Odd ‘Buckyball’ Molecules May Have Use in AIDS Drug
It was late one night in the lab. Simon Friedman, a 27-year-old graduate student in pharmaceutical chemistry at UC San Francisco, was yukking it up with a friend about all the novel ways scientists were trying to stop the AIDS virus from reproducing in the test tube.
“What are they gonna try next?” his colleague cracked. “Buckyballs?”
But the joke, it turned out, was no joke at all. In a finding that brings together two of the hottest areas in science today, Friedman reports that buckyballs--recently discovered molecules so nicknamed because their shape resembles the late R. Buckminster Fuller’s multisided geodesic domes--do indeed stop the human immunodeficiency virus from multiplying.
The finding, reported in this week’s Journal of the American Chemical Society, is apparently the first biological application of buckyballs. It works by blocking a crucial enzyme called protease.
Friedman hopes it can be the first step toward creating a successful “protease inhibitor”--a new type of AIDS drug, still unapproved, that researchers elsewhere are working furiously to develop.
The buckyball is “a highly novel molecule, and it makes sense that as people explore this for more and more things, they will find new and exciting and unusual uses,” said Joel M. Hawkins, a UC Berkeley chemist. “It has a very surprising structure and it itself is full of surprises.”
More formally known as fullerenes or C-60, buckyballs are hollow, soccer-ball-shaped molecules composed of 60 carbon atoms. They form a third, newfound type of pure carbon, life’s essential element. Less than a decade ago, carbon was thought to appear in a pristine state only as diamonds and graphite.
Since their discovery, buckeyballs have been hailed in the press as a means to create everything from superconductors to better lubricants.
When his friend, Diane Roe, made the joke about the newfound molecules, Friedman said the thought occurred to him that their unique shape might enable buckyballs to fit into the space that protease normally uses to attach to a crucial protein.
That attachment must occur for the virus to multiply; if buckyballs could stop it from happening, Friedman reasoned, they might be on to something important.
After a computer model looked promising, he checked his findings in the test tube.
Of course, development of a protease inhibitor using buckyballs is a long way off, and the young scientist is cautious.
“To be really frank,” he said, “I’d have to say the chances are not great. Success in the final analysis would be to develop a (drug) that is therapeutically useful. But at times, we have to be willing to accept lesser goals--i.e., that we are moving in the right direction.”
