Monrovia, California (PressExposure) March 22, 2012 -- Nathanael Gray, Principal Investigator, Biological Chemistry & Molecular Pharmacology at Dana Farber Cancer Institute to give a Featured Presentation on "Development and Characterization of Covalent Kinase Inhibitors" at the 7th Protein Kinases in Drug Discovery Conference (May 30-31, 2012 in Boston, MA).
There is an ever increasing demand for new protein kinase inhibitors both as potential therapeutics and as tools for dissecting complex signaling pathways. The vast majority of currently developed kinase inhibitors targets the ATP-binding site and bind in a reversible fashion. An alternative mode of kinase inhibition involves developing compounds that form permanent covalent bonds with nucleophilic residues such as cysteines or lysines. A survey of the kinome reveals that there are over 150 kinases that possess a potentially accessible cysteine in or around the ATP-binding site. Despite this abundance of potential targets only a very limited of selective covalent kinase inhibitors are currently known. Dr. Gray will describe two distinct and general methods for efficiently developing novel covalent inhibitors with examples provided for T790M EGFR, FGFR and JNK.
Benefits of Talk:
Broad survey of kinase potential targetable by covalent inhibitors
Description of general approaches for covalent kinase modification
Specific examples of covalent inhibitors of T790M EGFR, FGFR and JNK
Examples for how covalent inhibitors can be characterized
GTC announces its 7th Annual Protein Kinases in Drug Discovery Conference (May 30-31, 2012 in Boston, MA). To remain competitive in the kinase field, it will require you to stay abreast with recent development trends and technological advancements aimed at circumventing these issues. We will also provide you with a broad overview of the role kinases play in various types of cancer as well as introduce you to several novel kinases and inhibitor candidates.
The sessions for the 2012 agenda include:
1) Overcoming Challenges in Kinase Drug Development
2) Trends in Drug Design - Structure/Selectivity/Pathway/Epigenetics
3) Oncology Kinases & Inhibitor Candidates
4) Other Kinases & Inhibitor Candidates.
The top companies and experts in the field of Protein Kinases will come together to discuss the latest discoveries. Companies include ArQule, Avila, Beactica AB, Amgen, Bristol-Myers-Squibb, Eli Lilly, Pfizer, Roche, Merck and more!
Keynote & Featured Speakers Include:
Michael Yaffe, Professor, Biology & Biological Engineering, Massachusetts Institute of Technology
Nathanael Gray, Principal Investigator, Biological Chemistry & Molecular Pharmacology, Dana Farber Cancer Institute
Craig C Mello, Nobel Laureate & Distinguished Professor, Molecular Medicine, University of Massachusetts Medical School; HHMI
George Church, Professor, Genetics; Director, Center for Computational Genetics, Harvard Medical School
Steven Burrill, Chief Executive Officer, Burrill & Company
This conference is part of the Omics Evolution Summit which consists of five other conferences:
2nd Genomic & Proteomic Drug Discovery
2nd Next Generation Sequencing
Genome-wide Partnering and Dealmaking
2nd Epigentics in Drug Discovery
3rd RNAi Research and Development
For more information, please visit http://www.gtcbio.com