Targeting Protein Kinases For Cancer Therapy

Author : David J. Matthews,Mary E. Gerritsen
Publisher : John Wiley & Sons
Page : 719 pages
File Size : 55,9 Mb
Release : 2011-09-20
Category : Medical
ISBN : 9781118210772

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Targeting Protein Kinases for Cancer Therapy by David J. Matthews,Mary E. Gerritsen Pdf

An expert guide to targeting protein kinases in cancer therapy Research has shown that protein kinases can instigate the formation and spread of cancer when they transmit faulty signals inside cells. Because of this fact, pharmaceutical scientists have targeted kinases for intensive study, and have been working to develop medicinal roadblocks to sever their malignant means of communication. Complete with full-color presentations, Targeting Protein Kinases for Cancer Therapy defines the structural features of protein kinases and examines their cellular functions. Combining kinase biology with chemistry and pharmacology applications, this book enlists emerging data to drive the discovery of new cancer-fighting drugs. Valuable information includes: Comprehensive overviews of the major kinase families involved in oncology, integrating protein structure and function, and providing important tools to assist pharmaceutical researchers to understand and work in this dynamic area of cancer drug research Focus on small molecule inhibitors as well as other therapeutic modalities Discussion of kinase inhibitors that have entered clinical trials for the treatment of cancer, with an emphasis on molecules that have progressed to late stage clinical trials and, in a few cases, to market Providing a platform for further study, this important work reviews both the successes and challenges of kinase inhibitor therapy, and provides insight into future directions in the war against cancer.

Author : Doriano Fabbro,Frank McCormick
Publisher : Springer Science & Business Media
Page : 599 pages
File Size : 48,7 Mb
Release : 2007-11-13
Category : Science
ISBN : 9781592599622

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Protein Tyrosine Kinases by Doriano Fabbro,Frank McCormick Pdf

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.

Author : Anonim
Publisher : BoD – Books on Demand
Page : 164 pages
File Size : 45,8 Mb
Release : 2021-12-08
Category : Medical
ISBN : 9781838809065

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Protein Kinases by Anonim Pdf

For the past two decades, the protein kinase family has been an intense area of research for developing anticancer drugs. Despite tremendous advancements in kinase drug expansion, many kinases are still unexplored. As such, this book includes research and review articles from experts that focus on protein kinase signalling pathways as a molecular drug target. Chapters include illustrations and cover such topics as the mechanism of action and anticancer activity of protein kinase inhibitors on various cancer types. They also discuss new opportunities, challenges, and future perspectives in the field.

Author : Marcelo G. Kazanietz
Publisher : Springer Science & Business Media
Page : 494 pages
File Size : 48,5 Mb
Release : 2010-06-10
Category : Medical
ISBN : 9781607615439

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Protein Kinase C in Cancer Signaling and Therapy by Marcelo G. Kazanietz Pdf

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).

Author : Bert Klebl,Gerhard Müller,Michael Hamacher
Publisher : John Wiley & Sons
Page : 570 pages
File Size : 50,6 Mb
Release : 2011-03-16
Category : Science
ISBN : 9783527633494

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Protein Kinases as Drug Targets by Bert Klebl,Gerhard Müller,Michael Hamacher Pdf

This timely guide to kinase inhibitor drug development is the first to cover the entire drug pipeline, from target identification to compound development and clinical application. Edited by the pioneers in the field, on the drug development side this ready reference discusses classical medicinal chemistry approaches as well as current chemical genomics strategies. On the clinical side, both current and future therapeutic application areas for kinase inhibitor drugs are addressed, with a strong focus on oncology drugs. Backed by recent clinical experience with first-generation drugs in the battle against various forms of cancer, this is crucial reading for medicinal, pharmaceutical and biochemists, molecular biologists, and oncologists, as well as those working in the pharmaceutical industry.

Author : Huan Ren
Publisher : BoD – Books on Demand
Page : 136 pages
File Size : 52,8 Mb
Release : 2019-09-25
Category : Medical
ISBN : 9781789848083

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Tyrosine Kinases as Druggable Targets in Cancer by Huan Ren Pdf

Protein tyrosine kinase (PTK) deregulation contributes to growth of cancer and many other diseases. The development of small-molecule tyrosine kinase inhibitors (TKIs) that target the deregulated PTKs, such as epidermal growth factor receptor (EGFR) in non-small-cell lung cancer (NSCLC) and Bcr-ABL in chronic myeloid leukemia (CML), has revolutionized disease management. In this book, we examine a few aspects of PTKs and cancer, considering efficacy, predictive markers to therapeutic response, limitations, and future directions in TKI treatment. In this rapidly evolving field, overcoming therapeutic resistance is most challenging, and multi-targeting directs the next-generation TKIs and combination therapy as ongoing strategies in cancer treatment.

Author : Anonim
Publisher : Academic Press
Page : 292 pages
File Size : 49,9 Mb
Release : 2018-11-21
Category : Medical
ISBN : 9780128127384

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Protein Kinase Inhibitors as Sensitizing Agents for Chemotherapy by Anonim Pdf

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

Author : James W. Janetka,Roseann M. Benson
Publisher : John Wiley & Sons
Page : 488 pages
File Size : 49,9 Mb
Release : 2018-05-10
Category : Science
ISBN : 9781119300205

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Extracellular Targeting of Cell Signaling in Cancer by James W. Janetka,Roseann M. Benson Pdf

International experts present innovative therapeutic strategies to treat cancer patients and prevent disease progression Extracellular Targeting of Cell Signaling in Cancer highlights innovative therapeutic strategies to treat cancer metastasis and prevent tumor progression. Currently, there are no drugs available to treat or prevent metastatic cancer other than non-selective, toxic chemotherapy. With contributions from an international panel of experts in the field, the book integrates diverse aspects of biochemistry, molecular biology, protein engineering, proteomics, cell biology, pharmacology, biophysics, structural biology, medicinal chemistry and drug development. A large class of proteins called kinases are enzymes required by cancer cells to grow, proliferate, and survive apoptosis (death) by the immune system. Two important kinases are MET and RON which are receptor tyrosine kinases (RTKs) that initiate cell signaling pathways outside the cell surface in response to extracellular ligands (growth factors.) Both kinases are oncogenes which are required by cancer cells to migrate away from the primary tumor, invade surrounding tissue and metastasize. MET and RON reside on both cancer cells and the support cells surrounding the tumor, called the microenvironment. MET and RON are activated by their particular ligands, the growth factors HGF and MSP, respectively. Blocking MET and RON kinase activation and downstream signaling is a promising therapeutic strategy for preventing tumor progression and metastasis. Written for cancer physicians and biologists as well as drug discovery and development teams in both industry and academia, this is the first book of its kind which explores novel approaches to inhibit MET and RON kinases other than traditional small molecule kinase inhibitors. These new strategies target key tumorigenic processes on the outside of the cell, such as growth factor activation by proteases. These unique strategies have promising potential as an improved alternative to kinase inhibitors, chemotherapy, or radiation treatment.

Author : Marcelo G. Kazanietz
Publisher : Humana Press
Page : 494 pages
File Size : 43,6 Mb
Release : 2011-07-21
Category : Medical
ISBN : 1607615452

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Protein Kinase C in Cancer Signaling and Therapy by Marcelo G. Kazanietz Pdf

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).

Author : Vittorio de Franciscis
Publisher : Nova Publishers
Page : 258 pages
File Size : 42,9 Mb
Release : 2007
Category : Health & Fitness
ISBN : 1600212433

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Signalling Molecules as Targets in Cancer Therapy by Vittorio de Franciscis Pdf

This book presents state-of-the-art information on the molecules of cell signalling pathways that represent actual or future targets for cancer therapy. By giving an update of the most promising approaches in this rapidly evolving field, the book contributes to the translation of the recent advances in the knowledge of intracellular signalling into the generation of innovative biomolecules as specific tools to target the most promising tumour-specific candidates. The book begins logically with the molecules first encountered along the signalling pathways, the membrane receptors for growth factors (Part I). Next, Part II presents several examples of intracellular molecular targets that are situated one step beyond in the pathways, while Part III addresses the difficult task of tuning the delicate balance between cell death and survival. In Part IV, the reader is taken into the practical problems raised by the therapy of specific cancers (glioma, childhood leukaemia), and into an original strategy from the field of nuclear medicine with the potential to generate innovative molecular-targeted cancer therapies.

Author : Richard M. Schultz
Publisher : Springer Science & Business Media
Page : 303 pages
File Size : 44,7 Mb
Release : 2006-01-24
Category : Medical
ISBN : 9783764374143

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Advances in Targeted Cancer Therapy by Richard M. Schultz Pdf

There have been tremendous advances in our understanding of molecular and tumor biology during the past few years. In the field of cancer therapeutics, it is expected that cytotoxic drug approaches will be gradually replaced with treatments based on biological targeted approaches. Hopefully these new targeted therapies will significantly increase efficacy and lack the devastating and troublesome side effects elicited by cytotoxic chemotherapy. This volume is the first book to cover the general topic of targeted cancer therapy. It presents a range of targets such as tumor angiogenesis, cell cycle control and cell signalling, COX-2, apoptosis/cell survival, invasion and metastasis and approaches like kinase inhibitors, antisense, and antibody-based therapeutics. The emphasis is on preclinical development, including target validation, development of biomarkers, strategies for combination approaches, and development of resistance. The particular challenges involved in translating these data to clinical application are discussed. This volume should be of broad general interest to researchers and clinicians involved in cancer therapy as well as other scientists interested in current strategies for cancer treatment.

Author : Alastair D. Reith
Publisher : Springer Science & Business Media
Page : 367 pages
File Size : 54,7 Mb
Release : 2008-02-02
Category : Science
ISBN : 9781592590599

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Protein Kinase Protocols by Alastair D. Reith Pdf

As key components of many cell signaling pathways, protein kinases are implicated in a broad variety of diseases, including cancers and neurodegenerative conditions, and offer considerable potential as tractable targets for therapeutic intervention. In Protein Kinase Protocols, a panel of highly skilled laboratory investigators describe both basic and more sophisticated methods for the analysis of kinase-mediated signaling cascades, with emphasis on the identification of proteins according to their interactive relationships and the analysis of their functional properties. Described in step-by-step detail, these readily reproducible techniques offer novices quick access to a complicated field, and provide more experienced investigators many novel time-saving ploys. Emphasis is given to the critical technical steps that are often omitted from methods published in the primary literature. There are also tips on potential pitfalls and copious notes on how to adjust the protocols to work in related systems. Broad in its range of techniques and thoroughly detailed to help ensure experimental success, Protein Kinase Protocols offers both novice and experienced investigators powerful tools for understanding the functional roles of specific protein kinases within signaling cascades and for identification and evaluation of novel therapeutic targets.

Author : Vitaly A. Polunovsky,Peter J. Houghton
Publisher : Springer Science & Business Media
Page : 307 pages
File Size : 43,8 Mb
Release : 2010-07-23
Category : Medical
ISBN : 9781603272711

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mTOR Pathway and mTOR Inhibitors in Cancer Therapy by Vitaly A. Polunovsky,Peter J. Houghton Pdf

The main objective of this book is to provide an up-to-date survey of the rapidly advancing eld of cancer therapy. Moreover, since our knowledge in this area rapidly evolves, some data have got obsolete during the process of book editing. Our understanding of the mechanisms involved in cancer genesis and progression underwent unprecedented expansion during the last decade, opening a new era of cancer treatment – targeted therapy. The surge in this area results in no small part from studies conducted jointly by basic health scientists and clinical investigators. It is our hope that this book will help foster even further collaboration between investigators in these two disciplines. The target of rapamycin (TOR) was rst identi ed in Saccharomyces cerevisiae and subsequently in mammals (mTOR) as a conserved atypical serine/threonine kinase. In mammalian cells, mTOR exists in at least two multi-protein complexes that have critical roles in regulating cellular homeostasis and survival. As with many other areas of science, discovery of TOR signaling was fortuitous. Rapamycin was isolated as a product of the soil bacteria Streptomyces hygroscopicus, identi ed in a soil sample taken from the island of Rapa Nui (Easter Island). Rapamycin was rst discovered to be a potent antifungal agent and next as an immune suppressive drug. It was only later that it was found to be active as an antitumor agent in non-clinical models; although it was not developed for this indication. The history of rapamycin presents one of the rst examples of chemical genetics.

Author : Anonim
Publisher : Unknown
Page : 128 pages
File Size : 55,5 Mb
Release : 19??
Category : Electronic
ISBN : 1461464382

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Encyclopedia of Signaling Molecules by Anonim Pdf

Author : E. J. Corey,Yong-Jin Wu
Publisher : John Wiley & Sons
Page : 404 pages
File Size : 45,7 Mb
Release : 2023-09-06
Category : Medical
ISBN : 9781394207107

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Molecules Engineered Against Oncogenic Proteins and Cancer by E. J. Corey,Yong-Jin Wu Pdf

Molecules Engineered Against Oncogenic Proteins and Cancer A comprehensive review of the latest molecular advances in cancer treatment Featuring 91 total small molecule kinase/KRAS inhibitors, 80 of which are FDA-approved, Molecules Engineered Against Oncogenic Proteins and Cancer documents the recent scientific advances that have transformed one of medicine’s most challenging areas—cancer treatment. Most of these inhibitors specifically block oncogene-induced carcinogenic proteins with results that have dramatically advanced the treatment of cancer. In addition, the structural formulas of more than 100 kinase/KRAS inhibitors in clinical trials are presented. With a very well-known chemist as an author, Molecules Engineered Against Oncogenic Proteins and Cancer includes information on: Each molecule’s structure, function of the kinase target and relevance to cancer, the drug discovery process, and molecular details of drug action Mutated protein kinases as oncoproteins and targets for inhibition, along with the details of discovery for each antitumor antikinase agent History of oncoprotein inhibitors and their role in advancing the treatment and understanding of cancer The discovery process as a whole, effective strategies for innovation, ongoing challenges, and a glimpse of the future of the field Combining the most significant recent discoveries in a unique and useful way, Molecules Engineered Against Oncogenic Proteins and Cancer is an essential resource for researchers and students in bioscience, medicine, chemistry, and oncology as well as for those at industrial companies involved in therapeutic discovery.