Drug resistance. Population transcriptomics of human malaria parasites reveals the mechanism of artemisinin resistance

Science. 2015 Jan 23;347(6220):431-5. doi: 10.1126/science.1260403. Epub 2014 Dec 11.

Abstract

Artemisinin resistance in Plasmodium falciparum threatens global efforts to control and eliminate malaria. Polymorphisms in the kelch domain-carrying protein K13 are associated with artemisinin resistance, but the underlying molecular mechanisms are unknown. We analyzed the in vivo transcriptomes of 1043 P. falciparum isolates from patients with acute malaria and found that artemisinin resistance is associated with increased expression of unfolded protein response (UPR) pathways involving the major PROSC and TRiC chaperone complexes. Artemisinin-resistant parasites also exhibit decelerated progression through the first part of the asexual intraerythrocytic development cycle. These findings suggest that artemisinin-resistant parasites remain in a state of decelerated development at the young ring stage, whereas their up-regulated UPR pathways mitigate protein damage caused by artemisinin. The expression profiles of UPR-related genes also associate with the geographical origin of parasite isolates, further suggesting their role in emerging artemisinin resistance in the Greater Mekong Subregion.

Publication types

  • Research Support, N.I.H., Intramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antimalarials / pharmacology*
  • Artemisinins / pharmacology*
  • Chaperonin Containing TCP-1 / genetics
  • Chaperonin Containing TCP-1 / metabolism
  • Drug Resistance / genetics*
  • Humans
  • Malaria / drug therapy*
  • Malaria / parasitology
  • Malaria, Falciparum / drug therapy*
  • Malaria, Falciparum / parasitology
  • Plasmodium falciparum / drug effects*
  • Plasmodium falciparum / genetics*
  • Transcriptome
  • Unfolded Protein Response / genetics*

Substances

  • Antimalarials
  • Artemisinins
  • artemisinin
  • Chaperonin Containing TCP-1

Supplementary concepts

  • Acute malaria

Associated data

  • GEO/GSE59099