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Ref Type Journal Article
PMID (18223206)
Authors Friday BB, Adjei AA
Title Advances in targeting the Ras/Raf/MEK/Erk mitogen-activated protein kinase cascade with MEK inhibitors for cancer therapy.
Journal Clinical cancer research : an official journal of the American Association for
Vol 14
Issue 2
Date 2008 Jan 15
URL
Abstract Text The identification of intracellular signaling cascades important for the growth and survival of cancer cells has led to the development of targeted cancer therapeutics aimed at blocking these signals. The mitogen-activated protein kinase (MAPK) pathway has a well-defined role in cancer biology and has been an important target in the development of targeted therapies. Recently, several small-molecule inhibitors of MAPK/extracellular signal-regulated kinase kinase (MEK), a key intermediary of MAPK signaling, have been developed and are currently being tested in clinical trials. Herein, we review the MAPK pathway, the development of small-molecule MEK inhibitors, and the results obtained to date with MEK inhibitors in human cancer trials.

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Molecular Profile Treatment Approach
MAP2K1 I103_K104del MEK inhibitor (Pan)
MAP2K1 L101_E102del MEK inhibitor (Pan)
MAP2K1 F53I MEK1 Inhibitor
MAP2K1 E120Q MEK inhibitor (Pan)
MAP2K1 I107_R108del MEK inhibitor (Pan)
MAP2K1 E144K MEK1 Inhibitor
MAP2K1 P124R MEK inhibitor (Pan)
MAP2K1 N109_R113del MEK1 Inhibitor
MAP2K1 Q56_V60del MEK1 Inhibitor
MAP2K1 P124R MEK1 Inhibitor
MAP2K1 S218D MEK inhibitor (Pan)
MAP2K1 act mut MEK1 Inhibitor
MAP2K1 K57_G61del MEK1 Inhibitor
MAP2K1 Q56P MEK inhibitor (Pan)
MAP2K1 I107_R108del MEK1 Inhibitor
MAP2K1 I112_R113del MEK inhibitor (Pan)
MAP2K1 E203V MEK inhibitor (Pan)
MAP2K1 F53V MEK inhibitor (Pan)
MAP2K1 amp MEK inhibitor (Pan)
MAP2K1 N122D MEK inhibitor (Pan)
MAP2K1 F53L MEK1 Inhibitor
MAP2K1 I111_I112del MEK1 Inhibitor
MAP2K1 E203K MEK1 Inhibitor
MAP2K1 S123T MEK inhibitor (Pan)
MAP2K1 F53L MEK inhibitor (Pan)
MAP2K1 V60M MEK1 Inhibitor
MAP2K1 L101_E102del MEK1 Inhibitor
MAP2K1 I104_P105del MEK inhibitor (Pan)
MAP2K1 F53I MEK inhibitor (Pan)
MAP2K1 I111_I112del MEK inhibitor (Pan)
MAP2K1 D65N MEK inhibitor (Pan)
MAP2K1 A106_I107del MEK inhibitor (Pan)
MAP2K1 amp MEK1 Inhibitor
MAP2K1 E41_L54del MEK1 Inhibitor
MAP2K1 E41_L54del MEK inhibitor (Pan)
MAP2K1 K57_G61del MEK inhibitor (Pan)
MAP2K1 P306H MEK1 Inhibitor
MAP2K1 R47Q MEK1 Inhibitor
MAP2K1 Q56P MEK1 Inhibitor
MAP2K1 K57C MEK inhibitor (Pan)
MAP2K1 E203V MEK1 Inhibitor
MAP2K1 E120Q MEK1 Inhibitor
MAP2K1 S218D MEK1 Inhibitor
MAP2K1 K57N MEK inhibitor (Pan)
MAP2K1 K59del MEK inhibitor (Pan)
MAP2K1 Q58_E62del MEK1 Inhibitor
MAP2K1 N122D MEK1 Inhibitor
MAP2K1 P105_A106del MEK inhibitor (Pan)
MAP2K1 Q58_E62del MEK inhibitor (Pan)
MAP2K1 T28I MEK inhibitor (Pan)
MAP2K1 Y134C MEK inhibitor (Pan)
MAP2K1 K57C MEK1 Inhibitor
MAP2K1 F53V MEK1 Inhibitor
MAP2K1 L37P MEK inhibitor (Pan)
MAP2K1 F53S MEK inhibitor (Pan)
MAP2K1 I104_P105del MEK1 Inhibitor
MAP2K1 L37P MEK1 Inhibitor
MAP2K1 G128D MEK inhibitor (Pan)
MAP2K1 N109_R113del MEK inhibitor (Pan)
MAP2K1 R108_N109del MEK inhibitor (Pan)
MAP2K1 Q110_I111del MEK1 Inhibitor
MAP2K1 Q110_I111del MEK inhibitor (Pan)
MAP2K1 I204T MEK1 Inhibitor
MAP2K1 T28I MEK1 Inhibitor
MAP2K1 P105_I107delinsL MEK1 Inhibitor
MAP2K1 K57N MEK1 Inhibitor
MAP2K1 S123T MEK1 Inhibitor
MAP2K1 R108_N109del MEK1 Inhibitor
MAP2K1 D67N MEK inhibitor (Pan)
MAP2K1 F53_Q58del MEK inhibitor (Pan)
MAP2K1 R47Q MEK inhibitor (Pan)
MAP2K1 P105_I107delinsL MEK inhibitor (Pan)
MAP2K1 Y134C MEK1 Inhibitor
MAP2K1 act mut MEK inhibitor (Pan)
MAP2K1 E144K MEK inhibitor (Pan)
MAP2K1 I103_K104del MEK1 Inhibitor
MAP2K1 I112_R113del MEK1 Inhibitor
MAP2K1 D67N MEK1 Inhibitor
MAP2K1 P105_A106del MEK1 Inhibitor
MAP2K1 F53_Q58del MEK1 Inhibitor
MAP2K1 I204T MEK inhibitor (Pan)
MAP2K1 D65N MEK1 Inhibitor
MAP2K1 K59del MEK1 Inhibitor
MAP2K1 V60M MEK inhibitor (Pan)
MAP2K1 A106_I107del MEK1 Inhibitor
MAP2K1 Q56_V60del MEK inhibitor (Pan)
MAP2K1 N109_Q110del MEK1 Inhibitor
MAP2K1 G128D MEK1 Inhibitor
MAP2K1 N109_Q110del MEK inhibitor (Pan)
MAP2K1 F53S MEK1 Inhibitor
MAP2K1 E203K MEK inhibitor (Pan)
MAP2K1 R49L MEK inhibitor (Pan)
MAP2K1 P306H MEK inhibitor (Pan)
MAP2K1 F129L MEK1 Inhibitor
MAP2K1 F129L MEK inhibitor (Pan)
MAP2K1 R49L MEK1 Inhibitor
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
Drug Name Trade Name Synonyms Drug Classes Drug Description
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References