Target Information

Target General Infomation
Target ID
T59626
Former ID
TTDC00129
Target Name
Leukotriene B4 receptor 1
Gene Name
LTB4R
Synonyms
Chemoattractant receptor-like 1; LTB4-R; LTB4-R 1; Leukotriene B(4) receptor BLT1; P2Y purinoceptor 7; P2Y7; LTB4R
Target Type
Clinical Trial
Disease Asthma [ICD10: J45]
Allergy [ICD9: 995.3; ICD10: T78.4]
Cystic fibrosis [ICD9: 277; ICD10: E84]
Human immunodeficiency virus infection [ICD9: 279.3; ICD10: B20-B26]
Inflammatory disease [ICD9: 140-229, 147, 173, 573.3, 710-719; ICD10: C11, C44, K75.9, M00-M25]
Inflammatory bowel disease [ICD9: 555, 556; ICD10: K50, K51]
Osteoporosis [ICD9: 733.0, V07.4; ICD10: M80-M81, Z79.890]
Pancreatic cancer [ICD9: 140-199, 140-229, 157, 210-229; ICD10: C25]
Psoriasis [ICD9: 696; ICD10: L40]
Renal cancer [ICD9: 140-229, 189; ICD10: C64]
Rheumatoid arthritis [ICD9: 710-719, 714; ICD10: M05-M06]
Function
Receptor for extracellular ATP > UTP and ADP.The activity of this receptor is mediated by G proteins which activate a phosphatidylinositol-calcium second messenger system. May be the cardiac P2Y receptor involved in the regulation of cardiac muscle contraction through modulation of L-type calcium currents. Is a receptor for leukotriene B4, a potent chemoattractant involved in inflammation and immune response.
BioChemical Class
GPCR rhodopsin
Target Validation
T59626
UniProt ID
Q15722
Sequence
MNTTSSAAPPSLGVEFISLLAIILLSVALAVGLPGNSFVVWSILKRMQKRSVTALMVLNL
ALADLAVLLTAPFFLHFLAQGTWSFGLAGCRLCHYVCGVSMYASVLLITAMSLDRSLAVA
RPFVSQKLRTKAMARRVLAGIWVLSFLLATPVLAYRTVVPWKTNMSLCFPRYPSEGHRAF
HLIFEAVTGFLLPFLAVVASYSDIGRRLQARRFRRSRRTGRLVVLIILTFAAFWLPYHVV
NLAEAGRALAGQAAGLGLVGKRLSLARNVLIALAFLSSSVNPVLYACAGGGLLRSAGVGF
VAKLLEGTGSEASSTRRGGSLGQTARSGPAALEPGPSESLTASSPLKLNELN
Drugs and Mode of Action
Drug(s) Amelubant Drug Info Discontinued in Phase 2 Cystic fibrosis [1], [2]
CI-949 Drug Info Discontinued in Phase 2 Asthma [3]
CP-195543 Drug Info Discontinued in Phase 2 Rheumatoid arthritis [4], [5]
LTB 019 Drug Info Discontinued in Phase 2 Asthma [6]
LTB4 Drug Info Discontinued in Phase 2 Human immunodeficiency virus infection [7], [8]
LY-223982 Drug Info Discontinued in Phase 2 Asthma [9], [10]
LY293111 Drug Info Discontinued in Phase 2 Pancreatic cancer [11], [12]
SB-201993 Drug Info Discontinued in Phase 2 Psoriasis [13]
SC-41930 Drug Info Discontinued in Phase 2 Inflammatory bowel disease [14], [15]
Biomed 101 Drug Info Discontinued in Phase 1 Renal cancer [16]
CP-105696 Drug Info Discontinued in Phase 1 Inflammatory bowel disease [17], [18]
DW-1350 Drug Info Terminated Osteoporosis [19]
LY-210073 Drug Info Terminated Asthma [20]
LY-255283 Drug Info Terminated Asthma [21], [22]
LY-292728 Drug Info Terminated Discovery agent [23]
RG-14893 Drug Info Terminated Asthma [24]
Ro-25-4094 Drug Info Terminated Inflammatory disease [25]
RP-66153 Drug Info Terminated Asthma [26]
RP-66364 Drug Info Terminated Inflammatory disease [27]
RP-69698 Drug Info Terminated Inflammatory disease [28]
SB-201146 Drug Info Terminated Discovery agent [29]
SB-209247 Drug Info Terminated Psoriasis [30]
SC-51146 Drug Info Terminated Discovery agent [31]
SC-53228 Drug Info Terminated Asthma [32]
U 75302 Drug Info Terminated Allergy [33], [34]
Inhibitor (3S,4R)-3-Benzyl-7-isopropyl-chroman-4-ol Drug Info [35]
(LTB4-(Csa)4)2-Glu-H Conjugate Drug Info [36]
CP-105696 Drug Info [35]
DTPA Conjugate Drug Info [36]
HYNIC Analogue Drug Info [36]
LEUCETTAMIDINE Drug Info [37]
LEUCETTAMINE A Drug Info [37]
LEUKOTRIENE_B4 Drug Info [38]
LY-255283 Drug Info [39]
LY-282210 Drug Info [40]
LY-292728 Drug Info [40]
SB-201146 Drug Info [41]
SB-201993 Drug Info [41]
SC-41390 Drug Info [38]
SC-50073 Drug Info [38]
SC-50135 Drug Info [38]
SC-50676 Drug Info [38]
SC-51146 Drug Info [38]
SC-52073 Drug Info [38]
SC-52569 Drug Info [38]
SC-53228 Drug Info [38]
SC-53229 Drug Info [38]
Antagonist Amelubant Drug Info [42], [43]
CP-195543 Drug Info [44]
LTB 019 Drug Info [45]
LY293111 Drug Info [46], [47], [48]
SB-209247 Drug Info [49]
U 75302 Drug Info [50]
Binder Biomed 101 Drug Info [51]
Modulator CI-949 Drug Info [52]
DW-1350 Drug Info [53]
LY-210073 Drug Info [20]
LY-223982 Drug Info [54]
RG-14893 Drug Info [55]
Ro-25-4094 Drug Info [56]
RP-66153 Drug Info [57]
RP-66364 Drug Info [58]
RP-69698 Drug Info [59]
SC-41930 Drug Info [60]
Agonist LTB4 Drug Info [61]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Neuroactive ligand-receptor interaction
NetPath Pathway IL4 Signaling Pathway
Reactome Leukotriene receptors
G alpha (q) signalling events
WikiPathways Nucleotide GPCRs
GPCRs, Class A Rhodopsin-like
Gastrin-CREB signalling pathway via PKC and MAPK
Spinal Cord Injury
GPCR ligand binding
GPCR downstream signaling
References
REF 1ClinicalTrials.gov (NCT02251210) Efficacy and Safety of BIIL 284 BS in Adult Patients With Active Rheumatoid Arthritis. U.S. National Institutes of Health.
REF 2(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: 8463).
REF 3Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000104)
REF 4ClinicalTrials.gov (NCT00424294) A Study Of CP-195543 And Celecoxib Dual Therapy In Subjects With Rheumatoid Arthritis. U.S. National Institutes of Health.
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: 6155).
REF 6Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015581)
REF 7ClinicalTrials.gov (NCT00251537) A Pilot Study of LTB4 in HIV-1 Infected Adults. U.S. National Institutes of Health.
REF 8(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: 2487).
REF 9(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: 3415).
REF 10Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002326)
REF 11(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: 2948).
REF 12Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003262)
REF 13Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003335)
REF 14(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: 6156).
REF 15Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001549)
REF 16ClinicalTrials.gov (NCT00004890) Biomed 101 and Interleukin-2 in Treating Patients With Kidney Cancer. U.S. National Institutes of Health.
REF 17(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 18Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005644)
REF 19Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026567)
REF 20Design, synthesis, and pharmacological evaluation of potent xanthone dicarboxylic acid leukotriene B4 receptor antagonists. J Med Chem. 1993 Jun 11;36(12):1726-34.
REF 21(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 22Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001833)
REF 23Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007211)
REF 24Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001715)
REF 25Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005401)
REF 26Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003980)
REF 27Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003795)
REF 28Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003683)
REF 29Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003774)
REF 30Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006734)
REF 31Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002332)
REF 32Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006478)
REF 33(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: 3325).
REF 34Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000072)
REF 353-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 36J Med Chem. 2005 Oct 6;48(20):6442-53.Synthesis of leukotriene B4 antagonists labeled with In-111 or Tc-99m to image infectious and inflammatory foci.
REF 37New leukotriene B4 receptor antagonist: leucettamine A and related imidazole alkaloids from the marine sponge Leucetta microraphis. J Nat Prod. 1993 Jan;56(1):116-21.
REF 38Synthesis and pharmacological activity of SC-53228, a leukotriene B4 receptor antagonist with high intrinsic potency and selectivity, Bioorg. Med. Chem. Lett. 4(6):811-816 (1994).
REF 39J Med Chem. 1993 Nov 26;36(24):3978-81.o-phenylphenols: potent and orally active leukotriene B4 receptor antagonists.
REF 40J Med Chem. 1993 Nov 26;36(24):3982-4.Biphenylyl-substituted xanthones: highly potent leukotriene B4 receptor antagonists.
REF 41J Med Chem. 1996 Sep 13;39(19):3837-41.(E)-3-[6-[[(2,6-dichlorophenyl)thio]methyl]-3-(2-phenylethoxy)-2- pyridinyl]-2-propenoic acid: a high-affinity leukotriene B4 receptor antagonist with oral antiinflammatory activity.
REF 42Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2005 Jan-Feb;27(1):49-77.
REF 43Leukotriene receptor antagonists in children with cystic fibrosis lung disease : anti-inflammatory and clinical effects. Paediatr Drugs. 2005;7(6):353-63.
REF 44The synthesis of CP-195543, an LTB4 antagonist for the treatment of inflammatory diseases. Curr Opin Drug Discov Devel. 1999 Nov;2(6):550-6.
REF 45Effect of the oral leukotriene B4 receptor antagonist LTB019 on inflammatory sputum markers in patients with chronic obstructive pulmonary disease. Pulm Pharmacol Ther. 2008;21(2):409-17.
REF 46Leukotriene B4 receptor inhibitor LY293111 induces cell cycle arrest and apoptosis in human anaplastic large-cell lymphoma cells via JNK phosphorylation. Leukemia. 2005 Nov;19(11):1977-84.
REF 47A phase I study of oral LY293111 given daily in combination with irinotecan in patients with solid tumours. Invest New Drugs. 2007 Jun;25(3):217-25. Epub 2006 Dec 5.
REF 48The Role of PPARgamma Receptors and Leukotriene B(4) Receptors in Mediating the Effects of LY293111 in Pancreatic Cancer. PPAR Res. 2008;2008:827096. Epub 2009 Jan 27.
REF 49Formation and protein binding of the acyl glucuronide of a leukotriene B4 antagonist (SB-209247): relation to species differences in hepatotoxicity. Drug Metab Dispos. 2005 Feb;33(2):271-81. Epub 2004 Nov 2.
REF 50A second leukotriene B(4) receptor, BLT2. A new therapeutic target in inflammation and immunological disorders. J Exp Med. 2000 Aug 7;192(3):421-32.
REF 51Biomed 101, a leukotriene B4 inhibitor, may decrease IL-2 toxicity. 2003 ASCO Annual Meeting. 2003.
REF 52Inhibition of histamine, leukotriene C4/D4, and thromboxane B2 release from human leukocytes and human chopped lung mast cells by the allergic mediator release inhibitor, CI-949. J Allergy Clin Immunol. 1990 Dec;86(6 Pt 1):902-8.
REF 53Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026850)
REF 54Specific inhibition of leukotriene B4-induced neutrophil activation by LY223982. J Pharmacol Exp Ther. 1992 Dec;263(3):1009-14.
REF 55Structure-activity relationships study of two series of leukotriene B4 antagonists: novel indolyl and naphthyl compounds substituted with a 2-[methyl(2-phenethyl)amino]-2-oxoethyl side chain. J Med Chem. 1996 Sep 13;39(19):3756-68.
REF 56Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005401)
REF 57Omega-[(omega-arylalkyl)thienyl]alkanoic acids: from specific LTA4 hydrolase inhibitors to LTB4 receptor antagonists. J Med Chem. 1992 Aug 21;35(17):3170-9.
REF 58WO patent application no. 1997,0297,75, Compositions comprising a cyclooxygenase-2 inhibitor and a leukotriene b4 receptor antagonist.
REF 59omega-[(4,6-Diphenyl-2-pyridyl)oxy]alkanoic acid derivatives: a new family of potent and orally active LTB4 antagonists. J Med Chem. 1992 Nov 13;35(23):4315-24.
REF 60Multiple actions of the leukotriene B4 receptor antagonist SC-41930. J Pharmacol Exp Ther. 1992 Jan;260(1):187-91.
REF 61LTB4 promotes insulin resistance in obese mice by acting on macrophages, hepatocytes and myocytes. Nat Med. 2015 Mar;21(3):239-47.

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