Scripps Research team creates new synthetic compound with HIV-fighting promise

Discovery stems from library created using natural Japanese-plant compounds as starting point

LA JOLLA, CA – January 18, 2011 – Using chemical compounds found in a Japanese plant as a lead and the clever application of ultraviolet light, a Scripps Research Institute team has created a unique library of dozens of synthetic compounds to test for biomedical potential. Already, one of the compounds has shown great promise in inhibiting replication of HIV particles and fighting inflammation.

With the report of their work scheduled to appear in the online Early Edition of Proceedings of the National Academy of Sciences this week, the researchers now plan to optimize the compound's pharmaceutical potential so that it can be pursued as a drug candidate.

The plant Hypericum chinense, known in Japan as biyouyanagi, produces beautiful yellow flowers and, as it happens, potent chemical compounds known as biyouyanagins that have already shown promising anti-HIV and anti-tumor activity. That got the attention of K.C. Nicolaou, who holds the titles chair of the Department of Chemistry, Aline W. and L.S. Skaggs Professor of Chemical Biology, and Darlene Shiley Chair in Chemistry at Scripps Research. Nicolaou's interest was also piqued because the plant is from the same family that produces St. John's wort, and the biyouyanagins possess an intriguing molecular architecture.

"It was the perfect recipe for convincing a synthetic chemist to get into the game," said Nicolaou, who spearheaded the project in collaboration with a number of Scripps Research colleagues. "It seemed like there was so much to be discovered."

http://www.sciencedaily.com/releases/2011/01/110119132520.htm

Complete Structure of HIV’s Outer Shell Revealed

ScienceDaily (Jan. 20, 2011) — A team of scientists at The Scripps Research Institute and the University of Virginia has determined the structure of the protein package that delivers the genetic material of the human immunodeficiency virus (HIV) to human cells.

If formation of the mature capsid is disrupted, the virus is no longer infectious. Thus, new drugs targeting capsid formation could provide valuable additions to the arsenal of existing drugs against HIV.