MK2a inhibitor CMPD1 abrogates chikungunya virus infection by modulating actin remodeling pathway

PLoS Pathog. 2021 Nov 15;17(11):e1009667. doi: 10.1371/journal.ppat.1009667. eCollection 2021 Nov.

Abstract

Chikungunya virus (CHIKV) epidemics around the world have created public health concern with the unavailability of effective drugs and vaccines. This emphasizes the need for molecular understanding of host-virus interactions for developing effective targeted antivirals. Microarray analysis was carried out using CHIKV strain (Prototype and Indian) infected Vero cells and two host isozymes, MAPK activated protein kinase 2 (MK2) and MAPK activated protein kinase 3 (MK3) were selected for further analysis. The substrate spectrum of both enzymes is indistinguishable and covers proteins involved in cytokines production, endocytosis, reorganization of the cytoskeleton, cell migration, cell cycle control, chromatin remodeling and transcriptional regulation. Gene silencing and drug treatment were performed in vitro and in vivo to unravel the role of MK2/MK3 in CHIKV infection. Gene silencing of MK2 and MK3 abrogated around 58% CHIKV progeny release from the host cell and a MK2 activation inhibitor (CMPD1) treatment demonstrated 68% inhibition of viral infection suggesting a major role of MAPKAPKs during late CHIKV infection in vitro. Further, it was observed that the inhibition in viral infection is primarily due to the abrogation of lamellipodium formation through modulation of factors involved in the actin cytoskeleton remodeling pathway. Moreover, CHIKV-infected C57BL/6 mice demonstrated reduction in the viral copy number, lessened disease score and better survivability after CMPD1 treatment. In addition, reduction in expression of key pro-inflammatory mediators such as CXCL13, RAGE, FGF, MMP9 and increase in HGF (a CHIKV infection recovery marker) was observed indicating the effectiveness of the drug against CHIKV. Taken together it can be proposed that MK2 and MK3 are crucial host factors for CHIKV infection and can be considered as important target for developing effective anti-CHIKV strategies.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Actins / drug effects
  • Actins / metabolism*
  • Anilides / pharmacology*
  • Animals
  • Antiviral Agents / pharmacology*
  • Chikungunya Fever / prevention & control*
  • Chikungunya Fever / virology
  • Chikungunya virus / drug effects*
  • Chlorocebus aethiops
  • Cytoskeleton / drug effects*
  • Intracellular Signaling Peptides and Proteins / antagonists & inhibitors*
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Protein Serine-Threonine Kinases / antagonists & inhibitors*
  • Tetrahydronaphthalenes / pharmacology*
  • Vero Cells
  • Virus Release

Substances

  • 5-((3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthalenyl)methyl)-N-(2,4,6-trimethoxyphenyl)-2-furamide
  • Actins
  • Anilides
  • Antiviral Agents
  • Intracellular Signaling Peptides and Proteins
  • Tetrahydronaphthalenes
  • MAP-kinase-activated kinase 2
  • Protein Serine-Threonine Kinases

Grants and funding

This study has been funded by the Department of Science and Technology (DST-SERB), New Delhi, India, vide grant no EMR/2016/000854. https://www.serbonline.in/SERB/HomePage. It was also supported by Institute of Life Sciences, Bhubaneswar, under Department of Biotechnology and National Institute of Science Education and Research (NISER), Bhubaneswar, under Department of Atomic Energy (DAE), Government of India. We wish to acknowledge the University Grant Commission (UGC), New Delhi, India for the fellowship to PM during this study. The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.