Discovery and Optimization of a Novel Series of Dyrk1B Kinase Inhibitors To Explore a MEK Resistance Hypothesis

Potent and selective inhibitors of Dyrk1B kinase were developed to explore the hypothesis, based on siRNA studies, that Dyrk1B may be a resistance mechanism in cells undergoing a stress response.

Saved in:
Bibliographic Details
Published in:Journal of medicinal chemistry 2015-03, Vol.58 (6), p.2834-2844
Main Authors: Kettle, Jason G, Ballard, Peter, Bardelle, Catherine, Cockerill, Mark, Colclough, Nicola, Critchlow, Susan E, Debreczeni, Judit, Fairley, Gary, Fillery, Shaun, Graham, Mark A, Goodwin, Louise, Guichard, Sylvie, Hudson, Kevin, Ward, Richard A, Whittaker, David
Format: Article
Language:English
Subjects:
Animals
Cell Line, Tumor
Chlorocebus aethiops
COS Cells
Drug Discovery
Drug Resistance
Dyrk Kinases
Humans
MAP Kinase Kinase Kinases - antagonists & inhibitors
MAP Kinase Kinase Kinases - metabolism
Models, Molecular
Protein Kinase Inhibitors - chemistry
Protein Kinase Inhibitors - pharmacokinetics
Protein Kinase Inhibitors - pharmacology
Protein Serine-Threonine Kinases - antagonists & inhibitors
Protein Serine-Threonine Kinases - chemistry
Protein Serine-Threonine Kinases - genetics
Protein Serine-Threonine Kinases - metabolism
Protein-Tyrosine Kinases - antagonists & inhibitors
Protein-Tyrosine Kinases - chemistry
Protein-Tyrosine Kinases - genetics
Protein-Tyrosine Kinases - metabolism
Rats, Wistar
RNA Interference
RNA, Small Interfering - genetics
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Potent and selective inhibitors of Dyrk1B kinase were developed to explore the hypothesis, based on siRNA studies, that Dyrk1B may be a resistance mechanism in cells undergoing a stress response.
ISSN:0022-2623
1520-4804
DOI:10.1021/acs.jmedchem.5b00098