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":"LNS8801：一种适合临床开发的 G 蛋白偶联雌激素受体对映体纯激动剂。","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":"{\"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}","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}
LNS8801: An Enantiomerically Pure Agonist of the G Protein-Coupled Estrogen Receptor Suitable for Clinical Development.
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.
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