandins. 1992 Oct;44(4):261-75.
REF 19(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. (Target id: 268).

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