Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
 

 

Target Validation Information
TTD IDTTDC00017
Target NameCalcitonin gene-related peptide 1    
Type of TargetClinical trial target    
Drug Potency against TargetSodium oxybateIC50 = 0.24 nM[1]
Sodium oxybateIC50 = 2400 nM[2]
Sodium oxybateIC50 = 50000 nM[3]
OlcegepantIC50 = 0.03 nM[4]
Ac-WVTHRLAGLLSRSGGVVRKNFVPTDVGPFAF-NH2IC50 = 0.2 nM[5]
Ac-WVTHQLAGLLSQSGGVVRKNFVPTDVGPFAF-NH2IC50 = 0.53 nM[5]
Ac-WVTH[Cit]LAGLLSRSGGVVRKNFVPTDVGPFAF-NH2IC50 = 0.57 nM[5]
Ac-WVTHRLAGLLS[Cit]SGGVVRKNFVPTDVGPFAF-NH2IC50 = 0.58 nM[5]
WVTHRLAGLLSRSGGVVKNNFVPTNVGSKAF-NH2IC50 = 0.64 nM[5]
Ac-VTHRLAGLLSRSGGVVRKNFVPTDVGPFAF-NH2IC50 = 0.71 nM[5]
Ac-WVEHRLKGELSRKGGVV[hArg]KNFVPTDVGPFAF-NH2IC50 = 1.02 nM[5]
Ac-VTHRLAGLLSRSGGVVKNNFVPTDVGPFAF-NH2IC50 = 1.74 nM[5]
Ac-WVTH[hArg]LAGLLS[hArg]SGGVVRKNFVPTDVGPFAF-NH2IC50 = 20.4 nM[5]
VTHRLAGLLSRSGGVVKNNFVPTNVGSKAF-NH2IC50 = 4.87 nM[5]
[Aib29,Asp31,Pro34,Phe35]CGRP(27-37)IC50 = 740 nM[5]
Ac-WVTH[Cit]LAGLLS[Cit]SGGVVRKNFVPTDVGPFAF-NH2IC50 = 8.9 nM[5]
Action against Disease ModelOlcegepantIn an in vivo model, BIBN4096BS in doses between 1 and 30 micrograms kg-1 (i.v.) inhibited the effects of CGRP, released by stimulation of the trigeminal ganglion, on facial blood flow in marmoset monkeys[6]
The Effect of Target Knockout, Knockdown or Genetic VariationsThe use of CGRP knockout mice has let to characterize the endogenous role of CGRP showing that the local release of this neuropeptide protects from ethanol injury and favours ulcer healing. Decreased levels of gastric CGRP-like immunoreactivity (li) were observed during acetic acid-, cysteamine-, concentrated ethanol- or water immersion stress-ulcers. Restoration of CGRP-li was found in animals bearing ulcers in healing status and delayed healing in mice knockout to CGRP. CGRP was able to release somatostatin from gastric D cells but its main effects on the stomach homeostasis rely on local vasodilator action during increased acid-back diffusion.[7]
Ref 1Curr Opin Pharmacol. 2007 Dec;7(6):583-92. Epub 2007 Nov 9.Progress in developing cholecystokinin (CCK)/gastrin receptor ligands that have therapeutic potential. To Reference
Ref 2Curr Top Med Chem. 2006;6(4):361-76.Characterization and inhibition of SARS-coronavirus main protease. To Reference
Ref 3Curr Top Med Chem. 2004;4(10):1017-33.Chemokine receptor-directed agents as novel anti-HIV-1 therapies. To Reference
Ref 4Curr Top Med Chem. 2008;8(16):1468-79.The tortuous road to an ideal CGRP function blocker for the treatment of migraine. To Reference
Ref 5J Med Chem. 2008 Dec 25;51(24):7889-97.Identification of potent, selective, and metabolically stable peptide antagonists to the calcitonin gene-related peptide (CGRP) receptor. To Reference
Ref 6Br J Pharmacol. 2000 Feb;129(3):420-3.Pharmacological profile of BIBN4096BS, the first selective small molecule CGRP antagonist. To Reference
Ref 7Curr Pharm Des. 2009;15(30):3571-6.Role of calcitonin gene-related Peptide in gastric mucosal defence and healing. 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