Article

Targeting Unique Ligand Binding Domain Structural Features Downregulates DKK1 in Y537S ESR1 Mutant Breast Cancer Cells

2024-06-25

Abstract excerpt

<title>Abstract</title> <p>Resistance to endocrine therapies remains a major clinical hurdle in breast cancer. Mutations to estrogen receptor alpha (ERα) arise after continued therapeutic pressure. Next generation selective estrogen receptor modulators and degraders/downregulators (SERMs and SERDs) show clinical efficacy, but responses are often non-durable. A tyrosine to serine point mutation at position 537 in...

Topics

Open a Topic to create a Post that cites this publication.

Identifiers and source

Literature Corpus work: 9cb990fc-6f6c-5218-a362-741fd330d6e9
DOI: 10.21203/rs.3.rs-4542467/v1

Open publication

Related research

Semantic proximity does not establish scientific evidence.

Click a neighbor to travelStep 1 · 12 closest

Targeting Unique Ligand Binding Domain Structural Features Downregulates DKK1 in Y537S ESR1 Mutant Breast Cancer CellsDOI 10.21203/rs.3.rs-4542467/v1Read

Targeting Unique Ligand Binding Domain Structural Features Downregulates DKK1 in Y537S ESR1 Mutant Breast Cancer CellsSemantic proximity Read

L370F and Y537S ESR1 mutations determine distinct endocrine therapy sensitivities and metabolic vulnerabilities that define new opportunities for synergistic therapeutic combinationsSemantic proximity Read

ESR1 activating mutations: From structure to clinical application.Semantic proximity Read

Estrogen Receptor Alpha Mutations, Truncations, Heterodimers, and Therapies.Semantic proximity Read

The SERM/SERD Bazedoxifene Disrupts ESR1 Helix 12 to Overcome Acquired Hormone Resistance in Breast Cancer CellsSemantic proximity Read

Decoding estrogen receptor and GPER biology: structural insights and therapeutic advances in ERα−positive breast cancerSemantic proximity Read

Activating ESR1 mutations in hormone-resistant metastatic breast cancer.Semantic proximity Read

Estrogen Receptor Alpha and ESR1 Mutations in Breast Cancer.Semantic proximity Read

Current Therapeutic Opportunities for Estrogen Receptor Mutant Breast CancerSemantic proximity Read

Kinome Reprogramming Is a Targetable Vulnerability in ESR1 Fusion-Driven Breast Cancer.Semantic proximity Read

The natural L370F ERα Variant Confers Endocrine Resistance and Sensitivity to ATRA in Metastatic Breast Cancer CellsSemantic proximity Read

Elacestrant in metastatic breast cancer: current advancements and future perspectives.Semantic proximity Read