AT-1002 a 6-mer synthetic peptide belongs to an emerging novel class of compounds that reversibly increase paracellular transport of molecules across the epithelial barrier. AT-1002 can undergo Cys-Cys dimerization[1]. Undifferentiated Caco-2 cells are treated with AT-1002 and viability is assessed by measuring cellular ATP content. Treatment with AT-1002 for up to 3 h does not affect cell viability at any concentration. In particular, the viability of Caco-2 cells is not affected by 5 mg/mL AT-1002. AT-1002 reduces cell viability after 24 h at concentrations of 2.5 mg/mL and higher. However, the cells remain viable after 24 h if the cells are washed after exposure to AT-1002 for 3 h indicating that AT-1002 does not irreversibly damage cells[2]. AT-1002 treatment results in 3-fold increase in phosphotyrosine content of zonula occludens-1 (ZO-1)[2].
Kinase Assay
Cell Assay
Animal Administration
References
[1]. Li M, et al. Structure-activity relationship studies of permeability modulating peptide AT-1002. Bioorg Med Chem Lett. 2008 Aug 15;18(16):4584-6.
[2]. Gopalakrishnan S, et al. Mechanism of action of ZOT-derived peptide AT-1002, a tight junction regulator and absorption enhancer. Int J Pharm. 2009 Jan 5;365(1-2):121-30.
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