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Tyrosine kinase inhibitor (TKI) with selective activity against RET, VEGFR-2 and EGFR: Medullary thyroid cancer. Diarrhoea, hypertension, QT interval prolongation, depression, electrolyte anomalies, hypothyroidism and GI perforation (uncommon). 2.3 mTOR inhibitors: Everolimus: PO: mTOR inhibitor.
Similarly, both dual-specificity MAP kinase phosphatases and MAP-specific tyrosine phosphatases bind to MAP kinases through the same docking site. [34] [35] D-motifs can even be found in certain MAPK pathway regulators and scaffolds (e.g. in the mammalian JIP proteins). [citation needed] Other, less well characterised substrate-binding sites ...
A MEK inhibitor is a chemical or drug that inhibits the mitogen-activated protein kinase kinase enzymes MEK1 and/or MEK2. They can be used to affect the MAPK/ERK pathway which is often overactive in some cancers.
Mitogen Activated Protein (MAP) kinase kinase kinase (MAPKKK, [1] MKKK, [2] M3K, [3] or, MAP3K [4]) is a serine/threonine-specific protein kinase which acts upon MAP kinase kinase. Subsequently, MAP kinase kinase activates MAP kinase. Several types of MAPKKK can exist but are mainly characterized by the MAP kinases they activate.
Mitogen-activated protein kinase kinase (also known as MAP2K, MEK, MAPKK) is a dual-specificity kinase enzyme which phosphorylates mitogen-activated protein kinase (MAPK). MAP2K is classified as EC 2.7.12.2 .
Binimetinib, sold under the brand name Mektovi, is an anti-cancer medication used to treat various cancers. [4] Binimetinib is a selective inhibitor of MEK, a central kinase in the tumor-promoting MAPK pathway. [5] Inappropriate activation of the pathway has been shown to occur in many cancers. [5]
A protein kinase inhibitor (PKI) is a type of enzyme inhibitor that blocks the action of one or more protein kinases. Protein kinases are enzymes that phosphorylate (add a phosphate , or PO 4 , group) to a protein and can modulate its function.
Activated p38 MAP kinase has been shown to phosphorylate and activate MAPKAP kinase 2 and to phosphorylate the transcription factors ATF2, Mac, MEF2, and p53. [ 4 ] p38 also has been shown to phosphorylate post-transcriptional regulating factors like TTP , [ 5 ] and in fruit flies it plays a role in regulating the circadian clock.