The present study characterized Chinese hamster ovary cells overexpressing a human intestinal peptide transporter, CHO/hPEPT1 cells, as an in vitro model for peptidomimetic drugs. The kinetic parameters of Gly-Sar uptake were determined in three different cell culture systems such as untransfected CHO cells (CHO-K1), transfected CHO cells (CHO/hPEPT1) and Caco-2 cells. Vmax in CHO/hPEPT1 cells ...

During the past two decades, great strides have been made in the design of peptidomimetic drugs for the treatment of viral infections, despite the stigma of poor drug-like properties, low oral absorption, and high clearance associated with such compounds. This Account summarizes the progress made toward overcoming such liabilities and highlights the drug discovery efforts that have focused spec...

In this paper, we report the relationship between anti-MERS-CoV activities of HKU4 derived peptides for some peptidomimetic compounds and various descriptors using quantitative structure activity relationships (QSAR) methods. The used were computed ChemSketch, Marvin Sketch ChemOffice software. principal components analysis (PCA) multiple linear regression (MLR) methods to propose a model with ...

1 Lysine-enriched analogs of the cecropin-mellitin hybrid peptide, CA1-7 M2-9 (designated 2 CM15), designed with optimized amphipathicity retained antimicrobial activity similar to 3 wild type CM15 and had substantially reduced hemolytic activity and cytotoxicity 4 towards cultured macrophages, resulting in enhanced selectivity. These lysine-enriched 5 analogs provide templates for improved CM1...