LNS8801: An Enantiomerically Pure Agonist of the G Protein–Coupled Estrogen Receptor Suitable for Clinical Development
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.
Authors
- Christopher A. Natale (ORCID: https://orcid.org/0000-0003-4949-3849)
- Tina Garyantes (ORCID: https://orcid.org/0000-0002-9465-1976)
- Richard Zhuang
- Wolfgang Lüke
- John T. Seykora (ORCID: https://orcid.org/0000-0003-0383-031X)
- Cristina Aguirre‐Portolés (ORCID: https://orcid.org/0000-0001-9074-8386)
- Todd W. Ridky (ORCID: https://orcid.org/0000-0001-8482-1284)
- Christopher Kent Arnatt (ORCID: https://orcid.org/0000-0002-9445-4796)
- Sophia Mercado
- Israel Olayide
Institutions
- University of Missouri–St. Louis (US)
- Elusys Therapeutics (United States) (US)
- Saint Louis University (US)
- University of Pennsylvania (US)
Publication Details
- Journal
- Cancer Research Communications
- Published
- 2025-03-11
- DOI
- https://doi.org/10.1158/2767-9764.crc-24-0632
- Citations
- 6
- Primary Topic
- Estrogen and related hormone effects
- Type
- article
- Field-Weighted Citation Impact
- 10.90