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Author: Khusru Asadullah
Publisher:
ISBN: 9788178952574
Category : Anti-inflammatory agents
Languages : en
Pages : 162
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Book Description
Whereas G protein-coupled and nuclear receptors have been in the focus of the pharmaceutical industry since decades, protein kinases became interesting drug targets more recently. Several protein kinase inhibitors are well established for the treatment of tumors in the meantime, many more are in clinical development. Inside into the biology of protein kinases and progress in technologies to target these molecules, however, fostered the discovery and development of protein kinase inhibitors for the treatment of inflammation, too. They are particular promising since they are key factors in signal transduction with major impact for initiating, propagation and regulation of immunological responses. In addition, they are well drugable by small molecular weight inhibitors, opening the chance to discover oral bioavailable drugs. When considering kinases as targets in inflammation, however, there are several issues too. These are mainly the selectivity of both the target and the inhibitor and the associated side effect profile of corresponding drugs. In contrast to application in oncology where efficacy is more or less the most important criteria, a high safety profile is key for the chronic treatment of usual non-life treating inflammatory and autoimmune diseases. Having said this, however, clearly better drugs with a favorable therapeutic index (effect / side effect ratio) are needed for these indications, too. Thus, to be considered as a really promising drug target the protein kinase of interest should be significantly involved in the inflammatory process - otherwise insufficient efficacy and potency would have to be expected - without being involved in other physiological processes of essential biological importance or a very selective expression pattern. The same is true with the specifity of the inhibitors itself. So a compound hitting just one other kinase a little may not be acceptable, depending on the function of these off target molecule. Consequently, a solid target identification and validation is needed before lead identification and optimization with the goal of achieving high specifity is started. Despite all these challenges major progress has been made and the first promising kinase inhibitors are moving into the clinic for anti-inflammatory therapy. There are many more on the horizon and it s pretty likely that protein kinase inhibitors will enrich the spectrum of therapy for chronic inflammatory and autoimmune diseases. Within this issue an overview is given on recent progress in the field of protein kinase inhibitors for the treatment of inflammation addressing the opportunities and chances on one hand and the issues and hurdles on the other hand. We are very pleased that we were able to convince real experts to contribute to this hot topic issue. Starting with some general points the recent findings are issued and should enabled the reader to keep up with this fast developing field that is of substantial interest for basic and clinical orientated scientists on one hand and academia as well as pharmaceutical industry on the other hand. All chapters in this book have been published before as articles in a hot topic issue of Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Volume 6, Number 1, February 2007 and are reprinted here with permission by Bentham Science Publishers Ltd.
Author: Khusru Asadullah
Publisher:
ISBN: 9788178952574
Category : Anti-inflammatory agents
Languages : en
Pages : 162
Get Book Here
Book Description
Whereas G protein-coupled and nuclear receptors have been in the focus of the pharmaceutical industry since decades, protein kinases became interesting drug targets more recently. Several protein kinase inhibitors are well established for the treatment of tumors in the meantime, many more are in clinical development. Inside into the biology of protein kinases and progress in technologies to target these molecules, however, fostered the discovery and development of protein kinase inhibitors for the treatment of inflammation, too. They are particular promising since they are key factors in signal transduction with major impact for initiating, propagation and regulation of immunological responses. In addition, they are well drugable by small molecular weight inhibitors, opening the chance to discover oral bioavailable drugs. When considering kinases as targets in inflammation, however, there are several issues too. These are mainly the selectivity of both the target and the inhibitor and the associated side effect profile of corresponding drugs. In contrast to application in oncology where efficacy is more or less the most important criteria, a high safety profile is key for the chronic treatment of usual non-life treating inflammatory and autoimmune diseases. Having said this, however, clearly better drugs with a favorable therapeutic index (effect / side effect ratio) are needed for these indications, too. Thus, to be considered as a really promising drug target the protein kinase of interest should be significantly involved in the inflammatory process - otherwise insufficient efficacy and potency would have to be expected - without being involved in other physiological processes of essential biological importance or a very selective expression pattern. The same is true with the specifity of the inhibitors itself. So a compound hitting just one other kinase a little may not be acceptable, depending on the function of these off target molecule. Consequently, a solid target identification and validation is needed before lead identification and optimization with the goal of achieving high specifity is started. Despite all these challenges major progress has been made and the first promising kinase inhibitors are moving into the clinic for anti-inflammatory therapy. There are many more on the horizon and it s pretty likely that protein kinase inhibitors will enrich the spectrum of therapy for chronic inflammatory and autoimmune diseases. Within this issue an overview is given on recent progress in the field of protein kinase inhibitors for the treatment of inflammation addressing the opportunities and chances on one hand and the issues and hurdles on the other hand. We are very pleased that we were able to convince real experts to contribute to this hot topic issue. Starting with some general points the recent findings are issued and should enabled the reader to keep up with this fast developing field that is of substantial interest for basic and clinical orientated scientists on one hand and academia as well as pharmaceutical industry on the other hand. All chapters in this book have been published before as articles in a hot topic issue of Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Volume 6, Number 1, February 2007 and are reprinted here with permission by Bentham Science Publishers Ltd.
Author: Klaus Okkenhaug
Publisher: Frontiers Media SA
ISBN: 2889194191
Category : Immunologic diseases. Allergy
Languages : en
Pages : 140
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Book Description
The PI3Ks control many key functions in immune cells. PI3Ks phosphorylate PtdIns(4,5)P2 to yield PtdIns(3,4,5)P3. Initially, PI3K inhibitors such as Wortmannin, LY294002 and Rapamycin were used to establish a central role for Pi3K pathway in immune cells. Considerable progress in understanding the role of this pathway in cells of the immune system has been made in recent years, starting with analysis of various PI3K and Pten knockout mice and subsequently mTOR and Foxo knockout mice. Together, these experiments have revealed how PI3Ks control B cell and T cell development, T helper cell differentiation, regulatory T cell development and function, B cell and T cell trafficking, immunoglobulin class switching and much, much more. The PI3Kd inhibitor idelalisib has recently been approved for the treatment of B cell lymphoma. Clinical trials of other PI3K inhibitors in autoimmune and inflammatory diseases are also in progress. This is an opportune time to consider a Research Topic considering when what we have learned about the PI3K signalling module in lymphocyte biology and how this is making an impact on clinical immunology and haematology.
Author: Richard A. Ward
Publisher: Royal Society of Chemistry
ISBN: 1849731748
Category : Medical
Languages : en
Pages : 333
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Book Description
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.
Author: Z.-H. Liui
Publisher: Karger Medical and Scientific Publishers
ISBN: 3318026514
Category : Science
Languages : en
Pages : 274
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Book Description
The podocyte is a key cell that forms the last barrier of the kidney filtration unit. One of the most exciting developments in the field of nephrology in the last decade has been the elucidation of its biology and its role in the pathophysiology of inherited and acquired glomerular disease, termed podocytopathy. In this publication, world-renowned experts summarize the most recent findings and advances in the field: they describe the unique biological features and injury mechanisms of the podocyte, novel techniques used in their study, and diagnosis and potential therapeutic approaches to glomerular diseases. Due to its broad scope, this publication is of great value not only for clinical nephrologists and researchers, but also for students, residents, fellows, and postdocs.
Author: Gerard Drewes
Publisher: Humana Press
ISBN: 9781617793639
Category : Science
Languages : en
Pages : 0
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Book Description
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.
Author: Bharat B. Aggarwal
Publisher: Springer
ISBN: 3034808372
Category : Medical
Languages : en
Pages : 489
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Book Description
This volume examines in detail the role of chronic inflammatory processes in the development of several types of cancer. Leading experts describe the latest results of molecular and cellular research on infection, cancer-related inflammation and tumorigenesis. Further, the clinical significance of these findings in preventing cancer progression and approaches to treating the diseases are discussed. Individual chapters cover cancer of the lung, colon, breast, brain, head and neck, pancreas, prostate, bladder, kidney, liver, cervix and skin as well as gastric cancer, sarcoma, lymphoma, leukemia and multiple myeloma.
Author: Ana Cuenda
Publisher: MDPI
ISBN: 3036508589
Category : Science
Languages : en
Pages : 194
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Book Description
p38 Mitogen activated protein kinases (p38MAPK) are a group of evolutionary conserved protein kinases which are central for cell adaptation to environmental changes as well as for immune response, inflammation, tissue regeneration and tumour formation. The interest in this group of protein kinases has grown continually since their discovery. Recent studies using new genetic and pharmacological tools are providing helpful information on the function of these stress-activated protein kinases and show that they have an acute impact on the development of prevalent diseases related to inflammation, diabetes, neurodegeneration, and cancer. In this Special Issue we present novel advances and review the knowledge on the identification of p38MAPK substrates, functions, and regulation; mechanisms underlying the role of p38MAPK in malignant transformation and other pathologies; and therapeutic opportunities associated with regulation of p38MAPK activity.
Author: Jean-Paul Renaud
Publisher: John Wiley & Sons
ISBN: 1118900502
Category : Medical
Languages : en
Pages : 1367
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Book Description
With the most comprehensive and up-to-date overview of structure-based drug discovery covering both experimental and computational approaches, Structural Biology in Drug Discovery: Methods, Techniques, and Practices describes principles, methods, applications, and emerging paradigms of structural biology as a tool for more efficient drug development. Coverage includes successful examples, academic and industry insights, novel concepts, and advances in a rapidly evolving field. The combined chapters, by authors writing from the frontlines of structural biology and drug discovery, give readers a valuable reference and resource that: Presents the benefits, limitations, and potentiality of major techniques in the field such as X-ray crystallography, NMR, neutron crystallography, cryo-EM, mass spectrometry and other biophysical techniques, and computational structural biology Includes detailed chapters on druggability, allostery, complementary use of thermodynamic and kinetic information, and powerful approaches such as structural chemogenomics and fragment-based drug design Emphasizes the need for the in-depth biophysical characterization of protein targets as well as of therapeutic proteins, and for a thorough quality assessment of experimental structures Illustrates advances in the field of established therapeutic targets like kinases, serine proteinases, GPCRs, and epigenetic proteins, and of more challenging ones like protein-protein interactions and intrinsically disordered proteins
Author: Bharat B. Aggarwal
Publisher: Springer Science & Business Media
ISBN: 0387464018
Category : Medical
Languages : en
Pages : 502
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Book Description
The medicinal uses of Curcumin (also called turmeric) have been known and described for more than 5000 years. A large body of recent research suggests that curcumin is potentially useful in the treatment of inflammatory diseases, through modulation of numerous molecular targets. This is the first monograph to focus on the potential use of curcumin in the treatment of cancer, diabetes, cardiovascular diseases, arthritis, Alzheimer’s, psoriasis and more.
Author: Jean-Marc Cavaillon
Publisher: John Wiley & Sons
ISBN: 3527338993
Category : Medical
Languages : en
Pages : 1818
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Book Description
Dieses Fachbuch erläutert die molekularen Grundlagen von Entzündungen, spannt den Bogen zu Infektionskrankheiten und den Zusammenhang zwischen Entzündungen und chronischen Erkrankungen, behandelt abschließend den Heilungsprozess und zeigt Therapiemöglichkeiten.