Allosteric Modulator Congress

Background

Allosteric modulators are an emerging class of orally available small molecule therapeutic agents that may be able to offer patients better outcomes than with traditional small molecule therapies. This potential stems from their ability to offer greater selectivity and better modulatory control at disease mediating receptors. Modulators bind to regulatory sites distinct from the active site on the protein, resulting in conformational changes that may profoundly influence protein function. The advent of functional assays as the screening method of choice is leading to an increase in the number of allosteric modulators identified.

Allosteric modulation is generating a great deal of excitement among researchers. Since orthosteric modulators need to compete with natural ligands, they require higher doses, raising safety issues. Allosteric modulators do not compete and may be effective at lower, safer doses.