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gastrin/cholecystokinin type B receptor; CCK-B receptor; CCK-BR; cholecystokinin-2 receptor; CCK2-R (CCKBR, CCKRB)
Function:
- receptor for gastrin & cholecystokinin
- the CKK-B receptors occur throughout the CNS where they modulate anxiety, analgesia, arousal, & neuroleptic activity
- mediates its action by association with G proteins that activate a phosphatidylinositol-Ca+2 second messenger system
- isoform 2 may regulate cancer cell proliferation via a gastrin-independent mechanism
Structure: belongs to the G-protein coupled receptor 1 family
Compartment: cell membrane
Alternative splicing: named isoforms=3
Expression:
- isoform 1 is expressed in brain, pancreas, stomach,
- within the stomach, expressed at high levels in the mucosa of the gastric fundus & at low levels in the antrum & duodenum
- isoform 1 is not expressed in heart, placenta, liver, lung, skeletal muscle, or kidney
- isoform 3 is expressed in brain, pancreas, stomach
Pathology:
- isoform 1 is expressed in the colon cancer cell line LoVo & the T-lymphoblastoma Jurkat, but not in the stomach cancer cell line AGS
- expressed at high levels in the small cell lung cancer cell line H510, at lower levels in H345, H69 & GLC28
- not expressed in GLC19
- isoform 2 is present in pancreatic cancer cells & colorectal cancer cells, but not in normal pancreas or colonic mucosa
- isoform 3 is expressed in the stomach cancer cell line AGS & the colon cancer cell line LoVo; it is also expressed in normal stomach
General
cholecystokinin [CCK] receptor
glycoprotein
G-protein coupled receptor; serpentine receptor
Properties
SIZE: entity length = 447 aa
MW = 48 kD
COMPARTMENT: plasma membrane
MOTIF: exoplasmic domain {1-57}
MOTIF: N-glycosylation site {N7}
N-glycosylation site {N30}
N-glycosylation site {N36}
transmembrane domain {58-79}
cytoplasmic loop {80-87}
transmembrane domain {88-109}
exoplasmic loop {110-131}
MOTIF: cysteine residue {C127}
MODIFICATION: cysteine residue {C205}
transmembrane domain {132-150}
cytoplasmic loop {151-170}
transmembrane domain {171-189}
exoplasmic loop {190-219}
MOTIF: cysteine residue {C205}
MODIFICATION: cysteine residue {C127}
transmembrane domain {220-242}
cytoplasmic loop {243-333}
transmembrane domain {334-355}
exoplasmic loop {356-373}
transmembrane domain {374-394}
cytoplasmic domain {395-447}
MOTIF: cysteine residue {C408}
MODIFICATION: palmitate
COMPARTMENT: membrane
Database Correlations
OMIM 118445
UniProt P32239
Pfam PF00001
Kegg hsa:887
References
- UniProt :accession P32239
- Wikipedia; Note: cholecystokinin receptor entry
http://en.wikipedia.org/wiki/cholecystokinin_receptor