4.3 Article

A new small-molecule KRE2 inhibitor against invasive Candida parapsilosis infection

期刊

FUTURE MICROBIOLOGY
卷 12, 期 14, 页码 1283-1295

出版社

FUTURE MEDICINE LTD
DOI: 10.2217/fmb-2017-0065

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invasive candidiasis; KRE2 protein; virtual screening

资金

  1. Cnpq
  2. Capes
  3. Fundacao Araucaria

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Aim: To investigate the antifungal activity of MOL3, a small molecule that was selected by virtual screening, against Candida spp. Materials & methods: The antifungal activity of MOL3 was evaluated using standard strains and clinical isolates. Activity was evaluated in both in vitro tests and animal models. Results: The minimum fungicidal concentration of MOL3 against Candida spp. ranged from 16 to 128 mg/l. MOL3 at the sub-minimum fungicidal concentration inhibited hyphal elongation. The remaining yeast cells presented morphological changes and were metabolically inactive. MOL3 was toxicologically inert both in vitro and in the animal model. MOL3 also reduced experimental systemic infection by C. parapsilosis in mice. Conclusion: The selection of MOL3 by virtual screening was successful, revealing a promising antifungal candidate.

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