Analysis of protein kinases by quantitative chemical proteomics

2007 ◽  
Vol 2007 (Fall) ◽  
Author(s):  
Henrik Daub ◽  
Jesper V. Olsen ◽  
Michaela Bairlein ◽  
Florian Gnad ◽  
Felix Oppermann ◽  
...  
Keyword(s):  
Protein Kinases ◽  
Chemical Proteomics ◽  
Quantitative Chemical

scholarly journals Protocol for clickable photoaffinity labeling and quantitative chemical proteomics

2021 ◽  
Vol 2 (2) ◽  
pp. 100593
Author(s):  
Wankyu Lee ◽  
Zhen Huang ◽  
Christopher W. am Ende ◽  
Uthpala Seneviratne
Keyword(s):  
Photoaffinity Labeling ◽  
Chemical Proteomics ◽  
Quantitative Chemical

A Quantitative Chemical Proteomics Approach for Site-specific Stoichiometry Analysis of Ubiquitination

2018 ◽  
Vol 58 (2) ◽  
pp. 537-541 ◽  
Author(s):  
Yunan Li ◽  
Jonathan Evers ◽  
Ang Luo ◽  
Luke Erber ◽  
Zachary Postler ◽  
...  
Keyword(s):  
Chemical Proteomics ◽  
Site Specific ◽  
Proteomics Approach ◽  
Quantitative Chemical

scholarly journals Quantitative Chemical Proteomics Reveals New Potential Drug Targets in Head and Neck Cancer

2011 ◽  
Vol 10 (12) ◽  
pp. M111.011635 ◽  
Author(s):  
Zhixiang Wu ◽  
Jessica B. Doondeea ◽  
Amin Moghaddas Gholami ◽  
Melanie C. Janning ◽  
Simone Lemeer ◽  
...  
Keyword(s):  
Head And Neck Cancer ◽  
Head And Neck ◽  
Neck Cancer ◽  
Drug Targets ◽  
Potential Drug ◽  
Chemical Proteomics ◽  
Potential Drug Targets ◽  
Quantitative Chemical

scholarly journals Chemical proteomics reveals target selectivity of clinical Jak inhibitors in human primary cells

2019 ◽  
Vol 9 (1) ◽  
Author(s):  
H. Christian Eberl ◽  
Thilo Werner ◽  
Friedrich B. Reinhard ◽  
Stephanie Lehmann ◽  
Douglas Thomson ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Protein Kinases ◽  
Kinase Inhibitors ◽  
Dissociation Constants ◽  
Peripheral Blood Mononuclear ◽  
Mass Spectrometry Experiment ◽  
Chemical Proteomics ◽  
Human Primary Cells ◽  
Lipid Kinases ◽  
Single Mass

Abstract Kinobeads are a set of promiscuous kinase inhibitors immobilized on sepharose beads for the comprehensive enrichment of endogenously expressed protein kinases from cell lines and tissues. These beads enable chemoproteomics profiling of kinase inhibitors of interest in dose-dependent competition studies in combination with quantitative mass spectrometry. We present improved bead matrices that capture more than 350 protein kinases and 15 lipid kinases from human cell lysates, respectively. A multiplexing strategy is suggested that enables determination of apparent dissociation constants in a single mass spectrometry experiment. Miniaturization of the procedure enabled determining the target selectivity of the clinical BCR-ABL inhibitor dasatinib in peripheral blood mononuclear cell (PBMC) lysates from individual donors. Profiling of a set of Jak kinase inhibitors revealed kinase off-targets from nearly all kinase families underpinning the need to profile kinase inhibitors against the kinome. Potently bound off-targets of clinical inhibitors suggest polypharmacology, e.g. through MRCK alpha and beta, which bind to decernotinib with nanomolar affinity.

scholarly journals Quantitative Chemical Proteomics Reveals Resveratrol Inhibition of A549 Cell Migration Through Binding Multiple Targets to Regulate Cytoskeletal Remodeling and Suppress EMT

2021 ◽  
Vol 12 ◽  
Author(s):  
Xiao Chen ◽  
Yutong Wang ◽  
Jing Tian ◽  
Yurou Shao ◽  
Bo Zhu ◽  
...  
Keyword(s):  
Cell Migration ◽  
A549 Cell ◽  
A549 Cells ◽  
Multiple Targets ◽  
Chemical Proteomics ◽  
Protein Targets ◽  
Cytoskeletal Remodeling ◽  
Quantitative Chemical

Resveratrol (RSV), a health-promoting natural product, has been shown to affect various cellular processes in tumor cells. However, the specific protein targets of RSV and the mechanism of action (MOA) of its anticancer effect remain elusive. In this study, the pharmacological activity of RSV was first evaluated in A549 cells, and the results showed that RSV significantly inhibited A549 cell migration but did not affect cell viability. To elucidate the underlying mechanism, a quantitative chemical proteomics approach was employed to identify the protein targets of RSV. A total of 38 target proteins were identified, and proteomic analysis showed that the targets were mainly involved in cytoskeletal remodeling and EMT, which were verified by subsequent in vitro and in vivo assays. In conclusion, RSV inhibits A549 cell migration by binding to multiple targets to regulate cytoskeletal remodeling and suppress EMT.

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