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Synonyms: Constella® | Linzess® | MM-416775
linaclotide is an approved drug (FDA and EMA (2012))
Compound class: Peptide or derivative
Comment: Linaclotide represents a first-in-class, oral guanylate cyclase 2C activator . It is a synthetic analogue of pathological heat-stable bacterial enterotoxins, and retains the same intrachain disulfide bond structure essential for biological activity.
Marketed formulations contain linaclotide acetate (PubChem CID 16158207). See also plecanatide, the second approved GC-C activator.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
View more information in the IUPHAR Pharmacology Education Project: linactolide
1. Bharucha AE, Waldman SA. (2010)
Taking a lesson from microbial diarrheagenesis in the management of chronic constipation.
Gastroenterology, 138 (3): 813-7. [PMID:20114092]
2. Busby RW, Bryant AP, Bartolini WP, Cordero EA, Hannig G, Kessler MM, Mahajan-Miklos S, Pierce CM, Solinga RM, Sun LJ et al.. (2010)
Linaclotide, through activation of guanylate cyclase C, acts locally in the gastrointestinal tract to elicit enhanced intestinal secretion and transit.
Eur J Pharmacol, 649 (1-3): 328-35. [PMID:20863829]
3. Harris LA, Crowell MD. (2007)
Linaclotide, a new direction in the treatment of irritable bowel syndrome and chronic constipation.
Curr Opin Mol Ther, 9 (4): 403-10. [PMID:17694454]
4. Shailubhai K. (2002)
Therapeutic applications of guanylate cyclase-C receptor agonists.
Curr Opin Drug Discov Devel, 5 (2): 261-8. [PMID:11926132]