Target intelligence / Profile preview

Retinoic acid receptor-related orphan receptor gamma t (RORγt)

Target
RORγt
Molecular classification
Nuclear hormone receptor, Transcription factor, Receptor, NR1 subfamily
01

Overview

Retinoic acid receptor-related orphan receptor gamma t (RORγt) is a nuclear hormone receptor and transcription factor, encoded as an isoform of the RORC gene. It is a master regulator in the development and function of T helper 17 (Th17) cells, which are critical for immune responses and play key roles in autoimmune diseases. RORγt acts as a DNA-binding transcription factor, and upon ligand binding to its ligand-binding domain (LBD), undergoes conformational changes that allow recruitment of coactivators or corepressors, thereby regulating the expression of target genes. Small molecule modulators targeting the LBD have been developed for therapeutic purposes.

02

Mechanism of action

Ligand-dependent DNA-binding transcription factor recruiting coactivators or corepressors to regulate gene expression.

03

Biological functions

Immune regulationTh17 cell differentiationTranscriptional regulationLymphoid organogenesis
04

Disease associations

Autoimmune diseasesInflammationCancer
05

Safety considerations

Potential for immunosuppressionOff-target effects due to nuclear receptor family similarity

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