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  • 09월 05일 17시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

제120회 대한화학회 학술발표회, 총회 및 기기전시회 안내 Insights of a Lead Optimization Study and Biological Evaluation of Novel 4-Hydroxytamoxifen Analogs as Estrogen-Related Receptor γ (ERRγ) Inverse Agonists

2017년 9월 5일 13시 55분 29초
MEDI.P-368 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
10월 19일 (목요일) 11:00~12:30
Medicinal Chemistry
저자 및
Jina Kim, Sung Jin Cho*
New Drug Development Center, Daegu Gyeongbuk Medical Innovation Foundation, Korea
Estrogen-related receptor γ (ERRγ) has recently been recognized as an attractive target for treating inflammation, cancer, and metabolic disorders. We evaluated the in vitro pharmacology as well as the absorption, distribution, metabolism, excretion, and toxicity (ADMET) properties of chemical entities that not only were shown to be highly selective agonists for ERRγ but also exhibited enhanced pharmacokinetic profile compared with GSK5182. The newly synthesized GSK5182 analogs had comparable potency to GSK5182 and were far more selective for ERRγ over the ERRα, -β, and ERα. The in vivo pharmacokinetic profiles were further evaluated, as they possessed superior in vitro ADMET profiles compared to the other compounds. Additionally, it was reported that GSK5182 facilitates the responsiveness to radioiodine therapy by modulating sodium iodide symporter (NIS) function in anaplastic thyroid cancer (ATC) cells through the ERRγ and MAP kinase signaling pathway. Thus, GSK5182 derivatives possess advantageous druglike properties and can be used to potentially treat various ERRγ-related disorders.