Resistance mutation info of target

Target General Information
Target ID T35486
Target Name GTPase Nras (NRAS) Target Info
Gene Name NRAS
Species Homo sapiens
Uniprot ID RASN_HUMAN
Sequence MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAG
QEEYSAMRDQYMRTGEGFLCVFAINNSKSFADINLYREQIKRVKDSDDVPMVLVGNKCDL
PTRTVDTKQAHELAKSYGIPFIETSAKTRQGVEDAFYTLVREIRQYRMKKLNSSDDGTQG
CMGLPCVVM [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 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: G12D
Drugs
Drug Name Dabrafenib Drug Info [556039]
Targeted Disease Melanoma
Mutation Prevalence 1 out of 10 patients
Mutation Info Missense: Q61H
Drugs
Drug Name Vemurafenib Drug Info [555981]
Targeted Disease Melanoma
Mutation Prevalence 1 out of 76 patients
Mutation Info Missense: Q61K
Drugs
Drug Name Dabrafenib Drug Info [555981]
Targeted Disease Melanoma
Mutation Prevalence 4 out of 76 patients
Drug Name Vemurafenib Drug Info [555781], [555981], [556067]
Targeted Disease Melanoma
Mutation Prevalence 4 out of 76 patients
Mutation Info Missense: Q61R
Drugs
Drug Name Vemurafenib Drug Info [555781], [555981]
Targeted Disease Melanoma
Mutation Prevalence 3 out of 76 patients
Drug Name Pembrolizumab Drug Info [556087]
Targeted Disease Melanoma
Mutation Prevalence 2 out of 49 patients
Reference
Ref 555781Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation. Nature. 2010 Dec 16;468(7326):973-7. doi: 10.1038/nature09626. Epub 2010 Nov 24.
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 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 556067Melanoma patient derived xenografts acquire distinct Vemurafenib resistance mechanisms. Am J Cancer Res. 2015 Mar 15;5(4):1507-18. eCollection 2015.
Ref 556087Circulating tumor DNA to monitor treatment response and detect acquired resistance in patients with metastatic melanoma. Oncotarget. 2015 Dec 8;6(39):42008-18. doi: 10.18632/oncotarget.5788.

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