San Diego, CA, September 07, 2013 --(PR.com
)-- Maureen Beresini, Senior Scientist at Genentech will give a presentation on “From HTS to Mechanism: Kinase Screening Strategies That Maximize Hit Value” at the 2nd Protein Kinases & Drug Design Conference to be held in San Diego, CA on October 24-25, 2013 by GTC.
In recent years, kinase screening has evolved to address our growing understanding of kinase signaling, activation states, and resistance mechanisms. Pre-clinical and clinical data have illustrated that kinase inhibitors can allosterically activate or inhibit signaling, revealed mechanisms of resistance to targeted inhibitors, and importantly, demonstrated that differential binding modes can lead to vastly different functional effects. These data have influenced the way we do drug discovery, and in effect, the way we conduct HTS campaigns.
To address these unique therapeutic needs, there has been a growing demand to efficiently identify inhibitors with defined mechanisms of action from HTS campaigns. This includes identifying lead matter with specific modes of inhibition, specific selectivity signatures, targeting active vs. inactive states, or with long residence times. Additionally, assay technologies, reagents, and instrumentation continue to evolve, and thus, provide the tools necessary to effectively target our screening campaigns.
Accordingly, we devise screening strategies unique to each kinase. A solid understanding of the kinase and a clearly defined target candidate profile are used to develop a well-targeted primary screening assay and a suite of follow-up assays that efficiently characterize primary hits and identify those with desired modes of action.
This presentation will describe three critical avenues for maximizing HTS hit value:
1. Minimizing detection interference
2. Minimizing nonspecific inhibition
3. Maximizing fit to desired mechanism of action.
Examples will be used to illustrate how primary screens coupled with information-rich IC50 evaluations have been used to direct hit triage efforts towards the most favorable compounds.
Kinases, key drivers of malignant transformation and major contributors to a variety of other human pathologies, have emerged as some of the most exciting targets in drug discovery. However, with initial well documented success stories came realization that many hurdles lie in the path of successful development of new drugs, targeting kinase signaling. GTC’s 2nd Protein Kinases & Drug Design Conference will bring together speakers representing world leading academic centers and pharmaceutical companies to discuss how to overcome the many hurdles and answer exciting key questions.
This conference is part of our Protein Discovery Summit 2013, which includes three additional parallel conferences shown below:
Protein Kinases & Drug Design
Antibody & Protein Therapeutics
Protein Expression, Purification & Characterization
For more information, please visit www.gtcbio.com