Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDS00199

Target Information
NameEndothelin B receptor    
Type of targetSuccessful target    
SynonymsET-B    
Endothelin receptor B    
Endothelin receptor Non-selective type    
DiseaseAtopic asthma
[ICD9: 493   ICD10: J45]
[1]
Glial proliferation[2]
Melanoma
[ICD9: 172   ICD10: C43]
[3]
Neuronal injury[2]
Drug(s)BosentanApprovedPulmonary arterial hypertension[4]
SPI-1620Phase ICarcinoma, Adjunct to Chemotherapy[5][6]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayCalcium signaling pathway
Melanogenesis
Neuroactive ligand-receptor interaction
UniProt IDP24530
FunctionNon-specific receptor for endothelin 1, 2, and 3. Mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system.    
SequenceMQPPPSLCGRALVALVLACGLSRIWGEERGFPPDRATPLLQTAEIMTPPTKTLWPKGSNA SLARSLAPAEVPKGDRTAGSPPRTISPPPCQGPIEIKETFKYINTVVSCLVFVLGIIGNS TLLRIIYKNKCMRNGPNILIASLALGDLLHIVIDIPINVYKLLAEDWPFGAEMCKLVPFI QKASVGITVLSLCALSIDRYRAVASWSRIKGIGVPKWTAVEIVLIWVVSVVLAVPEAIGF DIITMDYKGSYLRICLLHPVQKTAFMQFYKTAKDWWLFSFYFCLPLAITAFFYTLMTCEM LRKKSGMQIALNDHLKQRREVAKTVFCLVLVFALCWLPLHLSRILKLTLYNQNDPNRCEL LSFLLVLDYIGINMASLNSCINPIALYLVSKRFKNCFKSCLCCWCQSFEEKQSLEEKQSC LKFKANDHGYDNFRSSNKYSSS
Related US Patent6,358,983
6,509,341
Target ValidationClick to Find Target Validation Information.    
InhibitorAc-W-F-F-N-Y-Y-W[7]
Ac-bhg-F-N-Y-Y-W[7]
Ac-w-F-F-N-Y-Y-W[7]
BMS-193884[8]
BOSENTAN SODIUM[9]
Compound ET-3[10]
Compound RES-701-1 (1-10)/[A15]ET-1[10]
Compound RES-701-1 (1-10)/[A15]ET-3[10]
Compound RES-701-1 (1-10)/[A15]SRTX6b[10]
Compound SRTX6b[10]
Compound [S15]ET-1[10]
ET-1[11]
ET-1[10]
Endothelin-3[12]
IRL-1722[11]
IRL-1841[11]
IRL-2500[11]
PD-155080[13]
PD-156707[13]
PD-163140[13]
RES-701-1[10]
RES-701-1[10]
RES-701-1-C-terminal analogue[14]
RES-701-1-C-terminal analogue[14]
RES-701-1-C-terminal analogue[14]
RES-701-1-C-terminal analogue[14]
RES-701-1-C-terminal analogue[14]
RES-701-1-C-terminal analogue[14]
RES-701-1-C-terminal analogue[14]
RES-701-1-C-terminal analogue[14]
RES-701-1-C-terminal analogue[14]
Trp-Ile-Ile-Asp-Leu-Hisc (Cys-Ser-Val-Tyr-Phe-Cys)[15]
Trp-Ile-Ile-Asp-Leu-Hisc (Cys-Val-Tyr-Phe-Cys)[15]
W-F-F-N--Y-Y-W[7]
bhg-F-N-Y-Y-W[7]
linear peptide of RES-701-1[10]
AgonistSPI-1620[5][6]
AntagonistBQ788[16]
Bosentan[4]
Bosentan hydrate[17]
LU302872[18]
PD142893[19]
Sarafotoxin 6C[19]
MultitargetBosentan[4]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Variants of endothelin-1 and its receptors in atopic asthma. Biochem Biophys Res Commun. 1999 Aug 19;262(1):259-62. To Reference
Ref 2Expression of endothelin-B receptors by glia in vivo is increased after CNS injury in rats, rabbits, and humans. Exp Neurol. 1997 May;145(1):180-95. To Reference
Ref 3Endothelin B receptor blockade inhibits dynamics of cell interactions and communications in melanoma cell progression. Cancer Res. 2004 Feb 15;64(4):1436-43. To Reference
Ref 4Pulmonary arterial hypertension: the most devastating vascular complication of systemic sclerosis. Rheumatology (Oxford). 2009 Jun;48 Suppl 3:iii25-31. To Reference
Ref 5Spectrum. Product Development Pipeline. 2009. To Reference
Ref 6Spectrum. Report of Spectrum. Apr 15 2008. To Reference
Ref 7Bioorg. Med. Chem. Lett. 5(6):621-626 (1995) To Reference
Ref 8J Med Chem. 2000 Aug 10;43(16):3111-7.Biphenylsulfonamide endothelin receptor antagonists. 2. Discovery of 4'-oxazolyl biphenylsulfonamides as a new class of potent, highly selective ET(A) antagonists. To Reference
Ref 9J Med Chem. 2001 Oct 11;44(21):3369-77.Potent and selective ET-A antagonists. 2. Discovery and evaluation of potent and water soluble N-(6-(2-(aryloxy)ethoxy)-4-pyrimidinyl)sulfonamide derivatives. To Reference
Ref 10Bioorg. Med. Chem. Lett. 7(13):1715-1720 (1997) To Reference
Ref 11Bioorg. Med. Chem. Lett. 6(19):2323-2328 (1996) To Reference
Ref 12J Med Chem. 2008 Nov 27;51(22):7094-8.cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia. To Reference
Ref 13Bioorg. Med. Chem. Lett. 7(3):297-302 (1997) To Reference
Ref 14Bioorg. Med. Chem. Lett. 6(7):775-778 (1996) To Reference
Ref 15Bioorg. Med. Chem. Lett. 4(4):567-572 (1994) To Reference
Ref 16BQ788, an endothelin ET(B) receptor antagonist, attenuates stab wound injury-induced reactive astrocytes in rat brain. Glia. 1999 May;26(3):268-71. To Reference
Ref 17Nat Rev Drug Discov. 2003 Jan;2(1):38-51.Knockouts model the 100 best-selling drugs--will they model the next 100? To Reference
Ref 18Influence of endothelin receptor antagonists on myocardial protein kinase C isoforms in uraemic cardiomyopathy. Clin Sci (Lond). 2002 Aug;103 Suppl 48:276S-279S. To Reference
Ref 19Human optic nerve head astrocytes as a target for endothelin-1. Invest Ophthalmol Vis Sci. 2002 Aug;43(8):2704-13. 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