The antifungal peptide CGA-N12 inhibits cell wall synthesis of Candida tropicalis by interacting with KRE9

Biochem J. 2020 Feb 14;477(3):747-762. doi: 10.1042/BCJ20190678.

Abstract

CGA-N12, an antifungal peptide derived from chromogranin A, has specific antagonistic activity against Candida spp., especially against Candida tropicalis, by inducing cell apoptosis. However, the effect of CGA-N12 on the Candida cell wall is unknown. The Candida protein KRE9, which possesses β-1,6-glucanase activity, was screened by affinity chromatography after binding to CGA-N12. In this study, the effect of CGA-N12 on KRE9 and the interaction between CGA-N12 and KRE9 was studied to clarify the effect of CGA-N12 on C. tropicalis cell wall synthesis. The effect of CGA-N12 on recombinant KRE9 β-1,6-glucanase activity was investigated by analyzing the consumption of glucose. The results showed that CGA-N12 inhibited the activity of KRE9. After C. tropicalis was treated with CGA-N12, the structure of the C. tropicalis cell wall was damaged. The interaction between CGA-N12 and KRE9 was analyzed by isothermal titration calorimetry (ITC). The results showed that their interaction process was involved an endothermic reaction, and the interaction force was mainly hydrophobic with a few electrostatic forces. The results of the fluorescence resonance energy transfer (FRET) assay showed that the distance between CGA-N12 and KRE9 was 7 ∼ 10 nm during their interaction. Therefore, we concluded that the target of CGA-N12 in the C. tropicalis cell membrane is KRE9, and that CGA-N12 weakly binds to KRE9 within a 7 ∼ 10 nm distance and inhibits KRE9 activity.

Keywords: 6-Glucanase; Antifungal peptide; CGA-N12; KRE9 protein; fluorescence resonance energy transfer; isothermal titration calorimetry; β-1.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antifungal Agents / pharmacology*
  • Candida tropicalis / drug effects*
  • Candida tropicalis / metabolism
  • Cell Wall / drug effects*
  • Cell Wall / metabolism
  • Chromogranin A / pharmacology*
  • Fluorescence Resonance Energy Transfer / methods
  • Glycoproteins / drug effects
  • Glycoproteins / metabolism
  • Glycoside Hydrolases / drug effects*
  • Glycoside Hydrolases / metabolism
  • Peptides / pharmacology

Substances

  • Antifungal Agents
  • Chromogranin A
  • Glycoproteins
  • Peptides
  • Glycoside Hydrolases