Gastrin/cholecystokinin type B receptor

Details

Name
Gastrin/cholecystokinin type B receptor
Synonyms
  • CCK-B receptor
  • CCK2-R
  • CCKRB
  • Cholecystokinin-2 receptor
Gene Name
CCKBR
Organism
Humans
Amino acid sequence
>lcl|BSEQ0002303|Gastrin/cholecystokinin type B receptor
MELLKLNRSVQGTGPGPGASLCRPGAPLLNSSSVGNLSCEPPRIRGAGTRELELAIRITL
YAVIFLMSVGGNMLIIVVLGLSRRLRTVTNAFLLSLAVSDLLLAVACMPFTLLPNLMGTF
IFGTVICKAVSYLMGVSVSVSTLSLVAIALERYSAICRPLQARVWQTRSHAARVIVATWL
LSGLLMVPYPVYTVVQPVGPRVLQCVHRWPSARVRQTWSVLLLLLLFFIPGVVMAVAYGL
ISRELYLGLRFDGDSDSDSQSRVRNQGGLPGAVHQNGRCRPETGAVGEDSDGCYVQLPRS
RPALELTALTAPGPGSGSRPTQAKLLAKKRVVRMLLVIVVLFFLCWLPVYSANTWRAFDG
PGAHRALSGAPISFIHLLSYASACVNPLVYCFMHRRFRQACLETCARCCPRPPRARPRAL
PDEDPPTPSIASLSRLSYTTISTLGPG
Number of residues
447
Molecular Weight
48418.51
Theoretical pI
10.24
GO Classification
Functions
1-phosphatidylinositol-3-kinase regulator activity / cholecystokinin receptor activity / gastrin receptor activity / phosphatidylinositol phospholipase C activity / type B gastrin/cholecystokinin receptor binding
Processes
cell proliferation / cell surface receptor signaling pathway / cholecystokinin signaling pathway / digestion / digestive tract development / feeding behavior / gastric acid secretion / gland development / phospholipase C-activating G-protein coupled receptor signaling pathway / positive regulation of cell proliferation / positive regulation of cytosolic calcium ion concentration / regulation of phosphatidylinositol 3-kinase activity / sensory perception
Components
cytosol / integral component of plasma membrane / plasma membrane
General Function
Type b gastrin/cholecystokinin receptor binding
Specific Function
Receptor for gastrin and cholecystokinin. 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 that activate a phosphatidylinositol-calcium second messenger system.Isoform 2 is constitutively activated and may regulate cancer cell proliferation via a gastrin-independent mechanism.
Pfam Domain Function
Transmembrane Regions
58-79 88-109 132-150 171-189 220-242 334-355 374-394
Cellular Location
Cell membrane
Gene sequence
>lcl|BSEQ0019073|Gastrin/cholecystokinin type B receptor (CCKBR)
ATGGAGCTGCTAAAGCTGAACCGGAGCGTGCAGGGAACCGGACCCGGGCCGGGGGCTTCC
CTGTGCCGCCCGGGGGCGCCTCTCCTCAACAGCAGCAGTGTGGGCAACCTCAGCTGCGAG
CCCCCTCGCATTCGCGGAGCCGGGACACGAGAATTGGAGCTGGCCATTAGAATCACTCTT
TACGCAGTGATCTTCCTGATGAGCGTTGGAGGAAATATGCTCATCATCGTGGTCCTGGGA
CTGAGCCGCCGCCTGAGGACTGTCACCAATGCCTTCCTCCTCTCACTGGCAGTCAGCGAC
CTCCTGCTGGCTGTGGCTTGCATGCCCTTCACCCTCCTGCCCAATCTCATGGGCACATTC
ATCTTTGGCACCGTCATCTGCAAGGCGGTTTCCTACCTCATGGGGGTGTCTGTGAGTGTG
TCCACGCTAAGCCTCGTGGCCATCGCACTGGAGCGGTACAGCGCCATCTGCCGACCACTG
CAGGCACGAGTGTGGCAGACGCGCTCCCACGCGGCTCGCGTGATTGTAGCCACGTGGCTG
CTGTCCGGACTACTCATGGTGCCCTACCCCGTGTACACTGTCGTGCAACCAGTGGGGCCT
CGTGTGCTGCAGTGCGTGCATCGCTGGCCCAGTGCGCGGGTCCGCCAGACCTGGTCCGTA
CTGCTGCTTCTGCTCTTGTTCTTCATCCCGGGTGTGGTTATGGCCGTGGCCTACGGGCTT
ATCTCTCGCGAGCTCTACTTAGGGCTTCGCTTTGACGGCGACAGTGACAGCGACAGCCAA
AGCAGGGTCCGAAACCAAGGCGGGCTGCCAGGGGCTGTTCACCAGAACGGGCGTTGCCGG
CCTGAGACTGGCGCGGTTGGCGAAGACAGCGATGGCTGCTACGTGCAACTTCCACGTTCC
CGGCCTGCCCTGGAGCTGACGGCGCTGACGGCTCCTGGGCCGGGATCCGGCTCCCGGCCC
ACCCAGGCCAAGCTGCTGGCTAAGAAGCGCGTGGTGCGAATGTTGCTGGTGATCGTTGTG
CTTTTTTTTCTGTGTTGGTTGCCAGTTTATAGTGCCAACACGTGGCGCGCCTTTGATGGC
CCGGGTGCACACCGAGCACTCTCGGGTGCTCCTATCTCCTTCATTCACTTGCTGAGCTAC
GCCTCGGCCTGTGTCAACCCCCTGGTCTACTGCTTCATGCACCGTCGCTTTCGCCAGGCC
TGCCTGGAAACTTGCGCTCGCTGCTGCCCCCGGCCTCCACGAGCTCGCCCCAGGGCTCTT
CCCGATGAGGACCCTCCCACTCCCTCCATTGCTTCGCTGTCCAGGCTTAGCTACACCACC
ATCAGCACACTGGGCCCTGGCTGA
Chromosome Location
11
Locus
11p15.4
External Identifiers
ResourceLink
UniProtKB IDP32239
UniProtKB Entry NameGASR_HUMAN
GenBank Protein ID306489
GenBank Gene IDL08112
GenAtlas IDCCKBR
HGNC IDHGNC:1571
General References
  1. Pisegna JR, de Weerth A, Huppi K, Wank SA: Molecular 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. [PubMed:1280419]
  2. Lee YM, Beinborn M, McBride EW, Lu M, Kolakowski LF Jr, Kopin AS: The human brain cholecystokinin-B/gastrin receptor. Cloning and characterization. J Biol Chem. 1993 Apr 15;268(11):8164-9. [PubMed:7681836]
  3. Ito M, Matsui T, Taniguchi T, Tsukamoto T, Murayama T, Arima N, Nakata H, Chiba T, Chihara K: Functional characterization of a human brain cholecystokinin-B receptor. A trophic effect of cholecystokinin and gastrin. J Biol Chem. 1993 Aug 25;268(24):18300-5. [PubMed:8349705]
  4. Song I, Brown DR, Wiltshire RN, Gantz I, Trent JM, Yamada T: The human gastrin/cholecystokinin type B receptor gene: alternative splice donor site in exon 4 generates two variant mRNAs. Proc Natl Acad Sci U S A. 1993 Oct 1;90(19):9085-9. [PubMed:8415658]
  5. Herget T, Sethi T, Wu SV, Walsh JH, Rozengurt E: Cholecystokinin stimulates Ca2+ mobilization and clonal growth in small cell lung cancer through CCKA and CCKB/gastrin receptors. Ann N Y Acad Sci. 1994 Mar 23;713:283-97. [PubMed:8185170]
  6. Ito M, Iwata N, Taniguchi T, Murayama T, Chihara K, Matsui T: Functional characterization of two cholecystokinin-B/gastrin receptor isoforms: a preferential splice donor site in the human receptor gene. Cell Growth Differ. 1994 Oct;5(10):1127-35. [PubMed:7848914]
  7. Miyake A: A truncated isoform of human CCK-B/gastrin receptor generated by alternative usage of a novel exon. Biochem Biophys Res Commun. 1995 Mar 8;208(1):230-7. [PubMed:7887934]
  8. Hellmich MR, Rui XL, Hellmich HL, Fleming RY, Evers BM, Townsend CM Jr: Human colorectal cancers express a constitutively active cholecystokinin-B/gastrin receptor that stimulates cell growth. J Biol Chem. 2000 Oct 13;275(41):32122-8. [PubMed:10913157]
  9. Schmitz F, Schrader H, Otte J, Schmitz H, Stuber E, Herzig K, Schmidt WE: Identification of CCK-B/gastrin receptor splice variants in human peripheral blood mononuclear cells. Regul Pept. 2001 Sep 15;101(1-3):25-33. [PubMed:11495676]
  10. Smith JP, Verderame MF, McLaughlin P, Martenis M, Ballard E, Zagon IS: Characterization of the CCK-C (cancer) receptor in human pancreatic cancer. Int J Mol Med. 2002 Dec;10(6):689-94. [PubMed:12429993]
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  13. O'Briant KC, Ali SY, Weier HU, Bepler G: An 84-kilobase physical map and repeat polymorphisms of the gastrin/cholecystokinin brain receptor region at the junction of chromosome segments 11p15.4 and 15.5. Chromosome Res. 1998 Aug;6(5):415-8. [PubMed:9872672]
  14. Sethi T, Herget T, Wu SV, Walsh JH, Rozengurt E: CCKA and CCKB receptors are expressed in small cell lung cancer lines and mediate Ca2+ mobilization and clonal growth. Cancer Res. 1993 Nov 1;53(21):5208-13. [PubMed:8221657]
  15. Zimonjic DB, Popescu NC, Matsui T, Ito M, Chihara K: Localization of the human cholecystokinin-B/gastrin receptor gene (CCKBR) to chromosome 11p15.5-->p15.4 by fluorescence in situ hybridization. Cytogenet Cell Genet. 1994;65(3):184-5. [PubMed:8222757]
  16. Giragossian C, Mierke DF: Intermolecular interactions between cholecystokinin-8 and the third extracellular loop of the cholecystokinin-2 receptor. Biochemistry. 2002 Apr 9;41(14):4560-6. [PubMed:11926817]

Drug Relations

Drug Relations
DrugBank IDNameDrug groupPharmacological action?ActionsDetails
DB00183PentagastrinapprovedyesagonistDetails
DB08862Cholecystokininapproved, investigationalunknownagonistDetails