Crystallographic landscape provides molecular insights into the modes of action of diverse ROR-γt modulators

C Suri, A Awasthi, S Asthana - Drug Discovery Today, 2022 - Elsevier
… of ROR-γt modulators, both agonist and inverse-agonists. Here, we review advances in the
development of ROR-γt … on the rich crystallography landscape for ROR-γt co-crystals that has …

Small molecule inhibitors of ROR γt: Targeting T h17 cells and other applications

JR Huh, DR Littman - European journal of immunology, 2012 - Wiley Online Library
… For example, using these small molecule compounds, we demonstrated that RORγt is
required for the maintenance of IL-17 expression in mouse and human effector T cells. Here, we …

[HTML][HTML] Small-molecule RORγt antagonists inhibit T helper 17 cell transcriptional network by divergent mechanisms

S Xiao, N Yosef, J Yang, Y Wang, L Zhou, C Zhu, C Wu… - Immunity, 2014 - cell.com
… of three small-molecule RORγt inhibitors that potently … molecular mechanism underlying
the effect of these compounds, we characterized the direct transcriptional targets of RORγt

[HTML][HTML] Molecular mechanism of action of RORγt agonists and inverse agonists: Insights from molecular dynamics simulation

N Sun, C Yuan, X Ma, Y Wang, X Gu, W Fu - Molecules, 2018 - mdpi.com
… 1 and inverse agonist 2 bind with the RORγt-LBD, we performed molecular docking by using
the Schrodinger 3.5 software package. The co-crystal structure of RORγt-LBD (PDB code: …

Retinoic Acid Receptor-Related Orphan Receptor γt (RORγt) Agonists as Potential Small Molecule Therapeutics for Cancer Immunotherapy: Miniperspective

R Qiu, Y Wang - Journal of Medicinal Chemistry, 2018 - ACS Publications
… the reported RORγt sterol and … small molecule RORγt agonists, their structural insights, and
the common ground of their MOAs. Finally, we discuss the potential of small molecule RORγt

Structural States of RORγt: X‐ray Elucidation of Molecular Mechanisms and Binding Interactions for Natural and Synthetic Compounds

J Kallen, A Izaac, C Be, L Arista, D Orain… - …, 2017 - Wiley Online Library
insight into the molecular mechanisms that lead to agonism, antagonism, or inverse agonism.
We report new molecular mechanisms for RORγt … new mechanistic insights should prove …

Common themes emerge in the transcriptional control of T helper and developmental cell fate decisions regulated by the T‐box, GATA and ROR families

SA Miller, AS Weinmann - Immunology, 2009 - Wiley Online Library
… the molecular events that contribute to the ability of T‐bet, GATA‐3 and RORγt to define T …
unexpected insights into the molecular mechanisms utilized in T helper cell differentiation. …

[HTML][HTML] AhR–ROR-γt complex is a therapeutic target for MAP4K3/GLKhighIL-17Ahigh subpopulation of systemic lupus erythematosus

HC Chuang, YM Chen, MH Chen, WT Hung… - The FASEB …, 2019 - ncbi.nlm.nih.gov
ROR-γt Ser-489 phosphorylation and the AhR–ROR-γt complex (18), we further studied
whether ROR-γt Ser-489 phosphorylation and the AhR–ROR-γt … data showed that ROR-γt Ser-…

[HTML][HTML] Transcription factor retinoid-related orphan receptor γt: a promising target for the treatment of psoriasis

L Tang, X Yang, Y Liang, H Xie, Z Dai… - Frontiers in …, 2018 - frontiersin.org
… , we explore the small molecules that target retinoid-related orphan receptor γt (RORγt), a …
for Th17 cell differentiation, targeting RORγt via small molecular inverse agonists may be a …

The Th17 immune response is controlled by the Rel–RORγ–RORγT transcriptional axis

Q Ruan, V Kameswaran, Y Zhang, S Zheng… - Journal of Experimental …, 2011 - rupress.org
… Importantly, similar to the reported effect of RORγT, RORγ also drove the expression of
other Th17 signature molecules such as IL-17F, CCR6, IL-22, and IL-23R (Fig. 2, C and D). …