Discovery of N-(Indazol-3-yl)piperidine-4-carboxylic Acids as RORγt Allosteric Inhibitors for Autoimmune Diseases
H Zhang, BT Lapointe, N Anthony… - ACS Medicinal …, 2020 - ACS Publications
The clinical success of anti-IL-17 monoclonal antibodies (ie, Cosentyx and Taltz) has
validated Th17 pathway modulation for the treatment of autoimmune diseases. The nuclear …
validated Th17 pathway modulation for the treatment of autoimmune diseases. The nuclear …
[HTML][HTML] Small molecule inhibitors of RORγt for Th17 regulation in inflammatory and autoimmune diseases
J Zeng, M Li, Q Zhao, M Chen, L Zhao, S Wei… - Journal of …, 2023 - Elsevier
As a ligand-dependent transcription factor, retinoid-associated orphan receptor γt (RORγt)
that controls T helper (Th) 17 cell differentiation and interleukin (IL)-17 expression plays a …
that controls T helper (Th) 17 cell differentiation and interleukin (IL)-17 expression plays a …
Covalent occlusion of the RORγt ligand binding pocket allows unambiguous targeting of an allosteric site
FA Meijer, MCM van den Oetelaar… - ACS Medicinal …, 2021 - ACS Publications
The nuclear receptor RORγt is a key positive regulator in the differentiation and proliferation
of T helper 17 (Th17) cells and the production of proinflammatory cytokines like IL-17a …
of T helper 17 (Th17) cells and the production of proinflammatory cytokines like IL-17a …
Discovery of a series of pyrazinone RORγ antagonists and identification of the clinical candidate BI 730357
C Harcken, J Csengery, M Turner, L Wu… - ACS Medicinal …, 2021 - ACS Publications
The interleukin (IL)-23/T helper (Th) 17 axis plays a critical role in autoimmune diseases,
and there is an increasing number of biologic therapies that target IL-23 and IL-17. The …
and there is an increasing number of biologic therapies that target IL-23 and IL-17. The …
Retinoic acid receptor-related orphan receptor gamma-t (RORγt) inhibitors in clinical development for the treatment of autoimmune diseases: a patent review (2016 …
N Sun, H Guo, Y Wang - Expert Opinion on Therapeutic Patents, 2019 - Taylor & Francis
Introduction: RORγt is critical for the differentiation of Th17 cells and the production of IL-17.
Inhibition of RORγt is considered as a promising strategy to treat Th17-mediated …
Inhibition of RORγt is considered as a promising strategy to treat Th17-mediated …
Defining Target Engagement Required for Efficacy In Vivo at the Retinoic Acid Receptor-Related Orphan Receptor C2 (RORγt)
CW Lugar, CA Clarke, R Morphy, H Rudyk… - Journal of Medicinal …, 2021 - ACS Publications
The Th17 pathway has been implicated in autoimmune diseases. The retinoic acid receptor-
related orphan receptor C2 (RORγt) is a master regulator of Th17 cells and controls the …
related orphan receptor C2 (RORγt) is a master regulator of Th17 cells and controls the …
Discovery of 2-oxo-1, 2-dihydrobenzo [cd] indole-6-sulfonamide derivatives as new RORγ inhibitors using virtual screening, synthesis and biological evaluation
Y Zhang, X Xue, X Jin, Y Song, J Li, X Luo… - European journal of …, 2014 - Elsevier
Retinoic acid receptor-related orphan receptor γ (RORγ), a member of the nuclear hormone
receptor superfamily, is a promising therapeutic target for treating Th17-mediated …
receptor superfamily, is a promising therapeutic target for treating Th17-mediated …
Structure-Based and Property-Driven Optimization of N-Aryl Imidazoles toward Potent and Selective Oral RORγt Inhibitors
K Hoegenauer, J Kallen… - Journal of medicinal …, 2019 - ACS Publications
Retinoic acid receptor-related orphan receptor gamma-t (RORγt) is considered to be the
master transcription factor for the development of Th17 cells that produce proinflammatory …
master transcription factor for the development of Th17 cells that produce proinflammatory …
Crystallographic landscape provides molecular insights into the modes of action of diverse ROR-γt modulators
ROR-γt, the master regulator of Th-17 cells, is activated by the binding of small molecules at
its orthosteric site, followed by the recruitment of co-activators or co-repressors in the ligand …
its orthosteric site, followed by the recruitment of co-activators or co-repressors in the ligand …
Benzoxazepines Achieve Potent Suppression of IL‐17 Release in Human T‐Helper 17 (TH17) Cells through an Induced‐Fit Binding Mode to the Nuclear Receptor …
RI Olsson, Y Xue, S von Berg, A Aagaard… - …, 2016 - Wiley Online Library
RORγt, an isoform of the retinoic acid‐related orphan receptor gamma (RORc, RORγ), has
been identified as the master regulator of T‐helper 17 (TH17) cell function and development …
been identified as the master regulator of T‐helper 17 (TH17) cell function and development …