Abstract
The RAF-MEK and PI3K-AKT pathways are both frequently deregulated in cancer, and often play a critical role in oncogenesis. In the previous years, major progress has been made in the development of targeted drugs against signaling kinases which are involved in carcinogenesis. Currently, targeted drugs against RAF, MEK, PI3K and AKT (among several others) have entered clinical investigation. Here we describe tumor causing mutations of these kinases, as well as the small molecule inhibitors that target these kinases, which contributes to improved ways of treating human cancer.
Keywords: AKT, Antitumor activity, Inhibitors, MEK, PI3K, RAF, Targeted drugs
Current Cancer Therapy Reviews
Title:Recent Developments in Targeted Therapies of the RAF-MEK and PI3KAKT Pathways in Cancer Treatment
Volume: 8 Issue: 3
Author(s): Lobke G.M. Cremers and Johannes Boonstra
Affiliation:
Keywords: AKT, Antitumor activity, Inhibitors, MEK, PI3K, RAF, Targeted drugs
Abstract: The RAF-MEK and PI3K-AKT pathways are both frequently deregulated in cancer, and often play a critical role in oncogenesis. In the previous years, major progress has been made in the development of targeted drugs against signaling kinases which are involved in carcinogenesis. Currently, targeted drugs against RAF, MEK, PI3K and AKT (among several others) have entered clinical investigation. Here we describe tumor causing mutations of these kinases, as well as the small molecule inhibitors that target these kinases, which contributes to improved ways of treating human cancer.
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G.M. Cremers Lobke and Boonstra Johannes, Recent Developments in Targeted Therapies of the RAF-MEK and PI3KAKT Pathways in Cancer Treatment, Current Cancer Therapy Reviews 2012; 8 (3) . https://dx.doi.org/10.2174/157339412802653209
DOI https://dx.doi.org/10.2174/157339412802653209 |
Print ISSN 1573-3947 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6301 |
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argeted Protein Degradation is gaining momentum in cancer therapy, it facilitate targeting undruggable proteins, it overcome cancer resistance and avoid undesirable side effects. Thus small molecules degraders have emerged as novel therapeutic strategy. Targeted protein degradation (TPD), the process of eliminating a protein of interest hold a great promise for ...read more
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