heat-stable enterotoxin receptor; STA receptor; hSTAR; intestinal guanylate cyclase; GC-C (GUCY2C, GUC2C, STAR)
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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
More general terms
References
- ↑ UniProt http://www.uniprot.org/uniprot/P25092.html
- ↑ Journal Watch 20:15, 2000
- ↑ 3.0 3.1 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: https://www.ncbi.nlm.nih.gov/pubmed/10610624
- ↑ 4.0 4.1 Prescriber's Letter 19(12): 2012 New Drug: Linzess (Linaclotide) Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=281204&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 5.0 5.1 FDA News Release. Jan 19, 2017 FDA approves Trulance for Chronic Idiopathic Constipation. http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm537725.htm