Macropinocytosis as a Key Determinant of Peptidomimetic Uptake in Cancer Cells.

ABSTRACT: Peptides and peptidomimetics represent the middle space between small molecules and large proteins-they retain the relatively small size and synthetic accessibility of small molecules while providing high binding specificity for biomolecular partners typically observed with proteins. During the course of our efforts to target intracellular protein-protein interactions in cancer, we observed that the cellular uptake of peptides is critically determined by the cell line-specifically, we noted that peptides show better uptake in cancer cells with enhanced macropinocytic indices. Here, we describe the results of our analysis of cellular penetration by different classes of conformationally stabilized peptides. We tested the uptake of linear peptides, peptide macrocycles, stabilized helices, β-h

SUBMITTER: Yoo DY 

PROVIDER: S-EPMC7755425 | biostudies-literature | 2020 Aug

REPOSITORIES: biostudies-literature