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Protein Kinase C In Cancer Signaling And Therapy
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Book Synopsis Protein Kinase C in Cancer Signaling and Therapy by : Marcelo G. Kazanietz
Download or read book Protein Kinase C in Cancer Signaling and Therapy written by Marcelo G. Kazanietz and published by Springer Science & Business Media. This book was released on 2010-06-10 with total page 492 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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).
Book Synopsis Protein Kinase C in Cancer Signaling and Therapy by : Marcelo G. Kazanietz
Download or read book Protein Kinase C in Cancer Signaling and Therapy written by Marcelo G. Kazanietz and published by Humana Press. This book was released on 2011-07-21 with total page 494 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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).
Book Synopsis Targeting Protein Kinases for Cancer Therapy by : David J. Matthews
Download or read book Targeting Protein Kinases for Cancer Therapy written by David J. Matthews and published by John Wiley & Sons. This book was released on 2011-09-20 with total page 719 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
Book Synopsis Protein Kinase C by : Dean J. Pierce
Download or read book Protein Kinase C written by Dean J. Pierce and published by . This book was released on 2018 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
Book Synopsis Mechanisms of Regulation of Protein Kinase C and Its Tumor Suppressor Function in Cancer by : Corina Elena Antal
Download or read book Mechanisms of Regulation of Protein Kinase C and Its Tumor Suppressor Function in Cancer written by Corina Elena Antal and published by . This book was released on 2015 with total page 147 pages. Available in PDF, EPUB and Kindle. Book excerpt: The serine/threonine protein kinase C (PKC) family has been extensively studied over the last 35 years, yet fundamental questions regarding the regulation of its signaling and its dysregulation in disease remain unanswered. PKC is involved in a multitude of cellular processes and precise control of the amplitude of PKC signaling is essential for maintaining cellular homeostasis. This thesis expands on the knowledge of PKC at the molecular level by unveiling how intramolecular conformational changes tune the affinity of PKC for its ligands, and at the pathophysiological level by overturning a 30-year-old scientific dogma on the role of PKC in cancer. First, mechanistic studies reveal that processing phosphorylations promote intramolecular interactions that clamp PKC in a closed conformation to prevent signaling in the absence of agonists, but allow efficient activation in response to small changes in agonist levels. These studies offer novel means of therapeutically targeting PKC with molecules or peptides that can either disrupt these interactions to activate PKC or maintain them closed to inhibit PKC activity. Second, analysis of PKC gene family mutations in human cancers reveals that they are loss-of-function, and that this loss-of-function confers a growth advantage, both in vitro and in vivo. These data suggest that therapies should focus on restoring, not inhibiting, PKC activity in the treatment of cancer. Taken together, this thesis identifies novel strategies to modulate PKC activity in therapies and, most importantly, establishes that PKC is a tumor suppressor.
Book Synopsis Cancer Signaling by : Christoph Wagener
Download or read book Cancer Signaling written by Christoph Wagener and published by John Wiley & Sons. This book was released on 2016-12-12 with total page 356 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
Book Synopsis Protein Kinase C Protocols by : Alexandra C. Newton
Download or read book Protein Kinase C Protocols written by Alexandra C. Newton and published by Springer Science & Business Media. This book was released on 2008-02-03 with total page 565 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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).
Book Synopsis Protein Kinase CK2 Cellular Function in Normal and Disease States by : Khalil Ahmed
Download or read book Protein Kinase CK2 Cellular Function in Normal and Disease States written by Khalil Ahmed and published by Springer. This book was released on 2015-03-03 with total page 386 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
Book Synopsis Protein Tyrosine Kinases by : Doriano Fabbro
Download or read book Protein Tyrosine Kinases written by Doriano Fabbro and published by Springer Science & Business Media. This book was released on 2007-11-13 with total page 599 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
Download or read book Protein Kinases written by and published by BoD – Books on Demand. This book was released on 2021-12-08 with total page 164 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
Book Synopsis Protein Kinase Inhibitors as Sensitizing Agents for Chemotherapy by :
Download or read book Protein Kinase Inhibitors as Sensitizing Agents for Chemotherapy written by and published by Academic Press. This book was released on 2018-11-21 with total page 292 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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
Book Synopsis Extracellular Targeting of Cell Signaling in Cancer by : James W. Janetka
Download or read book Extracellular Targeting of Cell Signaling in Cancer written by James W. Janetka and published by John Wiley & Sons. This book was released on 2018-05-10 with total page 486 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
Book Synopsis Protein Kinase C[epsilon] Signal Transduction Pathways to the Development of Squamous Cell Carcinoma and a Myeloproliferative-like Disease by : Deric Lane Wheeler
Download or read book Protein Kinase C[epsilon] Signal Transduction Pathways to the Development of Squamous Cell Carcinoma and a Myeloproliferative-like Disease written by Deric Lane Wheeler and published by . This book was released on 2004 with total page 280 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Book Synopsis Encyclopedia of Signaling Molecules by : Sangdun Choi
Download or read book Encyclopedia of Signaling Molecules written by Sangdun Choi and published by Springer. This book was released on 2017-12-15 with total page 6330 pages. Available in PDF, EPUB and Kindle. Book excerpt: The second edition of this encyclopedia presents over 400 biologically important signaling molecules and the content is built on the core concepts of their functions along with early findings written by some of the world’s foremost experts. The molecules are described by recognized leaders in each molecule. The interactions of these single molecules in signal transduction networks will also be explored. This encyclopedia marks a new era in overview of current cellular signaling molecules for the specialist and the interested non-specialist alike. Currently, there are more than 30,000 genes in human genome. However, not all the proteins encoded by these genes work equally in order to maintain homeostasis. Understanding the important signaling molecules as completely as possible will significantly improve our research-based teaching and scientific capabilities.
Book Synopsis Spatiotemporal Regulation of Protein Kinase C Signaling by : Lisa Leon Gallegos
Download or read book Spatiotemporal Regulation of Protein Kinase C Signaling written by Lisa Leon Gallegos and published by . This book was released on 2009 with total page 200 pages. Available in PDF, EPUB and Kindle. Book excerpt: Protein kinase C (PKC) is an archetypal mediator of cellular signaling. PKC consists of 10 Ser/Thr kinases that participate in a wide range of cellular processes, including proliferation, apoptosis, learning and memory, and cell migration. PKC signaling is controlled by lipid second messengers and protein scaffolding. For proper cellular PKC signaling, location and timing of activation are critical. Aberrant PKC signaling is known to occur in disease states, notably cancer. The goal of this thesis is to examine how spatial and temoral specificity are achieved in cellular PKC signaling, and how this regulation is altered in cancer. Understanding the nuances of PKC regulation in cells and mis-regulation in disease will undoubtedly inform efforts to therapeutically target this enzyme family.
Book Synopsis Protein Kinase Inhibitors by : Md. Imtaiyaz Hassan
Download or read book Protein Kinase Inhibitors written by Md. Imtaiyaz Hassan and published by Academic Press. This book was released on 2022-05-19 with total page 832 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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
Book Synopsis Protein Kinase C-eta Signalling in Breast Cancer by : Deepanwita Pal
Download or read book Protein Kinase C-eta Signalling in Breast Cancer written by Deepanwita Pal and published by . This book was released on 2016 with total page 107 pages. Available in PDF, EPUB and Kindle. Book excerpt: Protein kinase C-eta (PKCη) is a novel member of the PKC family that is important for several cellular processes. PKCη is overexpressed in breast cancer and has been associated with chemotherapeutic resistance. PKCη is the only phorbol ester-sensitive PKC isozyme that resists downregulation upon prolonged treatment with tumorpromoting phorbol esters suggesting its unique regulation. The purpose of this dissertation is to elucidate the mechanism of PKCη regulation and its functional relevance in breast cancer. We have shown that PKCη is upregulated by several structurally and functionally distinct PKC activators in contrast to other PKC isozymes. Activator-induced upregulation of PKCη was associated with its phosphorylation. Our results indicate that novel PKCs are involved in the upregulation of PKCη by PKC activators. We also made a novel observation that PKCη is downregulated via two distinct mechanisms. While inhibition of PKC caused the downregulation of PKCη via proteasome-independent pathway, inhibition of PDK1 led to PKCη downregulation via proteasome-dependent pathway. We further demonstrated that PKCη is important for the growth and survival of breast cancer cells. The unique regulation of PKCη and its implications on breast cancer growth and survival suggests that this pathway could be selectively exploited for targeted therapies for breast cancer.
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