Target General Information
Target ID T74312
Target Name Receptor-type tyrosine-protein kinase (FLT3)
Gene Name FLT3
Species Homo sapiens
UniProt ID FLT3_HUMAN
Sequence MPALARDGGQLPLLVVFSAMIFGTITNQDLPVIKCVLINHKNNDSSVGKSSSYPMVSESP
EDLGCALRPQSSGTVYEAAAVEVDVSASITLQVLVDAPGNISCLWVFKHSSLNCQPHFDL
QNRGVVSMVILKMTETQAGEYLLFIQSEATNYTILFTVSIRNTLLYTLRRPYFRKMENQD
ALVCISESVPEPIVEWVLCDSQGESCKEESPAVVKKEEKVLHELFGTDIRCCARNELGRE
CTRLFTIDLNQTPQTTLPQLFLKVGEPLWIRCKAVHVNHGFGLTWELENKALEEGNYFEM
STYSTNRTMIRILFAFVSSVARNDTGYYTCSSSKHPSQSALVTIVEKGFINATNSSEDYE
IDQYEEFCFSVRFKAYPQIRCTWTFSRKSFPCEQKGLDNGYSISKFCNHKHQPGEYIFHA
ENDDAQFTKMFTLNIRRKPQVLAEASASQASCFSDGYPLPSWTWKKCSDKSPNCTEEITE
GVWNRKANRKVFGQWVSSSTLNMSEAIKGFLVKCCAYNSLGTSCETILLNSPGPFPFIQD
NISFYATIGVCLLFIVVLTLLICHKYKKQFRYESQLQMVQVTGSSDNEYFYVDFREYEYD
LKWEFPRENLEFGKVLGSGAFGKVMNATAYGISKTGVSIQVAVKMLKEKADSSEREALMS
ELKMMTQLGSHENIVNLLGACTLSGPIYLIFEYCCYGDLLNYLRSKREKFHRTWTEIFKE
HNFSFYPTFQSHPNSSMPGSREVQIHPDSDQISGLHGNSFHSEDEIEYENQKRLEEEEDL
NVLTFEDLLCFAYQVAKGMEFLEFKSCVHRDLAARNVLVTHGKVVKICDFGLARDIMSDS
NYVVRGNARLPVKWMAPESLFEGIYTIKSDVWSYGILLWEIFSLGVNPYPGIPVDANFYK
LIQNGFKMDQPFYATEEIYIIMQSCWAFDSRKRPSFPNLTSFLGCQLADAEEAMYQNVDG
RVSECPHTYQNRRPFSREMDLGLLSPQAQVEDS [Homo sapiens]
Drug and Corresponding Resistance Mutations
Mutation Info Missense: D835F
Drugs
Drug Name Quizartinib Drug Info [3]
Targeted Disease Acute Myeloid Leukaemia
Mutation Info Missense: D835H
Drugs
Drug Name Sorafenib Drug Info [1], [5]
Targeted Disease Acute Myeloid Leukaemia
Mutation Prevalence 4 out of 13 patients
Mutation Info Missense: D835V
Drugs
Drug Name Quizartinib Drug Info [3]
Targeted Disease Acute Myeloid Leukaemia
Mutation Info Missense: D835Y
Drugs
Drug Name Sunitinib Drug Info [1]
Targeted Disease Acute Myeloid Leukaemia; Gastrointestinal Stromal Tumor
Mutation Prevalence 1 out of 6 patients
Drug Name Quizartinib Drug Info [2], [3]
Targeted Disease Acute Myeloid Leukaemia
Drug Name Sorafenib Drug Info [5]
Targeted Disease Acute Myeloid Leukaemia
Mutation Info Missense: F691L
Drugs
Drug Name Quizartinib Drug Info [3], [4]
Targeted Disease Acute Myeloid Leukaemia
Drug Name Sorafenib Drug Info [1]
Targeted Disease Acute Myeloid Leukaemia
Mutation Prevalence 2 out of 6 patients
References
REF 1 Emergence of polyclonal FLT3 tyrosine kinase domain mutations during sequential therapy with sorafenib and sunitinib in FLT3-ITD-positive acute myeloid leukemia. Clin Cancer Res. 2013 Oct 15;19(20):5758-68.
REF 2 Selective FLT3 inhibition of FLT3-ITD+ acute myeloid leukaemia resulting in secondary D835Y mutation: a model for emerging clinical resistance patterns. Leukemia. 2012 Jul;26(7):1462-70.
REF 3 Validation of ITD mutations in FLT3 as a therapeutic target in human acute myeloid leukaemia. Nature. 2012 Apr 15;485(7397):260-3.
REF 4 The secondary FLT3-ITD F691L mutation induces resistance to AC220 in FLT3-ITD+ AML but retains in vitro sensitivity to PKC412 and Sunitinib. Leukemia. 2013 Jun;27(6):1416-8.
REF 5 Sorafenib treatment of FLT3-ITD(+) acute myeloid leukemia: favorable initial outcome and mechanisms of subsequent nonresponsiveness associated with the emergence of a D835 mutation. Blood. 2012 May 31;119(22):5133-43.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.