Stephan Grant, Senior Director of Oncology Research Unit and Head of Biochemistry & Primary Screening, To Give a Featured Presentation at the 2nd Protein Kinases & Drug Design Conference (Oct 23-25, 2013 in San Diego)
Online PR News – 08-August-2013 – San Diego – Stephan Grant, Senior Director of Oncology Research Unit and Head of Biochemistry & Primary Screening, will give a featured presentation on “Critical Influences on Kinase Inhibitor Binding From Outside the ATP Binding Site” at the 2nd Protein Kinases & Drug Design Conference to be held in San Diego, CA on October 23-25, 2013 by GTC.
The reversible phosphorylation of proteins is a highly coordinated cellular signaling process. Multiple regulatory mechanisms exist that control the activity of cellular protein kinases that catalyze the ATP-dependent phosphorylation of proteins. Aberrant activation of protein kinases can disrupt normal cellular function, leading in some cases to oncogenic transformation and tumorigenesis. Targeted inhibitors of protein kinases have thus been developed as therapeutic anti-cancer drugs. The discovery and development of targeted kinase inhibitors has often utilized a structure-based approach to the design of small molecule drugs that bind specifically within the ATP binding site of a target kinase. While ATP-directed inhibitors have been successfully developed for protein kinases in this fashion, it has become apparent that various regulatory mechanisms can also influence the binding of a small molecule drug to the catalytic kinase domain. Steve Grant’s presentation will highlight some examples from their own drug discovery projects where kinase inhibition was regulated by influences from outside the ATP binding site. An understanding of such interactions can have an impact on kinase drug discovery and inhibitor design principles. Dr. Grant’s research group provides the primary in vitro pharmacology support for preclinical cancer research projects including drug discovery efforts on protein kinase inhibitors.
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 consists of this and three other parallel conferences shown below:
Protein Kinases & Drug Design
Antibody & Protein Therapeutics
Protein Expression, Purification & Characterization
For more information, please visit www.gtcbio.com