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Literature summary for 1.1.1.3 extracted from

  • Skwarecki, A.S.; Schielmann, M.; Martynow, D.; Kawczynski, M.; Wisniewska, A.; Milewska, M.J.; Milewski, S.
    Antifungal dipeptides incorporating an inhibitor of homoserine dehydrogenase (2018), J. Pept. Sci., 24, e3060 .
    View publication on PubMed
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Inhibitors

Inhibitors Comment Organism Structure
5-hydroxy-4-oxo-L-norvaline HONV, the mechanism of antifungal action of HONV dipeptides (determined against Candida albicans strain ATCC 10231 cells in three different growth media) involves uptake by the oligopeptide transport system, subsequent intracellular cleavage by cytosolic peptidases, and inhibition of homoserine dehydrogenase by the released HONV. Chemical synthesis of HONV and construction of HONV dipeptides as potential antifungal agents, overview. Six dipeptides with L-alanine, L-valine, L-norvaline (Nva), L-leucine, L-isoleucine, and L-phenylalanine as the N-terminal residues are obtained, Gly-HONV and D-Leu-HONV are synthesized and evaluated for comparative purposes. Antifungal in vitro activity and MIC values of HONV and its dipeptides, overview. Activity of HONV strongly depends on growth medium composition. Dipeptide (S)-2-N-[(R)-leucyl]amino-5-hydroxy-4-oxopentanoic acid (D-Leu-HONV) is inactive in all growth media. Antifungal activity of the compounds against different Candida species. Lack of activity of HONV-containing dipeptides against the Candida albicans opt1-opt5DELTA ptr2DELTA ptr22DELTA mutant clearly indicates that these compounds are transported to Candida albicans cells by the oligopeptide transport system, most probably by the di-tripeptide permeases Ptr2p and Ptr22, uptake rates into Candida albicans strain ATCC 10231 cells at pH 5.0 and pH 7.0 are determined, the initial uptake velocities are generally higher at pH 5.0 than at pH 7.0 Candida albicans
glycyl-5-hydroxy-4-oxo-L-norvaline i.e. (S)-2-N-glycylamino-5-hydroxy-4-oxopentanoic acid Candida albicans
L-alanyl-5-hydroxy-4-oxo-L-norvaline i.e. (S)-2-N-[(S)-alanyl]amino-5-hydroxy-4-oxopentanoic acid Candida albicans
L-isoleucyl-5-hydroxy-4-oxo-L-norvaline i.e. (S)-2-N-[(S)-isoleucyl]amino-5-hydroxy-4-oxopentanoic acid Candida albicans
L-leucyl-5-hydroxy-4-oxo-L-norvaline i.e. (S)-2-N-[(S)-leucyl]amino-5-hydroxy-4-oxopentanoic acid Candida albicans
L-norvalyl-5-hydroxy-4-oxo-L-norvaline i.e. (S)-2-N-[(S)-norvalyl]amino-5-hydroxy-4-oxopentanoic acid Candida albicans
L-phenylalanyl-5-hydroxy-4-oxo-L-norvaline i.e. (S)-2-N-[(S)-phenylalanyl]amino-5-hydroxy-4-oxopentanoic acid Candida albicans
L-valyl-5-hydroxy-4-oxo-L-norvaline i.e. (S)-2-N-[(S)-valyl]amino-5-hydroxy-4-oxopentanoic acid Candida albicans

Organism

Organism UniProt Comment Textmining
Candida albicans Q5AIA2
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Candida albicans ATCC MYA-2876 Q5AIA2
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