Target General Information
Target ID T89055
Target Name Dual specificity mitogen-activated protein kinase kinase 2 (MAP2K2)
Gene Name MAP2K2
Species Homo sapiens
UniProt ID MP2K2_HUMAN
Sequence MLARRKPVLPALTINPTIAEGPSPTSEGASEANLVDLQKKLEELELDEQQKKRLEAFLTQ
KAKVGELKDDDFERISELGAGNGGVVTKVQHRPSGLIMARKLIHLEIKPAIRNQIIRELQ
VLHECNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKEAKRIPEEILGKVSIAVLRG
LAYLREKHQIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMAPERLQ
GTHYSVQSDIWSMGLSLVELAVGRYPIPPPDAKELEAIFGRPVVDGEEGEPHSISPRPRP
PGRPVSGHGMDSRPAMAIFELLDYIVNEPPPKLPNGVFTPDFQEFVNKCLIKNPAERADL
KMLTNHTFIKRSEVEEVDFAGWLCKTLRLNQPGTPTRTAV [Homo sapiens]
Drug and Corresponding Resistance Mutations
Mutation Info Missense: C125S
Drugs
Drug Name Vemurafenib Drug Info [1]
Targeted Disease Melanoma
Mutation Prevalence 1 out of 76 patients
Drug Name Trametinib Drug Info [1]
Targeted Disease Cutaneous Melanoma
Mutation Prevalence 1 out of 4 patients
Drug Name Dabrafenib Drug Info [1], [6]
Targeted Disease Melanoma
Mutation Prevalence 2 out of 10 patients
Mutation Info Missense: E207K
Drugs
Drug Name Dabrafenib Drug Info [6]
Targeted Disease Melanoma
Mutation Prevalence 1 out of 10 patients
Mutation Info Missense: F57C
Drugs
Drug Name Vemurafenib Drug Info [3]
Targeted Disease Melanoma
Mutation Prevalence 1 out of 30 patients
Mutation Info Missense: L46F
Drugs
Drug Name Trametinib Drug Info [1]
Targeted Disease Cutaneous Melanoma
Drug Name Dabrafenib Drug Info [1]
Targeted Disease Melanoma
Mutation Prevalence 3 out of 76 patients
Mutation Info Missense: N126D
Drugs
Drug Name Trametinib Drug Info [1]
Targeted Disease Cutaneous Melanoma
Drug Name Dabrafenib Drug Info [1]
Targeted Disease Melanoma
Mutation Prevalence 1 out of 76 patients
Mutation Info Missense: Q60P
Drugs
Drug Name Vemurafenib Drug Info [2]
Targeted Disease Melanoma
Mutation Prevalence 3 out of 5 patients
Drug Name Dabrafenib Drug Info [2], [5]
Targeted Disease Melanoma
Mutation Prevalence 3 out of 5 patients
Drug Name Tremetinib Drug Info [2]
Targeted Disease Cutaneous Melanoma
Mutation Prevalence 3 out of 5 patients
Mutation Info Missense: V215E
Drugs
Drug Name PD0325901 Drug Info [4]
Targeted Disease Cancer; Non-small Cell Lung Cancer
Mutation Info Missense: V35M
Drugs
Drug Name Vemurafenib Drug Info [1]
Targeted Disease Melanoma
Mutation Prevalence 1 out of 76 patients
Drug Name Trametinib Drug Info [1]
Targeted Disease Cutaneous Melanoma
Drug Name Dabrafenib Drug Info [1]
Targeted Disease Melanoma
References
REF 1 The genetic landscape of clinical resistance to RAF inhibition in metastatic melanoma. Cancer Discov. 2014 Jan;4(1):94-109.
REF 2 MAP kinase pathway alterations in BRAF-mutant melanoma patients with acquired resistance to combined RAF/MEK inhibition. Cancer Discov. 2014 Jan;4(1):61-8.
REF 3 BRAF inhibitor resistance mechanisms in metastatic melanoma: spectrum and clinical impact. Clin Cancer Res. 2014 Apr 1;20(7):1965-77.
REF 4 ERK inhibition overcomes acquired resistance to MEK inhibitors. Mol Cancer Ther. 2012 May;11(5):1143-54.
REF 5 Co-clinical assessment identifies patterns of BRAF inhibitor resistance in melanoma. J Clin Invest. 2015 Apr;125(4):1459-70.
REF 6 Increased MAPK reactivation in early resistance to dabrafenib/trametinib combination therapy of BRAF-mutant metastatic melanoma. Nat Commun. 2014 Dec 2;5:5694.

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