6knr
Crystal structure of Estrogen-related receptor gamma ligand-binding domain with DN200699
Structural highlights
FunctionERR3_HUMAN Orphan receptor that acts as transcription activator in the absence of bound ligand. Binds specifically to an estrogen response element and activates reporter genes controlled by estrogen response elements (By similarity).[1] [2] [3] Publication Abstract from PubMedEstrogen-related receptor gamma (ERRgamma) is the NR3B subgroup of associated transcription factors. In this report, a new generation of a potent and selective ERRgamma 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 ERRgamma 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 ERRgamma-related cancers. An orally available inverse agonist of estrogen-related receptor gamma showed expanded efficacy for the radioiodine therapy of poorly differentiated thyroid cancer.,Kim J, Hwang H, Yoon H, Lee JE, Oh JM, An H, Ji HD, Lee S, Cha E, Ma MJ, Kim DS, Lee SJ, Kadayat TM, Song J, Lee SW, Jeon JH, Park KG, Lee IK, Jeon YH, Chin J, Cho SJ Eur J Med Chem. 2020 Jul 14;205:112501. doi: 10.1016/j.ejmech.2020.112501. PMID:32758860[4] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
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