Artemisinin ‘Bomb’ Attacks Many Proteins
Celia Henry Arnaud · C&EN Global Enterprise · 2016
First isolated in the 1970s, artemisinin is an effective drug against malaria, but questions remain about how it works. With the help of chemical proteomics, researchers have now shown that artemisinin kills the malaria parasite Plasmodium falciparum by indiscriminately binding to proteins in many of the organism’s key biochemical pathways. To identify the drug’s binding partners, a team led by Qingsong Lin, Kevin S. W. Tan, and Jigang Wang of National University of Singapore synthesized an alkyne-tagged artemisinin analog (Nat. Commun. 2015, DOI: 10.1038/ncomms10111). After incubating the probe with live malaria parasites and attaching biotin to its alkyne tag, the team fished out all the proteins to which artemisinin binds. The researchers did this by incubating the mixture with streptavidin-labeled beads that strongly attract biotin. They then identified the purified proteins with mass spectrometry. The researchers were unsurprised to find that the probe bound to a whopping 124 different proteins.