Literature DB >> 3149235

Antifungal peptides with novel specific inhibitors of glucosamine 6-phosphate synthase.

S Milewski1, H Chmara, R Andruszkiewicz, E Borowski, M Zaremba, J Borowski.   

Abstract

N3-4-Methoxyfumaroyl-L-2,3-diaminopropanoic acid (FMDP) has been found to be a strong and selective inhibitor of glucosamine 6-phosphate synthase from Candida albicans. Incorporation of FMDP into a dipeptide structure has produced effective antifungal agents (portage transport). A number of dipeptides containing FMDP have been synthesized, with Nva-FMDP showing the highest in vitro activity against different fungi, including Candida albicans (MIC90 = 2.2 micrograms/ml for 50 clinical strains), Cryptococcus neoformans and Aspergillus spp. This compound, when tested in a general candidiosis model infection in mice, gave PD50/10 and CD50/10 values of 5.0 and 1.63 mg/kg, respectively. Meanwhile, the LD50 value after i.v. administration was higher than 300 mg/kg.

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Year:  1988        PMID： 3149235

Source DB:  PubMed          Journal:  Drugs Exp Clin Res        ISSN： 0378-6501


  9 in total

1.  Mechanism of action of anticandidal dipeptides containing inhibitors of glucosamine-6-phosphate synthase.

Authors:  S Milewski; R Andruszkiewicz; L Kasprzak; J Mazerski; F Mignini; E Borowski
Journal:  Antimicrob Agents Chemother       Date:  1991-01       Impact factor: 5.191

2.  Role for chitin and chitooligomers in the capsular architecture of Cryptococcus neoformans.

Authors:  Fernanda L Fonseca; Leonardo Nimrichter; Radames J B Cordero; Susana Frases; Jessica Rodrigues; David L Goldman; Ryszard Andruszkiewicz; Slawomir Milewski; Luiz R Travassos; Arturo Casadevall; Marcio L Rodrigues
Journal:  Eukaryot Cell       Date:  2009-07-17

3.  A theoretical study of glucosamine synthase. II. Combined quantum and molecular mechanics simulation of sulfhydryl attack on the carboxyamide group.

Authors:  A Tempczyk; M Tarnowska; A Liwo; E Borowski
Journal:  Eur Biophys J       Date:  1992       Impact factor: 1.733

4.  Investigation of the inhibition pathway of glucosamine synthase by N3-(4-methoxyfumaroyl)-L-2,3-diaminopropanoic acid by semiempirical quantum mechanical and molecular mechanics methods.

Authors:  M Tarnowska; S Oldziej; A Liwo; Z Grzonka; E Borowski
Journal:  Eur Biophys J       Date:  1992       Impact factor: 1.733

5.  Isolation and characterization of the GFA1 gene encoding the glutamine:fructose-6-phosphate amidotransferase of Candida albicans.

Authors:  R J Smith; S Milewski; A J Brown; G W Gooday
Journal:  J Bacteriol       Date:  1996-04       Impact factor: 3.490

6.  Design, synthesis and validation of anti-microbial coumarin derivatives: An efficient green approach.

Authors:  Mohd Shahnawaz Khan; Ranu Agrawal; Mohammad Ubaidullah; Md Imtaiyaz Hassan; Nazia Tarannum
Journal:  Heliyon       Date:  2019-10-18

7.  Fluconazole resistant Candida auris clinical isolates have increased levels of cell wall chitin and increased susceptibility to a glucosamine-6-phosphate synthase inhibitor.

Authors:  Garima Shahi; Mohit Kumar; Andrzej S Skwarecki; Matt Edmondson; Atanu Banerjee; Jane Usher; Neil A R Gow; Sławomir Milewski; Rajendra Prasad
Journal:  Cell Surf       Date:  2022-02-25

8.  Inhibitors of glucosamine-6-phosphate synthase as potential antimicrobials or antidiabetics - synthesis and properties.

Authors:  Joanna Stefaniak; Michał G Nowak; Marek Wojciechowski; Sławomir Milewski; Andrzej S Skwarecki
Journal:  J Enzyme Inhib Med Chem       Date:  2022-12       Impact factor: 5.756

Review 9.  Cell compensatory responses of fungi to damage of the cell wall induced by Calcofluor White and Congo Red with emphasis on Sporothrix schenckii and Sporothrix globosa. A review.

Authors:  Jorge A Ortiz-Ramírez; Mayra Cuéllar-Cruz; Everardo López-Romero
Journal:  Front Cell Infect Microbiol       Date:  2022-09-23       Impact factor: 6.073
  9 in total

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