Design of Caspase Inhibitors as Potential Clinical Agents

ISBN-13: 9780367386573 / Angielski / Miękka / 2019 / 312 str.

Tom O'Brien; Steven D. Linton

Opis

Caspases (cysteine aspartyl proteases) represent one of the most specific protease families described to date. As caspase family members are involved in pro-inflammatory responses, inhibition of caspase activity represents a novel yet core approach to disease treatment. Design of Caspase Inhibitors as Potential Clinical Agents discusses the role of caspases in inducing cell death. It reviews recent efforts to develop small molecule inhibitors that are capable of modulating caspase activity. The text also examines the difficulties encountered in transitioning small molecule inhibitors from the lab to clinical use, and discusses how these challenges can best be overcome to allow continued progress.

Spis treści

Mammalian Caspase Activation Pathways in Apoptosis and Inflammation. Role of Caspases in Inflammation-Driven Diseases. Role of Caspases in Apoptotic-Driven Indications. Kinetics and Catalytic Activity of Caspases. Nonpeptide Small Molecule Inhibitors of Caspases. Identification of Inflammatory Caspase Inhibitors. Identification of Apoptotic Caspase Inhibitors. Discovery of a First-in-Class Apoptotic Caspase Inhibitor. Emricasan (PF-03491390/IDN-6556). Novel Approaches to Caspase Inhibitor Discovery. Therapeutic Potential for Caspase Inhibitors: Present and Future. Index.

O autorze

Tom O’Brien, Steven D. Linton