Multi-targeted Tyrosine Kinase Inhibitors in the Treatment of Cancer and Neurodegenerative Disorders
Multi-targeted Tyrosine Kinase Inhibitors in the Treatment of Cancer and Neurodegenerative Disorders

Author: Halilibrahim Ciftci

Publisher: Frontiers Media SA

Published: 2024-08-07

Total Pages: 124

ISBN-13: 2832552951

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Tyrosine kinases, which catalyze the transfer of a phosphate from ATP to a hydroxyl group of a tyrosine residue, play a plethora of roles in the regulation of diverse functions in normal cells including cell growth, motility, differentiation, and metabolism. Moreover, they are also associated with oncogenesis. Tyrosine kinases are mainly classified as receptor tyrosine kinases and non-receptor tyrosine kinases, including crucial members. Epidermal growth factor receptor (EGFR) belongs to the ERBB family of receptor tyrosine kinases along with three other closely related receptors, namely HER-2, HER-3 and HER-4. EGFR and HER-2, lead to autophosphorylation of the intracellular domain through tyrosine kinase activity and subsequent stimulation of downstream cascade that may result in proliferation, suppression of apoptosis, metastasis and angiogenesis. On the other hand, c-Abl (Abl-1) is a non-receptor tyrosine kinase, which is also essential in the regulation of several antiapoptotic and proliferative signal transduction pathways. They have mainly been identified as important targets for several types of cancer such as EGFR for non-small-cell lung cancer, glioma and colorectal cancer, HER-2 for breast and colorectal cancers and Abl for chronic myeloid leukemia. One of the major platforms that they have participated in is neurodegenerative disorders such as Parkinson’s disease, Alzheimer’s disease and amyotrophic lateral sclerosis. Aberrant activity of tyrosine kinases, in particular EGFR and Abl, have been reported to induce apoptosis and cell cycle arrest in response to a wide range of stimuli resulting in neurodegeneration and neuroinflammation. The main goal of this Research Topic is to identify new and potent effective tyrosine kinase inhibitors to be effective in cancer and neurodegenerative disorders.

Kinase Drug Discovery
Kinase Drug Discovery

Author: Richard A. Ward

Publisher: Royal Society of Chemistry

Published: 2012

Total Pages: 333

ISBN-13: 1849731748

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Kinase drug discovery remains an area of significant interest across academia and in the pharmaceutical industry. There are now around 13 FDA approved small molecule drugs which target kinases and many more compounds in various stages of clinical development. Although there have been a number of reviews/publications on kinase research, this book fills a gap in the literature by considering the current and future opportunities and challenges in targeting this important family of enzymes. The book is forward-looking and identifies a number of hot topics and key areas for kinase drug discovery over the coming years. It includes contributions from highly respected authors with a combined experience in the industry of well over 200 years, which has resulted in a book of great interest to the kinase field and across drug discovery more generally. Readers will gain a real insight into the huge challenges and opportunities which this target class has presented drug discovery scientists. The many chapters cover a wide breadth of topics, are well written and include high quality colour and black and white images. Topics covered include an outline of how medicinal chemistry has been able to specifically exploit this unique target class, along with reflections on the mechanisms of kinases inhibitors. Also covered is resistance to kinase inhibitors caused by amino acid mutations, case studies of kinase programs and reviews areas beyond protein kinases and beyond the human kinome. Also described are modern approaches to finding kinase leads and the book finishes with a reflection of how kinase drug discovery may progress over the coming years.

Protein Kinase Inhibitors as Sensitizing Agents for Chemotherapy
Protein Kinase Inhibitors as Sensitizing Agents for Chemotherapy

Author:

Publisher: Academic Press

Published: 2018-11-21

Total Pages: 294

ISBN-13: 0128127384

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Tyrosine Kinase Inhibitors as Sensitizing Agents for Chemotherapy, the fourth volume in the Cancer Sensitizing Agents for Chemotherapy Series, focuses on strategic combination therapies that involve a variety of tyrosine kinase inhibitors working together to overcome multi-drug resistance in cancer cells. The book discusses several tyrosine kinase inhibitors that have been used as sensitizing agents, such as EGFR, BCR-ABL, ALK and BRAF. In each chapter, readers will find comprehensive knowledge on the inhibitor and its action, including its biochemical, genetic, and molecular mechanisms' emphases. This book is a valuable source for oncologists, cancer researchers and those interested in applying new sensitizing agents to their research in clinical practice and in trials. - Summarizes the sensitizing role of some tyrosine kinase inhibitors in existing research - Brings recent findings in several cancer types, both experimental and clinically, with a particular emphases on underlying biochemical, genetic, and molecular mechanisms - Provides an updated and comprehensive knowledge regarding the field of combinational cancer treatment

Kinase Drug Discovery
Kinase Drug Discovery

Author: Richard A Ward

Publisher: Royal Society of Chemistry

Published: 2018-10-31

Total Pages: 430

ISBN-13: 1788015630

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Kinase inhibition remains an area of significant interest, and growing importance, across academia and the pharmaceutical industry. There are now many marketed drugs that target kinases and a significant number of compounds are currently in various stages of clinical development. This book is a forward-looking analysis of a number of key areas for kinase inhibition in the coming years and builds on the first volume. This includes topics such as screening approaches to target kinases along with different modes of inhibition such as allosteric and covalent. Novel approaches such as macrocyclisation are considered along with how the properties of kinase inhibitors have evolved, including the potential for brain penetration. Recent areas of great importance also covered include cutting edge molecular modelling approaches and the importance of kinase mutations. The evolving biology of kinases has also resulted in increased interest in the immuno-oncology area and also pseudokinases as a target family. As with the first volume the book finishes with a forward looking view of how research against this fascinating target class may evolve.

Cyclin Dependent Kinase 5 (Cdk5)
Cyclin Dependent Kinase 5 (Cdk5)

Author: Nancy Y. Ip

Publisher: Springer Science & Business Media

Published: 2009-02-28

Total Pages: 326

ISBN-13: 0387788875

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Cyclin Dependent Kinase 5 provides a comprehensive and up-to-date collection of reviews on the discovery, signaling mechanisms and functions of Cdk5, as well as the potential implication of Cdk5 in the treatment of neurodegenerative diseases. Since the identification of this unique member of the Cdk family, Cdk5 has emerged as one of the most important signal transduction mediators in the development, maintenance and fine-tuning of neuronal functions and networking. Further studies have revealed that Cdk5 is also associated with the regulation of neuronal survival during both developmental stages and in neurodegenerative diseases. These observations indicate that precise control of Cdk5 is essential for the regulation of neuronal survival. The pivotal role Cdk5 appears to play in both the regulation of neuronal survival and synaptic functions thus raises the interesting possibility that Cdk5 inhibitors may serve as therapeutic treatment for a number of neurodegenerative diseases.

HER2-Positive Breast Cancer
HER2-Positive Breast Cancer

Author: Sara Hurvitz

Publisher: Elsevier Health Sciences

Published: 2018-07-26

Total Pages: 265

ISBN-13: 0323581234

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Get a quick, expert overview of clinically-focused topics and guidelines that are relevant to testing for HER2, which contributes to approximately 25% of breast cancers today. This concise resource by Drs. Sara Hurvitz, and Kelly McCann consolidates today's available information on this growing topic into one convenient resource, making it an ideal, easy-to-digest reference for practicing and trainee oncologists. - Covers the diagnosis, treatments and targeted therapies, and management of breast cancers that are HER2-positive. - Contains sections on background and testing, advanced disease, therapeutics, and toxicity considerations. - Includes a timely section on innovative future therapies.

Contemporary Chemical Approaches for Green and Sustainable Drugs
Contemporary Chemical Approaches for Green and Sustainable Drugs

Author: Marianna Torok

Publisher: Elsevier

Published: 2022-08-26

Total Pages: 568

ISBN-13: 0128232714

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Contemporary Chemical Approaches for Green and Sustainable Drugs provides readers with the knowledge they need to integrate sustainable approaches into their work. Sections cover different aspects of green and sustainable drug development from design to disposal, including computer-aided drug design, green resourcing of drugs and drug candidates, an overview of the health concerns of pharmaceutical pollution, and a survey of potential chemical methods for its reduction. Drawing together the knowledge of a global team of experts, this book provides an inclusive overview of the chemical tools and approaches available for minimizing the negative environmental impact of current and newly developed drugs. This will be a useful guide for all academic and industrial researchers across green and sustainable chemistry, medicinal chemistry, environmental chemistry and pharmaceutical science. - Provides an integrative overview of the environmental risks of drugs and drug by products to support chemists in pre-emptively addressing these issues - Highlights the advantages of computer-aided drug design, green and sustainable sourcing, and novel methods for the production of safer, more effective drugs - Presents individual chapters written by renowned experts with diverse backgrounds - Reflects research in practice through selected case studies and extensive state-of-the-art reference sections to serve as a starting point in the design of any specialized environmentally-conscious medicinal chemistry project

Chemical Proteomics
Chemical Proteomics

Author: Gerard Drewes

Publisher: Humana Press

Published: 2011-11-08

Total Pages: 0

ISBN-13: 9781617793639

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The multidisciplinary science of chemical proteomics studies how small molecules of synthetic or natural origin bind to proteins and modulate their function. In Chemical Proteomics: Methods and Protocols, expert researchers in the field provide key techniques to investigate chemical proteomics focusing on analytical strategies, how probes are generated, techniques for the discovery of small molecule targets and the probing of target function, and small molecule ligand and drug discovery. Written in the highly successful Methods in Molecular BiologyTM series format, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and key tips on troubleshooting and avoiding known pitfalls. Authoritative and practical, Chemical Proteomics : Methods and Protocols seeks to provide methodologies that will contribute to a wider application of chemical proteomics methods in biochemical and cell biological laboratories.

Leucine-Rich Repeat Kinase 2 (LRRK2)
Leucine-Rich Repeat Kinase 2 (LRRK2)

Author: Hardy J. Rideout

Publisher: Springer

Published: 2017-03-28

Total Pages: 280

ISBN-13: 3319499696

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This is the first book to assemble the leading researchers in the field of LRRK2 biology and neurology and provide a snapshot of the current state of knowledge, encompassing all major aspects of its function and dysfunction. The contributors are experts in cell biology and physiology, neurobiology, and medicinal chemistry, bringing a multidisciplinary perspective on the gene and its role in disease. The book covers the identification of LRRK2 as a major contributor to the pathogenesis of Parkinson's Disease. It also discusses the current state of the field after a decade of research, putative normal physiological roles of LRRK2, and the various pathways that have been identified in the search for the mechanism(s) of its induction of neurodegeneration.

Protein Carbonylation
Protein Carbonylation

Author: Joaquim Ros

Publisher: John Wiley & Sons

Published: 2017-06-26

Total Pages: 416

ISBN-13: 1119074916

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Protein carbonylation has attracted the interest of a great number of laboratories since the pioneering studies at the Earl Stadtman’s lab at NIH started in early 1980s. Since then, detecting protein carbonyls in oxidative stress situations became a highly efficient tool to uncover biomarkers of oxidative damage in normal and altered cell physiology. In this book, research groups from several areas of interest have contributed to update the knowledge regarding detection, analyses and identification of carbonylated proteins and the sites where these modifications occur. The scientific community will benefit from these reviews since they deal with specific, detailed technical approaches to study formation and detection of protein carbonyls. Moreover, the biological impact of such modifications in metabolic, physiologic and structural functions and, how these alterations can help understanding the downstream effects on cell function are discussed. Oxidative stress occurs in all living organisms and affects proteins and other macromolecules: Protein carbonylation is a measure of oxidative stress in biological systems Mass spectrometry, fluorescent labelling, antibody based detection, biotinylated protein selection and other methods for detecting protein carbonyls and modification sites in proteins are described Aging, neurodegenerative diseases, obstructive pulmonary diseases, malaria, cigarette smoke, adipose tissue and its relationship with protein carbonylation Direct oxidation, glycoxidation and modifications by lipid peroxidation products as protein carbonylation pathways Emerging methods for characterizing carbonylated protein networks and affected metabolic pathways