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Targeting STATs for cancer therapy: “Undruggable” no more
We are in the midst of an exciting transition in the treatment of cancers, from the empirically developed non-specifically cytotoxic drugs to the era of rationally derived molecularly targeted therapies. Over the past 15 years, our understanding of the mutations that drive cancer pathogenesis has gr...
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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Landes Bioscience
2012
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Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3670283/ https://www.ncbi.nlm.nih.gov/pubmed/24058782 http://dx.doi.org/10.4161/jkst.22528 |
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author | Frank, David A. |
author_facet | Frank, David A. |
author_sort | Frank, David A. |
collection | PubMed |
description | We are in the midst of an exciting transition in the treatment of cancers, from the empirically developed non-specifically cytotoxic drugs to the era of rationally derived molecularly targeted therapies. Over the past 15 years, our understanding of the mutations that drive cancer pathogenesis has grown enormously, which has rapidly led to the development of drugs to target the associated gene products. Almost all of this focus has been on kinases, largely tyrosine kinases that are activated by translocations, point mutations, insertions and deletions. Although this approach will continue to bear fruit for some time, there is increasing evidence that the returns will be diminishing. First, dominant activating mutations in kinases are less frequent then initially expected particularly in common human cancers, and thus the number of patient whose tumors have suitable targets may be limited. The second cause for concern is the rapid development of resistance that often occurs, arising either from mutations in the target kinase or activation of a parallel pathway. Thus, the desire to target a common convergence point of multiple pathways that directly contributes to the oncogenic phenotype is highly desirable. This goal has led to consideration of transcription factors as therapeutic targets. |
format | Online Article Text |
id | pubmed-3670283 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2012 |
publisher | Landes Bioscience |
record_format | MEDLINE/PubMed |
spelling | pubmed-36702832013-09-19 Targeting STATs for cancer therapy: “Undruggable” no more Frank, David A. JAKSTAT Special Focus Letter from the Guest Editor We are in the midst of an exciting transition in the treatment of cancers, from the empirically developed non-specifically cytotoxic drugs to the era of rationally derived molecularly targeted therapies. Over the past 15 years, our understanding of the mutations that drive cancer pathogenesis has grown enormously, which has rapidly led to the development of drugs to target the associated gene products. Almost all of this focus has been on kinases, largely tyrosine kinases that are activated by translocations, point mutations, insertions and deletions. Although this approach will continue to bear fruit for some time, there is increasing evidence that the returns will be diminishing. First, dominant activating mutations in kinases are less frequent then initially expected particularly in common human cancers, and thus the number of patient whose tumors have suitable targets may be limited. The second cause for concern is the rapid development of resistance that often occurs, arising either from mutations in the target kinase or activation of a parallel pathway. Thus, the desire to target a common convergence point of multiple pathways that directly contributes to the oncogenic phenotype is highly desirable. This goal has led to consideration of transcription factors as therapeutic targets. Landes Bioscience 2012-10-01 2012-10-01 /pmc/articles/PMC3670283/ /pubmed/24058782 http://dx.doi.org/10.4161/jkst.22528 Text en Copyright © 2012 Landes Bioscience http://creativecommons.org/licenses/by-nc/3.0/ This is an open-access article licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported License. The article may be redistributed, reproduced, and reused for non-commercial purposes, provided the original source is properly cited. |
spellingShingle | Special Focus Letter from the Guest Editor Frank, David A. Targeting STATs for cancer therapy: “Undruggable” no more |
title | Targeting STATs for cancer therapy: “Undruggable” no more |
title_full | Targeting STATs for cancer therapy: “Undruggable” no more |
title_fullStr | Targeting STATs for cancer therapy: “Undruggable” no more |
title_full_unstemmed | Targeting STATs for cancer therapy: “Undruggable” no more |
title_short | Targeting STATs for cancer therapy: “Undruggable” no more |
title_sort | targeting stats for cancer therapy: “undruggable” no more |
topic | Special Focus Letter from the Guest Editor |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3670283/ https://www.ncbi.nlm.nih.gov/pubmed/24058782 http://dx.doi.org/10.4161/jkst.22528 |
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