Blue Bell, Pennsylvania
February 8, 2006
Locus Pharmaceuticals, Inc.,
a computationally-based drug design and development company,
announced today the continuation of its multi-stage research
collaboration with Dow
AgroSciences LLC, a subsidiary of The Dow Chemical Company
(NYSE:DOW), focused on agrochemicals and biotechnology
innovation. The collaboration involves the application of Locus'
proprietary computational technologies to design and develop
novel small molecules to treat fungal targets identified by Dow
AgroSciences. Financial and other terms of the agreement have
not been disclosed. However, if the collaboration is successful,
Locus will realize certain milestones and royalties and will
have an exclusive option to human therapeutic applications.
"We are delighted that Dow
AgroSciences will be moving to the next stage in the
collaboration we entered into just over a year ago," said
Jeffrey S. Wiseman, Ph.D., Vice President, Technology &
Informatics at Locus. "This project has been technically
challenging since we have needed to compute binding to a protein
with more than 1,400 residues, which may well be the largest
protein surface ever comprehensively sampled for drug binding
calculations."
"We are very pleased with the
progress of our collaboration with Locus and, in particular, the
large increase in potency achieved in the first round of
chemical designs compared to known leads," said Dr. Bill
Kleschick, director of Discovery Research at Dow AgroSciences.
"We look forward to moving to Stage II where we will be working
with Locus to optimize these designs."
Locus' core technology is
fragment-based, computational drug design which Locus has
combined with highly integrated medicinal chemistry and biology
capabilities.
Starting with a protein crystal
structure, an in silico collection of 40,000 molecular fragments
and one of the world's largest privately-owned Linux-based
supercomputer clusters, Locus identifies optimum ligand binding
sites on protein targets and computes the binding affinity of
molecular fragments to these sites. The fragments are then
assembled computationally into drug candidates with accurately
predicted binding potency. Other Locus technologies model
physically realistic, long-range timescales of protein motion
and incorporate appropriate chemical properties. The result is a
'virtual library' of drug candidates that exceeds the size and
diversity of any physical screening library by orders of
magnitude. Because of the speed and accuracy with which these
virtual libraries are constructed and evaluated, Locus typically
needs to synthesize only hundreds of compounds to generate
highly potent lead molecules.
Locus Pharmaceuticals, Inc.
is a world leader in computational drug design. These
proprietary computational approaches are combined with in-house
expertise in chemistry, biology and crystallography to create a
fully integrated drug discovery and development platform.
Locus' internal development
programs are focused on oral drug therapies for humans that
address major unmet medical needs, principally in cancer and
inflammation. Locus expects to file an IND early this year for
LP-261, Locus' lead oncology compound. In its inflammation
program, Locus created uniquely selective p38 inhibitors that
target an allosteric binding site rather than the ATP site,
which may offer an improved safety profile compared to other p38
compounds under development. Earlier stage projects include a
program to develop multi-kinase inhibitors, a Heat Shock Protein
90 program which is being conducted in a collaboration with the
National Cancer Institute (NCI) and a gp41 program for AIDS/HIV.
All of the Company's development programs emanate from its
computational technology. Locus is privately-held.
Dow AgroSciences LLC, based
in Indianapolis, Indiana, USA, is a global leader in providing
pest management and biotechnology products that improve the
quality and quantity of the earth's food supply and contribute
to the health and quality of life of the world's growing
population. Dow AgroSciences has approximately 5,500 people in
more than 50 countries dedicated to its business, and has
worldwide sales of US $3.4 billion. Dow AgroSciences is a wholly
owned subsidiary of The Dow Chemical Company. |