Protein Degradation with New Chemical Modalities

Successful Strategies in Drug Discovery and Chemical Biology

Edited by Hilmar Weinmann, Craig Crews

Publication date:

07 October 2020

Length of book:

359 pages

Publisher

Royal Society of Chemistry

ISBN-13: 9781839160776

BOOK DESCRIPTION
TABLE OF CONTENTS

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.

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; Structure-based PROTACs Design; Plate-Based High Throughput Cellular Degradation Assays to Identify PROTACS 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; Classes, Modes-of-action and Selection of New Modalities in Drug Discovery; Small Molecule Targeted Degradation of RNA