Resistance mutation info of target
Target General Information | |||||||||||||||||||||||
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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] |
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Drug and Corresponding Resistance Mutations | |||||||||||||||||||||||
Mutation Info | Missense: D835F | ||||||||||||||||||||||
Drugs |
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Mutation Info | Missense: D835H | ||||||||||||||||||||||
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Mutation Info | Missense: D835V | ||||||||||||||||||||||
Drugs |
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Mutation Info | Missense: D835Y | ||||||||||||||||||||||
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Mutation Info | Missense: F691L | ||||||||||||||||||||||
Drugs |
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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. |
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