Topoisomerase Inhibitors: Classification, Mechanisms of Action and Adverse Effects


Raj Kumar (Editor)
Centre for Human Genetics and Molecular Medicine, Central University of Punjab, Bathinda, India

Sandeep Singh (Editor)
Pharmaceutical Sciences and Natural Products & Human Genetics and Molecular Medicine, Central University of Punjab, Bathinda, India

Series: Cancer Etiology, Diagnosis and Treatments
BISAC: MED071000

This book aims to assist the scientists working with the medicinal, biochemical, biophysical, genetic and pharmacological aspects of topoisomerases and their inhibitors. The book has covered various aspects of topoisomerases like classification, structural aspects, basic genetics and mutations, disease implications and cell signaling networks, which may be helpful for researchers of the field for better therapeutics. Chapter One deals with structure, functions and role and of human topoisomerase-I in cancer progression. It describes a detailed classification, mechanism of action and recent updates on the development of camptothecin and non-camptothecin derivatives, along with their Structure-Activity Relationships (SAR) as topoisomerase-I inhibitors. Chapters Two and Three cover X-ray co-crystal structures, biological functions and the significant role of topoisomerase-II isoforms in cancer. A thorough discussion on classification and various pharmacoinformatics techniques employed in delineating the binding mode of topoisomerase-II inhibitors and their mechanism of action is well presented. Chapter Four deals not only with adverse effects associated with the use of topoisomerase-I and II inhibitors, but also includes approaches to overcome them. Chapter Five discusses various disorders associated with SNPs in topoisomerases and risks associated with their pharmacogenetics. Chapter Six sheds light on interactions and cross-talks between topoisomerases and histone deacetylases, leading to their significant role in drug resistance. The work is expected to assist the scientists to selectively design dual/multi-inhibitors of topoisomerases and histone deacetylases. The authors are thankful to the reviewers, who were so kind in reviewing and making suggestions for improving this book. This book could not have been completed without their commendable efforts. (Imprint: Nova Biomedical)

Table of Contents

Table of Contents


Chapter 1. Human Topoisomerase I and Its Inhibitors: Recent Developments
Richa Minhas, Sunaina, Gulshan Bansal and Yogita Bansal

Chapter 2. Pharmacoinformatics Studies on Human Topoisomerase II: Exploring the Mechanism of Enzyme Inhibition
Neha Tripathi, Rahul Deb, Sankar K. Guchhait and Prasad V. Bharatam

Chapter 3. Targeting Human Topoisomerase-II: Opportunities in Cancer Chemotherapy
Suyog M. Amrutkar and Kiran D. Bhilare

Chapter 4. Adverse Effects of Topoisomerase Inhibitors: Limits the Dosage for Anticancer Therapy
Simrandeep Jugait, Priyanka Narwani,Aparna Areti and Ashutosh Kumar

Chapter 5. Topoisomerases Genetics and Its Associated Diseases
Gurpreet Kaur, Gaurav Joshi, Praveen Sharma, Raj Kumar and Sandeep Singh

Chapter 6. Interaction between Topoisomerases and Histone Deacetylases: Role in Cancer Progression and Therapeutic Interventions
Gaurav Joshi, Ankush Thakur, Gurpreet Kaur, Sourav Kalra, Sandeep Singh and Raj Kumar

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