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| Type |
Poster Presentation |
| Area |
Medicinal Chemistry |
| Room No. |
Event Hall |
| Time |
4월 19일 (목요일) 11:00~12:30 |
| Code |
MEDI.P-615 |
| Subject |
Insights of a Lead Optimization Study and Biological Evaluation of Novel GSK5182 Analogs as Estrogen-Related Receptor γ (ERRγ) Inverse Agonists
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| Authors |
Jina Kim, Su-Jeong Lee, sugyeong Kwon, Jungwook Chin*, Sung Jin Cho*
New Drug Development Center, Daegu Gyeongbuk Medical Innovation Foundation, Korea
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| Abstract |
On the basis of the structural motifs of GSK5182, we have successfully demonstrated the synthesis of compound libraries that are more selective against ERRγ inverse agonists with improved absorption, distribution, metabolism, excretion, and toxicity (ADMET) profiles. Moreover, we have broadened the therapeutic scope of these compounds based on our findings that GSK5182 facilitates the responsiveness to radioiodine therapy by modulating sodium iodine symporter (NIS) function in anaplastic thyroid cancer (ATC) cells via ERRγ and MAP kinase signaling pathway. On the basis of these encouraging results, we have validated the most promising compound of GSK5182 analog from our previous studies for its ability to enhance NIS protein function, which is a key protein for radioiodine therapy, in ATC cells. However, we remain attentive to the development of small ERRγ ligands with much more enhanced pharmacological and ADMET profiles. |
| E-mail |
jina@dgmif.re.kr |
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121st General Meeting of the KCS