Protein Kinase Inhibitors

Protein Kinase Inhibitors

From Discovery to Therapeutics

1st Edition - May 19, 2022

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  • Editors: Md. Imtaiyaz Hassan, Saba Noor
  • Paperback ISBN: 9780323912877
  • eBook ISBN: 9780323913492

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Description

Protein Kinase Inhibitors: From Discovery to Therapeutics offers a foundational, pragmatic overview of protein kinases inhibitors and their potential role in disease modulation and treatment. Here, international experts in the field offer an integrated discussion of kinase inhibitor biology, biomarker discovery, and methods for drug design and development. After a brief overview of kinases and kinase inhibitors, subsequent chapters discuss individual kinases that are representative of the wider kinases and kinase families, including their roles in disease pathogenesis, underlying mechanisms, potential inhibitors and their modes of action for therapeutic modulation. Several potential drugs under different stages of clinical trials are discussed, including their relevance to cancer, diabetes, obesity, cardiovascular, neurological, and auto-immune and inflammatory disease, among other disorders. The book also addresses the challenges and opportunities for future kinase inhibitor development.

Key Features

  • Provides a thorough overview of kinase inhibitor biology and its role in disease progression and modulation
  • Examines protein kinase inhibitor drugs in various stages of clinical trials and development
  • Offers methods and protocols for protein kinase inhibitor research studies and drug design and development
  • Includes chapter contributions from international leaders in the field

Readership

Basic and translational researchers in biochemistry, molecular biology, cellular biology, genetics, pathology, oncology; life science researchers; biotechnologists; developmental biologists. Clinicians and graduate students in the biosciences

Table of Contents

  • Cover
  • Title page
  • Table of Contents
  • Copyright
  • Contributors
  • Preface
  • Chapter 1: Kinase inhibitors: An overview
  • Abstract
  • 1: Introduction
  • 2: Human kinome
  • 3: Kinase directed signaling networks
  • 4: Kinase as a drug target
  • 5: Kinase inhibitors
  • 6: Structural features of kinase inhibitors
  • 7: History of kinase inhibitor
  • 8: Current scenario in kinase inhibitor development
  • 9: Success stories
  • 10: Conclusion and future prospect
  • References
  • Chapter 2: Protein kinase inhibitors and cancer targeted therapy
  • Abstract
  • 1: Introduction
  • 2: Protein kinases features
  • 3: Chemical kinase inhibitor
  • 4: Natural bioactive as kinase inhibitors
  • 5: Nanomaterial-based kinase targeting
  • 6: Epilogue and perspective
  • References
  • Chapter 3: Drug discovery for cancer therapy with special reference to inhibitors of protein kinase pathway
  • Abstract
  • Acknowledgment
  • Overview
  • Topics
  • Reading outcomes
  • 1: Introduction
  • 2: Classification, structure, function, and regulation
  • 3: Oncogenic activation of protein kinase
  • 4: Kinase inhibitors
  • 5: Challenges
  • 6: Future prospects
  • 7: Summary
  • References
  • Chapter 4: An insight on PI3K/AKT/MTOR inhibitors in cancer: Opportunity and translational perspectives
  • Abstract
  • 1: Introduction
  • 2: Significance of PI3K/AKT/mTOR pathway in cancer
  • 3: Therapeutic indications of PI3K inhibitors and mTOR inhibitors available in market
  • 4: Drug development in cancer therapy: Translational perspectives
  • 5: Challenges in inhibition of PI3K/AKT/mTOR pathway
  • 6: Conclusion and future perspective
  • References
  • Chapter 5: Recent advances in the therapeutic development of ERK inhibitors
  • Abstract
  • Conflict of interests
  • 1: Introduction
  • 2: ERK family members
  • 3: ERK signaling in the cellular homeostasis
  • 4: ERK in the pathophysiology of human diseases
  • 5: Current status of ERK inhibitors
  • 6: Mechanistic insights into ERK inhibition
  • 7: Concluding remarks and future perspectives
  • References
  • Chapter 6: Emerging small-molecule inhibitors of ATM kinase targeting cancer therapy
  • Abstract
  • 1: Introduction
  • 2: Functions of ATM
  • 3: Functionally interacting partners of ATM
  • 4: Association of ATM with diseases
  • 5: Inhibitors of ATM kinase
  • 6: Clinical trials on ATM kinase inhibitors
  • 7: Conclusion and outlook
  • References
  • Chapter 7: Targeting pyruvate kinase M2 signaling for development of effective cancer therapy
  • Abstract
  • 1: Introduction
  • 2: PKM2 regulation
  • 3: PKM2 interactions in nucleus
  • 4: PKM2 as a therapeutic target in cancer
  • 5: PKM2 in cancer signaling
  • 6: Mechanism of action of PKM2 inhibitors
  • 7: PKM2 inhibitors in clinical trails
  • 8: Conclusions and future prospects
  • References
  • Chapter 8: Serum and glucocorticoid-regulated kinase 1: A potential target for anticancer therapy
  • Abstract
  • 1: Introduction
  • 2: SGK1
  • 3: SGK1 as a potential drug target
  • 4: SGK1 structure
  • 5: SGK1 inhibitors
  • 6: Conclusion and future directions
  • References
  • Chapter 9: Akt inhibitors in cancer therapy
  • Abstract
  • 1: Introduction
  • 2: Akt structure and function
  • 3: Akt is associated with malignant disease
  • 4: Akt as a target for cancer therapy
  • 5: Akt inhibitors
  • 6: Conclusions and future directions
  • References
  • Chapter 10: Aurora kinase: An emerging potential target in therapeutics
  • Abstract
  • 1: Introduction
  • 2: Aurora kinase inhibitors (AKIs)
  • 3: Association of Aurora kinases with diseases
  • 4: AK dysregulation in the presence of pathogens and related diseases
  • 5: Implications of inhibitors in the therapeutic management of disease
  • 6: Conclusion and future perspectives
  • Conflict of interest
  • References
  • Chapter 11: The retroactive and future potentials of Aurora kinases in the treatment of cancer
  • Abstract
  • 1: Introduction to Aurora kinase
  • 2: Aurora kinase signaling pathway
  • 3: Aurora-A small molecule inhibitors
  • 4: Aurora-B small molecule inhibitors
  • 5: Dual Aurora-A and Aurora-B small molecule inhibitors
  • 6: PAN Aurora kinase inhibitors (Aurora-A, Aurora-B, and Aurora-C kinases inhibitors)
  • 7: Summary and future prospects
  • References
  • Chapter 12: Targeting the altered tyrosine kinases in colorectal cancer: From inhibitors to drugs
  • Abstract
  • 1: Introduction
  • 2: Classification of protein kinase family
  • 3: Kinome databases
  • 4: Protein kinases as a therapeutic target in mCRC
  • 5: Insights into multikinase inhibitors (MKIs)
  • 6: Monoclonal antibodies as a blocker of tyrosine kinase activity
  • 7: Receptor tyrosine kinases: Targeted therapeutic approach
  • 8: Resistance to kinase inhibitors (KIs): A major problem
  • 9: Potential protein kinases for future therapeutic purposes
  • 10: Challenges and future directions
  • 11: Concluding remarks
  • References
  • Chapter 13: PTEN-induced kinase1 (PINK1): More than just mitochondrial quality control
  • Abstract
  • 1: Introduction
  • 2: Expression and subcellular localization of PINK1
  • 3: Gene structure and regulation
  • 4: Protein sequence and 3D structure
  • 5: Functional role of PINK1
  • 6: Association of PINK1 with diseases
  • 7: Therapeutic implications in cancer
  • 8: Conclusion and future prospects
  • Conflict of interests
  • References
  • Chapter 14: ROCKs as a potential drug target to combat Alzheimer's disease
  • Abstract
  • 1: Alzheimer's disease overview
  • 2: Cytotoxic necrotizing factor 1
  • 3: Rac 1 inhibitors
  • 4: NSAIDs
  • 5: Overview of ROCKS
  • 6: Functions of ROCK
  • 7: Controlling blood-brain barrier in AD through ROCKs
  • 8: Controlling neuroinflammation in AD through ROCK inhibition
  • 9: Neuroprotection and neuroregeneration of AD through ROCK inhibition
  • 10: Protection of dendritic spines in AD through ROCK inhibition
  • 11: ROCK in mouse model of AD
  • 12: Future challenges
  • 13: Conclusion
  • References
  • Chapter 15: Protein kinase inhibitors from discovery to therapeutics
  • Abstract
  • 1: Introduction
  • 2: Structures and isoforms of PDK
  • 3: Isoforms of PDK
  • 4: Expression and transcriptional regulation of PDKs and their relevance in disease therapy
  • 5: Efficacy study of PDK inhibitors
  • 6: Future of PDK inhibitors
  • References
  • Chapter 16: Polo-like kinases: An antimitotic drug target for cancer therapy
  • Abstract
  • 1: Introduction
  • 2: The PLK family
  • 3: Molecular architecture of PLK1
  • 4: Functions of PLK1
  • 5: Mechanism and regulation
  • 6: PLK1 expression and cancer
  • 7: PLK1 inhibitors
  • 8: Conclusion
  • References
  • Chapter 17: Src kinase: An attractive therapeutic target for prostate cancer
  • Abstract
  • Acknowledgment
  • 1: Introduction
  • 2: Structure and physiological functions of Src kinase
  • 3: Src kinase and signaling pathways
  • 4: Role of Src kinase in prostate cancer
  • 5: SFK inhibitors and their pharmacological effects
  • 6: Conclusions and future directions
  • References
  • Chapter 18: Kinase inhibition in Alzheimer’s disease
  • Abstract
  • 1: Introduction
  • 2: Kinases involved in tau phosphorylation
  • 3: Kinases involved in APP phosphorylation
  • 4: Implications of tau phosphorylation
  • 5: Implications of Aβ phosphorylation
  • 6: Protein kinase inhibitors in Alzheimer's disease
  • 7: Conclusion, future prospects, and challenges
  • References
  • Chapter 19: Therapeutic targeting of glycogen synthase kinase-3: Strategy to address neurodegenerative diseases
  • Abstract
  • 1: Introduction
  • 2: Structural features of GSK-3
  • 3: Association of GSK-3 with neurodegenerative diseases
  • 4: GSK-3 and cell signaling
  • 5: GSK-3 inhibitors
  • 6: GSK3 inhibitors: Clinical status
  • 7: Future prospective and challenges
  • 8: Conclusions
  • References
  • Chapter 20: Microtubule affinity regulating kinase 4: A potential drug target from cancers to neurodegenerative diseases
  • Abstract
  • Acknowledgments
  • 1: Introduction
  • 2: MARK4 in human diseases
  • 3: Structural features of MARK4 and strategies for designing MARK4 inhibitors
  • 4: Current MARK4-focused therapeutic strategies
  • 5: Conclusion and perspectives
  • References
  • Chapter 21: Receptor tyrosine kinase-like orphan receptors ROR1/2: Insights into the mechanism of action, inhibition, and therapeutic potential
  • Abstract
  • Acknowledgment
  • 1: Introduction
  • 2: Structural characteristics of ROR proteins ROR1 and ROR2
  • 3: Expression analysis and biological implications in human disease
  • 4: ROR1/2 as potential targets in human cancer
  • 5: ROR1 inhibitors
  • 6: ROR2 inhibitors
  • 7: Conclusion
  • References
  • Chapter 22: Therapeutic potential of leucine-rich repeat kinase 2 inhibitors for Parkinson's disease treatment
  • Abstract
  • Acknowledgment
  • 1: Introduction
  • 2: Domain organization in LRRK2
  • 3: LRRK2 as a modulator of signaling pathways
  • 4: Mutations in LRRK2 and their impact on PD pathogenesis
  • 5: Inhibitors of LRRK2 and their pharmacological effects
  • 6: Assays for screening LRRK2 inhibitors
  • 7: Conclusions and future directions
  • References
  • Chapter 23: Calcium calmodulin-dependent protein kinase as a potential drug target
  • Abstract
  • 1: Introduction
  • 2: Pathological role of CaMKII
  • 3: CaMKII inhibitors
  • 4: Conclusion and future perspectives
  • References
  • Chapter 24: Therapeutics of platelet-derived growth factor and signaling in different organs
  • Abstract
  • 1: Introduction
  • 2: Tyrosine kinase
  • 3: PDGF structure
  • 4: PDGF in physiology
  • 5: PDGFR signaling
  • 6: PDGF signaling in organogenesis
  • 7: Skin
  • 8: Testis
  • 9: Kidney
  • 10: Lens
  • 11: Recent advances in drugs targeting platelet-derived growth factor
  • 12: Potential inhibitors in preclinical and clinical trials for the PDGF kinases
  • 13: Conclusive remarks
  • References
  • Chapter 25: EGFRC797S mutation and fourth-generation EGFR tyrosine kinase inhibitors
  • Abstract
  • 1: Introduction
  • 2: EGFR C797S mutation
  • 3: Fourth-generation EGFR-TKIs
  • 4: In vitro activities and in vivo efficacy of next-generation EGFR-TKIs
  • 5: Clinical status of EGFR-TKIs
  • 6: Prospects and challenges
  • References
  • Further reading
  • Chapter 26: Bacterial histidine kinases as potential antibacterial drug targets
  • Abstract
  • 1: Introduction
  • 2: HKs in bacterial resistance
  • 3: HKs as potential antibacterial drug targets
  • 4: Structures and signaling mechanism of histidine kinases
  • 5: Conclusion
  • 6: Future prospects
  • References
  • Chapter 27: Bacterial protein kinases: A target to inhibit the bacterial infections
  • Abstract
  • Acknowledgment
  • 1: Introduction
  • 2: Serine/threonine protein kinases
  • 3: Protein tyrosine kinase
  • 4: Bacterial arginine kinase
  • 5: Histidine kinase
  • 6: Targeting bacterial kinases as therapeutics
  • 7: Conclusion
  • References
  • Chapter 28: Nanotechnology-based targeted delivery systems for protein kinase inhibitors in Cancer therapy
  • Abstract
  • 1: Introduction
  • 2: Nano-delivery for protein kinase inhibitors
  • 3: Conclusion
  • References
  • Index

Product details

  • No. of pages: 830
  • Language: English
  • Copyright: © Academic Press 2022
  • Published: May 19, 2022
  • Imprint: Academic Press
  • Paperback ISBN: 9780323912877
  • eBook ISBN: 9780323913492

About the Editors

Md. Imtaiyaz Hassan

Dr. Md. Imtaiyaz Hassan, Ph.D., FRSB., FRSC., is Assistant Professor at the Centre for Interdisciplinary Research in Basic Sciences, in Jamia Millia Islamia, New Delhi, India. His research focuses on and design and development of potent and selective kinase inhibitors, as well as understanding the mechanism of folding and dynamic behavior of potential drug targets. Dr. Hassan has published widely in such peer reviewed journals as the International Journal of Biological Macromolecules, Spectrochimica Acta, Scientific Reports, and the OMICS A Journal of Integrative Biology.

Affiliations and Expertise

Assistant Professor, Centre for Interdisciplinary Research in Basic Sciences, Jamia Millia Islamia, New Delhi, India

Saba Noor

Dr. Saba Noor is a Research Associate at the Centre for Interdisciplinary Research in Basic Sciences, Jamia Millia Islamia, New Delhi, India. Dr. Noor has expertise in molecular oncology, and her current research interests lie in development of kinase inhibitors for use in cancer therapeutics. She has published in such peer reviewed journals as Frontiers in Microbiology and International Journal of Biological Macromolecules, among other journals.

Affiliations and Expertise

Research Associate, Centre for Interdisciplinary Research in Basic Sciences, Jamia Millia Islamia, New Delhi, India

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