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  • [Eur J Med Chem .] An orally available inverse agonist of estrogen-related receptor gamma showed expanded efficacy for the radioiodine therapy of poorly differentiated thyroid cancer

    대구경북첨단의료산업진흥재단 / 김지나, 전용현*, 진정욱*, 조성진*

  • 출처
    Eur J Med Chem
  • 등재일
    2020 Jul 14
  • 저널이슈번호
    205:112501. doi: 10.1016/j.ejmech.2020.112501. Online ahead of print.
  • 내용

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    Abstract
    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.

     

    Affiliations

    Jina Kim  1 , Hayoung Hwang  2 , Heeseok Yoon  2 , Jae-Eon Lee  3 , Ji Min Oh  4 , Hongchan An  2 , Hyun Dong Ji  4 , Seungmi Lee  5 , Eunju Cha  2 , Min Jung Ma  2 , Dong-Su Kim  2 , Su-Jeong Lee  2 , Tara Man Kadayat  2 , Jaeyoung Song  2 , Sang Woo Lee  4 , Jae-Han Jeon  6 , Keun-Gyu Park  7 , In-Kyu Lee  6 , Yong Hyun Jeon  8 , Jungwook Chin  9 , Sung Jin Cho  10
    1 New Drug Development Center, Daegu-Gyeongbuk Medical Innovation Foundation, Daegu, 41061, South Korea; College of Pharmacy, Research Institute of Pharmaceutical Sciences, Kyungpook National University, Daegu, 41566, South Korea.
    2 New Drug Development Center, Daegu-Gyeongbuk Medical Innovation Foundation, Daegu, 41061, South Korea.
    3 Department of Biomaterials Science, College of Natural Resources and Life Science/Life and Industry Convergence Research Institute, Pusan National University, Pusan, South Korea.
    4 Department of Nuclear Medicine, School of Medicine, Kyungpook National University Hospital, Daegu, South Korea.
    5 Leading-edge Research Center for Drug Discovery and Development for Diabetes and Metabolic Disease, Kyungpook National University Hospital, Daegu, 41404, South Korea.
    6 Leading-edge Research Center for Drug Discovery and Development for Diabetes and Metabolic Disease, Kyungpook National University Hospital, Daegu, 41404, South Korea; Department of Internal Medicine, School of Medicine, Kyungpook National University, Daegu, 41944, South Korea.
    7 Department of Internal Medicine, School of Medicine, Kyungpook National University, Daegu, 41944, South Korea.
    8 Laboratory Animal Center, Daegu-Gyeongbuk Medical Innovation Foundation, Daegu, 41061, South Korea. Electronic address: jeon9014@gmail.com.
    9 New Drug Development Center, Daegu-Gyeongbuk Medical Innovation Foundation, Daegu, 41061, South Korea. Electronic address: jwchin@dgmif.re.kr.
    10 New Drug Development Center, Daegu-Gyeongbuk Medical Innovation Foundation, Daegu, 41061, South Korea; Leading-edge Research Center for Drug Discovery and Development for Diabetes and Metabolic Disease, Kyungpook National University Hospital, Daegu, 41404, South Korea. Electronic address: sjcho@dgmif.re.kr.

  • 키워드
    ADMET; ATC; ERRγ inverse agonist; NIS; PDTC; X-ray crystallography.
  • 편집위원

    최근 대구경북첨단의료산업진흥재단에서 실험동물센터와 신약개발지원센터에서 탈분화갑상선암 치료제에 대한 연구논문이 발표가 되었습니다. 예전 미분화 갑상선암 치료제 후속 연구입니다.

    2020-09-01 11:10:20

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