Bioisosteres of the phenyl ring: recent strategic applications in lead optimization and drug design
MAM Subbaiah, NA Meanwell - Journal of Medicinal Chemistry, 2021 - ACS Publications
The benzene moiety is the most prevalent ring system in marketed drugs, underscoring its
historic popularity in drug design either as a pharmacophore or as a scaffold that projects …
historic popularity in drug design either as a pharmacophore or as a scaffold that projects …
Retinoic acid-related orphan receptor gamma t (RORγt) inverse agonists/antagonists for the treatment of inflammatory diseases–where are we presently?
C Gege - Expert Opinion on Drug Discovery, 2021 - Taylor & Francis
Introduction: The transcription factor retinoic acid-related orphan receptor gamma t (RORγt)
has been identified as the master regulator of TH17 cell differentiation and IL-17/22 …
has been identified as the master regulator of TH17 cell differentiation and IL-17/22 …
[HTML][HTML] A comprehensive review of discovery and development of drugs discovered from 2020–2022
To fully evaluate and define the new drug molecule for its pharmacological characteristics
and toxicity profile, pre-clinical and clinical studies are conducted as part of the drug …
and toxicity profile, pre-clinical and clinical studies are conducted as part of the drug …
Agonist lock touched and untouched retinoic acid receptor-related orphan receptor-γt (RORγt) inverse agonists: classification based on the molecular mechanisms of …
Retinoic acid receptor-related orphan receptor-gamma-t (RORγt) is a potential drug target
for autoimmune diseases with a clear biological mechanism in the Th17/IL-17 pathway. The …
for autoimmune diseases with a clear biological mechanism in the Th17/IL-17 pathway. The …
[HTML][HTML] RORγ is a context-specific master regulator of cholesterol biosynthesis and an emerging therapeutic target in cancer and autoimmune diseases
Aberrant cholesterol metabolism and homeostasis in the form of elevated cholesterol
biosynthesis and dysregulated efflux and metabolism is well recognized as a major feature …
biosynthesis and dysregulated efflux and metabolism is well recognized as a major feature …
Development and therapeutic potential of allosteric retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonists for autoimmune diseases
L Lu, N Sun, Y Wang - European Journal of Medicinal Chemistry, 2023 - Elsevier
The transcription factor retinoic acid receptor-related orphan receptor γt (RORγt) is an
attractive drug target for some autoimmune diseases owing to its roles in the differentiation …
attractive drug target for some autoimmune diseases owing to its roles in the differentiation …
RORγ structural plasticity and druggability
Retinoic acid receptor-related orphan receptor γ (RORγ) is a transcription factor regulating
the expression of the pro-inflammatory cytokine IL-17 in human T helper 17 (Th17) cells …
the expression of the pro-inflammatory cytokine IL-17 in human T helper 17 (Th17) cells …
AZD0284, a potent, selective, and orally bioavailable inverse agonist of retinoic acid receptor-related orphan receptor C2
Inverse agonists of the nuclear receptor RORC2 have been widely pursued as a potential
treatment for a variety of autoimmune diseases. We have discovered a novel series of …
treatment for a variety of autoimmune diseases. We have discovered a novel series of …
Impact of indazole scaffold as antibacterial and antifungal agent
Heterocycles consisting of a nitrogen atom, Indazole, is a pungent, biological, heterocyclic,
bicyclic compound possessing electron-rich portions. Indazole is composed of two nitrogen …
bicyclic compound possessing electron-rich portions. Indazole is composed of two nitrogen …
Discovery of RORγ Allosteric Fluorescent Probes and Their Application: Fluorescence Polarization, Screening, and Bioimaging
YC Yu, ZJ Tong, XT Liang, JZ Wu, YJ Xu… - Journal of medicinal …, 2024 - ACS Publications
Retinoic acid receptor-related orphan receptor γ (RORγ) acts as a crucial transcription factor
in Th17 cells and is involved in diverse autoimmune disorders. RORγ allosteric inhibitors …
in Th17 cells and is involved in diverse autoimmune disorders. RORγ allosteric inhibitors …