The last decade has seen a dramatic increase in the understanding of kinase biology. Yet, despite some high profile successes, the tendency of small molecules to interact with multiple kinases continues to present both opportunities and challenges to identifying and optimizing appropriate kinase inhibitors for specific disease indications.
The advent of kinome-wide compound annotation affords researchers key insights and knowledge of interaction patterns that build a foundation for further exploration of kinase inhibitor biology and therapeutic benefit. Since interactions between kinases and inhibitors can be highly activation state-dependent, a complete understanding of inhibitor binding requires not only detailed analysis of kinome-wide interaction patterns, but also the ability to characterize interactions across multiple activation states that are relevant to disease.
What will be covered
- Overview of the KINOMEscan assay technology
- Impact of activation state-dependent binding on selectivity
- Differentiating inhibitors based on activation state-specific binding
- Using activation state-specific biochemical data to predict & interpret potency in cellular assays
- Interaction pattern analysis: progress toward the discovery of target-selective inhibitors
Who should attend
- Oncology researchers
- Medicinal chemists & biologists
- Structural biologists
- Pharmacology/toxicology researchers
- Basic research scientists
- Drug discovery industry researchers