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 …

[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 …

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 …

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 …

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 …

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 …

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 …

Case study: cremophor EL-based liquid formulations as simple substitutes for amorphous solid dispersions in early preclinical in vivo studies

K Sigfridsson, X Zhang, A Llinas - Journal of Pharmacy and …, 2024 - academic.oup.com
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 …

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 …

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 …