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The Anti-Candida albicans Agent 4-AN Inhibits Multiple Protein Kinases
- Source :
- Molecules, Molecules, MDPI, 2019, 24 (1), pp.153. ⟨10.3390/molecules24010153⟩, Molecules, Vol 24, Iss 1, p 153 (2019), Volume 24, Issue 1
- Publication Year :
- 2019
- Publisher :
- HAL CCSD, 2019.
-
Abstract
- International audience; Small molecules containing quinone and/or oxime moieties have been found as promising anti-fungal agents. One of them is 4-AN, a recently reported potent anti-Candida compound, which inhibits the formation of hyphae, decreases the level of cellular phosphoproteome, and finally shows no toxicity towards human erythrocytes and zebrafish embryos. Here, further research on 4-AN is presented. The results revealed that the compound: (i) Kills Candida clinical isolates, including these with developed antibiotic resistance, (ii) affects mature biofilm, and (iii) moderately disrupts membrane permeability. Atomic force microscopy studies revealed a slight influence of 4-AN on the cell surface architecture. 4-AN was also shown to inhibit multiple various protein kinases, a characteristic shared by most of the ATP-competitive inhibitors. The presented compound can be used in novel strategies in the fight against candidiasis, and reversible protein phosphorylation should be taken into consideration as a target in designing these strategies.
- Subjects :
- Models, Molecular
Antifungal Agents
[SDV]Life Sciences [q-bio]
Cell
Drug Evaluation, Preclinical
Pharmaceutical Science
[CHIM.THER]Chemical Sciences/Medicinal Chemistry
Analytical Chemistry
0302 clinical medicine
Drug Discovery
Oximes
Candida albicans
Protein phosphorylation
antifungal agent
Phosphorylation
[SDV.MP.MYC]Life Sciences [q-bio]/Microbiology and Parasitology/Mycology
ComputingMilieux_MISCELLANEOUS
0303 health sciences
atomic force microscopy
biology
Molecular Structure
Kinase
Chemistry
Quinones
Drug Resistance, Microbial
Small molecule
medicine.anatomical_structure
Biochemistry
Chemistry (miscellaneous)
030220 oncology & carcinogenesis
Toxicity
Molecular Medicine
arylcyanomethylenequinones
Protein Binding
Membrane permeability
Surface Properties
4-AN
Microbial Sensitivity Tests
Article
lcsh:QD241-441
03 medical and health sciences
lcsh:Organic chemistry
medicine
Humans
[CHIM]Chemical Sciences
Physical and Theoretical Chemistry
Protein Kinase Inhibitors
030304 developmental biology
protein kinases
Organic Chemistry
Cell Membrane
Biofilm
Biological Transport
biology.organism_classification
Biofilms
Subjects
Details
- Language :
- English
- ISSN :
- 14203049
- Database :
- OpenAIRE
- Journal :
- Molecules, Molecules, MDPI, 2019, 24 (1), pp.153. ⟨10.3390/molecules24010153⟩, Molecules, Vol 24, Iss 1, p 153 (2019), Volume 24, Issue 1
- Accession number :
- edsair.doi.dedup.....e8ba6a679dc560fe4e507183c2d4badf
- Full Text :
- https://doi.org/10.3390/molecules24010153⟩