{"title":"Tamibarotene","authors":"","doi":"10.32388/xp52vn","DOIUrl":null,"url":null,"abstract":"An orally active, synthetic retinoid, developed to overcome all-trans retinoic acid (AT RA) resistance, with potential antineoplastic activity. As a specific retinoic acid receptor (RAR) alpha/beta agonist, tamibarotene is approximately ten times more potent than AT RA in inducing cell differentiation and apoptosis in HL-60 (human promyelocytic leukemia) cell lines in vitro. Due to a lower affinity for cellular retinoic acid binding protein (CRABP), tamibarotene may show sustained plasma levels compared to AT RA. In addition, this agent may exhibit a lower toxicity profile than AT RA, in part, due to the lack of affinity for the RAR-gamma receptor, the major retinoic acid receptor in the dermal epithelium. Qeios · Definition, February 7, 2020","PeriodicalId":85144,"journal":{"name":"Medicamentos de actualidad. Drugs of today","volume":"1 1","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2020-02-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"23","resultStr":"{\"title\":\"Tamibarotene\",\"authors\":\"\",\"doi\":\"10.32388/xp52vn\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"An orally active, synthetic retinoid, developed to overcome all-trans retinoic acid (AT RA) resistance, with potential antineoplastic activity. As a specific retinoic acid receptor (RAR) alpha/beta agonist, tamibarotene is approximately ten times more potent than AT RA in inducing cell differentiation and apoptosis in HL-60 (human promyelocytic leukemia) cell lines in vitro. Due to a lower affinity for cellular retinoic acid binding protein (CRABP), tamibarotene may show sustained plasma levels compared to AT RA. In addition, this agent may exhibit a lower toxicity profile than AT RA, in part, due to the lack of affinity for the RAR-gamma receptor, the major retinoic acid receptor in the dermal epithelium. Qeios · Definition, February 7, 2020\",\"PeriodicalId\":85144,\"journal\":{\"name\":\"Medicamentos de actualidad. Drugs of today\",\"volume\":\"1 1\",\"pages\":\"\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2020-02-07\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"23\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Medicamentos de actualidad. Drugs of today\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.32388/xp52vn\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Medicamentos de actualidad. Drugs of today","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.32388/xp52vn","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
An orally active, synthetic retinoid, developed to overcome all-trans retinoic acid (AT RA) resistance, with potential antineoplastic activity. As a specific retinoic acid receptor (RAR) alpha/beta agonist, tamibarotene is approximately ten times more potent than AT RA in inducing cell differentiation and apoptosis in HL-60 (human promyelocytic leukemia) cell lines in vitro. Due to a lower affinity for cellular retinoic acid binding protein (CRABP), tamibarotene may show sustained plasma levels compared to AT RA. In addition, this agent may exhibit a lower toxicity profile than AT RA, in part, due to the lack of affinity for the RAR-gamma receptor, the major retinoic acid receptor in the dermal epithelium. Qeios · Definition, February 7, 2020
求助内容：
应助结果提醒方式：
京公网安备 11010802042870号
