Literature summary for 2.7.12.2 extracted from

Borthakur, G.; Popplewell, L.; Boyiadzis, M.; Foran, J.; Platzbecker, U.; Vey, N.; Walter, R.B.; Olin, R.; Raza, A.; Giagounidis, A.; Al-Kali, A.; Jabbour, E.; Kadia, T.; Garcia-Manero, G.; Bauman, J.W.; Wu, Y.; Liu, Y.; Schramek, D.; Cox, D.S.; Wissel, P.; Kantarjian, H.
Activity of the oral mitogen-activated protein kinase kinase inhibitor trametinib in RAS-mutant relapsed or refractory myeloid malignancies (2016), Cancer, 122, 1871-1879.

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Inhibitors

Inhibitors	Comment	Organism	Structure
trametinib	a mitogen-activated protein kinase kinase 1 (MEK1)/MEK2 inhibitor with activity against multiple myeloid cell lines at low nanomolar concentrations, preferential activity among RAS-mutated myeloid malignancies. During clinical oral treatment, most commonly reported treatment-related adverse events are diarrhea, rash, nausea, and increased alanine aminotransferase levels, repeated cycles of trametinib are well tolerated with manageable or reversible toxicities, overview; a mitogen-activated protein kinase kinase 1 (MEK1)/MEK2 inhibitor with activity against multiple myeloid cell lines at low nanomolar concentrations, preferential activity among RAS-mutated myeloid malignancies. During clinical oral treatment, most commonly reported treatment-related adverse events are diarrhea, rash, nausea, and increased alanine aminotransferase levels, repeated cycles of trametinib are well tolerated with manageable or reversible toxicities, overview	Homo sapiens

Metals/Ions

Metals/Ions	Comment	Organism	Structure
Mg2+	required	Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
ATP + a protein	Homo sapiens	-	ADP + a phosphoprotein	-	?

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	P36507	MEK2	-
Homo sapiens	Q02750	MEK1	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
ATP + a protein	-	Homo sapiens	ADP + a phosphoprotein	-	?

Synonyms

Synonyms	Comment	Organism
MEK1	-	Homo sapiens
MEK2	-	Homo sapiens
mitogen-activated protein kinase kinase 1	-	Homo sapiens
mitogen-activated protein kinase kinase 2	-	Homo sapiens

Cofactor

Cofactor	Comment	Organism	Structure
ATP	-	Homo sapiens

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Release 2023.1 (January 2023)