Cholecystokinin receptor type A

Function

Receptor for cholecystokinin. Mediates pancreatic growth and enzyme secretion, smooth muscle contraction of the gall bladder and stomach. 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 proteins that activate a phosphatidylinositol-calcium second messenger system.

Classification

Family (Pfam)

PF00001 7tm_1, PF09193 CholecysA-Rec_N

InterPro

Cholcskin_rcpt, Cholcy_rcpt_A, CholecystokininA_recpt_N, CholecystokininA_recpt_N_sf, GPCR_Rhodpsn, GPCR_Rhodpsn_7TM

Functional cluster

Membrane Transporters & GPCRs

Experimental structures · PDB · 14

• 1D6G NMR
• 1HZN NMR
• 7EZH EM 3.20A
• 7EZK EM 3.10A
• 7EZM EM 2.90A
• 7F8U X-ray 2.80A
• 7F8X X-ray 3.00A
• 7F8Y X-ray 2.50A
• 7MBX EM 1.95A
• 7MBY EM 2.44A
• 7XOU EM 3.20A
• 7XOV EM 3.00A
• … and 2 more

A predicted model is available from AlphaFold.

Gene Ontology · 9

• GO:0016020 membrane
• GO:0005886 plasma membrane
• GO:0004951 cholecystokinin receptor activity
• GO:0017046 peptide hormone binding
• GO:0032870 cellular response to hormone stimulus
• GO:0038188 cholecystokinin signaling pathway
• GO:0007186 G protein-coupled receptor signaling pathway
• GO:0007200 phospholipase C-activating G protein-coupled receptor signaling pathway
• GO:0046883 regulation of hormone secretion

Drugs targeting this protein · 5

• SINCALIDE agonist
• CERULETIDE DIETHYLAMINE agonist
• CE-326597 agonist
• PROGLUMIDE antagonist
• DEXLOXIGLUMIDE antagonist

Related proteins · sequence + function similarity

• Cholecystokinin receptor type A 0.99
• Cholecystokinin receptor type A 0.99
• Cholecystokinin receptor type A 0.99
• Cholecystokinin receptor type A 0.98
• Cholecystokinin receptor type A 0.98
• Cholecystokinin receptor 0.94
• Neuromedin-U receptor 1 0.81
• Somatostatin receptor type 1 0.81
• Somatostatin receptor type 1 0.81
• Somatostatin receptor type 1 0.81
• Somatostatin receptor type 1 0.81
• Neuropeptide Y receptor type 2 0.81

Literature · 8 cited papers

• 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
• Intermolecular interactions between cholecystokinin-8 and the third extracellular loop of the cholecystokinin A receptor. Biochemistry · 2001
• Gene structure of human cholecystokinin (CCK) type-A receptor: body fat content is related to CCK type-A receptor gene promoter polymorphism. FEBS Lett. · 2000
• Molecular complex of cholecystokinin-8 and N-terminus of the cholecystokinin A receptor by NMR spectroscopy. Biochemistry · 1999
• Molecular cloning and functional expression of the human gallbladder cholecystokinin A receptor. Biochem. Biophys. Res. Commun. · 1993
• Molecular cloning, functional expression and chromosomal localization of the human cholecystokinin type A receptor. Biochem. Biophys. Res. Commun. · 1993
• Abnormal processing of the human cholecystokinin receptor gene in association with gallstones and obesity. Gastroenterology · 1995