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Contrasting effects of linaclotide and lubiprostone on restitution of epithelial cell barrier properties and cellular homeostasis after exposure to cell stressors.

BMC Pharmacol.. 2012; 
CuppolettiJohn,BlikslagerAnthony T,ChakrabartiJayati,NighotPrashant K,MalinowskaDanu
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Biochemicals … The active form of linaclotide, MM-419447, (CCEYCCNPACTGC) was prepared by solid phase synthesis and disulfide bridges at 1–6,2–10 and 5–13 were introduced using a random/ thermodynamic strategy (6TRT) by GenScript Corporation (Piscataway, NJ) using the 6TRT … Get A Quote

摘要

Linaclotide has been proposed as a treatment for the same gastrointestinal indications for which lubiprostone has been approved, chronic idiopathic constipation and irritable bowel syndrome with constipation. Stressors damage the epithelial cell barrier and cellular homeostasis leading to loss of these functions. Effects of active linaclotide on repair of barrier and cell function in pig jejunum after ischemia and in T84 cells after treatment with proinflammatory cytokines, interferon-γ and tumor necrosis factor-α were examined. Comparison with effects of lubiprostone, known to promote repair of barrier function was carried out.

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