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

Abstract excerpt

ABSTRACT: Estrogen effects in tissue are mediated in part through activation of the surface estrogen receptor G protein–coupled estrogen receptor (GPER), a broadly expressed G protein–coupled receptor that affects 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...

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