Father of chemical genetics to start
new program here
by Rebecca Arrington
By Elizabeth Kiem
Geysen takes delight in casting himself outside of the mold. I
like to say Ive never worked a day in my life as a proper
chemist, he declares.
is used to breaking new ground, both personally and professionally.
As U.Va.s newest Alfred Burger Professor in Biological and
Medicinal Chemistry, he is experiencing academia for the first
time in his career.
also is the father of combinatorial chemistry, a field that draws
on engineering, chemistry and robotics to make possible large-scale
molecular testing. He developed the technique in the mid-1980s,
creating the worlds first library of mimotopes,
peptides that mimic the reaction of antibodies and antigens and
are key to drug discovery.
collection of 1.28 billion compounds was actually made in duplicate;
one of the libraries now resides with the Smithsonian Institution,
the other in a drawer in Geysens new office, casually wrapped
in a plastic bag.
citing Geysen as one of its 2000 laureates, the Kilby International
Awards Foundation described him as the father of combinatorial
chemistry, a new science that allows multiple drug candidates
to be screened simultaneously. This extraordinary new process
dramatically accelerates the pace of pharmaceutical analysis,
development and delivery, ultimately providing medicines to patients
throughout the world.
chemistry a set of techniques for creating a multiplicity
of compounds and then testing them
for activity; particularly effective in drug discovery.
peptides that mimic the reaction of antibodies and
antigens and are key to drug discovery.
molecules synthetic structures with an atomic weight
of 500 or less. Nearly 98 percent of all newly discovered
drugs are small molecules.
network an artificial network of information processing
units capable of sophisticated computations similar to the
sort that the human brain performs.
department chair Timothy McDonald said Geysens arrival
is a landmark for the University. This is an extraordinarily
accomplished person who revolutionized the pharmaceutical industry
by creating an extremely powerful tool that goes by the trendy
term of chemical genetics, he said.
Australian-born Geysen brought his expertise to the United States
in 1993 when he agreed to develop a combinatorial program for
GlaxoSmithKline, thereby introducing the U.S. pharmaceutical industry
to the practice. From Triangle Research Park in North Carolina,
the move to Charlottesville has been just another step up for
Geysen in terms of quality of life.
a very attractive campus. Were not city people at all, and
Chapel Hill had lost a lot of its charm, he said.
of Charlottesvilles appeal is its proximity to other points
are lots of interesting day trips around, said Geysen, who
owns and pilots a small plane. He plans on getting out of town
frequently with his wife, Kay, who is wintering in
Australia for the next few months, to visit spots such as Tangier
Island and the National Air and Space Museum in Washington.
teaching in a professional forum has always struck Geysen as an
ideal way to wind up his career, it was the interdisciplinary
eagerness among the U.Va. faculty about his molecular library
that secured his contract.
been a strong advocate for a long time of the need for universities
to address the supply of small molecules for their internal research
programs in the area of drug discovery, he said. Drug
companies have a total monopoly on that.
In part, I am
here to supply this University.
$10 million worth of state-of-the-art technology and equipment
from Glaxo, Geysen will attempt to create a working inventory
of small molecules on the second floor of the chemistry building.
Three graduate researchers will become the first of Geysens
team, occupying four renovated labs. Only Harvard University has
undertaken a comparable task, but on a scale that Geysen says
leaves a lot to be desired.
a statistics thing. Its a lottery. Its no good having
a few hundred molecules
you just have to have a lot of
molecules. And its a very expensive operation, said
Geysen, noting that a single molecule in Glaxos supply of
100,000 was valued at $7,000. Combinatorial chemistry, with its
assembly-line efficiency, eases some cost, but the development
and maintenance costs of equipment can be pricey.
is clearly committed. We want to develop a center for chemical
genetics in order to modulate proteins rationally, said
McDonald. Harvards the leader, and we want to beat
hope is that when combinatorial chemistry becomes indispensable
for firms and industries beyond pharmacy, U.Va. will be the premier
school for training young chemists.
dont assume that Geysens biggest legacy will be in
combinatorial chemistry. He is building his seventh company around
a totally unrelated patent in artificial intelligence that would
develop a hardware equivalent of the human brain.
The idea that underpins the neural networks is the most
important idea Ill ever have in my career, he said.