Next Generation Kinase Inhibitors

Next Generation Kinase Inhibitors

Author: Paul Shapiro

Publisher: Springer Nature

Published: 2020-07-14

Total Pages: 224

ISBN-13: 3030482839

DOWNLOAD EBOOK

Protein kinases are fascinating enzymes that maintain the proper function of nearly every task performed by the cells of the human body. By extracting a phosphate from the energy molecule ATP and linking it to another protein, protein kinases alter the structure and ultimate function of other proteins. In this way, protein kinases help monitor the extracellular environment and integrate signaling cues that, for the most part, are beneficial for human health and survival. However, protein kinases are often dysregulated and responsible for the initiation and progression of many types of cancers, inflammatory disorders, and other diseases. Thus, decades of research have revealed much about how protein kinases are regulated and approaches to inhibit these enzymes to treat disease. However, nearly 30 years since the identification of the first clinically beneficial small molecule protein kinase inhibitor, there are only a few examples where these drugs provide sustained and durable patient responses. The goal of this book is to provide biomedical scientists, graduate, and professional degree students insight into different approaches using small molecules to block specific protein kinase functions that promote disease.


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

DOWNLOAD EBOOK

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


Protein Kinase Inhibitors

Protein Kinase Inhibitors

Author: Md. Imtaiyaz Hassan

Publisher: Academic Press

Published: 2022-05-19

Total Pages: 832

ISBN-13: 0323913490

DOWNLOAD EBOOK

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. - 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


Kinase Drug Discovery

Kinase Drug Discovery

Author: Richard A. Ward

Publisher: Royal Society of Chemistry

Published: 2012

Total Pages: 333

ISBN-13: 1849731748

DOWNLOAD EBOOK

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 Tyrosine Kinases

Protein Tyrosine Kinases

Author: Doriano Fabbro

Publisher: Springer Science & Business Media

Published: 2007-11-13

Total Pages: 599

ISBN-13: 1592599621

DOWNLOAD EBOOK

Leading researchers, from the Novartis group that pioneered Gleevec/GlivecTM and around the world, comprehensively survey the state of the art in the drug discovery processes (bio- and chemoinformatics, structural biology, profiling, generation of resistance, etc.) aimed at generating PTK inhibitors for the treatment of various diseases, including cancer. Highlights include a discussion of the rationale and the progress made towards generating "selective" low molecular-weight kinase inhibitors; an analysis of the normal function, role in disease, and application of platelet-derived growth factor antagonists; and a summary of the factors involved in successful structure-based drug design. Additional chapters address the advantages and disadvantages of in vivo preclinical models for testing protein kinase inhibitors with antitumor activity and the utility of different methods in the drug discovery and development process for determining "on-target" vs "off-target" effects of kinase inhibitors.


Molecular Docking for Computer-Aided Drug Design

Molecular Docking for Computer-Aided Drug Design

Author: Mohane S. Coumar

Publisher: Academic Press

Published: 2021-02-17

Total Pages: 522

ISBN-13: 0128223138

DOWNLOAD EBOOK

Molecular Docking for Computer-Aided Drug Design: Fundamentals, Techniques, Resources and Applications offers in-depth coverage on the use of molecular docking for drug design. The book is divided into three main sections that cover basic techniques, tools, web servers and applications. It is an essential reference for students and researchers involved in drug design and discovery. - Covers the latest information and state-of-the-art trends in structure-based drug design methodologies - Includes case studies that complement learning - Consolidates fundamental concepts and current practice of molecular docking into one convenient resource


Cancer Immunology and Immunotherapy

Cancer Immunology and Immunotherapy

Author: Mansoor M. Amiji

Publisher: Elsevier

Published: 2021-08-27

Total Pages: 548

ISBN-13: 0128233974

DOWNLOAD EBOOK

Delivery Technologies for Immuno-Oncology: Volume 1: Delivery Strategies and Engineering Technologies in Cancer Immunotherapy examines the challenges of delivering immuno-oncology therapies. Immuno-oncology (IO) is a growing field of medicine at the interface of immunology and cancer biology leading to development of novel therapeutic approaches, such as chimeric antigen receptor T-cell (CAR-T) and immune checkpoint blockade antibodies, that are clinically approved approaches for cancer therapy. Although currently approved IO approaches have shown tremendous promise for select types of cancers, broad application of IO strategies could even further improve the clinical success, especially for diseases such as pancreatic cancer, brain tumors where the success of IO so far has been limited. Nanotechnology-based targeted delivery strategies could improve the delivery efficiency of IO agents as well as provide additional avenues for novel therapeutic and vaccination strategies. Additionally, a number of locally-administered immunogenic scaffolds and therapeutic strategies, such as the use of STING agonist, could benefit from rationally designed biomaterials and delivery approaches. Delivery Technologies for Immuno-Oncology: Volume 1: Delivery Strategies and Engineering Technologies in Cancer Immunotherapy creates a comprehensive treaty that engages the scientific and medical community who are involved in the challenges of immunology, cancer biology, and therapeutics with possible solutions from the nanotechnology and drug delivery side. Comprehensive treaty covering all aspects of immuno-oncology (IO) Novel strategies for delivery of IO therapeutics and vaccines Forecasting on the future of nanotechnology and drug delivery for IO


Protein Kinase C in Cancer Signaling and Therapy

Protein Kinase C in Cancer Signaling and Therapy

Author: Marcelo G. Kazanietz

Publisher: Springer Science & Business Media

Published: 2010-06-10

Total Pages: 492

ISBN-13: 1607615436

DOWNLOAD EBOOK

Protein kinase C (PKC), a family of serine-threonine kinases, rocketed to the forefront of the cancer research field in the early 1980’s with its identification as an effector of phorbol esters, natural products with tumor promoting activity. Phorbol esters had long been of interest to the cancer research field due to early studies in the mouse skin carcinogenesis model, which showed that prolonged topical application of phorbol esters promoted the formation of skin tumors on mice previously treated with mutagenic agents. Research in the last years has established key roles for PKC isozymes in the control of cell proliferation, migration, adhesion, and malignant transformation. In addition, there is a large body of evidence linking PKC to invasion and cancer cell metastasis. Moreover, it is now well established that the expression of PKC isozymes is altered in various types of cancers. More importantly, small molecule inhibitors have been developed with significant anti-cancer activity. The relevance of PKC isozymes in cancer signaling is therefore remarkable. This book will have 4 sections. There will be 23 chapters. Each section will have a brief introduction by an expert in the field (~ 1-2 pages).


Kinomics

Kinomics

Author: Heinz-Bernhard Kraatz

Publisher: John Wiley & Sons

Published: 2015-11-16

Total Pages: 364

ISBN-13: 3527337652

DOWNLOAD EBOOK

Das umfassende Referenzwerk zur Kinase-Forschung: Ausführlich werden die Themen Kinase-Engineering, Peptidsubstrat-Engineering, das Design von Co-Substraten und Kinasehemmer erläutert sowie deren Anwendung in der Bio- und Pharmaforschung beschrieben.


Prognostic and Therapeutic Applications of RKIP in Cancer

Prognostic and Therapeutic Applications of RKIP in Cancer

Author: Benjamin Bonavida

Publisher: Academic Press

Published: 2020-02-05

Total Pages: 504

ISBN-13: 0128196122

DOWNLOAD EBOOK

Prognostic and Therapeutic Applications of RKIP in Cancer provides updated reviews on the chemistry, signaling, pre-clinical and clinical activities, and role of RKIP expression levels for diagnostics, prognosis and potential interventions. The development of novel compounds and conjugates that selectively induce RKIP expression in cancer open a novel era of new therapeutics and their potential in the treatment of highly resistant cancers and metastases. Edited and written by internationally renowned experts in the field of novel therapeutics for cancer, this book is a valuable source for cancer researchers, medical scientists, clinicians, clinical pharmacologists, and graduate students.