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
Mutation Info Deletion: D579
Mutation Info Missense: A829P
Mutation Info Missense: C809G
Mutation Info Missense: D716N
Mutation Info Missense: D816A
Mutation Info Missense: D816E
Mutation Info Missense: D816G
Mutation Info Missense: D816H
Mutation Info Missense: D820A
Mutation Info Missense: D820E
Mutation Info Missense: D820G
Mutation Info Missense: D820Y
Mutation Info Missense: H697Y
Mutation Info Missense: K642E
Mutation Info Missense: N680K
Mutation Info Missense: N822K
Mutation Info Missense: N822Y
Mutation Info Missense: S709F
Mutation Info Missense: S821F
Mutation Info Missense: T670E
Mutation Info Missense: T670I
Mutation Info Missense: V559I
Mutation Info Missense: V654A
Mutation Info Missense: Y578C
Mutation Info Missense: Y823D
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.