Discovery of New non-steroidal selective glucocorticoid receptor agonists

[Display omitted] •Virtual Screening utilizing a structure-based pharmacophore model of GR-LBD.•Discovery of two 1,3-benzothiazole analogs (1 and 13) acting as genuine SEGRA.•1 and 13 transrepress a subset of NFKB targets genes in a GR-dependent manner.•New proposed binding contacts of 1 and 13 at t...

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Bibliographic Details
Published in:	The Journal of steroid biochemistry and molecular biology Vol. 186; pp. 142 - 153
Main Authors:	Potamitis, Constantinos, Siakouli, Dimitra, Papavasileiou, Konstantinos D., Boulaka, Athina, Ganou, Vassiliki, Roussaki, Marina, Calogeropoulou, Theodora, Zoumpoulakis, Panagiotis, Alexis, Michael N., Zervou, Maria, Mitsiou, Dimitra J.
Format:	Journal Article
Language:	English
Published:	England Elsevier Ltd 01-02-2019 Elsevier BV
Subjects:	Anti-Inflammatory action Antiinflammatory agents Benzothiazole Glucocorticoid receptor Glucocorticoids Inflammation MD simulations NF-κB protein Pharmacophore model Selective agonists Side effects Virtual screening Anti-Inflammatory action RU486 NF-kB Virtual screening Selective agonists GR TNF IL6 IL8 SEGRA Dex Glucocorticoid receptor MD simulations CCL2 GRE HC GC Pharmacophore model FKBP5
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