Genetic Engineering News Reports on Medicinal Chemistry for Drug Discovery.

NEW ROCHELLE, N.Y. -- Medicinal chemistry is playing an increasingly critical role in drug discovery, reports Genetic Engineering News (GEN) (www.genengnews.com). Indeed, medicinal chemists have a strong influence in helping to determine a biotech company's ultimate "go/no-go" choice on whether to pursue potential new drug leads, according to the latest issue of GEN.

"Early decisions on whether a compound has a druglike or leadlike property are often made by a team led by medicinal chemists," says John Sterling, Editor-in-Chief of GEN. "When you realize that these decisions can have a significant impact on the eventual success, or failure, of a new drug, it's easy to understand how vital medicinal chemists are to drug discovery and development groups."

In terms of lead- and drug-likeness, medicinal chemists look for a noncovalent, high-affinity, chemically-stable, and reversibly binding ligand which can be taken forward into optimization and development. Certain physico-chemical properties, such as molecular weight less than 500, are linked with drug-likeness, and there are also specific properties linked with lead-likeness, e.g., lack of chemically reactive functional groups. A number of companies, such as Sepracor (NASDAQ:SEPR), NPS Pharmaceuticals (NASDAQ:NPSP), Neurogen (NASDAQ:NRGN), Neurocrine Biosciences (NASDAQ:NBIX), Arena Pharmaceuticals (NASDAQ:ARNA), Athena/Elan (NYSE:ELN), Abgenix (NASDAQ:ABGX), and Medarex (NASDAQ:MEDX) have already taken this message on board.

Cresset BioMolecular Discovery has latched onto a concept which holds that there is a new and better way of defining chemical diversity: in terms of electron fields. After all, protein targets do not interact with chemical structures; they do so with electrons. The field approach involves describing the target-drug binding environment more in terms of what the target actually "sees." If two diverse structures generate the same field pattern, they should show the same biological activity. The field method has been applied to the study of thrombin inhibitors and shows that chemically diverse actives look similar in terms of their electron fields. The aim now is to apply the method in virtual screening.

Paradigm Therapeutics is exploiting the use of silicon as an isostere for carbon in drug design in cases where the presence of silicon could improve the molecule's properties. Paradigm is the only reported company to commercialize this approach, known as the Silicon Switch, and has several programs moving toward lead optimization.

Also covered in the GEN article are Biotage (OTC:PYRSF.PK), Starpharma (OTC:SPHRY.PK), Johnson & Johnson Pharmaceutical R&D (NYSE:JNJ), Schering (NYSE:SHR), Esteve Laboratories (Barcelona, Spain), and Metabasis Therapeutics (NASDAQ:MBRX).

Genetic Engineering News is published 21 times a year by Mary Ann Liebert, Inc. For a copy of the May 15 issue, please call 914-740-2100, ext. 2122, or email: [e-mail].