'Click chemistry' reactions may boost cancer-fighting drug potency

IMAGE: Nobel laureate K. Barry Sharpless, PhD, TSRI W.M. Keck Professor of Chemistry at TSRI, co-led the study. view more 

Credit: Photo by Ike Sharpless

LA JOLLA, CA– Feb. 16, 2018– Researchers at The Scripps Research Institute (TSRI) have developed a quick and easy way to simultaneously modify dozens of drugs or molecules to improve their disease-fighting properties. Using the approach, scientists exchanged one chemical group for another in 39 cancer drugs–and discovered under lab conditions that the chemically altered versions of three of the drugs had more potent anti-cancer activity.

The results, published today in the Journal of the American Chemical Society, reveal a powerful application of so-called “click chemistry” to drug discovery.

“Usually you have to make thousands or millions of molecules and go through a big screening process to find one or two molecules that are interesting and might work,” says Peng Wu, PhD, a TSRI associate professor and one of the study’s lead authors. “With this new approach, you can save time and money by starting with drugs and molecules you know are already active and asking whether a quick modification makes any of them any better.”

“Our results suggest we will be able take


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