Mek inhibitors

Author: Prof. Dr. med. Peter Altmeyer

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Last updated on: 29.10.2020

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Synonym(s)

MEK inhibitor, MAP kinase inhibitor, MAP kinase inhibitor

Definition
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The MAP kinases MEK1 (MAP2K1) and MEK2 (MAP2K2), which are downstream of the tyrosine kinase receptors and RAF kinases, can be activated by various methods. inhibitors.

Field of application/use
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The protein kinases MEK1/2 are an important component of the Ras/Raf/MAPK signalling pathway. It is a cascade of different kinases that are connected in series and activate each other sequentially by phosphorylation and play a major role in the control of the cell cycle. MEK inhibitors intervene in this signalling cascade. They bind to MEK1 and MEK2 and prevent the further phosphorylation of transcription factors. This leads to the suspension of transcription and ultimately to the inhibition of tumour cell proliferation.

MEK inhibitors are mainly used for the therapy of malignant melanoma, but also for other tumors with BRAF mutation. Active ingredients:

Undesirable effects
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The cutaneous side effects of these inhibitors are manifold. Most of them correspond to those of EGFR antagonists (see there). In detail they are among the different types of EGFR antagonists. Drugs listed.

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Last updated on: 29.10.2020