Synthesis and bioactivity of pyrrole-conjugated phosphopeptides.

ABSTRACT: Here we report the synthesis and effect on the cell viability of pyrrole-conjugated phosphopeptides. Encouraged by the selective inhibition of cancer cells by a naphthyl-capped phosphopeptide (Nap-ff_py, 1), we conjugated the heteroaromatic dipyrrole or tripyrrole motif at the N-terminal of short peptides containing phosphotyrosine or phosphoserine and examined the bioactivity of the resulting phosphopeptides (2-10). Although most of the phosphopeptides exhibit comparable activities with that of 1 against HeLa cells at 200 μM, they, differing from 1, are largely compatible with HeLa cells at 400 μM. Enzymatic dephosphorylation of 2-10, at 400 μM is unable to induce a dramatic morphological transition of the peptide assemblies obser

SUBMITTER: Zhang Q 

PROVIDER: S-EPMC8822458 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature