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PmV inhibitory activity of the generated compounds (1st set).

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posted on 2015-11-13, 02:47 authored by Luca Gambini, Luca Rizzi, Alessandro Pedretti, Orazio Taglialatela-Scafati, Mario Carucci, Andrea Pancotti, Corinna Galli, Martin Read, Emanuele Giurisato, Sergio Romeo, Ilaria Russo

IC50 values, obtained in the presence of 3 μM of HRPII-PExEl substrate, are shown. They are averages of not less than three independent inhibition curves. Standard errors of the calculation of the IC50s by sigmoidal fitting are shown in column ‘±’. HEA indicates the hydroxyethylamino group that links P1, the non-amino acidic leucine analog, (3S)-3-amino-2-hydroxy-5-methylhexyl- group, and P1', the alanine. HnV is hydroxynorvaline, a non-natural amino acid. Relevant modifications of 1 as follows: Panel a, C-terminus; b, P1'; c, P2'; d, P2; e, P3. Amino acids are three-letter and colour coded except for ‘[Leu-HEA-…]’ corresponding to the (3S)-3-amino-2-hydroxy-5-methylhexyl- group, as follows: hydrophobic amino acids (aa) are in shades of yellow; aromatic aa, orange; positively charged aa, purple; polar aa, blue; and acidic aa, grey. NS = Not significant; ND = not determined; NA = not applicable.