Locus Announces Continuing AIDS Collaboration with Weill Cornell Medical College.

BLUE BELL, Pa. -- Locus Pharmaceuticals, Inc. announced today that it has agreed to license from Cornell Research Foundation a second proprietary crystal structure of the fusion protein gp41, a novel drug target for the treatment of HIV/AIDS. Locus plans to apply its proprietary computational technologies to this new structure to design small molecule inhibitors of HIV, the AIDS virus.

Dr. Min Lu, Associate Professor of Biochemistry at Weill Medical College of Cornell University in New York City, identified this novel and proprietary domain of gp41, and the 3-dimensional protein structure information forms the basis of the license. Dr. Lu is a recognized leader in the area of gp41 biology and the mechanism of HIV infection, and has been a key collaborator with Locus on this program. This is the second structure Locus has licensed from Dr. Lu's laboratory.

Most currently approved therapies for HIV infection involve approaches to suppress viral replication once the virus has entered the host cell. In contrast, gp41 inhibitors prevent HIV from ever getting into the cell, which may allow preventative therapy.

"HIV fusion and viral infection are dependent upon gp41. Therefore, blocking this protein's function with an oral drug would represent an important new treatment for suppressing and preventing HIV-1 infection," said William R. Moore, Jr., Ph.D., Vice President of Research and Development and Chief Science Officer at Locus.

"I am excited to be continuing my relationship with Locus. They bring unique computational capabilities to our collaboration, particularly with regard to binding site identification, drug design, and protein motion simulation," commented Dr. Lu.

Starting with a protein crystal structure, its in silico library of 40,000 molecular fragments, and one of the world's largest Linux-based supercomputer clusters, Locus computationally maps relevant ligand binding sites on protein targets, constructs antagonists to those sites, while simultaneously optimizing the drug candidate's ADMET properties. Locus creates and evaluates custom-built, project specific 'virtual libraries' of candidate ligands that surpass 1 billion potential compounds, exceeding the size of any physical screening library by orders of magnitude.

Locus can model physically realistic long-range timescales of protein motion (10 times longer than other approaches) and compute binding potencies in almost real time. Other computational methods with similar accuracy are 10,000 times slower. Locus typically needs to synthesize only hundreds of compounds from its virtual libraries to generate highly potent, orally-active lead molecules.

About Locus Pharmaceuticals

Locus Pharmaceuticals, Inc. is a world leader in computational drug design. Since 2000, Locus has developed unique and potentially transformational capabilities for the in silico design and optimization of small molecule drugs. These proprietary computational approaches are combined with in-house expertise in chemistry, biology and crystallography to create a fully integrated drug discovery platform. Locus believes that its capabilities offer the potential to substantially lower the cost of drug discovery and greatly increase the speed of advancing novel therapies to clinical trials and, ultimately, to the market.

Locus is developing oral drug therapies to address major unmet medical needs, principally in cancer and inflammation. All of the Company's development programs emanate from its computational technology. LP-261, Locus' lead oncology compound, is an orally-administered therapeutic that blocks tumor growth potentially through both anti-mitotic and anti-angiogenic mechanisms of action. It has also been shown to be active against resistant cell lines. Locus expects to file an IND for this compound around the end of this year.

In Locus' lead inflammation program, Locus has created uniquely selective, highly potent, and orally-active p38 inhibitors that target an allosteric binding site rather than the ATP site, which other drug developers are pursuing. Allosteric sites may offer an improved safety profile over ATP site inhibitors as well as provide a dual mode of action.

In addition to the AIDS/HIV program, other earlier stage projects include a program to develop multi-kinase inhibitors that block several key growth stimulation pathways simultaneously, and Heat Shock Protein 90 which is being conducted under a Cooperative Research and Development Agreement (CRADA) with the National Cancer Institute (NCI).

Locus is privately-held and has approximately 40 employees.