Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDC00129

Target Information
NameLeukotriene B4 receptor 1    
Type of targetClinical trial target    
SynonymsChemoattractant receptor-like 1    
LTB4-R    
LTB4-R 1    
Leukotriene B(4) receptor BLT1    
P2Y purinoceptor 7    
P2Y7    
DiseaseAdverse Effects, Chemotherapy[1]
Asthma
[ICD9: 493   ICD10: J45]
[2][3]
Cancer
[ICD9: 140-229   ICD10: C00-C96]
[4][5][6]
Chronic Obstructive Pulmonary Disease (COPD)
[ICD9: 490-492, 494-496   ICD10: J40-J44, J47]
[2][3]
Cystic Fibrosis
[ICD9: 277.0   ICD10: E84]
[2][3]
Immunological disorders[7]
Inflammation[7]
Renal Cell Carcinoma
[ICD9: 189   ICD10: C64]
[1]
Rheumatoid arthritis
[ICD9: 714   ICD10: M05-M06]
[2][3]
Drug(s)Biomed 101Phase Ia completedRenal Cell Carcinoma, Chemotherapy Adverse Effects[8]
AmelubantDiscontinued in Phase IRheumatoid Arthritis[2][3]
AmelubantDiscontinued in Phase IIChronic Obstructive Pulmonary Disease, Cystic Fibrosis, Asthma[2][3]
LTB 019DiscontinuedChronic Obstructive Pulmonary Disease[9]
LY-293111Discontinued in Phase IIPancreatic cancer[10]
LY293111Discontinued in Phase IIPancreatic cancer[4][5][6]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayNeuroactive ligand-receptor interaction
UniProt IDQ15722
FunctionReceptor 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 control.    
SequenceMNTTSSAAPPSLGVEFISLLAIILLSVALAVGLPGNSFVVWSILKRMQKRSVTALMVLNL ALADLAVLLTAPFFLHFLAQGTWSFGLAGCRLCHYVCGVSMYASVLLITAMSLDRSLAVA RPFVSQKLRTKAMARRVLAGIWVLSFLLATPVLAYRTVVPWKTNMSLCFPRYPSEGHRAF HLIFEAVTGFLLPFLAVVASYSDIGRRLQARRFRRSRRTGRLVVLIILTFAAFWLPYHVV NLAEAGRALAGQAAGLGLVGKRLSLARNVLIALAFLSSSVNPVLYACAGGGLLRSAGVGF VAKLLEGTGSEASSTRRGGSLGQTARSGPAALEPGPSESLTASSPLKLNELN
Related US Patent6,133,286
6,160,012
6,291,531
6,340,706
6,576,669
6,583,177
6,617,345
Target ValidationClick to Find Target Validation Information.    
Inhibitor (3S,4R)-3-Benzyl-7-isopropyl-chroman-4-ol[11]
(LTB4-[12]
CP-105696[11]
DTPA Conjugate[12]
HYNIC Analogue[12]
HYNIC Conjugate[12]
HYNIC Conjugate[12]
LEUCETTAMIDINE[13]
LEUCETTAMINE A[13]
LEUKOTRIENE_B4[14]
LY-255283[15]
LY-255283[16]
LY-282210[17]
LY-292728[17]
SB-201146[18]
SB-201993[18]
SB-209247,   Ticolubant[18]
SC-41390[14]
SC-48928[14]
SC-50073[14]
SC-50135[14]
SC-50676[14]
SC-51146[14]
SC-52073[14]
SC-52569[14]
SC-53228[14]
SC-53229[14]
AntagonistAmelubant[2][3]
LTB 019[9]
LY-293111[10]
LY293111[4][5][6]
U 75302[7]
BinderBiomed 101[8]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1CenterWatch. Drugs in Clinical Trials Database. CenterWatch. 2008. To Reference
Ref 2Leukotriene receptor antagonists in children with cystic fibrosis lung disease : anti-inflammatory and clinical effects. Paediatr Drugs. 2005;7(6):353-63. To Reference
Ref 3Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2005 Jan-Feb;27(1):49-77. To Reference
Ref 4The 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. To Reference
Ref 5A 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. To Reference
Ref 6Leukotriene 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. To Reference
Ref 7A 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. To Reference
Ref 8Biomed 101, a leukotriene B4 inhibitor, may decrease IL-2 toxicity. 2003 ASCO Annual Meeting. 2003 To Reference
Ref 9Effect 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. To Reference
Ref 10Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91. To Reference
Ref 11Bioorg. Med. Chem. Lett. 7(17):2307-2312 (1997) To Reference
Ref 12J 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. To Reference
Ref 13J. Nat. Prod. 56(1):116-121 (1993) To Reference
Ref 14Bioorg. Med. Chem. Lett. 4(6):811-816 (1994) To Reference
Ref 15J Med Chem. 1993 Nov 26;36(24):3978-81.o-phenylphenols: potent and orally active leukotriene B4 receptor antagonists. To Reference
Ref 16Bioorg. Med. Chem. Lett. 3(10):1985-1990 (1993) To Reference
Ref 17J Med Chem. 1993 Nov 26;36(24):3982-4.Biphenylyl-substituted xanthones: highly potent leukotriene B4 receptor antagonists. To Reference
Ref 18J 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. To Reference



 

Welcome to sign our Guestbook.

If you find any error in data or bug in web service, please kindly report it to Dr. Zhu.


Dr. Chen Yuzong
Deputy Director of Center for Computational Science and Engineering
Professor in Department of Pharmacy
National University of Singapore, Singapore


All rights reserved.

   
 
 
Computer-aided Drug Design
about BIDD |  databases |  software |  teaching |  research |  links

 

Department of Computational Science | National University of Singapore | Blk S17, 3 Science Drive 2, Singapore 117543