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Recent advances in methods to assess the activity of the kinome

Protein and lipid kinases are deregulated in most, if not all, cancers and are among the most valuable therapeutic targets in these diseases. Despite the introduction of dozens of effective kinase inhibitors into clinical practice, the development of drug resistance remains a major barrier to treatm...

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Detalles Bibliográficos
Autores principales: Radu, Maria, Chernoff, Jonathan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: F1000Research 2017
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5490475/
https://www.ncbi.nlm.nih.gov/pubmed/28713564
http://dx.doi.org/10.12688/f1000research.10962.1
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author Radu, Maria
Chernoff, Jonathan
author_facet Radu, Maria
Chernoff, Jonathan
author_sort Radu, Maria
collection PubMed
description Protein and lipid kinases are deregulated in most, if not all, cancers and are among the most valuable therapeutic targets in these diseases. Despite the introduction of dozens of effective kinase inhibitors into clinical practice, the development of drug resistance remains a major barrier to treatment because of adaption of cellular signaling pathways to bypass targeted kinases. So that the basal and adaptive responses of kinases in cancer can be better understood, new methods have emerged that allow simultaneous and unbiased measurement of the activation state of a substantial fraction of the entire kinome. Here, we discuss such kinome-profiling methodologies, emphasizing the relative strengths and weaknesses of each approach.
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spelling pubmed-54904752017-07-13 Recent advances in methods to assess the activity of the kinome Radu, Maria Chernoff, Jonathan F1000Res Review Protein and lipid kinases are deregulated in most, if not all, cancers and are among the most valuable therapeutic targets in these diseases. Despite the introduction of dozens of effective kinase inhibitors into clinical practice, the development of drug resistance remains a major barrier to treatment because of adaption of cellular signaling pathways to bypass targeted kinases. So that the basal and adaptive responses of kinases in cancer can be better understood, new methods have emerged that allow simultaneous and unbiased measurement of the activation state of a substantial fraction of the entire kinome. Here, we discuss such kinome-profiling methodologies, emphasizing the relative strengths and weaknesses of each approach. F1000Research 2017-06-26 /pmc/articles/PMC5490475/ /pubmed/28713564 http://dx.doi.org/10.12688/f1000research.10962.1 Text en Copyright: © 2017 Radu M and Chernoff J http://creativecommons.org/licenses/by/4.0/ This is an open access article distributed under the terms of the Creative Commons Attribution Licence, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Review
Radu, Maria
Chernoff, Jonathan
Recent advances in methods to assess the activity of the kinome
title Recent advances in methods to assess the activity of the kinome
title_full Recent advances in methods to assess the activity of the kinome
title_fullStr Recent advances in methods to assess the activity of the kinome
title_full_unstemmed Recent advances in methods to assess the activity of the kinome
title_short Recent advances in methods to assess the activity of the kinome
title_sort recent advances in methods to assess the activity of the kinome
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5490475/
https://www.ncbi.nlm.nih.gov/pubmed/28713564
http://dx.doi.org/10.12688/f1000research.10962.1
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