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

Glaucio Monteiro FerreiraThales KronenbergerÉryka Costa de AlmeidaJoseane SampaioClélia Ferreira TerraErnani PintoGustavo Henrique Goulart Trossini
Published in: Molecules (Basel, Switzerland) (2019)
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 disturbance of the Zn2+ cofactor complex and highlights the importance of hydrophobicity for the site.
Keyphrases
  • protein kinase
  • endothelial cells
  • squamous cell carcinoma
  • anti inflammatory
  • transcription factor