Drug Discovery on 7TM Receptors

For more than 200 7TM receptors, the endogenous ligand - i.e. hormone, neurotransmitter etc. - have been identified. This group of 7TM receptors continues to expand as additional ligands are identified. Many of these newly identified 7TM receptors with known ligands constitute the targets of today’s drug discovery efforts.

Mainly based on the track record from monoamine receptors, 7TM receptors are in general considered to be relatively "easy drug targets", but there are increasingly many exceptions to this general presumption. Classical structure driven drug discovery as applied to soluble proteins involving protein production, crystallization and structure determination of ligand-receptor co-complexes has so far been unsuccessful, because 7TM receptors are difficult membrane proteins which are hard to produce in sufficient amounts and quality for crystallization and X-ray structure determination.

An Innovative Proprietary Discovery Platform

 
Standard drug discovery in today’s industry is based on high throughput screening, an expensive approach with clear limitations. Based on unique know-how of the structure-function relationship of 7TM receptors developed over 20 years of research, 7TM Pharma has established an efficient drug discovery engine specifically aimed at 7TM receptors – Site Directed Drug Discovery®. This knowledge- and structure-based approach facilitates generation of small compound libraries allowing for rapid screening and hit generation with limited resource requirements per target and rapid confirmation of the ability to generate chemistry on a novel target. This enables 7TM Pharma to work effectively on a number of targets in parallel in the process of establishing novel drug discovery programs.