Light-controlled inhibition of the circadian regulator RORγ DOI Creative Commons
Martin Reynders, Sabine Willems, Julian A. Marschner

et al.

Published: July 31, 2023

Retinoic acid receptor-related orphan receptor γ (RORγ) is a circadian regulator and has emerged as experimental therapeutic target in inflammation immunity. The cyclic temporal role of RORγ rhythms makes temporally-resolved pharmacological control this particularly intriguing. To achieve next-generation tools to study biology, we designed ligands featuring central azobenzene photoswitch, that act light-dependent inverse agonists. Structural optimization enabled efficient photocontrol over inhibition, with remarkable potency on excellent selectivity related receptors. These high-specificity photopharmaceuticals can serve high-precision the dynamic modulation signaling pathways inflammatory disorders.

Language: Английский

Light-controlled inhibition of the circadian regulator RORγ DOI Creative Commons
Martin Reynders, Sabine Willems, Julian A. Marschner

et al.

Published: July 31, 2023

Retinoic acid receptor-related orphan receptor γ (RORγ) is a circadian regulator and has emerged as experimental therapeutic target in inflammation immunity. The cyclic temporal role of RORγ rhythms makes temporally-resolved pharmacological control this particularly intriguing. To achieve next-generation tools to study biology, we designed ligands featuring central azobenzene photoswitch, that act light-dependent inverse agonists. Structural optimization enabled efficient photocontrol over inhibition, with remarkable potency on excellent selectivity related receptors. These high-specificity photopharmaceuticals can serve high-precision the dynamic modulation signaling pathways inflammatory disorders.

Language: Английский

Citations

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