Your browser doesn't support javascript.
loading
The ERK5 pathway in BRAFV600E melanoma cells plays a role in development of acquired resistance to dabrafenib but not vemurafenib.
Mondru, Anil Kumar; Wilkinson, Beth; Aljasir, Mohammad A; Alrumayh, Ahmed; Greaves, Georgia; Emmett, Maxine; Albohairi, Saad; Pritchard-Jones, Rowan; Cross, Michael J.
Afiliación
  • Mondru AK; Department of Pharmacology and Therapeutics, Institute of Systems, Molecular and Integrative Biology, University of Liverpool, UK.
  • Wilkinson B; Department of Pharmacology and Therapeutics, Institute of Systems, Molecular and Integrative Biology, University of Liverpool, UK.
  • Aljasir MA; Department of Pharmacology and Therapeutics, Institute of Systems, Molecular and Integrative Biology, University of Liverpool, UK.
  • Alrumayh A; Department of Pharmacology and Therapeutics, Institute of Systems, Molecular and Integrative Biology, University of Liverpool, UK.
  • Greaves G; Department of Pharmacology and Therapeutics, Institute of Systems, Molecular and Integrative Biology, University of Liverpool, UK.
  • Emmett M; Department of Pharmacology and Therapeutics, Institute of Systems, Molecular and Integrative Biology, University of Liverpool, UK.
  • Albohairi S; Department of Pharmacology and Therapeutics, Institute of Systems, Molecular and Integrative Biology, University of Liverpool, UK.
  • Pritchard-Jones R; Department of Molecular and Clinical Cancer Medicine, Institute of Systems, Molecular and Integrative Biology, University of Liverpool, UK.
  • Cross MJ; Department of Pharmacology and Therapeutics, Institute of Systems, Molecular and Integrative Biology, University of Liverpool, UK.
FEBS Lett ; 598(16): 2011-2027, 2024 Aug.
Article en En | MEDLINE | ID: mdl-38977937
ABSTRACT
Malignant melanoma, an aggressive skin cancer with a poor prognosis, frequently features BRAFV600E mutation resulting in activation of the MAPK pathway and melanocyte proliferation and survival. BRAFV600E inhibitors like vemurafenib and dabrafenib have enhanced patient survival, yet drug resistance remains a significant challenge. We investigated the role of the ERK5 pathway in BRAFV600E melanoma cells and cells with acquired resistance to PLX4720 (vemurafenib) and dabrafenib. In BRAFV600E melanoma, ERK5 inhibition minimally affected viability compared to ERK1/2 inhibition. In vemurafenib-resistant cells, ERK5 inhibition alone didn't impact viability or restore drug sensitivity to vemurafenib. However, in dabrafenib-resistant cells, ERK5 inhibition reduced viability and enhanced the anti-proliferative effect of MEK1/2 inhibition. Targeting the ERK5 pathway may represent a therapeutic opportunity in dabrafenib-resistant melanoma.
Asunto(s)
Palabras clave
Texto completo
Añadir a Mi BVS
Imprimir
XML
PubMed Links
Buscar en Google

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Oximas / Resistencia a Antineoplásicos / Proteínas Proto-Oncogénicas B-raf / Proteína Quinasa 7 Activada por Mitógenos / Vemurafenib / Imidazoles / Melanoma Límite: Humans Idioma: En Revista: FEBS Lett Año: 2024 Tipo del documento: Article Pais de publicación: Reino Unido
Texto completo
Añadir a Mi BVS
Imprimir
XML
PubMed Links
Buscar en Google

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Oximas / Resistencia a Antineoplásicos / Proteínas Proto-Oncogénicas B-raf / Proteína Quinasa 7 Activada por Mitógenos / Vemurafenib / Imidazoles / Melanoma Límite: Humans Idioma: En Revista: FEBS Lett Año: 2024 Tipo del documento: Article Pais de publicación: Reino Unido