Antifungal dipeptides incorporating an inhibitor of homoserine dehydrogenase. (11th January 2018)
- Record Type:
- Journal Article
- Title:
- Antifungal dipeptides incorporating an inhibitor of homoserine dehydrogenase. (11th January 2018)
- Main Title:
- Antifungal dipeptides incorporating an inhibitor of homoserine dehydrogenase
- Authors:
- Skwarecki, Andrzej S.
Schielmann, Marta
Martynow, Dorota
Kawczyński, Marcin
Wiśniewska, Aleksandra
Milewska, Maria J.
Milewski, Sławomir - Abstract:
- Abstract : The antifungal activity of 5‐hydroxy‐4‐oxo‐l ‐norvaline (HONV), exhibited under conditions mimicking human serum, may be improved upon incorporation of this amino acid into a dipeptide structure. Several HONV‐containing dipeptides inhibited growth of human pathogenic yeasts of the Candida genus in the RPMI‐1640 medium, with minimal inhibitory concentration values in the 32 to 64 μg mL −1 range. This activity was not affected by multidrug resistance that is caused by overexpression of genes encoding drug efflux proteins. The mechanism of antifungal action of HONV dipeptides involved uptake by the oligopeptide transport system, subsequent intracellular cleavage by cytosolic peptidases, and inhibition of homoserine dehydrogenase by the released HONV. The relative transport rates determined the anticandidal activity of HONV dipeptides. Abstract : Incorporation of 5‐hydroxy‐4‐oxo‐L‐norvaline (HONV) into a dipeptide structure following the "Trojan horse" strategy afforded compounds demonstrating higher than the mother amino acid antifungal in vitro activity in the RPMI‐1640 medium. The mechanism of antifungal action of HONV‐containing dipeptides involved uptake by the oligopeptide transport system, subsequent intracellular cleavage by cytosolic peptidases and inhibition of homoserine dehydrogenase by the released HONV.
- Is Part Of:
- Journal of peptide science. Volume 24:Number 1(2018)
- Journal:
- Journal of peptide science
- Issue:
- Volume 24:Number 1(2018)
- Issue Display:
- Volume 24, Issue 1 (2018)
- Year:
- 2018
- Volume:
- 24
- Issue:
- 1
- Issue Sort Value:
- 2018-0024-0001-0000
- Page Start:
- n/a
- Page End:
- n/a
- Publication Date:
- 2018-01-11
- Subjects:
- antifungal agents -- dipeptides -- homoserine dehydrogenase -- oligopeptide uptake
Peptides -- Periodicals
Peptides -- Periodicals
572.65 - Journal URLs:
- http://onlinelibrary.wiley.com/ ↗
- DOI:
- 10.1002/psc.3060 ↗
- Languages:
- English
- ISSNs:
- 1075-2617
- Deposit Type:
- Legaldeposit
- View Content:
- Available online (eLD content is only available in our Reading Rooms) ↗
- Physical Locations:
- British Library DSC - 5030.530000
British Library DSC - BLDSS-3PM
British Library STI - ELD Digital store - Ingest File:
- 5640.xml