Drug resistance. K13-propeller mutations confer artemisinin resistance in Plasmodium falciparum clinical isolates

Science. 2015 Jan 23;347(6220):428-31. doi: 10.1126/science.1260867. Epub 2014 Dec 11.

Abstract

The emergence of artemisinin resistance in Southeast Asia imperils efforts to reduce the global malaria burden. We genetically modified the Plasmodium falciparum K13 locus using zinc-finger nucleases and measured ring-stage survival rates after drug exposure in vitro; these rates correlate with parasite clearance half-lives in artemisinin-treated patients. With isolates from Cambodia, where resistance first emerged, survival rates decreased from 13 to 49% to 0.3 to 2.4% after the removal of K13 mutations. Conversely, survival rates in wild-type parasites increased from ≤0.6% to 2 to 29% after the insertion of K13 mutations. These mutations conferred elevated resistance to recent Cambodian isolates compared with that of reference lines, suggesting a contemporary contribution of additional genetic factors. Our data provide a conclusive rationale for worldwide K13-propeller sequencing to identify and eliminate artemisinin-resistant parasites.

Publication types

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

MeSH terms

  • Amino Acid Sequence
  • Antimalarials / pharmacology*
  • Artemisinins / pharmacology*
  • Cambodia
  • Drug Resistance / genetics*
  • Genetic Loci
  • Humans
  • Malaria, Falciparum / drug therapy
  • Malaria, Falciparum / parasitology
  • Molecular Sequence Data
  • Mutation
  • Plasmodium falciparum / drug effects*
  • Plasmodium falciparum / genetics*
  • Protein Structure, Tertiary
  • Protozoan Proteins / chemistry
  • Protozoan Proteins / genetics*

Substances

  • Antimalarials
  • Artemisinins
  • Protozoan Proteins
  • artemisinin