The Johns Hopkins Gazette: May 5, 2003
May 5, 2003
VOL. 32, NO. 33


JHU Chemist to Use Guggenheim to Develop Ways to Put Fluorine in Drugs

By Michael Purdy

Johns Hopkins Gazette Online Edition

Thomas Lectka, professor of chemistry in the Krieger School of Arts and Sciences, has won a Guggenheim Fellowship to develop easier ways to incorporate a little-used element from the periodic table into the design of new drugs.

The fellowship provides Lectka with approximately $35,000 to support his goal of making it easier for synthetic chemists to include the element fluorine in new drug designs. By substituting fluorine for hydrogen at certain key positions in drugs, it may be possible for researchers to block chemical reactions in the body that can either misdirect the activity of drug molecules or start processes that break down drug molecules, according to Lectka.

Although it offers some tantalizing advantages, fluorine also can be tricky for synthetic chemists to work with.

"Elemental fluorine is one of the most reactive molecules known, and among the least selective in its reactivity," Lectka explained. "As a result, unique glassware, apparatus and experimental protocols have evolved in the study of fluorine chemistry, and much effort has been expended to develop more selective fluorinating agents."

Guggenheim Fellowships are awarded by the John Simon Guggenheim Memorial Foundation to provide recipients with "blocks of time in which they can work with as much creative freedom as possible." The foundation was established by Sen. Simon Guggenheim in 1925 in memory of his son.

Lectka plans to use the Guggenheim grant to travel to the labs of chemists in the United States, Israel and Switzerland who are experts in techniques that will help him incorporate fluorine into research in his lab at Johns Hopkins. Lectka is an expert in asymmetric synthesis, a field that focuses on compounds available in both right- and left-handed forms known to scientists as enantiomers. Normal chemical synthesis produces both enantiomers, but chemists working in asymmetric synthesis develop techniques to produce only one enantiomer. Control over enantiomers is highly valued because a change from one form to another can dramatically alter a drug's biochemical properties, possibly changing an inert substance to a helpful drug or a harmful toxin.

Lectka also plans over the long term to develop "user-friendly" techniques for working with fluorine that will make it easier for other chemists to add the element's desirable properties to new drugs.

Guggenheim fellows are selected on the basis of distinguished achievement in the past and exceptional promise for future accomplishment. Fellows, who must apply to be considered, include writers, painters, sculptors, photographers, filmmakers, choreographers, physical and biological scientists, social scientists and scholars in the humanities.