Covalent Occlusion of the RORγt Ligand Binding Pocket Allows Unambiguous Targeting of an Allosteric Site

Femke A. Meijer,Maxime C.M. van den Oetelaar,Richard G. Doveston,Ella N. R. Sampers,Luc Brunsveld

Covalent Occlusion of the RORγt Ligand Binding Pocket Allows Unambiguous Targeting of an Allosteric Site

2021

Femke A. Meijer
Maxime C.M. van den Oetelaar
Richard G. Doveston
Ella N. R. Sampers
Luc Brunsveld

The nuclear receptor RORγt is a key positive regulator in the differentiation and proliferation of T helper 17 (Th17) cells and the production of proinflammatory cytokines like IL-17a. Dysregulatio...

Keywords:

Allosteric regulation
Regulator
Covalent bond
Ligand (biochemistry)
Cell biology
Chemistry
RAR-related orphan receptor gamma
Nuclear receptor
Proinflammatory cytokine

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