Crystal structure of PPARG and NCOR2 with BAY-9683, an inverse agonist

Crystal structure of PPARG and NCOR2 with BAY-9683, an inverse agonist Descriptor: Nuclear receptor corepressor 2, Peroxisome proliferator-activated receptor gamma, ~{N}1-[[3,4-bis(fluoranyl)phenyl]methyl]-4-chloranyl-6-fluoranyl-~{N}3-(3-methyl-5-morpholin-4-yl-pyridin-2-yl)benzene-1,3-dicarboxamide Authors: Friberg, A, Orsi, D.L, Pook, E, Siegel, S, Lemke, C.T, Stellfeld, T, Puetter, V, Goldstein, J. Deposit date: 2022-10-05 Release date: 2022-12-28 Last modified: 2024-11-13 Method: X-RAY DIFFRACTION (1.72 Å) Cite: Discovery and characterization of orally bioavailable 4-chloro-6-fluoroisophthalamides as covalent PPARG inverse-agonists. Bioorg.Med.Chem., 78, 2022结合反向激动剂BAY-9683的过氧化物酶体增殖物激活受体γ（Peroxisome proliferator-activated receptor gamma，PPARG）与核受体辅阻遏物2（Nuclear receptor corepressor 2，NCOR2）晶体结构 描述物：核受体辅阻遏物2（Nuclear receptor corepressor 2，NCOR2）、过氧化物酶体增殖物激活受体γ（Peroxisome proliferator-activated receptor gamma，PPARG），以及N1-[[3,4-二氟苯基]甲基]-4-氯-6-氟-N3-(3-甲基-5-吗啉代吡啶-2-基)苯-1,3-二甲酰胺 作者：Friberg, A、Orsi, D.L、Pook, E、Siegel, S、Lemke, C.T、Stellfeld, T、Puetter, V、Goldstein, J 存档日期：2022-10-05 发布日期：2022-12-28 最后修改日期：2024-11-13 检测方法：X射线衍射（1.72 Å） 引用文献：《可口服生物利用的共价PPARG反向激动剂4-氯-6-氟间苯二甲酰胺类的发现与表征》，Bioorg.Med.Chem., 78, 2022