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MEK and the inhibitors: from bench to bedside
Four distinct MAP kinase signaling pathways involving 7 MEK enzymes have been identified. MEK1 and MEK2 are the prototype members of MEK family proteins. Several MEK inhibitors are in clinical trials. Trametinib is being evaluated by FDA for the treatment of metastatic melanoma with BRAF V600 mutati...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
BioMed Central
2013
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3626705/ https://www.ncbi.nlm.nih.gov/pubmed/23587417 http://dx.doi.org/10.1186/1756-8722-6-27 |
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author | Akinleye, Akintunde Furqan, Muhammad Mukhi, Nikhil Ravella, Pavan Liu, Delong |
author_facet | Akinleye, Akintunde Furqan, Muhammad Mukhi, Nikhil Ravella, Pavan Liu, Delong |
author_sort | Akinleye, Akintunde |
collection | PubMed |
description | Four distinct MAP kinase signaling pathways involving 7 MEK enzymes have been identified. MEK1 and MEK2 are the prototype members of MEK family proteins. Several MEK inhibitors are in clinical trials. Trametinib is being evaluated by FDA for the treatment of metastatic melanoma with BRAF V600 mutation. Selumetinib has been studied in combination with docetaxel in phase II randomized trial in previously treated patients with advanced lung cancer. Selumetinib group had better response rate and progression-free survival. This review also summarized new MEK inhibitors in clinical development, including pimasertib, refametinib, PD-0325901, TAK733, MEK162 (ARRY 438162), RO5126766, WX-554, RO4987655 (CH4987655), GDC-0973 (XL518), and AZD8330. |
format | Online Article Text |
id | pubmed-3626705 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2013 |
publisher | BioMed Central |
record_format | MEDLINE/PubMed |
spelling | pubmed-36267052013-04-16 MEK and the inhibitors: from bench to bedside Akinleye, Akintunde Furqan, Muhammad Mukhi, Nikhil Ravella, Pavan Liu, Delong J Hematol Oncol Review Four distinct MAP kinase signaling pathways involving 7 MEK enzymes have been identified. MEK1 and MEK2 are the prototype members of MEK family proteins. Several MEK inhibitors are in clinical trials. Trametinib is being evaluated by FDA for the treatment of metastatic melanoma with BRAF V600 mutation. Selumetinib has been studied in combination with docetaxel in phase II randomized trial in previously treated patients with advanced lung cancer. Selumetinib group had better response rate and progression-free survival. This review also summarized new MEK inhibitors in clinical development, including pimasertib, refametinib, PD-0325901, TAK733, MEK162 (ARRY 438162), RO5126766, WX-554, RO4987655 (CH4987655), GDC-0973 (XL518), and AZD8330. BioMed Central 2013-04-12 /pmc/articles/PMC3626705/ /pubmed/23587417 http://dx.doi.org/10.1186/1756-8722-6-27 Text en Copyright © 2013 Akinleye et al.; licensee BioMed Central Ltd. http://creativecommons.org/licenses/by/2.0 This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/2.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Review Akinleye, Akintunde Furqan, Muhammad Mukhi, Nikhil Ravella, Pavan Liu, Delong MEK and the inhibitors: from bench to bedside |
title | MEK and the inhibitors: from bench to bedside |
title_full | MEK and the inhibitors: from bench to bedside |
title_fullStr | MEK and the inhibitors: from bench to bedside |
title_full_unstemmed | MEK and the inhibitors: from bench to bedside |
title_short | MEK and the inhibitors: from bench to bedside |
title_sort | mek and the inhibitors: from bench to bedside |
topic | Review |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3626705/ https://www.ncbi.nlm.nih.gov/pubmed/23587417 http://dx.doi.org/10.1186/1756-8722-6-27 |
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