ABSTRACT Clinical success of IL-17/IL-23 pathway biologics for the treatment of moderate to severe psoriasis suggests that targeting RORγt, a master regulator for the proliferation and function of Th17 cells, could be an effective alternative. However, oral RORγ antagonists (VTP43742, TAK828) with high systemic exposure showed toxicity in phase I/II clinical trials and terminated development.Read More
Discovery of Retinoic Acid-Related Orphan Receptor γt Inverse Agonists via Docking and Negative Image-Based Screening
ABSTRACT Retinoic acid-related orphan receptor γt (RORγt) has a vital role in the differentiation of T-helper 17 (TH17) cells. Potent and specific RORγt inverse agonists are sought for treating TH17-related diseases such as psoriasis, rheumatoid arthritis, and type 1 diabetes. Here, the aim was to discover novel RORγt ligands using both standard molecular docking andRead More
Metadichol, A Novel ROR Gamma Inverse Agonist and Its Applications in Psoriasis
ABSTRACT Psoriasis affects 3% of the population worldwide, and there is no known cure. Psoriasis is associated with an increased risk of psoriatic arthritis, lymphomas, cardiovascular disease, and Crohn’s disease. Psoriasis treatments today include steroid and vitamin D3 cream, ultraviolet light, and immune system suppressing medications such as methotrexate. The T cells responsible for psoriasisRead More
RAR-related Orphan Receptor Gamma (RORγ; NR1F3)
RAR-related Orphan Receptor Gamma (RORγ; NR1F3) Product Family Product Number Product Description Technical Manual IB0400 RORγ (NR1F3) IB04001-32 Human RORγ Reporter Assay System, 3 x 32 assays in 96-well format Technical Manual IB04001 Human RORγ Reporter Assay System, 1 x 96-well format assays Technical Manual IB04002 Human RORγ Reporter Assay System, 1 x 384-well formatRead More