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divertin
Mechanism of action:
- blocks MLCK1 recruitment without inhibiting enzymatic function
- blocks TNF-induced MLCK1 recruitment & downstream myosin light chain phosphorylation, intestinal barrier loss, & diarrhea in vitro & in vivo
- corrects intestinal barrier dysfunction & prevents disease development & progression in experimental inflammatory bowel disease
General
gastrointestinal agent
References
- Thomas, H.
Identifying a specific small molecule to reverse intestinal barrier loss.
Nat Rev Gastroenterol Hepatol 16, 325 2019
PMID: 30992543
https://www.nature.com/articles/s41575-019-0149-3
- Graham WV, He W, Marchiando AM et al
Intracellular MLCK1 diversion reverses barrier loss to restore mucosal homeostasis.
Nat Med 2019 Apr;25(4):690-700
PMID: 30936544 PMCID: PMC6461392 Free PMC article