Quantitative chemical proteomics reveals mechanisms of action of clinical ABL kinase inhibitors

M Bantscheff, D Eberhard, Y Abraham, S Bastuck… - Nature …, 2007 - nature.com
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 …

Optimized chemical proteomics assay for kinase inhibitor profiling

G Médard, F Pachl, B Ruprecht, S Klaeger… - Journal of proteome …, 2015 - ACS Publications
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 …

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 …

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 …

Chemical proteomics reveals the target landscape of 1,000 kinase inhibitors

M Reinecke, P Brear, L Vornholz, BT Berger… - Nature Chemical …, 2024 - nature.com
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 …

Broad-spectrum kinase profiling in live cells with lysine-targeted sulfonyl fluoride probes

Q Zhao, X Ouyang, X Wan, KS Gajiwala… - Journal of the …, 2017 - ACS Publications
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 …

The target landscape of clinical kinase drugs

S Klaeger, S Heinzlmeir, M Wilhelm, H Polzer, B Vick… - Science, 2017 - science.org
INTRODUCTION Molecularly targeted drugs such as imatinib and crizotinib have
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 …

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 …

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 …