Small molecule p38 inhibitors: novel structural features and advances from 2002-2005
John Hynes1, Katerina Leftheri
1Department of Discovery Chemistry, Pharmaceutical Research Institute, Bristol-Myers Squibb, PO Box 4000, Princeton, NJ 08543-4000, USA.
Abstract:
The discovery and development of selective, efficacious, and safe small molecule p38 mitogen-activated protein kinase inhibitors for the treatment of inflammatory diseases remains the focus of many pharmaceutical research programs. Advances in small molecule p38 inhibitor design in potency and oral efficacy have been accelerated with the large number of available inhibitor-enzyme x-ray structures. These advances have allowed for the discovery of diverse sets of inhibitors with the opportunity to map inhibitor interactions and design selective inhibitors. This review covers recent compound disclosures in the patent and published literature over the last three years. Many disclosures represent new chemotypes as well as creative modifications of known structures.
More Related Videos
10:01Structure-Guided Design and Development of Novel Cyclophilin A Inhibitors and Ganoderiol-F Derivatives: An In-Silico Approach
Published on: June 23, 2026
14:34A Bilingual Computational Workflow for Identifying Potential PLK1 Inhibitors in American Sign Language and English
Published on: April 3, 2026
Related Concept Videos
G Protein-coupled Receptors
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
Structure-Activity Relationships and Drug Design
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence its...
Phosphoinositides and PIPs
Different phosphoinositides are synthesized and recruited on the cytosolic face of the plasma membrane. The localization of specific phosphoinositides concentrated in separate membrane...
Pharmacogenomics: Identification of New Drug Targets
Drug Discovery: Overview
