 |
Business Wire - February 10, 2004
Locus Pharmaceuticals today announced that it has received a Notice of Allowance from the US Patent and Trademark Office for an innovative computational method for the design of new drugs. This is the first patent allowance for Locus's proprietary core technology. Application of the technology allows rapid calculation of the affinity of fragment molecules selected from Locus's proprietary fragment database to identify and characterize the ideal binding site on the surface of proteins that are disease targets. From such information, new drug molecules are computationally designed and synthesized by Locus scientists to impact on the targeted disease. This computerized technology significantly increases the speed and accuracy of the drug design process allowing more predictive lead generation compared to traditional drug discovery methods such as High Through-put Screening. Locus has applied this new drug discovery paradigm to develop novel therapies for AIDS, cancer and rheumatoid arthritis which are being advanced toward clinical studies.
"Considering the urgent need to improve drug discovery relative to cost, accuracy and speed, we believe Locus is effectively positioned to answer this challenge. With this critical vote of confidence from the patent office, we have further strengthened our competitive position and leadership role in computational directed drug discovery," said Dr. Joseph Reiser, President and CEO of Locus Pharmaceuticals.
The allowed patent application describes the use of the technology in mapping the surface of a protein target to determine its suitability for binding small, orally available drug compounds. This know-how is critical in determining the success in targeting a disease related protein by identifying design approaches to the most suitable points of intervention. As an example, purely experimental efforts to map protein surfaces in the past have taken years to accomplish what the Locus technology can achieve in months. The algorithms described apply the principles of statistical thermodynamic sampling to simultaneously calculate the potential energies for interaction of a given molecular fragment at as many as 100 million sites on a protein surface. The innovation in the technology is to efficiently convert these potential energies into interaction free energies, which are the results required for prediction of binding affinities. Such data have been previously elusive and intractable to computational approaches at speeds that are practical.
The allowed patent application is the first product of a broad strategy of intellectual property protection already submitted for patent review to further expand the scope and application of the Locus Core Technology.
According to Dr. Anton Hopfinger, Professor at the University of Illinois, an established expert in computer-assisted molecular design, "The patented Locus technology for the computational identification of ligand binding sites on a target protein is an extremely significant, and necessary, breakthrough in order to realize the efficient, effective and reliable design of drug-candidate molecules. In effect, Locus has found a way to not only find one, but all the needles in a haystack, as well as where and how they are positioned in the haystack."
This drug discovery technology was developed by Dr. Frank Guarnieri while at Sarnoff Corporation. Sarnoff, the Princeton, NJ-based innovation services and technology development company, uses its strength in electronic, biomedical, and information technology to generate successful new products for clients worldwide. Locus Pharmaceuticals was created in 1999, with Dr. Guarnieri as the Principal Scientific Founder, to extend and apply the Sarnoff technology in the practice of pharmaceutical drug discovery. Locus Pharmaceuticals is the exclusive licensee of Sarnoff's patents and technology and is currently deploying the technology in its own drug discovery efforts in the areas of cancer, AIDS, and inflammation.
Locus also collaborates on external discovery research programs in both the agricultural and pharmaceutical industries where this technology is deployed on targets proprietary to such partners. To date, Locus has entered such collaborations with Dupont's Crop Protection unit and Speedel Experimenta.
"In today's genomics-driven drug discovery environment there is an urgent need for technologies that produce results faster, more efficiently, and with greater accuracy," said Dr. Carmen Catanese, Executive Vice President of Sarnoff. "The computational drug design and discovery approach developed by Locus opens the door to finding novel drug therapies while shortening time to market for pharmaceuticals."
About Locus Pharmaceuticals
Locus Pharmaceuticals is a privately held pharmaceutical company focused on developing novel, small molecule therapeutics to address major unmet medical needs. Locus combines powerful and proprietary, fragment-based, computational technology with one of the world's fastest Linux-based supercomputer clusters to simultaneously identify relevant binding sites on protein disease targets and rapidly generate novel, drug-like, small molecules that bind specifically to those protein sites. In contrast to other computational approaches, the Locus technology requires only a high-resolution, 3-dimensional structure of the target protein to implement its drug discovery process. Presently, Locus Pharmaceuticals is synthesizing and testing novel, computationally predicted, drug candidates for the treatment of debilitating and life-threatening human diseases including HIV/AIDS, cancer and inflammation.
CONTACT: Locus Pharmaceuticals
Joseph Reiser, President and CEO, 215-358-2001
SOURCE: Locus Pharmaceuticals
040210
BW040206
Copyright © 2004 - Business Wire. All rights reserved. Reproduced with permission. Reproduction of this article (other than one copy for personal reference) must be cleared through the Business Wire, Permissions Desk, Business Wire, 1185 Avenue of the Americas, 3rd Floor, New York, NY 10036; Tel: (212) 575-8822; FAX: (212) 575-1854. http://www.businesswire.com.
AEGiS is made possible through unrestricted grants from Boehringer Ingelheim, Elton John AIDS Foundation, Bridgestone/Firestone Charitable Trust, the National Library of Medicine, and donations from users like you. Always watch for outdated information. This article first appeared in 2004. This material is designed to support, not replace, the relationship that exists between you and your doctor.
AEGiS presents published material, reprinted with permission and neither endorses nor opposes any material. All information contained on this website, including information relating to health conditions, products, and treatments, is for informational purposes only. It is often presented in summary or aggregate form. It is not meant to be a substitute for the advice provided by your own physician or other medical professionals. Always discuss treatment options with a doctor who specializes in treating HIV.
Copyright ©1980, 2004. AEGiS. All materials appearing on AEGiS are protected by copyright as a collective work or compilation under U.S. copyright and other laws and are the property of AEGiS, or the party credited as the provider of the content. .