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RORγT small molecule inverse agonist
- Development stage
- Unknown
- Modality
- Small Molecules
- Administration
- Oral, Topical
01
Overview
RORγT (RAR-related orphan receptor gamma T) small molecule inverse agonists are a class of targeted therapies designed to inhibit the transcriptional activity of RORγT, a nuclear receptor that serves as the master regulator for T helper 17 (Th17) cell differentiation and the production of pro-inflammatory cytokines such as IL-17. By suppressing RORγT activity, these inverse agonists aim to reduce pathogenic Th17 phenotypes and are primarily investigated for the treatment of autoimmune and inflammatory diseases. While direct targeting of RORγT has historically faced challenges, recent rational design approaches have focused on developing dual-acting or tuned modulators, such as those combining RORγT inverse agonism with Liver X Receptor alpha (LXRα) agonism, to enhance anti-inflammatory efficacy and improve therapeutic profiles.
- Other names
- RORC inhibitorRORC inverse agonistRORγt inhibitorRORγt inverse agonistRORγt small molecule inverse agonist
02
Targets
FXR (Farnesoid x-activated receptor)NR1H3 (Liver X receptor beta)PXR (Pregnane X receptor)RORA (Retinoic acid-related orphan receptor alpha)RORB (RORβ / RORB)RORγtRORC (Retinoic acid receptor-related orphan receptor gamma)
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