Jina Kim, Hayoung Hwang, Heeseok Yoon, Jae-Eon Lee, Ji Min Oh, Hongchan An, Hyun Dong Ji, Seungmi Lee, Eunju Cha, Min Jung Ma, Dong-Su Kim, Su-Jeong Lee, Tara Man Kadayat, Jaeyoung Song, Sang Woo Lee, Jae-Han Jeon, Keun-Gyu Park, In-Kyu Lee, Yong Hyun Jeon, Jungwook Chin, Sung Jin Cho
Estrogen-related receptor gamma (ERRγ) is the NR3B subgroup of associated transcription factors. In this report, a new generation of a potent and selective ERRγ inverse agonist (25) with good biocompatibility was proposed. We also explored the potential of the newly developed compound 25 in the PDTC model to expand the original indications from ATC. In addition, an X-ray crystallographic study of the ligand and ERRγ co-complex showed that 25 completely binds to the target protein (PDB 6KNR). Its medicinal chemistry, including a distinctive structural study to in vivo results, denotes that 25 may be directed towards the development of a pivotal treatment for ERRγ-related cancers...
July 14, 2020: European Journal of Medicinal Chemistry