Novel selective glucocorticoid receptor agonists (SEGRAs) with a covalent warhead for long-lasting inhibition.
The synthesis and in vitro properties of six analogues of the selective glucocorticoid receptor (GR) agonist GSK866, bearing a warhead for covalent linkage to the glucocorticoid receptor, is described.
Laboratory of Medicinal Chemistry, Department of Pharmaceutical Sciences, Faculty of Pharmaceutical, Biomedical and Veterinary Sciences, Campus Drie Eiken, Building A, Universiteitsplein 1, 2610 Antwerp, Belgium.
Oksana
O
Ryabtsova
Laboratory of Medicinal Chemistry, Department of Pharmaceutical Sciences, Faculty of Pharmaceutical, Biomedical and Veterinary Sciences, Campus Drie Eiken, Building A, Universiteitsplein 1, 2610 Antwerp, Belgium.
Jurgen
J
Joossens
Laboratory of Medicinal Chemistry, Department of Pharmaceutical Sciences, Faculty of Pharmaceutical, Biomedical and Veterinary Sciences, Campus Drie Eiken, Building A, Universiteitsplein 1, 2610 Antwerp, Belgium.
Pieter
P
Van Der Veken
Laboratory of Protein Chemistry, Proteomics and Epigenetic Signaling, Department of Biomedical Sciences, Faculty of Pharmaceutical, Biomedical and Veterinary Sciences, Campus Drie Eiken, Building A, Universiteitsplein 1, 2610 Antwerp, Belgium.
Wim
W
Vanden Berghe
Laboratory of Medicinal Chemistry, Department of Pharmaceutical Sciences, Faculty of Pharmaceutical, Biomedical and Veterinary Sciences, Campus Drie Eiken, Building A, Universiteitsplein 1, 2610 Antwerp, Belgium.
Koen
K
Augustyns
Laboratory of Medicinal Chemistry, Department of Pharmaceutical Sciences, Faculty of Pharmaceutical, Biomedical and Veterinary Sciences, Campus Drie Eiken, Building A, Universiteitsplein 1, 2610 Antwerp, Belgium. Electronic address: hans.dewinter@uantwerpen.be.
Hans
H
De Winter
D001665:Binding Sites; D015195:Drug Design; D006854:Hydrocortisone / Q000378:metabolism; D007700:Kinetics; D011965:Receptors, Glucocorticoid / Q000819:agonists* / Q000378:metabolism
D011965:Receptors, Glucocorticoid; D006854:Hydrocortisone
Covalent inhibition; GSK866; Glucocorticoid receptor; Inflammation; Segra