Details

Inducing Targeted Protein Degradation

From Chemical Biology to Drug Discovery and Clinical Applications
1. Aufl.

von: Philipp Cromm
133,99 €
Verlag:	Wiley-VCH
Format:	PDF
Veröffentl.:	09.11.2022
ISBN/EAN:	9783527350179
Sprache:	englisch
Anzahl Seiten:	384

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Beschreibungen

Titelbeschreibung

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: <ul><li>Cellular mechanisms of targeted protein degradation and current approaches to utilize these mechanisms for drug discovery </li> <li>A comparison of different induced degradation approaches, including PROTAC, molecular glues, LYTACs and ATTECs as well as additional post translational modifications</li> <li>Drug development aspects such as DMPK optimization and criteria for the selection of clinical candidates</li> <li>A discussion of the potential of targeted degradation for expanding the druggable space</li></ul> 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.

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

Autorenportrait

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.

Back cover copy

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: <ul><li>Cellular mechanisms of targeted protein degradation and current approaches to utilize these mechanisms for drug discovery </li> <li>A comparison of different induced degradation approaches, including PROTAC, molecular glues, LYTACs and ATTECs as well as additional post translational modifications</li> <li>Drug development aspects such as DMPK optimization and criteria for the selection of clinical candidates</li> <li>A discussion of the potential of targeted degradation for expanding the druggable space</li></ul> 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.