PROTAC-mediated Target Degradation: A Paradigm Changer in Drug Discovery?
Structural and Biophysical Principles of Degrader Ternary Complexes
Immediate and Selective Control of Protein Abundance Using the dTAG System
Developing Pharmacokinetic/Pharmacodynamic Relationships With PROTACs
New Activities of CELMoDs, Cereblon E3 Ligase-modulating Drugs
Plate-based High-throughput Cellular Degradation Assays to Identify PROTAC Molecules and Protein Degraders
PROTAC Targeting BTK for the Treatment of Ibrutinib-resistant B-cell Malignancies
An Efficient Approach Toward Drugging Undruggable Targets
E3-mediated Ubiquitin and Ubiquitin-like Protein Ligation: Mechanisms and Chemical Probes
Plant E3 Ligases as Versatile Tools for Novel Drug Development and Plant Bioengineering
Deubiquitinase Inhibitors: An Emerging Therapeutic Class
Targeting Translation Regulation for the Development of Novel Drugs
Small-molecule Targeted Degradation of RNA
About this book
Targeting protein degradation using small molecules is one of the most exciting small-molecule therapeutic strategies in decades and a rapidly growing area of research. In particular, the development of proteolysis targeting chimera (PROTACs) as potential drugs capable of recruiting target proteins to the cellular quality control machinery for elimination has opened new avenues to address traditionally ‘difficult to target’ proteins. This book provides a comprehensive overview from the leading academic and industrial experts on recent developments, scope and limitations in this dynamically growing research area; an ideal reference work for researchers in drug discovery and chemical biology as well as advanced students.