Therapeutic Targets Database
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TTD Target ID: TTDS00043

Target Information
NameGastrin/cholecystokinin type B receptor    
Type of targetSuccessful target    
SynonymsCCK-B receptor    
CCK-BR    
DiseaseAcid-related diseases
[ICD9: 531-534   ICD10: K25-K27]
[1]
Anxiety disorder, unspecified
[ICD9: 300   ICD10: F40-F42]
[2]
Cocaine dependence
[ICD9: 304.2   ICD10: F14.2]
[3]
Gastrin sensitive tumours
[ICD9: 140-199, 210-229   ICD10: C00-C75, C7A, C7B, D10-D36, D3A]
[4]
Gastrointestinal adenocarcinomas
[ICD9: 140-199   ICD10: C00-C75, C7A, C7B]
[5]
Gastrointestinal motility disorders[1]
Malignant gliomas
[ICD9: 191   ICD10: C71]
[5]
Medullary thyroid cancer
[ICD9: 193   ICD10: C73]
[5]
Neuroendocrine tumors
[ICD9: 209   ICD10: C7A, C7B, D3A]
[5]
Small cell lung cancer
[ICD9: 162.9   ICD10: C34.90]
[6]
Stromal ovarian tumors
[ICD9: 140-199, 183, 210-229   ICD10: C00-C75, C56, C7A, C7B, D10-D36, D3A]
[5]
Drug(s)CeruletideApprovedPancreatic malfunction[7]
PentagastrinApprovedDiagnostic aid for gastric acid secretory function[8][9][10][11]
GG-8573PreclinicalGallstone prophylaxis, Obesity[12]
PD-170292PreclinicalObesity[12]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayCalcium signaling pathway
Neuroactive ligand-receptor interaction
UniProt IDP32239
PDB Structure1L4T.    
FunctionReceptor for gastrin and cholecystokinin, and the ckk-b receptors occur throughout the central nervous system where they modulate anxiety, analgesia, arousal, and neuroleptic activity. this receptor mediates its action by association with G proteins.    
SequenceMELLKLNRSVQGTGPGPGASLCRPGAPLLNSSSVGNLSCEPPRIRGAGTRELELAIRITL YAVIFLMSVGGNMLIIVVLGLSRRLRTVTNAFLLSLAVSDLLLAVACMPFTLLPNLMGTF IFGTVICKAVSYLMGVSVSVSTLSLVAIALERYSAICRPLQARVWQTRSHAARVIVATWL LSGLLMVPYPVYTVVQPVGPRVLQCVHRWPSARVRQTWSVLLLLLLFFIPGVVMAVAYGL ISRELYLGLRFDGDSDSDSQSRVRNQGGLPGAVHQNGRCRPETGAVGEDSDGCYVQLPRS RPALELTALTAPGPGSGSRPTQAKLLAKKRVVRMLLVIVVLFFLCWLPVYSANTWRAFDG PGAHRALSGAPISFIHLLSYASACVNPLVYCFMHRRFRQACLETCARCCPRPPRARPRAL PDEDPPTPSIASLSRLSYTTISTLGPG
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
Inhibitor4- (4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one[13]
Asp-Tyr (OSO3H)-Met-Gly-Trp-Met-Asp-Phe[14]
Boc-Asp-Tyr (So3-)-Nle-Gly-Trp-Asp-Phe-NH2[15]
CI-988[16]
Cholecystokinin-9[17]
H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-Bo[18]
H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-H[18]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-D-Trp-H[19]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Ac[19]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Boc[19]
IQM-95333[20]
L-365260[21]
PD-134308[22]
PD-135118[16]
PD-135666[16]
PD-136621[16]
PD-137337[16]
PD-137342[16]
PD-138915[16]
PD-138916[16]
PD-138917[16]
PD-140547[16]
PD-140548[16]
PD-140723[16]
SINCALIDE[20]
SNF-9007[23]
Tetragastrin[24]
Tyr-D-Ala-Gly-D-Trp-NMeNle-Asp-Phe-NH2[23]
Tyr-D-Ala-Gly-D-Trp-Nle-Asp-Phe-NH2[23]
Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-NMeNle-D-Trp-Boc[19]
Tyr-D-Ala-Gly-Trp-NMeNle-Asp-Phe-NH2[23]
Tyr-D-Ala-Gly-Trp-Nle-Asp-Phe-NH2[23]
Tyr-D-Nle-Gly-D-Trp-NMeNle-Asp-Phe-NH2[23]
Tyr-D-Nle-Gly-D-Trp-Nle-Asp-Phe-NH2[23]
Tyr-D-Nle-Gly-Trp-NMeNle-Asp-Phe-NH2[23]
Tyr-D-Nle-Gly-Trp-Nle-Asp-Phe-NH2[23]
Tyr-D-Phe-Gly-D-Trp-NMeNle-Asp-Phe-NH2[23]
Tyr-D-Phe-Gly-D-Trp-Nle-Asp-Phe-NH2[23]
Tyr-D-Phe-Gly-Trp-NMeNle-Asp-Phe-NH2[23]
Tyr-D-Phe-Gly-Trp-Nle-Asp-Phe-NH2[23]
Tyr-D-Pro-Gly-Trp-NMeNle-Asp-Phe-NH2[23]
Tyr-Gly-Gly-Trp-NMeNle-Asp-Phe-NH2[23]
Tyr-Pro-Gly-Trp-NMeNle-Asp-Phe-NH2[23]
AgonistCeruletide[7]
PD-170292[12]
Pentagastrin[8][9][10][11]
AntagonistGG-8573[12]
GV-150013[3]
LY288513[2]
PD136450[4]
Spiroglumide[1]
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 2Behavioral and neurochemical study on the role of the brain cholecystokinin system in anxiety. Hokkaido Igaku Zasshi. 1998 Sep;73(5):463-73. To Reference
Ref 3The 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 4Cholecystokinin type B receptor antagonist PD-136,450 is a partial secretory agonist in the stomach and a full agonist in the pancreas of the rat. Gut. 1994 Feb;35(2):270-4. To Reference
Ref 5Cholecystokinin-B/Gastrin receptor-targeting peptides for staging and therapy of medullary thyroid cancer and other cholecystokinin-B receptor-expressing malignancies. Semin Nucl Med. 2002 Apr;32(2):97-109. To Reference
Ref 6Cholecystokinin-B/gastrin receptor: a novel molecular probe for human small cell lung cancer. Cancer Res. 1995 Jan 15;55(2):276-9. To Reference
Ref 7Comparison of postprandial and ceruletide serum bile acid stimulation in dogs. J Vet Intern Med. 2008 Jul-Aug;22(4):873-8. To Reference
Ref 8Functional interactions between endocannabinoid and CCK neurotransmitter systems may be critical for extinction learning. Neuropsychopharmacology. 2009 Jan;34(2):509-21. Epub 2008 Jun 25. To Reference
Ref 9Molecular cloning of the human brain and gastric cholecystokinin receptor: structure, functional expression and chromosomal localization. Biochem Biophys Res Commun. 1992 Nov 30;189(1):296-303. To Reference
Ref 10The effects of central administration of the CCK-B receptor agonist pentagastrin on feeding and cortisol release in sheep. Methods Find Exp Clin Pharmacol. 1996 May;18(4):235-8. To Reference
Ref 11The human brain cholecystokinin-B/gastrin receptor. Cloning and characterization. J Biol Chem. 1993 Apr 15;268(11):8164-9. To Reference
Ref 12Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60. To Reference
Ref 13J Med Chem. 2010 Sep 9;53(17):6386-97.Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential. To Reference
Ref 14Bioorg. Med. Chem. Lett. 3(5):889-894 (1993) To Reference
Ref 15J 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 16Bioorg. Med. Chem. Lett. 3(5):881-884 (1993) To Reference
Ref 17J Med Chem. 2004 Oct 7;47(21):5318-29.5-(tryptophylamino)-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based cholecystokinin receptor antagonists: reversal of CCK1 receptor subtype selectivity toward CCK2 receptors. To Reference
Ref 18J 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 19J 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 20J 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 21Bioorg. Med. Chem. Lett. 7(7):805-810 (1997) To Reference
Ref 22J Med Chem. 1997 Nov 21;40(24):3947-56.Synthesis and biological properties of new constrained CCK-B antagonists: discrimination of two affinity states of the CCK-B receptor on transfected CHO cells. To Reference
Ref 23J 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 24J 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



 

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