Protein Kinase C In Cancer Signaling And Therapy

Author : Marcelo G. Kazanietz
Publisher : Springer Science & Business Media
Page : 494 pages
File Size : 55,6 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 : Marcelo G. Kazanietz
Publisher : Humana Press
Page : 494 pages
File Size : 46,9 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 : David J. Matthews,Mary E. Gerritsen
Publisher : John Wiley & Sons
Page : 719 pages
File Size : 54,7 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 : Dean J. Pierce
Publisher : Unknown
Page : 0 pages
File Size : 54,5 Mb
Release : 2018
Category : Protein kinase C
ISBN : 1536132101

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Protein Kinase C by Dean J. Pierce Pdf

In this compilation, the authors review the structural basis of PKC isozymes and focus on the C1 domain, as well as the plausible binding mechanisms of its activators. Additionally, the recent molecular dynamics simulation studies of how phorbol esters or bryostatin bind to the activator pocket are described and some of the key amino acid residues recently identified as important for activator binding are investigated. The following chapter focuses on the expression pattern and function of PKCα in cancer cells, and newly emerging PKCα-targeted cancer therapies. PKCα acts directly and/or indirectly in various signaling mechanisms in cancer cells, including proliferation, survival, invasion, migration, apoptosis and drug resistance. A final review is provided which dissects the crosstalk between p53 and PKCδ in the context of apoptotic cell death and cancer therapy. PKCδ is implicated in a transcriptional regulation of the p53 tumor suppressor that is critical for cell cycle arrest and apoptosis in response to DNA damage.

Author : Doriano Fabbro,Frank McCormick
Publisher : Springer Science & Business Media
Page : 599 pages
File Size : 44,5 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 : Christoph Wagener,Carol Stocking,Oliver Müller
Publisher : John Wiley & Sons
Page : 356 pages
File Size : 46,7 Mb
Release : 2016-12-12
Category : Science
ISBN : 9783527336586

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Cancer Signaling by Christoph Wagener,Carol Stocking,Oliver Müller Pdf

Cancer, which has become the second-most prevalent health issue globally, is essentially a malfunction of cell signaling. Understanding how the intricate signaling networks of cells and tissues allow cancer to thrive - and how they can be turned into potent weapons against it - is the key to managing cancer in the clinic and improving the outcome of cancer therapies. In their ground-breaking textbook, the authors provide a compelling story of how cancer works on the molecular level, and how targeted therapies using kinase inhibitors and other modulators of signaling pathways can contain and eventually cure it. The first part of the book gives an introduction into the cell and molecular biology of cancer, focusing on the key mechanisms of cancer formation. The second part of the book introduces the main signaling transduction mechanisms responsible for carcinogenesis and compares their function in healthy versus cancer cells. In contrast to the complexity of its topic, the text is easy to read. 32 specially prepared teaching videos on key concepts and pathways in cancer signaling are available online for users of the print edition and have been integrated into the text in the enhanced e-book edition.

Author : Khalil Ahmed,Olaf-Georg Issinger,Ryszard Szyszka
Publisher : Springer
Page : 386 pages
File Size : 50,7 Mb
Release : 2015-03-03
Category : Medical
ISBN : 9783319145440

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Protein Kinase CK2 Cellular Function in Normal and Disease States by Khalil Ahmed,Olaf-Georg Issinger,Ryszard Szyszka Pdf

Protein kinase CK2 (formerly casein kinase II or 2) is known to play a critical role in the control of cell growth and cell death and is thus intimately involved in the development of cancer. More specifically, CK2 has been found to be elevated in all cancers examined. While CK2 levels are known to be high in proliferating normal cells, CK2 has also been found to be a potent suppressor of apoptosis and is a link to the cancer cell phenotype, which is characterized by deregulation of both cell proliferation and cell death. Indeed, it would appear that CK2 impacts many of the hallmarks of cancer and it has now gained considerable attention as a potential target for cancer therapy. Protein Kinase CK2 and Cellular Function in Normal and Disease States increases knowledge of the role of CK2 in the development of cellular dysfunction and emphasizes that this protein may serve as a target of drug development for improved cancer therapy. In addition, it is a handy tool that provides cancer researchers, graduate students, and all scientists involved in CK2 research with one main source for the latest advances in CK2 research. ​

Author : Anonim
Publisher : BoD – Books on Demand
Page : 164 pages
File Size : 40,8 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 : Alexandra C. Newton
Publisher : Springer Science & Business Media
Page : 565 pages
File Size : 50,7 Mb
Release : 2008-02-03
Category : Science
ISBN : 9781592593972

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Protein Kinase C Protocols by Alexandra C. Newton Pdf

Since the discovery that protein kinase C (PKC) transduces the ab- dance of signals that result in phospholipid hydrolysis, this enzyme has been at the forefront of research in signal transduction. Protein Kinase C Protocols covers fundamental methods for studying the structure, function, regulation, subcellular localization, and macromolecular interactions of PKC. Protein Kinase C Protocols is divided into 11 sections representing the major aspects of PKC regulation and function. Part I contains an introduction and a historical perspective on the discovery of PKC by Drs. Yasutomi Nishizuka and Ushio Kikkawa. Part II describes methods to purify PKC. Part III describes the standard methods for measuring PKC activity: its enzymatic activity and its stimulus-dependent translocation from the cytosol to the membrane. Part IV describes methods for measuring the membrane interaction of PKC in vivo and in vitro. Part V provides methodologies and techniques for measuring the ph- phorylation state of PKC, including a protocol for measuring the activity of PKC’s upstream kinase, PDK-1. Novel methods for identifying substrates are described in Part VI. Part VII presents protocols for expressing and analyzing the membrane targeting domains of PKC. Part VIII provides a comprehensive c- pilation of methods used to identify binding partners for PKC. Part IX describes pharmacological probes used to study PKC. The book ends with a presentation of genetic approaches to study PKC (Part X) and a discussion of approaches used to study PKC in disease (Part XI).

Author : Malay Chatterjee,Khosrow Kashfi
Publisher : Springer Science & Business Media
Page : 328 pages
File Size : 40,9 Mb
Release : 2011-12-02
Category : Medical
ISBN : 1461407303

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Cell Signaling & Molecular Targets in Cancer by Malay Chatterjee,Khosrow Kashfi Pdf

This book provides an overview of critical components of cell signaling machinery and its role in epithelial morphogenesis, proliferation, invasions and angiogenesis in human cancer and discusses novel types of protein kinase pathways.

Author : Ganji Purnachandra Nagaraju
Publisher : Springer
Page : 241 pages
File Size : 53,9 Mb
Release : 2018-09-27
Category : Medical
ISBN : 9789811314865

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Role of Tyrosine Kinases in Gastrointestinal Malignancies by Ganji Purnachandra Nagaraju Pdf

The aim of this book is to provide comprehensive overview of the role of different tyrosine kinases in the progression and metastasis of various cancers of the gastrointestinal tract such as esophagus, liver, pancreas, stomach, and colorectal. Activation of various signaling pathways and tyrosine kinases are responsible for resistance to chemo and radiotherapy in these gastrointestinal malignancies. Targeting these tyrosine kinases, which regulate the activities of survival pathways in growth, and metastasis is a rational strategy in gastrointestinal cancer therapy. Each chapter embedded in this book covers information pertaining to a specific tyrosine kinase and its impact on various malignancies, which is not only significant for basic and clinical research investigations but will also be valued by students at advanced undergraduate to postgraduate levels.

Author : John D. Haley,William John Gullick
Publisher : Springer Science & Business Media
Page : 393 pages
File Size : 55,9 Mb
Release : 2009-03-01
Category : Medical
ISBN : 9781597453561

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EGFR Signaling Networks in Cancer Therapy by John D. Haley,William John Gullick Pdf

The epidermal gro wth factor (EGF ) receptor and its downstream signal transduction networks have been implicated in the ontology and maintenance of tumor tissues, which has motivated the discovery and development of molecularly targeted anti-EGF receptor therapies. Over decades of study, the EGF receptor structure, its ligand binding domains, the physical biochemistry underlying its intrinsic tyrosine kinase catalytic function and the modular interactions with SH2, PTB, and SH3 domain containing signaling adaptor p- teins required for signal transduction, have been extensively dissected. Not only is the EGF receptor the nexus of many streams of information, but it also forms one part of a calcul- ing device by forming dimers and oligomers with the other three receptors in its family in response to at least eleven ligands (some of which are expressed in multiple forms with overlapping or quite distinct functions). This phenomenon, while recruiting to the inner surface of the cell membrane and activating multiple second messenger proteins, also allows the possibility of cross talk between these systems, permitting a further layer of information to be exchanged. Less well described are the cross re gulation of the EGF receptor and other anti-apoptotic, mitogenic and metabolic signaling systems. The study of these systems has yielded new surprises. One hurdle in these efforts has been that signal transduction pathways have frequently been defined in the generic absence of their tissue-specific or cell-interaction specific context.

Author : Shile Huang
Publisher : Unknown
Page : 204 pages
File Size : 41,5 Mb
Release : 2020
Category : Electronic
ISBN : 303943554X

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MTOR Signaling in Metabolism and Cancer by Shile Huang Pdf

The mechanistic/mammalian target of rapamycin (mTOR), a serine/threonine kinase, is a central regulator for human physiological activity. Deregulated mTOR signaling is implicated in a variety of disorders, such as cancer, obesity, diabetes, and neurodegenerative diseases. The papers published in this Special Issue summarize the current understanding of the mTOR pathway and its role in the regulation of tissue regeneration, regulatory T cell differentiation and function, and different types of cancer including hematologic malignancies, skin, prostate, breast, and head and neck cancer. The findings highlight that targeting mTOR pathway is a promising strategy to fight against certain human diseases.

Author : Alastair D. Reith
Publisher : Humana Press
Page : 365 pages
File Size : 44,8 Mb
Release : 2000-09-28
Category : Science
ISBN : 0896037002

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Protein Kinase Protocols by Alastair D. Reith Pdf

Author : Jung-Min Kee
Publisher : Unknown
Page : 394 pages
File Size : 47,5 Mb
Release : 2007
Category : Electronic
ISBN : STANFORD:36105129654047

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Design and Synthesis of Protein Kinase C Modulators as Therapeutic Leads by Jung-Min Kee Pdf