Computational chemogenomics Locus raised US$42.75 million

The Locus Discovery technology is based on a proprietary computational means of rapidly and accurately identifying the biologically relevant active binding site of proteins, and then designing small molecule antagonists or agonists of the protein's activit

Locus Discovery is a new computational drug design biopharmaceutical company. The company was organized in September 1999, and is based on technology exclusively licensed from the Sarnoff Corporation. The technology is a proprietary means of first rapidly and accurately identifying the biologically relevant active binding site of a protein, and then designing small molecule antagonists or agonists of the protein's activity. The technology utilizes proprietary analytical procedures and a specially built supercomputer and requires knowledge only of the structure of a protein -- neither the normal function nor ligand (substance which normally binds to the protein) need to be known.

Starting only with the structure of a protein, the Locus Discovery process rapidly identifies the biologically relevant active binding site of the protein, as well as predicts the chemistries of molecular classes that will effectively bind to that site. The process then allows the design of multiple structural classes of small molecule compounds that act as inhibitors or activators of the protein's activity, including accurately calculated potencies for each structure. Unlike traditional research approaches, the Locus Discovery process represents the ability to compress into a few weeks what previously took several years in the drug discovery process, enabling the identification of small molecule drugs substantially faster, with a much higher success rate, and on a much larger scale than has previously been possible. In addition, small molecule drugs can be orally active, meaning that the products can generally be taken in pill form. The Locus Discovery technology can be used to discover therapeutic compounds for many thousands of known protein targets, as well as thousands of new protein targets being identified through genomic research.

Accomplishments by Locus Discovery show that the basic technology and the same fundamental computational algorithms are generalizeable and applicable to the major classes of proteins: receptors, enzymes, and structural (anchor) proteins. Locus Discovery Inc. is currently undertaking a number of internal research programs targeting a variety of proteins. Some of the more advanced drug discovery programs include small molecule mimetics of erythropoetin, and broad-spectrum anti-viral compounds based on a novel anti-viral target called GP41.