Stefan Knapp, Uni. of Oxford to give Keynote Address at GTCbio’s Kinase Inhibitors Conf
03/01/2016

Stefan Knapp at University of Oxford will discuss, “Design Strategies for the Development of Selective Kinase Inhibitors” at GTCbio’s Kinase Inhibitors Conf

Online PR News – 01-March-2016 – Berlin – Stefan Knapp, Professor of Structural Biology at the University of Oxford, will give a keynote presentation on “Design Strategies for the Development of Selective Kinase Inhibitors” at GTCbio’s 2nd Kinase Inhibitors Design & Screening Conference on May 12-13, 2016 in Berlin, Germany.

Shown below is an abstract for Dr. Knapp’s presentation:

“Protein kinases have emerged as major drug targets but only few strategies for the development of selective inhibitors have been developed to date. Recent advances in kinase structural biology led to an excellent structural coverage of the human kinase family as well as a large number of structures of kinase inhibitor complexes which also provide insight into the remarkable domain plasticity of the kinases catalytic domain. More than 80 of novel structures originated from our laboratory at the SGC, enabling now a family wide structural and biophysical/biochemical analysis of this protein family. In this talk I will summarize a number of strategies that have emerged based on structural studies and family wide selectivity screening that led to the development of highly selective inhibitors. In this presentation I will discuss in particular the discovery of novel inhibitor binding sites including allosteric sites and the exploitation of unusual ATP site residues and structural elements for the design of highly selective inhibitors. Structural aspects optimizing inhibitor residence times and potential mechanisms leading to slow off-rate binding kinetics will also be discussed.”

Dr. Knapp’s work is in kinases and phosphatases as drug targets. Discoveries in numerous kinases map to loci associated with human diseases and amplicons identified in tumors. Dr. Knapp’s lab focuses on strategies to locate a family of related molecules in order to understand their signaling features, functions, and regulation.

The 2nd Kinase Inhibitors Design & Screening Conference brings together a mix of academic and industry authoritative experts from leading affiliations (Novartis, Barts Cancer Institute, Genentech, Sanofi-Aventis, Schrodinger, Netherlands Translational Research Center, etc.) to cover many current and relevant aspects of allosteric kinase inhibitors, covalent inhibitor strategies, irreversible and RAF inhibitors, mechanisms of kinase inhibitor resistance, and mutation-focused approaches towards kinase inhibition.

This conference is also part of our larger European Pharma Summit, which consists of three additional conferences:

3rd 3D Models & Drug Screening
3rd GPCR Targeted Screening
10th Drug Design & Medicinal Chemistry

For more information, please visit the website: http://www.gtcbio.com/kinaseinhibitors

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