drug screening Technology
from U.K.’s
Protherics
Adding "Virtual" to Existing "Physical" High-Throughput
Screening Capabilities Is Expected to Boost the Number and
Quality of Drug Leads
South San Francisco, Calif.,
July 12, 2001 --
Tularik
(Nasdaq: TLRK) announced
today that it acquired the
computer-aided molecular
design (CAMD) unit of
Protherics PLC, a U.K.-based
company.
David V. Goeddel, Ph.D.,
Tularik’s CEO, said the
acquisition, which includes
proprietary virtual molecular
screening software as well as a
team of
software designers,
computational chemists and
medicinal chemists, promises
to enhance Tularik’s drug
discovery efforts. "We will
integrate Protherics’ virtual
screening capability with our
own well established
high-throughput screening. This
will help us boost both the
number and quality of
leads for
Tularik’s proprietary
targets--targets we have
already validated as optimal
points for intervention in
important disease pathways,"
Dr. Goeddel said.
The key technology of the
Protherics’ CAMD unit is a set
of proprietary computational
software tools called
Prometheus. These tools
facilitate the identification of
novel compounds that bind
with high affinity to the active
site of cellular
receptors or
enzymes. The technology also
enables the rapid optimization
of early drug leads by
combining structural
information about
drug targets
with virtual screening
information gleaned from
compound libraries designed
around particular sets of
chemical leads.
According to Juan Jaen, Ph.D.,
Tularik’s Vice President,
chemistry, Tularik conducted a
comprehensive survey of
CAMD software packages for
virtual screening, and
Prometheus best fulfilled
Tularik’s needs. Prometheus
has been applied with great
success to the design of
inhibitors for various
proteases
involved in
blood clot
Formation, allergy, and
inflammation. More broadly,
Prometheus is applicable to
any protein target for which
3-dimensional structural
information is available.
"Rapid, cost-effective
identification and optimization
of lead compounds is crucial in
the
drug discovery process,"
said Dr. Jaen. "What CAMD
brings to Tularik is a very
effective application of
high-speed computational
methods to molecular design
and screening."
"At the same time, it’s
important to understand that
virtual screening doesn’t
replace, but rather
complements, ‘physical’
high-throughput screening," Dr.
Jaen continued. "What the
software and high-speed
computers enable us to do is
select a moderate number of
potentially active compounds
from existing commercial
compound libraries or from
Tularik’s proprietary virtual
libraries. Through an iterative
process, the technology then
enables us to distinguish potent
molecules from inactive or less
potent ones, with greater and
greater levels of precision."
"Just as important as
identifying an early
lead--whether it is from
standard high-throughput
screening or computational
methods--is the ability to
quickly optimize the drug-like
properties of the molecule,"
commented Nigel Walker,
Ph.D., Tularik’s Director,
structural biology. "The
CAMD approach is uniquely
suited to accomplish efficient
optimization by making full use
of the range of information
generated by Tularik’s
structural biology group."
"Ultimately, of course, actual
compounds need to be
synthesized, tested, and
optimized by our expert team of
medicinal chemists from both
Tularik and the new CAMD
group," Dr. Walker added. "In
short, it’s the synergy and
complementarity between the
‘virtual’ and the ‘physical’
approaches that appeals to us
and makes us look forward to
the application of the CAMD
technology to our discovery
efforts."