Resistance mutation info of target

Target General Information
Target ID T57700
Target Name Mast/stem cell growth factor receptor Kit (KIT) Target Info
Gene Name KIT
Species Homo sapiens
Uniprot ID KIT_HUMAN
Sequence MRGARGAWDFLCVLLLLLRVQTGSSQPSVSPGEPSPPSIHPGKSDLIVRVGDEIRLLCTD
PGFVKWTFEILDETNENKQNEWITEKAEATNTGKYTCTNKHGLSNSIYVFVRDPAKLFLV
DRSLYGKEDNDTLVRCPLTDPEVTNYSLKGCQGKPLPKDLRFIPDPKAGIMIKSVKRAYH
RLCLHCSVDQEGKSVLSEKFILKVRPAFKAVPVVSVSKASYLLREGEEFTVTCTIKDVSS
SVYSTWKRENSQTKLQEKYNSWHHGDFNYERQATLTISSARVNDSGVFMCYANNTFGSAN
VTTTLEVVDKGFINIFPMINTTVFVNDGENVDLIVEYEAFPKPEHQQWIYMNRTFTDKWE
DYPKSENESNIRYVSELHLTRLKGTEGGTYTFLVSNSDVNAAIAFNVYVNTKPEILTYDR
LVNGMLQCVAAGFPEPTIDWYFCPGTEQRCSASVLPVDVQTLNSSGPPFGKLVVQSSIDS
SAFKHNGTVECKAYNDVGKTSAYFNFAFKGNNKEQIHPHTLFTPLLIGFVIVAGMMCIIV
MILTYKYLQKPMYEVQWKVVEEINGNNYVYIDPTQLPYDHKWEFPRNRLSFGKTLGAGAF
GKVVEATAYGLIKSDAAMTVAVKMLKPSAHLTEREALMSELKVLSYLGNHMNIVNLLGAC
TIGGPTLVITEYCCYGDLLNFLRRKRDSFICSKQEDHAEAALYKNLLHSKESSCSDSTNE
YMDMKPGVSYVVPTKADKRRSVRIGSYIERDVTPAIMEDDELALDLEDLLSFSYQVAKGM
AFLASKNCIHRDLAARNILLTHGRITKICDFGLARDIKNDSNYVVKGNARLPVKWMAPES
IFNCVYTFESDVWSYGIFLWELFSLGSSPYPGMPVDSKFYKMIKEGFRMLSPEHAPAEMY
DIMKTCWDADPLKRPTFKQIVQLIEKQISESTNHIYSNLANCSPNRQKPVVDHSVRINSV
GSTASSSQPLLVHDDV [Homo sapiens]
Drug Resistance Mutation and Corresponding Drugs
Ref 536294Emerging treatments for pulmonary arterial hypertension. Expert Opin Emerg Drugs. 2006 Nov;11(4):609-19.
Ref 541030(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: 5687).
Ref 5287152006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
Ref 537114Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127.
Ref 541052(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: 5713).
Ref 468091(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: 4903).
Ref 5317832011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
Mutation Info Deletion: D579
Drugs
Drug Name Imatinib Drug Info [556058]
Targeted Disease Gastrointestinal Stromal Tumor
Mutation Prevalence 1 out of 33 patients
Mutation Info Missense: A829P
Drugs
Drug Name Imatinib Drug Info [555685]
Targeted Disease Gastrointestinal Stromal Tumor
Mutation Prevalence 2 out of 78 patients
Mutation Info Missense: C809G
Drugs
Drug Name Imatinib Drug Info [555643]
Targeted Disease Gastrointestinal Stromal Tumor
Mutation Prevalence 8 out of 10 patients in all KIT mutations
Mutation Info Missense: D716N
Drugs
Drug Name Imatinib Drug Info [555557]
Targeted Disease Gastrointestinal Stromal Tumor
Mutation Info Missense: D816A
Drugs
Drug Name Imatinib Drug Info [555685]
Targeted Disease Gastrointestinal Stromal Tumor
Mutation Prevalence 1 out of 78 patients
Mutation Info Missense: D816E
Drugs
Drug Name Imatinib Drug Info [555590], [555661]
Targeted Disease Gastrointestinal Stromal Tumor
Mutation Prevalence 14 out of 32 patients in all KIT mutations
Mutation Info Missense: D816G
Drugs
Drug Name Imatinib Drug Info [555557]
Targeted Disease Gastrointestinal Stromal Tumor
Drug Name Crizotinib Drug Info [556120]
Targeted Disease Lung Cancer
Mutation Info Missense: D816H
Drugs
Drug Name Imatinib Drug Info [555643]
Targeted Disease Gastrointestinal Stromal Tumor
Mutation Prevalence 8 out of 10 patients in all KIT mutations
Mutation Info Missense: D820A
Drugs
Drug Name Imatinib Drug Info [555607], [555685]
Targeted Disease Gastrointestinal Stromal Tumor
Mutation Prevalence 21 out of 33 patients in all KIT mutations
Mutation Info Missense: D820E
Drugs
Drug Name Imatinib Drug Info [556058]
Targeted Disease Gastrointestinal Stromal Tumor
Mutation Prevalence 3 out of 33 patients
Mutation Info Missense: D820G
Drugs
Drug Name Imatinib Drug Info [555607]
Targeted Disease Gastrointestinal Stromal Tumor
Mutation Prevalence 21 out of 33 patients in all KIT mutations
Mutation Info Missense: D820Y
Drugs
Drug Name Imatinib Drug Info [556058]
Targeted Disease Gastrointestinal Stromal Tumor
Mutation Prevalence 3 out of 33 patients
Mutation Info Missense: H697Y
Drugs
Drug Name Imatinib Drug Info [555625], [555811], [555938]
Targeted Disease Gastrointestinal Stromal Tumor
Mutation Info Missense: K642E
Drugs
Drug Name Imatinib Drug Info [555743], [556058]
Targeted Disease Gastrointestinal Stromal Tumor
Mutation Prevalence 1 out of 33 patients
Mutation Info Missense: N680K
Drugs
Drug Name Imatinib Drug Info [556058]
Targeted Disease Gastrointestinal Stromal Tumor
Mutation Prevalence 1 out of 33 patients
Mutation Info Missense: N822K
Drugs
Drug Name Imatinib Drug Info [555643]
Targeted Disease Gastrointestinal Stromal Tumor
Mutation Prevalence 8 out of 10 patients in all KIT mutations
Drug Name Sunitinib Drug Info [555799]
Targeted Disease Gastrointestinal Stromal Tumor
Mutation Info Missense: N822Y
Drugs
Drug Name Imatinib Drug Info [555607], [555672], [556058]
Targeted Disease Gastrointestinal Stromal Tumor
Mutation Prevalence 3 out of 33 patients
Mutation Info Missense: S709F
Drugs
Drug Name Imatinib Drug Info [555590]
Targeted Disease Gastrointestinal Stromal Tumor
Mutation Info Missense: S821F
Drugs
Drug Name Imatinib Drug Info [556051]
Targeted Disease Gastrointestinal Stromal Tumor
Mutation Prevalence 1 out of 3 patients
Mutation Info Missense: T670E
Drugs
Drug Name Imatinib Drug Info [555590], [556058]
Targeted Disease Gastrointestinal Stromal Tumor
Mutation Prevalence 14 out of 32 patients in all KIT mutations
Mutation Info Missense: T670I
Drugs
Drug Name Imatinib Drug Info [555685]
Targeted Disease Gastrointestinal Stromal Tumor
Mutation Prevalence 3 out of 78 patients
Mutation Info Missense: V559I
Drugs
Drug Name Imatinib Drug Info [555625], [555811], [555938]
Targeted Disease Gastrointestinal Stromal Tumor
Mutation Info Missense: V654A
Drugs
Drug Name Imatinib Drug Info [556058]
Targeted Disease Gastrointestinal Stromal Tumor
Mutation Prevalence 9 out of 33 patients
Mutation Info Missense: Y578C
Drugs
Drug Name Imatinib Drug Info [556058]
Targeted Disease Gastrointestinal Stromal Tumor
Mutation Prevalence 2 out of 33 patients
Mutation Info Missense: Y823D
Drugs
Drug Name Imatinib Drug Info [555743]
Targeted Disease Gastrointestinal Stromal Tumor
Mutation Prevalence 9 out of 32 patients
Drug Name Sunitinib Drug Info [532541]
Targeted Disease Gastrointestinal Stromal Tumor
Reference
Ref 555557Mechanisms of resistance to imatinib mesylate in gastrointestinal stromal tumors and activity of the PKC412 inhibitor against imatinib-resistant mutants. Gastroenterology. 2005 Feb;128(2):270-9.
Ref 555590Polyclonal evolution of multiple secondary KIT mutations in gastrointestinal stromal tumors under treatment with imatinib mesylate. Clin Cancer Res. 2006 Mar 15;12(6):1743-9.
Ref 555607Molecular correlates of imatinib resistance in gastrointestinal stromal tumors. J Clin Oncol. 2006 Oct 10;24(29):4764-74. Epub 2006 Sep 5.
Ref 555625Juxtamembrane-type c-kit gene mutation found in aggressive systemic mastocytosis induces imatinib-resistant constitutive KIT activation. Lab Invest. 2007 Apr;87(4):365-71. Epub 2007 Jan 29.
Ref 555643Clonal evolution of resistance to imatinib in patients with metastatic gastrointestinal stromal tumors. Clin Cancer Res. 2007 Sep 15;13(18 Pt 1):5398-405.
Ref 555661Surgical intervention following imatinib treatment in patients with advanced gastrointestinal stromal tumors (GISTs). J Surg Oncol. 2008 Jul 1;98(1):27-33. doi: 10.1002/jso.21065.
Ref 555672Heterogeneity of kinase inhibitor resistance mechanisms in GIST. J Pathol. 2008 Sep;216(1):64-74. doi: 10.1002/path.2382.
Ref 555685Primary and secondary kinase genotypes correlate with the biological and clinical activity of sunitinib in imatinib-resistant gastrointestinal stromal tumor. J Clin Oncol. 2008 Nov 20;26(33):5352-9. doi: 10.1200/JCO.2007.15.7461. Epub 2008 Oct 27.
Ref 555743Molecular mechanisms of secondary imatinib resistance in patients with gastrointestinal stromal tumors. J Cancer Res Clin Oncol. 2010 Jul;136(7):1065-71. doi: 10.1007/s00432-009-0753-7. Epub 2009 Dec 31.
Ref 555799Surgical intervention for imatinib and sunitinib-resistant gastrointestinal stromal tumors. Int J Clin Oncol. 2011 Dec;16(6):741-5. doi: 10.1007/s10147-011-0208-4. Epub 2011 Mar 12.
Ref 555811Novel, activating KIT-N822I mutation in familial cutaneous mastocytosis. Exp Hematol. 2011 Aug;39(8):859-65.e2. doi: 10.1016/j.exphem.2011.05.009. Epub 2011 May 27.
Ref 555938Secondary c-Kit mutations confer acquired resistance to RTK inhibitors in c-Kit mutant melanoma cells. Pigment Cell Melanoma Res. 2013 Jul;26(4):518-26. doi: 10.1111/pcmr.12107. Epub 2013 May 13.
Ref 532541Flumatinib, a selective inhibitor of BCR-ABL/PDGFR/KIT, effectively overcomes drug resistance of certain KIT mutants. Cancer Sci. 2014 Jan;105(1):117-25.
Ref 556051Detection of KIT and PDGFRA mutations in the plasma of patients with gastrointestinal stromal tumor. Target Oncol. 2015 Dec;10(4):597-601. doi: 10.1007/s11523-015-0361-1. Epub 2015 Mar 5.
Ref 556058Massively parallel sequencing fails to detect minor resistant subclones in tissue samples prior to tyrosine kinase inhibitor therapy. BMC Cancer. 2015 Apr 15;15:291. doi: 10.1186/s12885-015-1311-0.
Ref 556120An Activating KIT Mutation Induces Crizotinib Resistance in ROS1-Positive Lung Cancer. J Thorac Oncol. 2016 Aug;11(8):1273-81. doi: 10.1016/j.jtho.2016.04.001. Epub 2016 Apr 9.

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