Gastrin/cholecystokinin type B receptor

UniProt P32239 Organism Homo sapiens Gene CCKBR, CCKRB

Also known as: CCKBR, CCKRB

Function

Receptor for the peptide hormones gastrin and cholecystokinin (CCK). Expressed throughout the central nervous system, where it modulates processes such as anxiety, analgesia, arousal and neuroleptic activity. Couples to both GNAI1 and GNAQ signaling pathways, but not to GNAS. Upon gastrin activation, reduces glucose absorption in intestinal epithelial cells by downregulating SGLT1 and GLUT2 expression through suppression of the PI3K/Akt/eIF4B pathway (By similarity). In the kidney, decreases SGLT2 expression under high-glucose conditions via ERK/NF-kappa-B signaling (By similarity).

Classification

Family (Pfam): PF00001 7tm_1
InterPro: Cholcskin_rcpt, Gastrin_rcpt, GPCR_Rhodpsn, GPCR_Rhodpsn_7TM
Functional cluster: Nucleic Acid Metabolism & Repair Enzymes

Experimental structures · PDB · 5

1L4T NMR
7F8V EM 3.30A
7F8W EM 3.10A
7XOW EM 3.10A
8IA7 EM 3.10A

A predicted model is available from AlphaFold.

Gene Ontology · 14

Drugs targeting this protein · 4

ITRIGLUMIDE antagonist
CI-988 antagonist
PROGLUMIDE antagonist
NETAZEPIDE antagonist

Related proteins · sequence + function similarity

Co-cited proteins · studied together in the literature

Guanine nucleotide-binding protein G(q) subunit alpha 2 shared papers

Literature · 18 cited papers

Structural insights into human brain-gut peptide cholecystokinin receptors. Cell Discov. · 2022
Structures of the human cholecystokinin receptors bound to agonists and antagonists. Nat. Chem. Biol. · 2021
The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). Genome Res. · 2004
Complete sequencing and characterization of 21,243 full-length human cDNAs. Nat. Genet. · 2004
Characterization of the CCK-C (cancer) receptor in human pancreatic cancer. Int. J. Mol. Med. · 2002
Intermolecular interactions between cholecystokinin-8 and the third extracellular loop of the cholecystokinin-2 receptor. Biochemistry · 2002
Identification of CCK-B/gastrin receptor splice variants in human peripheral blood mononuclear cells. Regul. Pept. · 2001
Human colorectal cancers express a constitutively active cholecystokinin-B/gastrin receptor that stimulates cell growth. J. Biol. Chem. · 2000
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
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
Functional characterization of a human brain cholecystokinin-B receptor. A trophic effect of cholecystokinin and gastrin. J. Biol. Chem. · 1993
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
… and 6 more in the literature graph

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