Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDR00405

Target Information
NameB1 bradykinin receptor    
Type of targetClinical trial target    
SynonymsB1R    
BK-1 receptor    
Bradykinin subtype 1 receptor    
DiseaseDiabetic nephropathy
[ICD9: 250.4   ICD10: E10.2, E11.2, E13.2]
[1]
Inflammatory diseases[2]
Ischemic vascular disease
[ICD9: 325, 430-459   ICD10: G45-G46, I60-I95]
[3]
Prostate cancer
[ICD9: 185   ICD10: C61]
[4]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayCalcium signaling pathway
Complement and coagulation cascades
Neuroactive ligand-receptor interaction
Regulation of actin cytoskeleton
UniProt IDP46663
FunctionThis is a receptor for bradykinin. Could be a factor in chronic pain and inflammation.    
SequenceMASSWPPLELQSSNQSQLFPQNATACDNAPEAWDLLHRVLPTFIISICFFGLLGNLFVLL VFLLPRRQLNVAEIYLANLAASDLVFVLGLPFWAENIWNQFNWPFGALLCRVINGVIKAN LFISIFLVVAISQDRYRVLVHPMASRRQQRRRQARVTCVLIWVVGGLLSIPTFLLRSIQA VPDLNITACILLLPHEAWHFARIVELNILGFLLPLAAIVFFNYHILASLRTREEVSRTRC GGRKDSKTTALILTLVVAFLVCWAPYHFFAFLEFLFQVQAVRGCFWEDFIDLGLQLANFF AFTNSSLNPVIYVFVGRLFRTKVWELYKQCTPKSLAPISSSHRKEIFQLFWRN
Related US Patent6,479,515
6,500,831
6,531,480
Target ValidationClick to Find Target Validation Information.    
InhibitorH-DArg-Arg-Pro-Hyp-Gly-Igl-Ser-D-BT-OH (JMV1638)[5]
H-DArg-Arg-Pro-Hyp-Gly-Thi-Ser-D-BT-OH (JMV1431)[5]
H-Lys-Arg-Pro-Hyp-Gly-Igl-Ser-D-BT-OH (JMV1645)[5]
H-Lys-Arg-Pro-Hyp-Gly-Thi-Ser-D-BT-OH (JMV1669)[5]
des-Arg10-Kallidin[6]
des-Arg10-Leu9-Kallidin[6]
AntagonistB-9958[2]
Des-Arg (9)-[Leu[7]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Induction of B1 receptors in streptozotocin diabetic rats: possible involvement in the control of hyperglycemia-induced glomerular Erk 1 and 2 phosphorylation. Can J Physiol Pharmacol. 2002 Apr;80(4):328-33. To Reference
Ref 2B1 receptors as a new inflammatory target. Could this B the 1? Trends Pharmacol Sci. 1999 Mar;20(3):100-4. To Reference
Ref 3Targeting kinin B(1) receptor for therapeutic neovascularization. Circulation. 2002 Jan 22;105(3):360-6. To Reference
Ref 4Bradykinin receptor subtype 1 expression and function in prostate cancer. Cancer Res. 2003 May 1;63(9):2037-41. To Reference
Ref 5J Med Chem. 2000 Jun 15;43(12):2382-6.Synthesis and biological evaluation of bradykinin B(1)/B(2) and selective B(1) receptor antagonists. To Reference
Ref 6Bioorg Med Chem Lett. 2004 Dec 20;14(24):6045-8.Development of an efficient and selective radioligand for bradykinin B1 receptor occupancy studies. To Reference
Ref 7Evidence for the participation of kinins in Freund's adjuvant-induced inflammatory and nociceptive responses in kinin B1 and B2 receptor knockout mice. Neuropharmacology. 2001 Dec;41(8):1006-12. To Reference



 

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