Protein Kinases in Drug Discovery
- 1st Edition, Volume 124 - February 22, 2021
- Imprint: Academic Press
- Editor: Rossen Donev
- Language: English
- Hardback ISBN:9 7 8 - 0 - 3 2 3 - 8 5 3 1 3 - 2
- eBook ISBN:9 7 8 - 0 - 3 2 3 - 8 5 3 1 4 - 9
Protein Kinases in Drug Discovery, Volume 124 discusses the latest information on protein kinases and how they modify other proteins by chemically adding phosphate groups to them.… Read more
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Request a sales quoteProtein Kinases in Drug Discovery, Volume 124 discusses the latest information on protein kinases and how they modify other proteins by chemically adding phosphate groups to them. New chapters in this release include Transport Proteins and AMPs: Implications in Human Disease, Protein kinase CK2 inhibition as a pharmacological strategy, Emerging role of Protein kinase in diabetes mellitus: From Mechanism to therapy, Dual Roles of ATP-binding site in Protein Kinases: Orthosteric inhibition and Allosteric Regulation, Pseudokinases in drug discovery and development: progress, challenges and future prospects, Comparison of knowledge-based vs. combinatorial peptide library approaches for the identification of protein kinase substrates, and more.
- Contains timely chapters written by well-renown authorities in their field
- Includes a number of high-quality illustrations, figures and tables, and targets a very wide audience of specialists, researchers and students
- Integrates experimental and computational methods for studying the role of protein kinases in different diseases, along with sections on the design of suitable protein kinase inhibitors for use in the treatment of patients
Protein chemists, molecular cell biologists, immunologists, structural biologists, computational biochemists, medical doctors, pharmacologists and other researchers working in the field of transport proteins and drug design. Medical, biology and pharmacology students specializing in this field
- Cover image
- Title page
- Table of Contents
- Copyright
- Contributors
- Chapter One: Transporter proteins and its implication in human diseases
- Abstract
- 1: Drug transport proteins
- 2: ATP-driven transporters
- Chapter Two: Protein kinase CK2 inhibition as a pharmacological strategy
- Abstract
- 1: CK2: Structural and functional features
- 2: CK2 and human diseases
- 3: CK2 inhibitors
- 4: Conclusions and perspectives
- Acknowledgments
- Chapter Three: Emerging role of protein kinases in diabetes mellitus: From mechanism to therapy
- Abstract
- 1: Introduction
- 2: Protein kinases, inflammation and insulin resistance
- 3: Therapeutic molecules targeting protein kinases to manage DM
- 4: Concluding remarks
- Acknowledgments
- Chapter Four: Dual roles of ATP-binding site in protein kinases: Orthosteric inhibition and allosteric regulation
- Abstract
- 1: Introduction
- 2: Protein kinases catalytic domain
- 3: ATP-binding site
- 4: Orthosteric inhibition
- 5: Allosteric regulation
- 6: Conclusions and perspectives
- Declaration of competing interest
- Acknowledgment
- Chapter Five: Pseudokinases: Prospects for expanding the therapeutic targets armamentarium
- Abstract
- 1: Introduction
- 2: General characteristics of pseudokinases
- 3: Classification
- 4: Structural features and relevance to human diseases
- 5: Current scenario of pseudokinase-centered therapy
- 6: Challenges in developing pseudokinase-targeted therapy
- 7: Way forward
- 8: Conclusion
- Chapter Six: Chemogenomics and bioinformatics approaches for prioritizing kinases as drug targets for neglected tropical diseases
- Abstract
- 1: Introduction
- 2: Neglected tropical diseases paradigm
- 3: Bioinformatics tools and chemogenomics approaches
- 4: Protein kinases and kinome
- 5: Drug and target repurposing
- 6: Succesfull applications of target reporpusing for discovering kinase inhibitors in NTDs and malaria
- 7: Concluding remarks and future directions
- Acknowledgments
- Chapter Seven: Targeting malaria protein kinases
- Abstract
- 1: Introduction
- 2: Antimalarial drug resistance
- 3: Protein kinases
- 4: Plasmodium kinome
- 5: Conclusions and perspectives
- Acknowledgments
- Chapter Eight: Yeast-based high-throughput screens for discovery of kinase inhibitors for neglected diseases
- Abstract
- 1: Introduction
- 2: Yeast-based drug screens
- 3: Yeast-based drug screens by substitution
- 4: Yeast-based methods for tracking the mode of action of compounds
- 5: Yeast genetic interaction network
- 6: Conclusion
- Acknowledgments
- Conflict of interest
- Chapter Nine: Structural studies of full-length receptor tyrosine kinases and their implications for drug design
- Abstract
- 1: Introduction
- 2: Mechanistic questions about intact RTKs
- 3: RTKs of interest
- 4: Structural features of full-length type III RTKs identified by EM
- 5: Mechanistic insights from comparisons between class I and III RTKs
- 6: Comparing extracellular domains (ECD)
- 7: Comparing transmembrane domains
- 8: An emerging area of RTK structural study: JM regions
- 9: Tyrosine kinase domains
- 10: Comparison to other classes of RTKs
- 11: EGFR structure and pharmacological applications
- 12: Kit and PDGFR structures and pharmacological applications
- 13: New approaches to RTK structure-based drug discovery
- 14: Conclusions
- Edition: 1
- Volume: 124
- Published: February 22, 2021
- No. of pages (Hardback): 350
- No. of pages (eBook): 350
- Imprint: Academic Press
- Language: English
- Hardback ISBN: 9780323853132
- eBook ISBN: 9780323853149
RD
Rossen Donev
Rossen Donev received his PhD degree in 1999 from the Institute of Molecular Biology, Bulgarian Academy of Sciences. He did postdoctoral training at Imperial Cancer Research Fund, UK (renamed after the merger with Cancer Research Campaign to Cancer Research UK, London Research Institute) and Cardiff University. In 2007 he was awarded a New Investigator Grant Award from the Medical Research Council (UK) to establish himself as an independent Principle Investigator. In 2010 Dr. Donev was appointed Senior Lecturer at Swansea University. In 2016 Dr. Donev joined MicroPharm Ltd (UK) where currently he is Head of Research. He has published more than 60 research papers, chaired scientific meetings and given invited plenary talks. Rossen Donev has consulted on projects related to development of treatments for neurodevelopmental disorders and cancer therapies. He serves as Editor-in-Chief of the Advances in Protein Chemistry and Structural Biology and on editorial board of several other journals. His research interests include signaling pathways involved in neuropsychiatric disorders and tumor escape from the immune system, and development of therapeutic strategies for their treatment. More recently he has focused on development of immunotherapeutics for non-systemic applications.
Affiliations and expertise
Head of Research, MicroPharm Limited, UKRead Protein Kinases in Drug Discovery on ScienceDirect