Immunomodulatory Properties of BRAF and MEK Inhibitors Used for Melanoma Therapy-Paradoxical ERK Activation and Beyond.


Journal

International journal of molecular sciences
ISSN: 1422-0067
Titre abrégé: Int J Mol Sci
Pays: Switzerland
ID NLM: 101092791

Informations de publication

Date de publication:
13 Sep 2021
Historique:
received: 11 08 2021
revised: 08 09 2021
accepted: 10 09 2021
entrez: 28 9 2021
pubmed: 29 9 2021
medline: 21 10 2021
Statut: epublish

Résumé

The advent of mitogen-activated protein kinase (MAPK) inhibitors that directly inhibit tumor growth and of immune checkpoint inhibitors (ICI) that boost effector T cell responses have strongly improved the treatment of metastatic melanoma. In about half of all melanoma patients, tumor growth is driven by gain-of-function mutations of BRAF (v-rat fibrosarcoma (Raf) murine sarcoma viral oncogene homolog B), which results in constitutive ERK activation. Patients with a BRAF mutation are regularly treated with a combination of BRAF and MEK (MAPK/ERK kinase) inhibitors. Next to the antiproliferative effects of BRAF/MEKi, accumulating preclinical evidence suggests that BRAF/MEKi exert immunomodulatory functions such as paradoxical ERK activation as well as additional effects in non-tumor cells. In this review, we present the current knowledge on the immunomodulatory functions of BRAF/MEKi as well as the non-intended effects of ICI and discuss the potential synergistic effects of ICI and MAPK inhibitors in melanoma treatment.

Identifiants

pubmed: 34576054
pii: ijms22189890
doi: 10.3390/ijms22189890
pmc: PMC8469254
pii:
doi:

Substances chimiques

Protein Kinase Inhibitors 0
BRAF protein, human EC 2.7.11.1
Proto-Oncogene Proteins B-raf EC 2.7.11.1
MAP Kinase Kinase Kinases EC 2.7.11.25

Types de publication

Journal Article Review

Langues

eng

Sous-ensembles de citation

IM

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Auteurs

Thomas Jung (T)

Medical Center, Department of Dermatology, University Mainz, Langenbeckstraße 1, 55131 Mainz, Germany.

Maximilian Haist (M)

Medical Center, Department of Dermatology, University Mainz, Langenbeckstraße 1, 55131 Mainz, Germany.

Michael Kuske (M)

Medical Center, Department of Dermatology, University Mainz, Langenbeckstraße 1, 55131 Mainz, Germany.

Stephan Grabbe (S)

Medical Center, Department of Dermatology, University Mainz, Langenbeckstraße 1, 55131 Mainz, Germany.

Matthias Bros (M)

Medical Center, Department of Dermatology, University Mainz, Langenbeckstraße 1, 55131 Mainz, Germany.

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Classifications MeSH