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Past and Future Strategies to Inhibit Membrane Localization of the KRAS Oncogene
KRAS is one of the most studied oncogenes. It is well known that KRAS undergoes post-translational modifications at its C-terminal end. These modifications are essential for its membrane location and activity. Despite significant efforts made in the past three decades to target the mechanisms involv...
Autores principales: | , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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MDPI
2021
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8707736/ https://www.ncbi.nlm.nih.gov/pubmed/34947990 http://dx.doi.org/10.3390/ijms222413193 |
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author | Haidar, Malak Jacquemin, Patrick |
author_facet | Haidar, Malak Jacquemin, Patrick |
author_sort | Haidar, Malak |
collection | PubMed |
description | KRAS is one of the most studied oncogenes. It is well known that KRAS undergoes post-translational modifications at its C-terminal end. These modifications are essential for its membrane location and activity. Despite significant efforts made in the past three decades to target the mechanisms involved in its membrane localization, no therapies have been approved and taken into the clinic. However, many studies have recently reintroduced interest in the development of KRAS inhibitors, either by directly targeting KRAS or indirectly through the inhibition of critical steps involved in post-translational KRAS modifications. In this review, we summarize the approaches that have been applied over the years to inhibit the membrane localization of KRAS in cancer and propose a new anti-KRAS strategy that could be used in clinic. |
format | Online Article Text |
id | pubmed-8707736 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-87077362021-12-25 Past and Future Strategies to Inhibit Membrane Localization of the KRAS Oncogene Haidar, Malak Jacquemin, Patrick Int J Mol Sci Review KRAS is one of the most studied oncogenes. It is well known that KRAS undergoes post-translational modifications at its C-terminal end. These modifications are essential for its membrane location and activity. Despite significant efforts made in the past three decades to target the mechanisms involved in its membrane localization, no therapies have been approved and taken into the clinic. However, many studies have recently reintroduced interest in the development of KRAS inhibitors, either by directly targeting KRAS or indirectly through the inhibition of critical steps involved in post-translational KRAS modifications. In this review, we summarize the approaches that have been applied over the years to inhibit the membrane localization of KRAS in cancer and propose a new anti-KRAS strategy that could be used in clinic. MDPI 2021-12-07 /pmc/articles/PMC8707736/ /pubmed/34947990 http://dx.doi.org/10.3390/ijms222413193 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Review Haidar, Malak Jacquemin, Patrick Past and Future Strategies to Inhibit Membrane Localization of the KRAS Oncogene |
title | Past and Future Strategies to Inhibit Membrane Localization of the KRAS Oncogene |
title_full | Past and Future Strategies to Inhibit Membrane Localization of the KRAS Oncogene |
title_fullStr | Past and Future Strategies to Inhibit Membrane Localization of the KRAS Oncogene |
title_full_unstemmed | Past and Future Strategies to Inhibit Membrane Localization of the KRAS Oncogene |
title_short | Past and Future Strategies to Inhibit Membrane Localization of the KRAS Oncogene |
title_sort | past and future strategies to inhibit membrane localization of the kras oncogene |
topic | Review |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8707736/ https://www.ncbi.nlm.nih.gov/pubmed/34947990 http://dx.doi.org/10.3390/ijms222413193 |
work_keys_str_mv | AT haidarmalak pastandfuturestrategiestoinhibitmembranelocalizationofthekrasoncogene AT jacqueminpatrick pastandfuturestrategiestoinhibitmembranelocalizationofthekrasoncogene |