Resistance mutation info of target

Target General Information
Target ID T89055
Target Name Dual specificity mitogen-activated protein kinase kinase 2 (MAP2K2) Target Info
Gene Name MAP2K2
Species Homo sapiens
Uniprot ID MP2K2_HUMAN
Sequence MLARRKPVLPALTINPTIAEGPSPTSEGASEANLVDLQKKLEELELDEQQKKRLEAFLTQ
KAKVGELKDDDFERISELGAGNGGVVTKVQHRPSGLIMARKLIHLEIKPAIRNQIIRELQ
VLHECNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKEAKRIPEEILGKVSIAVLRG
LAYLREKHQIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMAPERLQ
GTHYSVQSDIWSMGLSLVELAVGRYPIPPPDAKELEAIFGRPVVDGEEGEPHSISPRPRP
PGRPVSGHGMDSRPAMAIFELLDYIVNEPPPKLPNGVFTPDFQEFVNKCLIKNPAERADL
KMLTNHTFIKRSEVEEVDFAGWLCKTLRLNQPGTPTRTAV [Homo sapiens]
Drug Resistance Mutation and Corresponding Drugs
Ref 524363ClinicalTrials.gov (NCT01898585) An Open-Label Study of Zelboraf (Vemurafenib) in Patients With Braf V600 Mutation Positive Metastatic Melanoma. U.S. National Institutes of Health.
Ref 541191(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5893).
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 5326512013 FDA drug approvals. Nat Rev Drug Discov. 2014 Feb;13(2):85-9.
Ref 541630(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6495).
Ref 542850(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7935).
Ref 547954Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020671)
Ref 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
Ref 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
Mutation Info Missense: C125S
Drugs
Drug Name Trametinib Drug Info [555981]
Targeted Disease Cutaneous Melanoma
Mutation Prevalence 1 out of 4 patients
Drug Name Vemurafenib Drug Info [555981]
Targeted Disease Melanoma
Mutation Prevalence 1 out of 76 patients
Drug Name Dabrafenib Drug Info [555981], [556039]
Targeted Disease Melanoma
Mutation Prevalence 2 out of 10 patients
Mutation Info Missense: E207K
Drugs
Drug Name Dabrafenib Drug Info [556039]
Targeted Disease Melanoma
Mutation Prevalence 1 out of 10 patients
Mutation Info Missense: F57C
Drugs
Drug Name Vemurafenib Drug Info [555991]
Targeted Disease Melanoma
Mutation Prevalence 1 out of 30 patients
Mutation Info Missense: L46F
Drugs
Drug Name Trametinib Drug Info [555981]
Targeted Disease Cutaneous Melanoma
Drug Name Dabrafenib Drug Info [555981]
Targeted Disease Melanoma
Mutation Prevalence 3 out of 76 patients
Mutation Info Missense: N126D
Drugs
Drug Name Trametinib Drug Info [555981]
Targeted Disease Cutaneous Melanoma
Drug Name Dabrafenib Drug Info [555981]
Targeted Disease Melanoma
Mutation Prevalence 1 out of 76 patients
Mutation Info Missense: Q60P
Drugs
Drug Name Vemurafenib Drug Info [555982]
Targeted Disease Melanoma
Mutation Prevalence 3 out of 5 patients
Drug Name Dabrafenib Drug Info [555982], [556049]
Targeted Disease Melanoma
Mutation Prevalence 3 out of 5 patients
Drug Name Tremetinib Drug Info [555982]
Targeted Disease Cutaneous Melanoma
Mutation Prevalence 3 out of 5 patients
Mutation Info Missense: V215E
Drugs
Drug Name PD0325901 Drug Info [555849]
Targeted Disease Non-small Cell Lung Cancer
Mutation Info Missense: V35M
Drugs
Drug Name Vemurafenib Drug Info [555981]
Targeted Disease Melanoma
Mutation Prevalence 1 out of 76 patients
Drug Name Trametinib Drug Info [555981]
Targeted Disease Cutaneous Melanoma
Drug Name Dabrafenib Drug Info [555981]
Targeted Disease Melanoma
Reference
Ref 555849ERK inhibition overcomes acquired resistance to MEK inhibitors. Mol Cancer Ther. 2012 May;11(5):1143-54. doi: 10.1158/1535-7163.MCT-11-1010. Epub 2012 Mar 8.
Ref 555981The genetic landscape of clinical resistance to RAF inhibition in metastatic melanoma. Cancer Discov. 2014 Jan;4(1):94-109. doi: 10.1158/2159-8290.CD-13-0617. Epub 2013 Nov 21.
Ref 555982MAP kinase pathway alterations in BRAF-mutant melanoma patients with acquired resistance to combined RAF/MEK inhibition. Cancer Discov. 2014 Jan;4(1):61-8. doi: 10.1158/2159-8290.CD-13-0631. Epub 2013 Nov 21.
Ref 555991BRAF inhibitor resistance mechanisms in metastatic melanoma: spectrum and clinical impact. Clin Cancer Res. 2014 Apr 1;20(7):1965-77. doi: 10.1158/1078-0432.CCR-13-3122. Epub 2014 Jan 24.
Ref 556039Increased MAPK reactivation in early resistance to dabrafenib/trametinib combination therapy of BRAF-mutant metastatic melanoma. Nat Commun. 2014 Dec 2;5:5694. doi: 10.1038/ncomms6694.
Ref 556049Co-clinical assessment identifies patterns of BRAF inhibitor resistance in melanoma. J Clin Invest. 2015 Apr;125(4):1459-70. doi: 10.1172/JCI78954. Epub 2015 Feb 23.

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