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Welcome to the 2010 Allosteric & orthosteric modulator congress
At Arrowhead’s 2010 Allosteric & Orthosteric Modulator Congress, presentations will highlight key developments in the field of allosteric and orthosteric modulator drug discovery and clinical development.
Our speakers will discuss key developments in the field, including the challenges facing researchers, the opportunities for pharma and recent successes in the field.
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 Will Attendees Meet?
- Drug discovery scientists
- Clinical development executives
- Neurobiology scientists
- Pharmacologists
- Group leaders
- Team leaders
- Principal investigators
- Product development manager/directors/vps
- Academic researchers
The following outlines the topics that will be discussed at the 2010 Allosteric and Orthosteric Modulator Congress
Allosteric regulation
- Models
- Activation and inhibition
- Effectors
GPCRs
- Physiological roles
- Link between GPCRs and allosteric modulation
Ion channels
- Biological role
- Ligand-gated ion channels and allosteric modulation
Kinases
- Drug design
- Protein kinase blocking ATP – allosteric modulation
Transporters
- Serotonin transporter (SERT)
- Glycine transporters
GABA receptors
- Ligand-gated ion channels
- GPCRs
Approaches for allosteric and orthosteric modulation
- Antibody
- Protein
- Small molecule
Screening technologies for allosteric and orthosteric modulators
- Functional assays
- Concentration/response (C/R) curve
Therapeutic benefits
- Anxiety
- Schizophrenia
- Depression
- Alzheimer’s disease
- Parkinson’s disease
- Other CNS disorders
- Gastroesophageal reflux disease (GERD)
- Migraines