Inhibition of Porcine Aminopeptidase M (pAMP) by the Pentapeptide Microginins.

ABSTRACT: Aminopeptidase M (AMP) inhibition is of interest for several diseases, such as highly vascularized cancer types. AMP can be inhibited by linear pentapeptides isolated from Microcystis aeruginosa LTPNA08 (MG7XX). Porcine AMP inhibition-a model for human AMP-activity was spectrophotometrically measured by the formation of p-nitroanilide from L-leucine-p-nitroanilide substrate by AMP. AMP inhibition by MG770 exhibited comparable inhibition levels to amastatin (IC₅₀ values: 1.20 ± 0.1 μM and 0.98 ± 0.1 μM, respectively), while MG756 was slightly less potent (with IC₅₀ values of 3.26 ± 0.5 μM). Molecular modelling suggests a potential binding mode, based on the interaction with the Zn²⁺ cofactor, where MG770's extra methyl group contributes to the disturb

SUBMITTER: Ferreira GM 

PROVIDER: S-EPMC6930480 | biostudies-literature | 2019 Nov

REPOSITORIES: biostudies-literature