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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...

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Detalles Bibliográficos
Autores principales: Haidar, Malak, Jacquemin, Patrick
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
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.
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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
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