Oss, August, 25th, 2016 – At the Discovery on Target (DOT) conference, to be held in Boston from September 19th to 22nd, Dr. Guido Zaman, Managing Director and Head of Biology at NTRC, will present on ResidenceTimer™, the platform for measurement of binding kinetics against kinases by surface plasmon resonance. At the conference results will be presented on the selectivity profiling and determination of binding kinetics of different PI-3 Kinase inhibitor subclasses; a comparison of reversible and irreversible EGFR inhibitor drugs; and the study of the relationship of kinase protein structure and target residence time for TTK/Mps1. It will be shown that optimization on increased target residence time can result in improved cellular activity of reversible kinase inhibitors. NTRC has developed and validated assays for more than fifty different protein tyrosine, serine/threonine, and lipid kinases.
The presentation on ResidenceTimer™ is scheduled on Thursday, September 22nd, at 9.15 a.m. in the ‘Kinase Inhibitor Discovery’ track. Title of presentation: ‘Kinetic selectivity and target residence time determine cellular activity of kinase inhibitors’. Guido Zaman will also chair the opening session of the Kinase Inhibitor symposium on Wednesday afternoon from 3.20 p.m.
At the same conference, in the track on ‘Targeting Histone Methyltransferases and Demethylases’, Dr. Suzanne van Gerwen will present a poster on OncolinesProfiler™. In OncolinesProfiler™ the activity of compound in proliferation assays on 66 cancer cell lines (Oncolines™) is compared to the profiles of 121 anti-cancer agents, including cytotoxic agents, approved targeted drugs, epigenetic modulators, and many investigational drugs. Results are presented for EZH2, PI-3 and Aurora kinase inhibitors. OncolinesProfiler™ can be used to get more insight into potential mechanism of action of new candidate drugs, and to determine similarity or differentiation from existing anti-cancer agents.
The poster on OncolinesProfiler™ will be presented on Tuesday, September 20th in the Exhibit Hall of the Westin Boston Waterfront Hotel where the conference takes place. Title of poster: ‘Comparative cancer cell line profiling differentiates the mechanism of action of different EZH2, PI3K/mTOR and Aurora kinase inhibitors’.
NTRC is a precision medicine company dedicated to the development of new anti-cancer drugs. NTRC facilitates the development of novel therapies by providing cancer cell line profiling services (Oncolines™, SynergyFinder™ and OncolinesProfiler™), target residence time measurements for protein kinases (ResidenceTimer™), and developing new enabling technologies, such as NFK GreenScreen™. In addition, NTRC develops own novel targeted therapies based on small molecules, such as inhibitors of the tryptophan metabolizing enzymes IDO1 and TDO for cancer immunotherapy and selective inhibitors of TTK (Mps1) protein kinase for chromosomal unstable tumours. For more information please visit www.ntrc.nl or contact [email protected]