Current Molecular Targets of Heterocyclic Compounds for Cancer Therapy

1st Edition - April 10, 2024
Editors: Vivek Asati, Ankur Vaidya
Language: English
Paperback ISBN:
9 7 8 - 0 - 3 2 3 - 9 6 1 2 1 - 9
eBook ISBN:
9 7 8 - 0 - 3 2 3 - 9 9 6 3 2 - 7

Current Molecular Targets of Heterocyclic Compounds for Cancer Therapy discusses recently developed treatments based on molecular targets which are genetically altered in cancer ce… Read more

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Current Molecular Targets of Heterocyclic Compounds for Cancer Therapy discusses recently developed treatments based on molecular targets which are genetically altered in cancer cells and are essential for tumor development and survival. Considerable research effort has been devoted to the development of targeted drugs that inhibit the action of pathogenic kinases, and clinical studies performed so far have validated the positive effects of kinase inhibitors for cancer treatment. Each chapter discusses a molecular target, such as ALK2, ATR, CK, Src-Abl, EGFR, Fyn-Blk-Lyn, IGFs, and PAK1.

The book's chapters are written by experts who actively work on the targets to help readers fully understand how they can be used. This is a valuable resource for cancer researchers, oncologists, graduate students and members of the biomedical field who are interested in the potential of novel cancer therapies based on molecular targets.

Cover image
Title page
Table of Contents
Copyright
Dedication
Contributors
Preface
Acknowledgments
Chapter 1. Activin receptor-like kinase-2 inhibitors
1. Introduction
2. Structure and types of ALK2
3. ALK2 signal transduction
4. Physiological role of ALK2
5. Disorders associated with ALK2
6. ALK2 inhibitors
7. Conclusions
Chapter 2. Ataxia telangiectasia and Rad3-related protein inhibitors
1. Introduction
2. ATM and ATR in relation to DNA damage response
3. Structure of the ataxia telangiectasia-mutated and Rad3-related checkpoints
4. Etiological association of ATM and ATR in precipitating cancer in at patients
5. Heterocyclics used for inhibiting ATM and ATR
6. ATM and ATR inhibitors currently under clinical trial
7. Closing statement
Chapter 3. Breakpoint cluster region Abelson kinase inhibitors
1. Introduction
2. BCR-AbL
3. Conclusions
Chapter 4. Casein kinase (CK) inhibitors
1. Introduction
2. Protein kinase CK1
3. Protein kinase CK2
4. Protein kinase Fam20C
5. Conclusions
Chapter 5. Recent updates on c-Src kinase and Src-Abl nonreceptor tyrosine kinases inhibitors
1. Introduction
2. Phosphorylation and dephosphorylation: Regulation of c-Src kinase activity
3. Src-Abl: Fusion protein and leukemia connection
Chapter 6. Cyclin-dependent kinase 4 and 6 in cancer: Exploration of CDK4/6 inhibitors as anticancer agents
1. Introduction
2. Different types of CDKs
3. Regulation by CDKs in cancer
4. Structure–activity relationship for the already reported CDK 4/6 inhibitors
Chapter 7. Impact of epidermal growth factor receptors as a key clinical target against cancer
1. Introduction
2. Conclusion
Chapter 8. Cancer and insulin-like growth factor inhibitors: Recent advancements and SAR analysis
1. Introduction
2. Insulin-like growth factors
3. Involvement of IGFs/IGFR in various diseases
4. Role of IGF in cancer
5. Clinical developments for IGFs
6. Recent development targeting IGFR
7. Conclusion
Chapter 9. Mitotic kinesin spindle protein (KSP/Eg5 ATPase) inhibitors
1. Introduction
2. Kinesin spindle protein inhibitors
3. Conclusion
4. Summary and future outlook
Abbreviation
Chapter 10. p21-Activated kinase 1 inhibitors
1. Introduction
2. PAK1 structure and regulation
3. PAK1 role in cancer
4. PAK1 inhibitors
5. Conclusion
Chapter 11. p38 mitogen-activated protein kinase inhibitors
1. Introduction
2. MAPK types and signal transduction
3. FDA-approved MAPK inhibitors
4. Mechanisms of resistance
5. Therapeutic strategies to overcome MAPK resistance
6. The future of MAPK inhibitors therapeutics
7. Summary and future outlook
Chapter 12. Proviral integration site for Moloney murine leukemia virus-1 (PIM-1) kinase inhibitors
1. Introduction
2. Structure of PIM-1
3. Physiological functions of PIM-1
4. Functional relevance of PIM-1 in carcinomas
5. PIM-1 kinase inhibitors
6. Summary
Chapter 13. Rearranged during transfection (RET) inhibitors
1. Introduction
2. Aberrant activation of RET in cancer and other diseases
3. Classes of RET inhibitors
4. Mechanisms of action
5. Therapeutic applications of RET inhibitors
6. Resistance mechanisms and overcoming resistance to RET inhibitors
7. Future perspectives and challenges of RET inhibitors
8. Conclusion
Chapter 14. Serine/threonine-protein kinase B-Raf inhibitors
1. Introduction
2. Mitogen-activated protein kinases
3. RAF—RAS—MEK—ERK (MAP kinase) signaling paths
4. BRAF as therapeutic target
5. B-RAF inhibitors
6. MEK inhibitors
7. Conclusion
8. Summary and future outlook
Abbreviation
Chapter 15. Tubulin polymerization inhibitors
1. Introduction
2. Induction of tubulin assembly—binding at taxoid and laulimalide site
3. Inhibition of tubulin assembly via β-tubulin alkylation or binding with colchicine or vinca domains
4. Recent developments in tubulin polymerization inhibitors
5. Summary and future outlook
Chapter 16. Tumor necrosis factor receptor–associated protein 1 (TRAP1) inhibitors
1. Introduction
2. Role of TRAP1 in cancers
3. TNF-α and cancer
4. TRAP1 as a target of oncotherapy
5. TRAP1 inhibitors
6. Conclusion and future prospects
Chapter 17. Vascular endothelial growth factor receptors (VEGFR/PDGFR) inhibitors
1. Introduction
2. Molecular mechanisms and clinical applications of angiogenesis
3. Inhibition of VEGFR and PDGFR signaling by small molecule drugs
4. The physicochemical properties of orally effective drugs
5. Adverse effect of VEGFR/PDGFR TKIs
6. FDA-approved VEGFR/PDGFR TKIs
7. Summary and future outlook
Index

Vivek Asati

Dr. Vivek Asati presently work as Associate Professor in the Department of Pharmaceutical Chemistry, ISF College of Pharmacy, Moga (Punjab), India. He previously worked as research associate in the Department of Pharmaceutical Sciences, Dr H.S. Gour University, Sagar (MP). He completed his PhD from the Institute of Pharmaceutical Sciences, GGV, Bilaspur. He has both research and industry experience gained at several organizations. His research areas include computer-aided drug designing and synthesis of various small molecule inhibitors. Dr. Asati has published research papers, book chapters, reviews in various peer-reviewed journals and presented own works at several national and international conferences. He Guided several M Pharm and PhD students and published patent.

Affiliations and expertise

Associate Professor, Department of Pharmaceutical Chemistry, ISF College of Pharmacy, Moga (Punjab), India

Ankur Vaidya

Dr. Ankur Vaidya did his graduation, post-graduation and PhD from Dept. of Pharmaceutical Sciences, Dr. H. S. Gour University, Sagar (M.P.) in 2004, 2008 and 2013 respectively. Dr. Vaidya has a teaching and research experience of many years and is currently working as Asst. Professor in Faculty of Pharmacy UPUMS, Saifai, Etawah (U.P.) India. Dr. Ankur has a key research interest in discovery of new anticancer agents with novel targets and published dozens outstanding publications in various International journals. Dr Vaidya has credited as reviewer of international journals of repute in the field of Pharmaceutical sciences. Dr. Ankur has guided several postgraduate theses and was also the recipient of AICTE-NDF (National Doctorate Fellowship) fellowship for PhD research project. Dr. Vaidya has published nternational book chapters, one International book authored and 1 national book. Dr. Ankur has participated/presented in various National and International conferences.

Affiliations and expertise

Assistant Professor, Faculty of Pharmacy, Uttar Pradesh University of Medical Sciences, Saifai, Etawah U.P. India