Marina I. Nelen

TL;DR: Evidence is presented that 7β, 27-dihydroxycholesterol and 7α,27-OHC are RORγt agonist ligands and may serve as potential endogenous R ORγt ligands in promoting the differentiation of mouse and human CD4+ Th17 cells, and it is shown that Th17, but not Th1 cells, preferentially produce these two oxysterols.

TL;DR: The results suggest that RORα could be involved in same disease mechanisms and gene signatures identified in this report could be valuable biomarkers for tracking the pharmacodynamic effects of compounds that modulate RORγt or ROR α activities in patients.

TL;DR: The X-ray structural description of aggregation-based inhibition of a protein-protein interaction involving tumor necrosis factor α (TNFα) is presented and an ordered conglomerate of an aggregating small-molecule inhibitor (JNJ525) induces a quaternary structure switch of TNFα that inhibits the protein- protein interaction between TNF α and T NFα receptors.

TL;DR: It is shown that HTVS can be effectively employed to identify a diverse set of potent hits for each protein system even when the gold standard, high resolution structural data or ligand binding data for benchmarking, is not available.

TL;DR: The discovery and evaluation of a new class of potent and selective RORγt inverse agonists based on a thiazole core is described, suggesting potential utility in treating autoimmune and inflammatory diseases such as psoriasis.