Resistance mutation info of drug

Drug General Information
Drug ID D0T8LL
Drug Name Endocrine Therapy Drug Info
Drug Resistance Mutations
Target Name Estrogen receptor (ESR1) Target Info
Gene Name ESR1
Uniprot ID ESR1_HUMAN
Species Homo sapiens
Reference Sequence MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAY
EFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPF
LQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAK
ETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQAC
RLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKR
SKKNSLALSLTADQMVSALLDAEPPILYSEYDPTRPFSEASMMGLLTNLADRELVHMINW
AKRVPGFVDLTLHDQVHLLECAWLEILMIGLVWRSMEHPGKLLFAPNLLLDRNQGKCVEG
MVEIFDMLLATSSRFRMMNLQGEEFVCLKSIILLNSGVYTFLSSTLKSLEEKDHIHRVLD
KITDTLIHLMAKAGLTLQQQHQRLAQLLLILSHIRHMSNKGMEHLYSMKCKNVVPLYDLL
LEMLDAHRLHAPTSRGGASVEETDQSHLATAGSTSSHSLQKYYITGEAEGFPATV [Hom
o sapiens]
Targeted Disease Breast Cancer
Drug Resistance Mutations
Mutation info Missense: D538G [556097]
Mutation Prevalence 9 out of 28 patients
Mutation info Missense: Y537S [556083]
Mutation Prevalence 5 out of 270 patients
Mutation info Missense: Y537N [556083]
Mutation Prevalence 4 out of 270 patients
Mutation info Missense: Y537C [555977], [556083], [556097]
Mutation Prevalence 4 out of 28 patients
Mutation info Missense: L536Q [555976]
Mutation Prevalence 1 out of 11 patients
Mutation info Missense: L536-D538 > P [556097]
Mutation Prevalence 1 out of 28 patients
References
Ref 1572605The ChEMBL database in 2017.
Ref 555976Activating ESR1 mutations in hormone-resistant metastatic breast cancer. Nat Genet. 2013 Dec;45(12):1446-51. doi: 10.1038/ng.2823. Epub 2013 Nov 3.
Ref 555977ESR1 ligand-binding domain mutations in hormone-resistant breast cancer. Nat Genet. 2013 Dec;45(12):1439-45. doi: 10.1038/ng.2822. Epub 2013 Nov 3.
Ref 556083Droplet digital polymerase chain reaction assay for screening of ESR1 mutations in 325 breast cancer specimens. Transl Res. 2015 Dec;166(6):540-553.e2. doi: 10.1016/j.trsl.2015.09.003. Epub 2015 Sep 14.
Ref 556097Incidence and clinical significance of ESR1 mutations in heavily pretreated metastatic breast cancer patients. Onco Targets Ther. 2015 Nov 11;8:3323-8. doi: 10.2147/OTT.S92443. eCollection 2015.

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