An analysis of successful hit-to-clinical candidate pairs
DG Brown - Journal of medicinal chemistry, 2023 - ACS Publications
An analysis of 156 published clinical candidates from the Journal of Medicinal Chemistry
between 2018 and 2021 was conducted to identify lead generation strategies most …
between 2018 and 2021 was conducted to identify lead generation strategies most …
[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 …
Insight into Stereocontrol in the Asymmetric Intramolecular Allylation with a tert-Butylsulfinamide Nucleophile: Application in the Synthesis of Chiral Isoindoline-1 …
CT Hung, BS Wu, CT Chou, C Sandford… - The Journal of Organic …, 2022 - ACS Publications
The asymmetric induction afforded by a chiral sulfinyl group in a palladium/Brønsted-acid-
catalyzed intramolecular allylic amination was investigated. Predictions of the …
catalyzed intramolecular allylic amination was investigated. Predictions of the …
Discovery of the First-in-Class RORγ Covalent Inhibitors for Treatment of Castration-Resistant Prostate Cancer
W Fang, J Zheng, L Deng, Y An, D Rong… - Journal of Medicinal …, 2024 - ACS Publications
Nuclear receptor receptor-related orphan receptor γ (RORγ) is a ligand-dependent
transcription factor and has been established as a key player in castration-resistant prostate …
transcription factor and has been established as a key player in castration-resistant prostate …
Discovery and SAR of JTE-151: A Novel RORγ Inhibitor for Clinical Development
T Maeba, K Hirata, M Kotoku, N Seki… - Journal of Medicinal …, 2024 - ACS Publications
A number of RORγ inhibitors have been reported over the past decade. There were also
several examples advancing to human clinical trials, however, none of them has reached …
several examples advancing to human clinical trials, however, none of them has reached …
Think Biologically, Act Chemically: Miniperspective
MJ LaMarche - Journal of Medicinal Chemistry, 2022 - ACS Publications
A drug is a sophisticated molecule, purposely evolved, resulting from the accumulation of
knowledge learned and exploited from simpler molecules over time. Advanced molecules …
knowledge learned and exploited from simpler molecules over time. Advanced molecules …
The evolution paths of some reprehensive scaffolds of RORγt modulators, a perspective from medicinal chemistry
Z Li, T Liu, X He, C Bai - European Journal of Medicinal Chemistry, 2022 - Elsevier
The ligand binding domain (LBD) of retinoid-related orphan nuclear receptor γt (RORγt) has
been exploited as a promising target for the new small molecule therapeutics to cure …
been exploited as a promising target for the new small molecule therapeutics to cure …
Case study: cremophor EL-based liquid formulations as simple substitutes for amorphous solid dispersions in early preclinical in vivo studies
Objectives The objective of the present case study was to increase the exposure of the
poorly soluble crystalline compound A. Methods Mice received 10 mg/kg of crystalline …
poorly soluble crystalline compound A. Methods Mice received 10 mg/kg of crystalline …
Insight into Janus kinases specificity: From molecular architecture to cancer therapeutics
TH Wei, MY Lu, SH Yao, YQ Hong, J Yang… - MedComm …, 2024 - Wiley Online Library
Abstract Janus Kinases (JAKs) play a crucial role as therapeutic targets for various cancers.
However, the current JAK inhibitors (JAKi) available have limited therapeutic benefits due to …
However, the current JAK inhibitors (JAKi) available have limited therapeutic benefits due to …
1F. Retinoic acid-related orphans in GtoPdb v. 2023.1
A Jetten, HS Kang, Y Takeda - IUPHAR/BPS Guide to …, 2023 - journals.ed.ac.uk
Retinoic acid receptor-related orphan receptors (ROR, nomenclature as agreed by the
nomenclature as agreed by the NC-IUPHAR NC-IUPHAR Subcommittee on Nuclear …
nomenclature as agreed by the NC-IUPHAR NC-IUPHAR Subcommittee on Nuclear …