Allosteric Modulator Congress
Venue: San Diego
|Event Date/Time: Nov 11, 2010||End Date/Time: Nov 12, 2010|
Screening for a specific target
Hit to lead generation
Lead optimization to clinical candidate
Medicinal chemistry and Structure Activity Relationships (SARs) of allosteric modulators
Therapeutic applications of Allosteric Modulators
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.