Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDC00082

Target Information
NameCholecystokinin type A receptor    
Type of targetClinical trial target    
SynonymsCCK-A receptor    
CCK-AR    
DiseaseAcid-related diseases
[ICD9: 531-534   ICD10: K25-K27]
[1]
Alcoholism
[ICD9: 303   ICD10: F10.2]
[2]
Gastroesophageal Reflux Disease (GERD)
[ICD9: 530   ICD10: K21]
[3][4][5]
Gastrointestinal Diseases and Disorders, miscellaneous[6][7][8]
Gastrointestinal motility disorders[1]
Irritable Bowel Syndrome (IBS)
[ICD9: 564.1   ICD10: K58]
[3][4][5]
Obesity
[ICD9: 278   ICD10: E66]
[9][10][11][12]
Pancreatic Cancer
[ICD9: 157   ICD10: C25]
[9][10]
Drug(s)DexloxiglumidePhase III completed, and Positive results in phase IIIIrritable Bowel Syndrome, Gastroesophageal Reflux Disease[3][4][5]
UCL-2000 and butabindidePhase IObesity[13]
GI 181771Discontinued in Phase IIObesity[11]
GI-181771Discontinued in Phase IIObesity[13]
LintitriptDiscontinuedPancreatic Cancer, Obesity[9][10]
TarazepideDiscontinuedMiscellaneous Gastrointestinal Disorders[6][7][8]
A-71378PreclinicalObesity[13]
A-74498PreclinicalObesity[13]
AR-R-1589PreclinicalObesity, Eating disorders[13]
FPL-14294PreclinicalObesity[13]
GG-8573PreclinicalGallstone prophylaxis, Obesity[13]
PD-170292PreclinicalObesity[13]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayCalcium signaling pathway
Neuroactive ligand-receptor interaction
UniProt IDP32238
PDB Structure1D6G; 1HZN; 1PB2.    
FunctionReceptor for cholecystokinin. Has a 1000-fold higher affinity for cck rather than for gastrin. It modulates feeding and dopamine-induced behavior in the central and peripheral nervous system. This receptor mediates its action by association with G protein.    
SequenceMDVVDSLLVNGSNITPPCELGLENETLFCLDQPRPSKEWQPAVQILLYSLIFLLSVLGNT LVITVLIRNKRMRTVTNIFLLSLAVSDLMLCLFCMPFNLIPNLLKDFIFGSAVCKTTTYF MGTSVSVSTFNLVAISLERYGAICKPLQSRVWQTKSHALKVIAATWCLSFTIMTPYPIYS NLVPFTKNNNQTANMCRFLLPNDVMQQSWHTFLLLILFLIPGIVMMVAYGLISLELYQGI KFEASQKKSAKERKPSTTSSGKYEDSDGCYLQKTRPPRKLELRQLSTGSSSRANRIRSNS SAANLMAKKRVIRMLIVIVVLFFLCWMPIFSANAWRAYDTASAERRLSGTPISFILLLSY TSSCVNPIIYCFMNKRFRLGFMATFPCCPNPGPPGARGEVGEEEEGGTTGASLSRFSYSH MSASVPPQ
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
Inhibitor1- (3,3-Diphenyl-allyl)-3-m-tolyl-urea[14]
1- (4-Chloro-phenyl)-3-[14]
1- (4-Chloro-phenyl)-3-[14]
3,4-Dichloro-N- (3,3-diphenyl-allyl)-benzamide[14]
Asp-Tyr (SO3H)-Met-Gly-Trp-Met-Asp-Phe-NH2[15]
Asp-Tyr (SO3Na)-Met-Gly-Trp-Met-Asp-Phe-NH2[16]
Boc-Asp-Tyr (So3-)-Nle-Gly-Trp-Asp-Phe-NH2[17]
Boc-D-Glu-Tyr (SO3H)-Nle-D-Lys-Trp-Nle-Asp-Phe-NH2[15]
Boc-D-Glu-Tyr (SO3H)-Nle-D-Nle-Trp-Nle-Asp-Phe-NH2[15]
Boc-Glu-Tyr (SO3H)-Nle-D-Lys-Trp-Nle-Asp-Phe-NH2[15]
Boc-Tyr (SO3H)-Nle-Gly-Trp-Nle-Asp-Phe-NH2[15]
Boc-cyclo- (Glu-Tyr-Nle-D-Lys)-Trp-Nle-Asp-Phe-NH2[15]
CI-988[18]
CR-1795[19]
CR-2345[19]
FR-175985[20]
H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-H[21]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-D-Trp-H[22]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Boc[22]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Trp-D-Nle-D-Asp-D-Phe-H[21]
IQM-95333[23]
L-365260[20]
L-708474[24]
L-740093[25]
PD-135118[18]
PD-135666[18]
PD-136621[18]
PD-137337[18]
PD-137342[18]
PD-138915[18]
PD-138916[18]
PD-140547[18]
PD-140548[18]
PD-140723[18]
Pranazepide[20]
SINCALIDE[26]
SNF-9007[27]
Tetragastrin[28]
Tyr-D-Ala-Gly-D-Trp-NMeNle-Asp-Phe-NH2[27]
Tyr-D-Ala-Gly-D-Trp-Nle-Asp-Phe-NH2[27]
Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-NMeNle-D-Trp-Boc[22]
Tyr-D-Ala-Gly-Trp-NMeNle-Asp-Phe-NH2[27]
Tyr-D-Ala-Gly-Trp-Nle-Asp-Phe-NH2[27]
Tyr-D-Nle-Gly-D-Trp-NMeNle-Asp-Phe-NH2[27]
Tyr-D-Nle-Gly-Trp-Nle-Asp-Phe-NH2[27]
Tyr-D-Phe-Gly-D-Trp-NMeNle-Asp-Phe-NH2[27]
Tyr-D-Phe-Gly-D-Trp-Nle-Asp-Phe-NH2[27]
Tyr-D-Phe-Gly-Trp-NMeNle-Asp-Phe-NH2[27]
Tyr-D-Phe-Gly-Trp-Nle-Asp-Phe-NH2[27]
VL-0395[29]
VL-0494[30]
VL-0699[31]
VL-1499[29]
VL-2799[32]
AgonistA-71378[13]
A-74498[13]
AR-R-1589[13]
FPL-14294[13]
GG-8573[13]
GI 181771[11]
GI-181771[13]
PD-170292[13]
UCL-2000 and butabindide[13]
AntagonistAsperlicin[33]
Devazepide[33]
Dexloxiglumide[3][4][5]
L-364,718[2]
Lintitript[9][10]
Lorglumide[34]
Loxiglumide[12]
Tarazepide[6][7][8]
MultitargetUCL-2000 and butabindide[13]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Effect of dexloxiglumide and spiroglumide, two new CCK-receptor antagonists, on gastric emptying and secretion in the rat: evaluation of their receptor selectivity in vivo. Aliment Pharmacol Ther. 1996 Jun;10(3):411-9. To Reference
Ref 2The role of cholecystokinin (CCK), CCK-A or CCK-B receptor antagonists in the spontaneous preference for drugs of abuse (alcohol or cocaine) in naive rats. Methods Find Exp Clin Pharmacol. 1998 Oct;20(8):679-97. To Reference
Ref 3Prokinetic drugs for feed intolerance in critical illness: current and potential therapies. Crit Care Resusc. 2009 Jun;11(2):132-43. To Reference
Ref 4Regulation of fat-stimulated neurotensin secretion in healthy subjects. J Clin Endocrinol Metab. 2008 May;93(5):1964-70. Epub 2008 Feb 26. To Reference
Ref 5Role of CCK and potential utility of CCK1 receptor antagonism in the treatment of pancreatitis induced by biliary tract obstruction. Br J Pharmacol. 2008 Apr;153(8):1650-8. Epub 2008 Feb 25. To Reference
Ref 6Melatonin as modulator of pancreatic enzyme secretion and pancreatoprotector. J Physiol Pharmacol. 2007 Dec;58 Suppl 6:65-80. To Reference
Ref 7The ghrelin pentapeptide inhibits the secretion of pancreatic juice in rats. J Physiol Pharmacol. 2006 Dec;57(4):691-700. To Reference
Ref 8Effects of intraduodenal administration of tarazepide on pancreatic secretion and duodenal EMG in neonatal calves. Regul Pept. 1998 Nov 30;78(1-3):113-23. To Reference
Ref 9A cholecystokinin-1 receptor agonist (CCK-8) mediates increased permeability of brain barriers to leptin. Br J Pharmacol. 2008 Jul;154(5):1009-15. Epub 2008 Apr 21. To Reference
Ref 10A novel role for cholecystokinin: regulation of mesenteric vascular resistance. Regul Pept. 2004 Sep 15;121(1-3):145-53. To Reference
Ref 11Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2003 Jul-Aug;25(6):483-506. To Reference
Ref 12Role of CCK(A) receptors in postprandial lower esophageal sphincter function in morbidly obese subjects. Dig Dis Sci. 2002 Nov;47(11):2531-7. To Reference
Ref 13Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60. To Reference
Ref 14J Med Chem. 1992 Mar 20;35(6):1042-9.Hybrid cholecystokinin-A antagonists based on molecular modeling of lorglumide and L-364,718. To Reference
Ref 15J Med Chem. 1989 Jun;32(6):1184-90.Synthesis and binding affinities of cyclic and related linear analogues of CCK8 selective for central receptors. To Reference
Ref 16Bioorg. Med. Chem. Lett. 3(5):855-860 (1993) To Reference
Ref 17J Med Chem. 1987 Aug;30(8):1366-73.Synthesis and biological activities of pseudopeptide analogues of the C-terminal heptapeptide of cholecystokinin. On the importance of the peptide bonds. To Reference
Ref 18Bioorg. Med. Chem. Lett. 3(5):881-884 (1993) To Reference
Ref 19Bioorg. Med. Chem. Lett. 3(5):861-866 (1993) To Reference
Ref 20Bioorg. Med. Chem. Lett. 7(2):169-174 (1997) To Reference
Ref 21J Med Chem. 2007 Jan 11;50(1):165-8.Partial retro-inverso, retro, and inverso modifications of hydrazide linked bifunctional peptides for opioid and cholecystokinin (CCK) receptors. To Reference
Ref 22J Med Chem. 2006 Mar 9;49(5):1773-80.Design and synthesis of novel hydrazide-linked bifunctional peptides as delta/mu opioid receptor agonists and CCK-1/CCK-2 receptor antagonists. To Reference
Ref 23J Med Chem. 1997 Oct 10;40(21):3402-7.Synthesis and stereochemical structure-activity relationships of 1,3-dioxoperhydropyrido[1,2-c]pyrimidine derivatives: potent and selective cholecystokinin-A receptor antagonists. To Reference
Ref 24J Med Chem. 1994 Mar 18;37(6):719-21.High-affinity and potent, water-soluble 5-amino-1,4-benzodiazepine CCKB/gastrin receptor antagonists containing a cationic solubilizing group. To Reference
Ref 25Bioorg. Med. Chem. Lett. 5(24):3023-3026 (1995) To Reference
Ref 26J Med Chem. 1989 Feb;32(2):445-9.Full agonists of CCK8 containing a nonhydrolyzable sulfated tyrosine residue. To Reference
Ref 27J Med Chem. 2006 May 18;49(10):2868-75.Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors. To Reference
Ref 28J Med Chem. 1987 Apr;30(4):729-32.Synthesis and binding affinities of analogues of cholecystokinin-(30-33) as probes for central nervous system cholecystokinin receptors. To Reference
Ref 29Bioorg Med Chem. 2009 Jul 15;17(14):5198-206. Epub 2009 Jun 2.2D-QSAR and 3D-QSAR/CoMFA analyses of the N-terminal substituted anthranilic acid based CCK(1) receptor antagonists: 'Hic Rhodus, hic saltus'. To Reference
Ref 30Bioorg Med Chem Lett. 2007 May 15;17(10):2749-55. Epub 2007 Mar 3.Synthesis and evaluation of novel benzimidazole derivative [Bz-Im] and its radio/biological studies. To Reference
Ref 31J Med Chem. 2006 Apr 20;49(8):2456-62.Anthranilic acid based CCK1 receptor antagonists and CCK-8 have a common step in their "receptor desmodynamic processes". To Reference
Ref 32Bioorg Med Chem. 2009 Mar 15;17(6):2336-50. Epub 2009 Feb 14.Anthranilic acid based CCK1 receptor antagonists: blocking the receptor with the same 'words' of the endogenous ligand. To Reference
Ref 33Mini Rev Med Chem. 2007 Nov;7(11):1108-19.Privileged structures: a useful concept for the rational design of new lead drug candidates. To Reference
Ref 34Behavioral and neurochemical study on the role of the brain cholecystokinin system in anxiety. Hokkaido Igaku Zasshi. 1998 Sep;73(5):463-73. 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