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TSRI Chemists Awarded $2.1 Million to Create Potential New Therapies with Click Chemistry

LA JOLLA, CA – January 12, 2016 – Scientists at The Scripps Research Institute (TSRI) have received a grant of more than $2.1 million from the National Institutes of Health’s National Institute of General Medical Sciences to create and screen a new library of drug candidates.

The researchers will use a branch of click chemistry—a method developed by TSRI Professor and Nobel laureate Barry Sharpless in the mid-1990s for quickly discovering new, or improving existing, chemical function. The new research could lead to novel therapeutics and improved positron emission tomography (PET) protocols for children with neurodevelopmental disorders.

“The idea is to make medicines that are more selective and more potent—letting us use a lower dose for the same effectiveness,” said Sharpless, also W.M. Keck Professor of Chemistry and member of the Skaggs Institute for Chemical Biology at TSRI, who will be principal investigator on the four-year project.

TSRI Associate Professor Peng Wu, co-investigator on the new grant, added that the research will take advantage of powerful new gas-based click chemistry reactions developed by the Sharpless lab in 2014. The SuFEx—Sulfur Fluoride Exchange—reactions enable the team to link molecules of their choice together using derivatives of a common commercial chemical considered essentially inert.

“The molecules will only react when they find the right partner,” said Wu.

The researchers will use these reactions to create potential “covalent drugs,” a class of therapeutics that includes penicillin and aspirin. The team will then explore the molecules’ reactivity in zebrafish to identify their potential as therapeutics.

The number of the grant is 1R01GM117145.

About The Scripps Research Institute

The Scripps Research Institute (TSRI) is one of the world's largest independent, not-for-profit organizations focusing on research in the biomedical sciences. TSRI is internationally recognized for its contributions to science and health, including its role in laying the foundation for new treatments for cancer, rheumatoid arthritis, hemophilia, and other diseases. An institution that evolved from the Scripps Metabolic Clinic founded by philanthropist Ellen Browning Scripps in 1924, the institute now employs more than 2,500 people on its campuses in La Jolla, CA, and Jupiter, FL, where its renowned scientists—including two Nobel laureates and 20 members of the National Academy of Science, Engineering or Medicine—work toward their next discoveries. The institute's graduate program, which awards PhD degrees in biology and chemistry, ranks among the top ten of its kind in the nation. For more information, see www.scripps.edu.

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Scripps Research Institute Professor and Nobel laureate Barry Sharpless is principal investigator of the new grant. (High-res image)

Scripps Research Institute Associate Professor Peng Wu is a co-investigator on the new grant. (High-res image)


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