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Elsevier

PROTACs Overcome Resistance to Cancer Therapies

  • 1st Edition - January 1, 2027
  • Latest edition
  • Editor: Daohong Zhou
  • Language: English

PROTACs Overcome Resistance to Cancer Therapies explores the transformative potential of proteolysis targeting chimeras (PROTACs) in addressing one of oncology’s greatest cha… Read more

Description

PROTACs Overcome Resistance to Cancer Therapies explores the transformative potential of proteolysis targeting chimeras (PROTACs) in addressing one of oncology’s greatest challenges: drug resistance. Edited by Dr. Daohong Zhou, this volume brings together leading experts to present the latest advances in targeted protein degradation for cancer treatment. The book covers foundational principles of PROTAC design, mechanisms of action, and their advantages over traditional small molecule inhibitors. It delves into strategies for targeting undruggable proteins, overcoming resistance in various cancer types, and mitigating emerging resistance to PROTACs. Case studies include BCL-xL, KRAS, STAT3, and EGFR-targeting PROTACs, with insights into clinical translation and precision medicine. This resource equips cancer researchers, oncologists, and pharmaceutical scientists with practical guidance and cutting-edge knowledge. It serves as both a reference and a roadmap for developing next-generation therapeutics, making it essential for those advancing cancer drug discovery and translational medicine.

Key features

  • Explains the foundational principles of targeted protein degradation and highlights how PROTACs surpass traditional small molecule inhibitors in efficacy and specificity.
  • Showcases diverse applications of PROTACs in targeting undruggable proteins and resistant mutations, supported by case studies and translational research insights
  • Equips researchers with methodologies for PROTAC design, optimization, and evaluation, while addressing emerging resistance mechanisms and clinical implications

Readership

Cancer researchers, Oncologists, Pharmaceutical scientists and medicinal chemists

Table of contents

1. General Introduction of PROTACs as Novel Therapeutics for Cancer

2. Methodologies to Prepare, Optimize, and Evaluate PROTACs

3. PROTACs and Precision Medicine

4. Using PROTACs to Target BCL-2 Family Antiapoptotic Proteins to Overcome Cancer Drug Resistance

5. Estrogen Receptor (ER) PROTAC Vepdegestrant (ARV-471) for Advanced Breast Cancer Treatment

6. Using PROTACs to Target BTK Mutants to Overcome Drug Resistance

7. STAT3 PROTACs

8. KRAS PROTACs

9. Mutant-Selective Allosteric EGFR Degraders

10. MDM2 PROTACs to Overcome Drug Resistance in p53-Mutated Cancer

11. ABCB1 and PROTAC Resistance

12. Mutations of the Genes in the Ubiquitin Proteasome System and PROTAC Resistance

13. General Conclusions, Challenges and Future Perspectives

Product details

  • Edition: 1
  • Latest edition
  • Published: January 1, 2027
  • Language: English

About the editor

DZ

Daohong Zhou

Dr. Daohong Zhou is a professor at the University of Texas Health San Antonio and holds the Joe R. and Terry Lozano Long Distinguished Chair of Developmental Therapeutics. He co-directs the Center of Innovative Drug Discovery and serves as Associate Director for Drug Development at the Mays Cancer Center. With over 200 publications, Dr. Zhou is a pioneer in senolytic and cancer therapeutics research. He discovered ABT263, a dual Bcl-2/Bcl-xL inhibitor, and developed several PROTACs targeting BCL-xL and other proteins. His work led to the FDA approval of DT2216 in phase I trials and the founding of Unity Biotechnology and Dialectic Therapeutics.
Affiliations and expertise
University of Texas, USA