Article

LNS8801: An enantiomerically pure agonist of the G protein-coupled estrogen receptor suitable for clinical development

2024-12-01

Abstract excerpt

Estrogen effects in tissue are mediated in part through activation of the surface estrogen receptor GPER, a broadly expressed G protein-coupled receptor that impacts a wide range of normal and pathologic processes, including metabolism, vascular health, inflammation, and cancer. A commonly used synthetic and specific GPER agonist, named G-1, antagonizes tumors by promoting cellular differentiation and enhancing tu...

Topics

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

Identifiers and source

Literature Corpus work: 38ef770b-0372-5649-804e-ba3450d08e69
DOI: 10.1101/2024.11.26.625421

Open publication

Related research

Semantic proximity does not establish scientific evidence.

Click a neighbor to travelStep 1 · 12 closest

LNS8801: An enantiomerically pure agonist of the G protein-coupled estrogen receptor suitable for clinical developmentDOI 10.1101/2024.11.26.625421Read

LNS8801: An Enantiomerically Pure Agonist of the G Protein–Coupled Estrogen Receptor Suitable for Clinical DevelopmentSemantic proximity Read

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

Advances in immune regulation of the G protein-coupled estrogen receptorSemantic proximity Read

Giredestrant reverses progesterone hypersensitivity driven by estrogen receptor mutations in breast cancer.Semantic proximity Read

A calixpyrrole derivative acts as a GPER antagonist: mechanisms and modelsSemantic proximity Read

Comparative G-Protein-Coupled Estrogen Receptor (GPER) Systems in Diabetic and Cancer Conditions: A ReviewSemantic proximity Read

Imlunestrant a next-generation oral SERD overcomes ESR1 mutant resistance in estrogen receptor-positive breast cancer.Semantic proximity Read

G Protein-Coupled Estrogen Receptor in Immune Cells and Its Role in Immune-Related DiseasesSemantic proximity Read

Estrogen biology: New insights into GPER function and clinical opportunitiesSemantic proximity Read

Signaling, physiological functions and clinical relevance of the G protein-coupled estrogen receptor GPERSemantic proximity Read

The Selective Estrogen Receptor Degrader ZN-c5 Has Broad Antitumor Activity in Wild-Type and Mutant ER-Positive Breast Cancer Models.Semantic proximity Read

Structurally Novel Antiestrogens Elicit Differential Responses from Constitutively Active Mutant Estrogen Receptors in Breast Cancer Cells and Tumors.Semantic proximity Read