Resistance mutation info of target

Target General Information
Target ID T89534
Target Name Estrogen receptor (ESR1) Target Info
Gene Name ESR1
Species Homo sapiens
Uniprot ID ESR1_HUMAN
Sequence MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAY
EFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPF
LQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAK
ETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQAC
RLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKR
SKKNSLALSLTADQMVSALLDAEPPILYSEYDPTRPFSEASMMGLLTNLADRELVHMINW
AKRVPGFVDLTLHDQVHLLECAWLEILMIGLVWRSMEHPGKLLFAPNLLLDRNQGKCVEG
MVEIFDMLLATSSRFRMMNLQGEEFVCLKSIILLNSGVYTFLSSTLKSLEEKDHIHRVLD
KITDTLIHLMAKAGLTLQQQHQRLAQLLLILSHIRHMSNKGMEHLYSMKCKNVVPLYDLL
LEMLDAHRLHAPTSRGGASVEETDQSHLATAGSTSSHSLQKYYITGEAEGFPATV [Hom
o sapiens]
Drug Resistance Mutation and Corresponding Drugs
Ref 536863Rational management of endocrine resistance in breast cancer: a comprehensive review of estrogen receptor biology, treatment options, and future directions. Cancer. 2008 Nov 1;113(9):2385-97.
Ref 538623(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: 1016).
Ref 1572605The ChEMBL database in 2017.
Mutation Info Missense: D538G
Drugs
Drug Name Endocrine Therapy Drug Info [556097]
Targeted Disease Breast Cancer
Mutation Prevalence 9 out of 28 patients
Mutation Info Missense: E380Q
Drugs
Drug Name Tamoxifen Drug Info [555976], [555977], [555988]
Targeted Disease Breast Cancer
Mutation Prevalence 11 out of 76 patients
Mutation Info Missense: L536-D538 > P
Drugs
Drug Name Endocrine Therapy Drug Info [556097]
Targeted Disease Breast Cancer
Mutation Prevalence 1 out of 28 patients
Mutation Info Missense: L536Q
Drugs
Drug Name Endocrine Therapy Drug Info [555976]
Targeted Disease Breast Cancer
Mutation Prevalence 1 out of 11 patients
Mutation Info Missense: P535H
Drugs
Drug Name Tamoxifen Drug Info [555976], [555977], [555988]
Targeted Disease Breast Cancer
Mutation Info Missense: Y537C
Drugs
Drug Name Endocrine Therapy Drug Info [555977], [556083], [556097]
Targeted Disease Breast Cancer
Mutation Prevalence 4 out of 28 patients
Mutation Info Missense: Y537N
Drugs
Drug Name Endocrine Therapy Drug Info [556083]
Targeted Disease Breast Cancer
Mutation Prevalence 4 out of 270 patients
Mutation Info Missense: Y537S
Drugs
Drug Name Endocrine Therapy Drug Info [556083]
Targeted Disease Breast Cancer
Mutation Prevalence 5 out of 270 patients
Reference
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 555988Emergence of constitutively active estrogen receptor- mutations in pretreated advanced estrogen receptor-positive breast cancer. Clin Cancer Res. 2014 Apr 1;20(7):1757-1767. doi: 10.1158/1078-0432.CCR-13-2332. Epub 2014 Jan 7.
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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