Inducing Targeted Protein Degradation

From Chemical Biology to Drug Discovery and Clinical Applications
1. Auflage 2023
ISBN: 978-3-527-35013-1
Verlag: Wiley-VCH GmbH

Buch, Englisch, 384 Seiten, Format (B × H): 173 mm x 248 mm, Gewicht: 884 g

Inducing Targeted Protein Degradation

Enables drug developers in academia and industry to expand the range of accessible drug targets through induced protein degradation

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.

Autoren/Hrsg.

Cromm, Philipp

Fachgebiete

• Naturwissenschaften Chemie Chemie Allgemein Pharmazeutische Chemie, Medizinische Chemie
• Naturwissenschaften Chemie Organische Chemie Biochemie
• Medizin | Veterinärmedizin Medizin | Public Health | Pharmazie | Zahnmedizin Vorklinische Medizin: Grundlagenfächer Molekulare Medizin, Zellbiologie

Inhaltsverzeichnis

Targeted Protein Degradation - The Story So Far
Cellular Principles of Targeted Protein Degradation
E3 Ubiquitin Ligases as Molecular Machines and Platforms for Drug Development
A Structural and Biophysical Perspective of Degrader Activity through Ternary Complex Formation
Computational Modeling of PROTAC Ternary Complexes and Linker Design
Molecular Glue Degraders: From Serendipity to Hunting and Design
Targeted Protein Degradation as a Therapeutic Strategy in Neurodegenerative Diseases
Insights and Future Perspectives of Covalent Protein Degraders
Extending the Degradation Toolkit - mRNA targeting as Alternative Means to Affect Protein Levels
The Future of Heterobifunctional Compounds: PROTACs and Beyond
Destruction with a Purpose: Targeted Protein Degradation in Drug Discovery
Taming the Beast: How to Optimize DMPK-PD Properties of Oral Degraders
PROTAC® Protein Degraders: Bridging the Divide from Chemical Biology Tools to Clinical Candidates

Über Autor(innen)

Philipp Cromm studied Chemistry at the Technical University Munich where he worked in the group of Horst Kessler. For his master's thesis he spent time with David J. Craik at the Institute for Molecular Bioscience and received his PhD under guidance of Herbert Waldmann at the Max-Planck-Institute for Molecular Physiology. Thereafter, he carried out postdoctoral studies in the group of Craig Crews at Yale University working on targeted protein degradation. In 2018 Philipp joined Bayer AG as a Medicinal Chemist.