Quantitative chemical proteomics reveals mechanisms of action of clinical ABL kinase inhibitors
We describe a chemical proteomics approach to profile the interaction of small molecules
with hundreds of endogenously expressed protein kinases and purine-binding proteins. This …
with hundreds of endogenously expressed protein kinases and purine-binding proteins. This …
Optimized chemical proteomics assay for kinase inhibitor profiling
Solid supported probes have proven to be an efficient tool for chemical proteomics. The
kinobeads technology features kinase inhibitors covalently attached to Sepharose for affinity …
kinobeads technology features kinase inhibitors covalently attached to Sepharose for affinity …
Cell-based proteome profiling of potential dasatinib targets by use of affinity-based probes
H Shi, CJ Zhang, GYJ Chen… - Journal of the American …, 2012 - ACS Publications
Protein kinases (PKs) play an important role in the development and progression of cancer
by regulating cell growth, survival, invasion, metastasis, and angiogenesis. Dasatinib (BMS …
by regulating cell growth, survival, invasion, metastasis, and angiogenesis. Dasatinib (BMS …
Chemical proteomics reveals target selectivity of clinical Jak inhibitors in human primary cells
HC Eberl, T Werner, FB Reinhard, S Lehmann… - Scientific reports, 2019 - nature.com
Kinobeads are a set of promiscuous kinase inhibitors immobilized on sepharose beads for
the comprehensive enrichment of endogenously expressed protein kinases from cell lines …
the comprehensive enrichment of endogenously expressed protein kinases from cell lines …
Chemical proteomics reveals the target landscape of 1,000 kinase inhibitors
Medicinal chemistry has discovered thousands of potent protein and lipid kinase inhibitors.
These may be developed into therapeutic drugs or chemical probes to study kinase biology …
These may be developed into therapeutic drugs or chemical probes to study kinase biology …
Broad-spectrum kinase profiling in live cells with lysine-targeted sulfonyl fluoride probes
Protein kinases comprise a large family of structurally related enzymes. A major goal in
kinase-inhibitor development is to selectively engage the desired kinase while avoiding …
kinase-inhibitor development is to selectively engage the desired kinase while avoiding …
The target landscape of clinical kinase drugs
INTRODUCTION Molecularly targeted drugs such as imatinib and crizotinib have
revolutionized the treatment of certain blood and lung cancers because of their remarkable …
revolutionized the treatment of certain blood and lung cancers because of their remarkable …
Label-free Kinase Profiling Using Phosphate Affinity Polyacrylamide Gel Electrophoresis* S
E Kinoshita-Kikuta, Y Aoki, E Kinoshita… - Molecular & Cellular …, 2007 - ASBMB
Herein we describe three applications of label-free kinase profiling using a novel type of
phosphate affinity polyacrylamide gel electrophoresis. The phosphate affinity site is a …
phosphate affinity polyacrylamide gel electrophoresis. The phosphate affinity site is a …
Enzyme inhibitor discovery by activity-based protein profiling
MJ Niphakis, BF Cravatt - Annual review of biochemistry, 2014 - annualreviews.org
Eukaryotic and prokaryotic organisms possess huge numbers of uncharacterized enzymes.
Selective inhibitors offer powerful probes for assigning functions to enzymes in native …
Selective inhibitors offer powerful probes for assigning functions to enzymes in native …
Target profiling of small molecules by chemical proteomics
U Rix, G Superti-Furga - Nature chemical biology, 2009 - nature.com
The medical and pharmaceutical communities are facing a dire need for new druggable
targets, while, paradoxically, the targets of some drugs that are in clinical use or …
targets, while, paradoxically, the targets of some drugs that are in clinical use or …