Abstract | BACKGROUND: METHODS:
Luciferase-GFP tagged MCF7 cells bearing wild-type, Y537S, or D538G ERα were injected into the mammary ducts of NSG mice (MIND model), which were subsequently treated with lasofoxifene or fulvestrant as single agents or in combination with palbociclib. Tumor growth and metastasis were monitored with in vivo and ex vivo luminescence imaging, terminal tumor weight measurements, and histological analysis. RESULTS: CONCLUSIONS: We report for the first time the anti- tumor activity of lasofoxifene in mouse models of endocrine therapy-resistant breast cancer. The results demonstrate the potential of using lasofoxifene as an effective therapy for women with advanced or metastatic ER+ breast cancers expressing the most common constitutively active ERα mutations.
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Authors | Muriel Lainé, Sean W Fanning, Ya-Fang Chang, Bradley Green, Marianne E Greene, Barry Komm, Justyna D Kurleto, Linda Phung, Geoffrey L Greene |
Journal | Breast cancer research : BCR
(Breast Cancer Res)
Vol. 23
Issue 1
Pg. 54
(05 12 2021)
ISSN: 1465-542X [Electronic] England |
PMID | 33980285
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Research Support, U.S. Gov't, Non-P.H.S.)
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Chemical References |
- ESR1 protein, human
- Estrogen Receptor alpha
- Piperazines
- Protein Kinase Inhibitors
- Pyridines
- Pyrrolidines
- Receptors, Estrogen
- Selective Estrogen Receptor Modulators
- Tetrahydronaphthalenes
- Fulvestrant
- Lasofoxifene
- palbociclib
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Topics |
- Animals
- Antineoplastic Combined Chemotherapy Protocols
(therapeutic use)
- Breast Neoplasms
(drug therapy, genetics, metabolism, pathology)
- Disease Models, Animal
- Estrogen Receptor alpha
(antagonists & inhibitors, chemistry, genetics)
- Female
- Fulvestrant
(therapeutic use)
- Humans
- MCF-7 Cells
- Mice
- Mutation
- Neoplasm Metastasis
(prevention & control)
- Piperazines
(therapeutic use)
- Protein Binding
- Protein Conformation
- Protein Kinase Inhibitors
(therapeutic use)
- Pyridines
(therapeutic use)
- Pyrrolidines
(chemistry, therapeutic use)
- Receptors, Estrogen
(genetics, metabolism)
- Selective Estrogen Receptor Modulators
(chemistry, therapeutic use)
- Tetrahydronaphthalenes
(chemistry, therapeutic use)
- Treatment Outcome
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