2. Academic Validation
  3. LNS8801: An Enantiomerically Pure Agonist of the G Protein-Coupled Estrogen Receptor Suitable for Clinical Development

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

  • Cancer Res Commun. 2025 Apr 1;5(4):556-568. doi: 10.1158/2767-9764.CRC-24-0632.
Christopher A Natale # 1 2,  Sophia Mercado # 2,  Richard Zhuang 2,  Cristina Aguirre-Portolés 2,  Israel Olayide 3,  Christopher K Arnatt 3,  John T Seykora 2,  Tina K Garyantes 1,  Wayne Luke 1,  Todd W Ridky 2
Affiliations

Affiliations

  • 1 Linnaeus Therapeutics, Haddonfield, New Jersey.
  • 2 Department of Dermatology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, Pennsylvania.
  • 3 Department of Chemistry and Biochemistry, Saint Louis University, St. Louis, Missouri.
  • # Contributed equally.
PMID: 40066851 DOI: 10.1158/2767-9764.CRC-24-0632
Abstract

GPER is broadly expressed in human tissues and has tumor-suppressive activity. No FDA-approved agents selectively target GPER. LNS8801 is a synthetic, orally bioavailable, enantiomerically pure, GPER agonist with potent Anticancer activity in vivo. LNS8801 response is attenuated by a common germline coding variant present in roughly half of humans.

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