Target Information
Target General Infomation | |||||
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Target ID |
T30563
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Former ID |
TTDR00545
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Target Name |
Leukotriene B4 receptor 2
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Gene Name |
LTB4R2
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Synonyms |
LTB4 receptor JULF2; LTB4-R2; Leukotriene B(4) receptor BLT2; Leukotriene B4 receptor BLT2; Seven transmembrane receptor BLTR2; LTB4R2
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Target Type |
Discontinued
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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.
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T30563
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UniProt ID | |||||
Sequence |
MAPSHRASQVGFCPTPERPLWRLPPTCRPRRMSVCYRPPGNETLLSWKTSRATGTAFLLL
AALLGLPGNGFVVWSLAGWRPARGRPLAATLVLHLALADGAVLLLTPLFVAFLTRQAWPL GQAGCKAVYYVCALSMYASVLLTGLLSLQRCLAVTRPFLAPRLRSPALARRLLLAVWLAA LLLAVPAAVYRHLWRDRVCQLCHPSPVHAAAHLSLETLTAFVLPFGLMLGCYSVTLARLR GARWGSGRHGARVGRLVSAIVLAFGLLWAPYHAVNLLQAVAALAPPEGALAKLGGAGQAA RAGTTALAFFSSSVNPVLYVFTAGDLLPRAGPRFLTRLFEGSGEARGGGRSREGTMELRT TPQLKVVGQGRGNGDPGGGMEKDGPEWDL |
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Drugs and Mode of Action | |||||
Inhibitor | (3S,4R)-3-Benzyl-7-isopropyl-chroman-4-ol | Drug Info | [551327] | ||
CP-105696 | Drug Info | [551327] | |||
LEUKOTRIENE_B4 | Drug Info | [551245] | |||
LY-255283 | Drug Info | [533797] | |||
LY-282210 | Drug Info | [533960] | |||
LY-292728 | Drug Info | [533960] | |||
SC-41390 | Drug Info | [551245] | |||
Agonist | 12-epi LTB4 | Drug Info | [526017] | ||
12-hydroxyheptadecatrienoic acid | Drug Info | [529399] | |||
12R-HETE | Drug Info | [534395] | |||
12S-HETE | Drug Info | [526017] | |||
20-hydroxy-LTB4 | Drug Info | [534395] | |||
CAY10583 | Drug Info | [527543] | |||
Antagonist | BIIL 260 | Drug Info | [528578] | ||
RO5101576 | Drug Info | [530774] | |||
ZK-158252 | Drug Info | [526017] | |||
Modulator | ONO-4057 | Drug Info | [526760] | ||
[3H]LTB4 | Drug Info | [543683] | |||
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 540308 | (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 540322 | (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 541347 | (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 544999 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001833) | ||||
Ref 545386 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003085) | ||||
Ref 526017 | Hydroxyeicosanoids 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 526760 | ONO-4057, a novel, orally active leukotriene B4 antagonist: effects on LTB4-induced neutrophil functions. Prostaglandins. 1992 Oct;44(4):261-75. | ||||
Ref 527543 | Characterization 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 528578 | Clinical 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 529399 | 12(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 530774 | Effects 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 533797 | J Med Chem. 1993 Nov 26;36(24):3978-81.o-phenylphenols: potent and orally active leukotriene B4 receptor antagonists. | ||||
Ref 533960 | J Med Chem. 1993 Nov 26;36(24):3982-4.Biphenylyl-substituted xanthones: highly potent leukotriene B4 receptor antagonists. | ||||
Ref 534395 | A G-protein-coupled receptor for leukotriene B4 that mediates chemotaxis. Nature. 1997 Jun 5;387(6633):620-4. | ||||
Ref 543683 | (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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