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About this book:

Since the breakthrough of the PROTAC technology in 2015, targeted protein degradation has revolutionized drug discovery, enabling pharma companies to develop completely novel therapeutics. Inducing Targeted Protein Degradation is a timely guide to navigating the complexities of the subject and understanding its practical application, with an eye on expanding the druggable space.

 

In Inducing Targeted Protein Degradation, readers will find the most recent information on:

 

Cellular mechanisms of targeted protein degradation and current approaches to utilize these mechanisms for drug discovery

A comparison of different induced degradation approaches, including PROTAC, molecular glues, LYTACs and ATTECs as well as additional post translational modifications

Drug development aspects such as DMPK optimization and criteria for the selection of clinical candidates

A discussion of the potential of targeted degradation for expanding the druggable space

 

Inducing Targeted Protein Degradation will serve as a practice-oriented reference on induced protein degradation for drug discovery professionals and for researchers employing chemical biology approaches.

 

Preface -- Chapter 1 Targeted Protein Degradation - The Story So Far -- 1.1 Introduction to Targeted Protein Degradation (TPD) -- 1.1.1 What Can Be Expected from this Book? -- 1.2 Development of Targeted Protein Degradation: Chronology and Milestones -- 1.2.1 Milestone 1: Early Monovalent Protein Degraders - The Surprising Biology of Fulvestrant -- 1.2.2 Milestone 2: The First PROTACs - From Peptidic Degraders to Chemical Biology Tools -- 1.2.3 Milestone 3: Improving Drug-Like Properties - SNIPERs and Peptidomimetic VHL Binders -- 1.2.4 Milestone 4: PROTACs on the Rise - Small-Molecule Degraders Achieve in vivo PoC -- 1.2.5 Milestone 5: Sticking It to the Man! Molecular Glues -- 1.2.6 Milestone 6: Human After All - TPD in Clinical Trials -- 1.2.7 Milestone 7: Beyond the Proteasome - Inducing Proximity to Modulate Protein Levels -- 1.2.7.1 Is TPD Just the Beginning? Bifunctional Modulators ofPost-transcriptional Modification -- 1.3 Conclusion and Outlook -- References -- Chapter 2 Cellular Principles of Targeted Protein Degradation -- 2.1 Basic Principles of Targeting Substrates to the Proteasome and Lysosomes -- 2.1.1 Ubiquitin-Proteasome System (UPS) -- 2.1.2 Lysosomal Targeting -- 2.2 Targeted Protein Degradation from the Cytosol and the Nucleus -- 2.2.1 Targeting to the Proteasome -- 2.2.1.1 Regulatory Target Recruitment -- 2.2.1.2 Target Engagement by the Ubiquitination Machinery -- 2.2.1.3 Engaging the Proteasome -- 2.2.2 Targeting to Lysosomes -- 2.3 Targeted Degradation from Membrane-Enclosed Organelles and the Extracellular Space -- 2.3.1 Degradation from the Plasma Membrane (PM) and the Extracellular Space -- 2.3.1.1 Internalization at the PM and Endosomal Sorting -- 2.3.1.2 Ubiquitination at the PM -- 2.3.2 Degradation from the Endoplasmic Reticulum (ER).