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heat-stable enterotoxin receptor; STA receptor; hSTAR; intestinal guanylate cyclase; GC-C (GUCY2C, GUC2C, STAR)
Function:
- activated by the endogenous peptide guanylin
- interacts via its C-terminal region with PDZK2
Structure:
- protein kinase domain is predicted to be catalytically inactive
- belongs to the adenylyl cyclase class-4/guanylyl cyclase family
- contains 1 guanylate cyclase domain
- contains 1 protein kinase domain
Compartment: membrane
Expression:
- intestine-specific
Pathology:
- receptor for the E.coli heat-stable enterotoxin (E.coli enterotoxin markedly stimulates the accumulation of cGMP in mammalian cells expressing GUCY2C
- reverse transcriptase, polymerase chain reaction analysis of lymph node biopsy specimens for GUCY2C mRNA taken during surgery for resection of colon cancer may allow for identification of submicroscopic metastases of tumor to local lymph nodes [3]
Pharmacology:
- GUCY2C agonists linaclotide (Linzess) [4] & plecanatide (Trulance) [5] FDA-approved for treatment of chronic constipation
General
cell surface receptor
glycoprotein
guanyl cyclase or guanylate cyclase
Properties
SIZE: entity length = 1073 aa
MW = 123 kD
COMPARTMENT: cellular membrane
MOTIF: signal sequence {1-23}
N-glycosylation site {N32}
N-glycosylation site {N75}
N-glycosylation site {N79}
N-glycosylation site {N195}
N-glycosylation site {N284}
N-glycosylation site {N307}
N-glycosylation site {N345}
N-glycosylation site {N357}
N-glycosylation site {N402}
transmembrane domain {431-454}
kinase domain
SITE: 489-749
MOTIF: ATP-binding site
NAME: ATP-binding site
Guanylate cyclase {824-954}
Database Correlations
OMIM 601330
UniProt P25092
PFAM correlations
Entrez Gene 2984
Kegg hsa:2984
ENZYME 4.6.1.2
References
- UniProt :accession P25092
- Journal Watch 20:15, 2000
- Cagir B et al
Guanylyl cyclase C messenger RNA is a biomarker for recurrent
stage II colorectal cancer.
Ann Intern Med 131:805, 1999
PMID: 10610624
- Prescriber's Letter 19(12): 2012
New Drug: Linzess (Linaclotide)
Detail-Document#: 281204
(subscription needed) http://www.prescribersletter.com
- FDA News Release. Jan 19, 2017
FDA approves Trulance for Chronic Idiopathic Constipation.
http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm537725.htm