Welcome to the Allosteric Modulator Drug Discovery Congress

This conference will highlight the entire drug discovery process as it pertains to the development of allosteric modulators and the challenges and recent successes associated with this exciting field.

Themes include:

• 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
  

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.

Why are allosteric modulators on the cutting edge of small molecule drug development?

• Allosteric modulators do not compete with endogenous ligands and therefore can exert their influence even if an endogenous ligand is bound to another site on the same target at the same time
• Allosteric modulators can be devoid of activity in the absence of endogenous ligands.  Allosteric modulators may offer a less disruptive way to influence the functioning of biological systems
• For targets where it has been difficult to make selective orthosteric modulators in some cases highly selective allosteric modulators can be made
• Since they bind on a distinct site, it is possible to combine allosteric modulators with orthosteric drugs

Who Should Attend?

• Drug discovery scientists
• Neurobiology scientists
• Pharmacologists
• Research scientists
• Senior research scientists
• Group leaders
• Team leaders
• Principal investigators
• Principal scientists
• Senior scientists
• Academic researchers