Inhibiting CK2α from Outside the Active Site
Poster Mar 03, 2017
Paul Brear[sup]1[/sup], Claudia De-Fusco[sup]2[/sup], Kathy Hadje Georgiou[sup]2[/sup], Nicola J. Francis-Newton[sup]3[/sup], Chris Stubbs[sup]2[/sup], Ashok R. Venkitaraman[sup]3[/sup], Chris Abell[sup]2[/sup], David Spring[sup]2[/sup], Marko Hyvonen[sup]1[/sup]
EKJ is a highly conserved kinase with pro survival and anti-apoptotic effects on cells. It is often overexpressed in cancer cells in which it promotes their proliferation by multiple mechanisms. A number of potent CK2a inhibitors,B that target only the ATP site, have been shown to inhibit the growth of a range of cancer cell lines and one of these, CX-4945 has progressed to phase II clinical trials. Although described as highly selective, CX-4945 inhibits at least 12 other kinases with nanomolar IC50's.
Strategies to inhibit CK2a without targeting the ATP binding site offer the promise of enhanced selectivity as well as new mechanisms of action. Here we report the creation and characterization of a unique inhibitor of CK2a that targets a novel cryptic pocket and was developed using fragment-based methods.
Analysis of Extract Drying Criteria for Oil & Grease Method 1664A/BPoster
Analysis of Extract Drying Criteria for Oil & Grease Method 1664A/BREAD MORE
New Biotransformation Prediction Engine Integrated into a Metabolite Identification SolutionPoster
Here we present a new prediction algorithm that determines the likelihood of biotransformation reactions, and subsequent metabolite identification, within an automated processing routine.READ MORE
A New Method for Analyzing MSe/All Ions Fragmentation in Xenobiotic Metabolism StudiesPoster
During early drug discovery, the study of metabolism plays an essential role in determining which drug candidates move forward into development and later stages. As an alternative to traditional Data Dependent Acquisition (DDA), the use of MSE/All Ions Fragmentation (AIF) has become common in metabolite identification workflows for the analysis of metabolic hot spots. Here we present a solution for analysis of MSE/AlF in metID studies.READ MORE