Christopher A Natale, Sophia Mercado, Richard Zhuang, Cristina Aguirre-Portolés, Israel Olayide, Christopher K Arnatt, John T Seykora, Tina K Garyantes, Wayne Luke, Todd W Ridky
{"title":"LNS8801: An Enantiomerically Pure Agonist of the G Protein-Coupled Estrogen Receptor Suitable for Clinical Development.","authors":"Christopher A Natale, Sophia Mercado, Richard Zhuang, Cristina Aguirre-Portolés, Israel Olayide, Christopher K Arnatt, John T Seykora, Tina K Garyantes, Wayne Luke, Todd W Ridky","doi":"10.1158/2767-9764.CRC-24-0632","DOIUrl":null,"url":null,"abstract":"<p><strong>Significance: </strong>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.</p>","PeriodicalId":72516,"journal":{"name":"Cancer research communications","volume":" ","pages":"556-568"},"PeriodicalIF":2.0000,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11969138/pdf/","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Cancer research communications","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1158/2767-9764.CRC-24-0632","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"ONCOLOGY","Score":null,"Total":0}
引用次数: 0
Abstract
Significance: 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.