Related Experiment Video
Updated: Aug 22, 2026

Structure-Guided Design and Development of Novel Cyclophilin A Inhibitors and Ganoderiol-F Derivatives: An In-Silico Approach
Published on: June 23, 2026
The development of new bicyclic pyrazole-based cytokine synthesis inhibitors
Jennifer A Townes1, Adam Golebiowski, Michael P Clark
1Procter and Gamble Pharmaceuticals, Health Care Research Center, 8700 Mason-Montgomery Rd, Mason, OH 45040, USA. townes.ja@pg.com
Abstract:
4-Aryl-5-pyrimidyl-based cytokine synthesis inhibitors of TNF-alpha production, which contain a novel bicyclic pyrazole heterocyclic core, are described. Many of these inhibitors showed low nanomolar activity against LPS-induced TNF-alpha production in a THP-1 cell-based assay and against human p38 alpha MAP kinase in an isolated enzyme assay. The X-ray crystal structure of a bicyclic pyrazole inhibitor co-crystallized with mutated p38 (mp38) is presented.
Related Concept Videos
Inhibitors of Viral Protein Synthesis
Antiviral Nucleoside Inhibitors
Inhibition of Cdk Activity
Positive Regulator Molecules
Inhibitors of Bacterial DNA Synthesis
Production of Pharmaceuticals
