Cox 2

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Improved Non-Steroid Anti-Inflammatory Drugs: COX-2 Enzyme Inhibitors

Author : Sir John R. Vane,Jack H. Botting,R.M. Botting
Publisher : Springer Science & Business Media
Page : 249 pages
File Size : 47,5 Mb
Release : 2012-12-06
Category : Medical
ISBN : 9789401090292

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Improved Non-Steroid Anti-Inflammatory Drugs: COX-2 Enzyme Inhibitors by Sir John R. Vane,Jack H. Botting,R.M. Botting Pdf

In 1971, Vane proposed that the mechanism of action of the aspirin-like drugs was through their inhibition of prostaglandin biosynthesis. Since then, there has been intense interest in the interaction between this diverse group of inhibitors and the enzyme known as cyclooxygenase (COX). It exists in two isoforms, COX-l and COX-2 (discovered some 5 years ago). Over the last two decades several new drugs have reached the market based on COX-l enzyme screens. Elucidation of the three-dimensional structure of COX-l has provided a new understanding for the actions of COX inhibitors. The constitutive isoform of COX, COX-l has clear physiological functions. Its activation leads, for instance, to the production of prostacyclin which when released by the endothelium is anti-thrombogenic and anti-atherosclerotic, and in the gastric mucosa is cyto protective. COX-l also generates prostaglandins in the kidney, where they help to maintain blood flow and promote natriuresis. The inducible isoform, COX-2, was discovered through its activity being increased in a number of cells by pro inflammatory stimuli. A year or so later, COX-2 was identified as a distinct isoform encoded by a different gene from COX-I. COX-2 is induced by inflammatory stimuli and by cytokines in migratory and other cells. Thus the anti-inflammatory actions of non-steroid anti-inflammatory drugs (NSAIDs) may be due to the inhibition of COX-2, whereas the unwanted side-effects such as irritation of the stomach lining and toxic effects on the kidney are due to inhibition of the constitutive enzyme, COX-I.

Selective COX-2 Inhibitors

Author : Sir John R. Vane,Jack H. Botting
Publisher : Springer Science & Business Media
Page : 153 pages
File Size : 47,5 Mb
Release : 2012-12-06
Category : Medical
ISBN : 9789401148726

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Selective COX-2 Inhibitors by Sir John R. Vane,Jack H. Botting Pdf

The mainstay of therapy for rheumatoid disease is the non-steroid antiinflammatory drugs (NSAIDs), despite their inherent gastrointestinal toxicity and ability to cause renal damage in susceptible patients. The theory that the beneficial and toxic effects of NSAIDs stem from a reduction in prostanoid production through inhibition of cyclooxygenase implied that particular toxicities were inevitable with NSAIDs and would always be correlated with efficacy. However, over the years, it became apparent that at therapeutic doses, some NSAIDs had greater toxic side-effects than others, a fact not explained by the general theory. A significant clarification arose from the discovery that there are two distinct isoforms of COX, a constitutive enzyme (COX-I) responsible for the production of prostanoids necessary for platelet aggregation and protection of the gastric mucosa and kidney; and an inducible enzyme (COX-2) that is newly synthesized at sites of tissue damage and produces prostaglandins that manifest pathological effects. It became clear that different NSAIDs had greater or lesser effects on COX-I when used in therapeutic doses, explaining the variation in side-effects. ' The elucidation of the crystal structure of these different enzymes and the skills of medicinal chemists have led to the synthesis of new chemicals with a selectivity for the inducible enzyme, and thus with therapeutic efficacy without those toxic effects result ing from inhibition of the constitutive enzyme.

COX-2 Inhibitor Research

Author : Maynard J. Howardell
Publisher : Nova Publishers
Page : 274 pages
File Size : 44,6 Mb
Release : 2006
Category : Medical
ISBN : 159454994X

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COX-2 Inhibitor Research by Maynard J. Howardell Pdf

COX-2 Inhibitors are newly developed drugs for inflammation that selectively block the COX-2 enzyme. Blocking this enzyme impedes the production of the chemical messengers (prostaglandins) that cause the pain and swelling of arthritis inflammation. Cox-2 inhibitors are a new class of nonsteroidal anti-inflammatory drugs (NSAIDS). Because they selectively block the Cox-2 enzyme and not the Cox-1 enzyme, these drugs are uniquely different from traditional NSAIDS. This book explores new research in this field.

Cox-2

Author : Joseph R. Bertino,Andrew J. Dannenberg,Raymond N. DuBois
Publisher : Karger Medical and Scientific Publishers
Page : 300 pages
File Size : 50,5 Mb
Release : 2003-01-01
Category : Medical
ISBN : 9783805575362

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Cox-2 by Joseph R. Bertino,Andrew J. Dannenberg,Raymond N. DuBois Pdf

Numerous investigators have found increased levels of cyclooxygenase-2 (COX-2) in both premalignant and malignant tissues. Moreover, animals engineered to be COX-2 deficient or treated with a selective COX-2 inhibitor showed reduced tumor formation and growth. The present book reviews these findings suggesting that COX-2 is a valid molecular target for the prevention and treatment of cancer. The first chapters are devoted to the epidemiology of nonsteroidal anti-inflammatory drugs (NSAIDs) and cancer, the pharmacology of COX-2 inhibitors and the regulation of COX-2 expression in human cancers. Besides, the book contains a series of chapters examining the link between COX-2 and cancer in specific organs (e.g. skin, breast, cervix, digestive tract, lung, etc.). Furthermore, several clinical trials assessing the potential of COX-2 inhibitors for preventing and treating cancer are described. The final chapter provides an up-to-date consideration of COX-independent targets of NSAIDs and related compounds in cancer prevention and treatment. This state-of-the-art publication is recommended reading not only for medical and radiation oncologists, but also for pharmacologists, gastroenterologists and other subspecialists.

Trends in COX-2 Inhibitor Research

Author : Maynard J. Howardell
Publisher : Nova Publishers
Page : 184 pages
File Size : 54,6 Mb
Release : 2006
Category : Anti-inflammatory agents
ISBN : 1600212220

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Trends in COX-2 Inhibitor Research by Maynard J. Howardell Pdf

Cox-2 Inhibitors are newly developed drugs for inflammation that selectively block the Cox-2 enzyme. Blocking this enzyme impedes the production of the chemical messengers (prostaglandins) that cause the pain and swelling of arthritis inflammation. Cox-2 inhibitors are a new class of non-steroidal anti-inflammatory drugs (NSAIDS). Because they selectively block the Cox-2 enzyme and not the Cox-1 enzyme, these drugs are uniquely different from traditional NSAIDS. This book explores new research in the field.

COX-2 Blockade in Cancer Prevention and Therapy

Author : Randall E. Harris
Publisher : Springer Science & Business Media
Page : 641 pages
File Size : 46,9 Mb
Release : 2002-10-03
Category : Medical
ISBN : 9781592593026

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COX-2 Blockade in Cancer Prevention and Therapy by Randall E. Harris Pdf

The revelation that aspirin and aspirin-like compounds have notableantineo plastic properties has revolutionized cancer research. COX-2 Blockade in Cancer Prevention and Therapy chronicles the evidence and presents exciting new op portunities for the use of cyclooxygenase-2 (COX-2) blockade in the prevention and treatment of cancer. The text is divided broadly into five areas. First, an historical overview documents the scientific discovery ofCOX-2 and the pharma ceutical development of nonsteroidal anti-inflammatory drugs (NSAIDs) designed for selective COX-2 inhibition. The process by which essential poly unsaturated fatty acids (PUF As) stimulate prostaglandin biosynthesis and cancer development, and its interruption by COX-2 inhibition, is elucidated. This is followed by a section on the epidemiology of NSAIDs and cancers of the colon and breast, and other anatomic sites. These chapters reflect significant cancer protection owing to the regular use of common NSAIDs such as aspirin and ibuprofen. A section on animal models of carcinogenesis presents comprehensive evidence that general NSAIDs inhibit a variety of malignant neoplasms in vivo, and highlights recent findings which show that COX-2 blocking agents produce striking chemopreventive effects against colon cancer and breast cancer as well as other malignancies. Genetic models are presented confirming the critical role of COX-2 in carcinogenesis. Section IV then discusses the molecular biology of COX -2 vis-a-vis the role of COX -2 and, to a lesser extent, COX -1, in modulating a number of important processes in molecular carcinogenesis such as mutagen esis, cell division, angiogenesis, cell differentiation, and apoptosis.

Synthesis and biological evaluation of 1,5-diphenylpyrrole derivatives as COX-2 selective inhibitors and NO-releasing agents and development of a novel BRD9 chemical probe

Author : Sara Consalvi
Publisher : Sapienza Università Editrice
Page : 130 pages
File Size : 50,6 Mb
Release : 2020-06-30
Category : Science
ISBN : 9788893771375

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Synthesis and biological evaluation of 1,5-diphenylpyrrole derivatives as COX-2 selective inhibitors and NO-releasing agents and development of a novel BRD9 chemical probe by Sara Consalvi Pdf

This PhD thesis consists of three projects: the first and the second ones, carried out at Sapienza University of Rome, deal with the design and synthesis of novel COX-2 selective inhibitors and dual COX-2 inhibitors/NO-releasing agents, respectively. The third project concerns the development of a novel BRD9 chemical probe and was realized at the University of Oxford (Department of Chemistry).

Eicosanoids and Other Bioactive Lipids in Cancer, Inflammation and Radiation Injury

Author : Santosh Nigam,Kenneth V. Honn,Lawrence J. Marnett,Thomas Walden Jr.
Publisher : Springer Science & Business Media
Page : 765 pages
File Size : 45,6 Mb
Release : 2012-12-06
Category : Medical
ISBN : 9781461535201

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Eicosanoids and Other Bioactive Lipids in Cancer, Inflammation and Radiation Injury by Santosh Nigam,Kenneth V. Honn,Lawrence J. Marnett,Thomas Walden Jr. Pdf

In recent decades eicosanoids have been attracting an increasing amount of attention as a result of their important physiological roles in many areas of biology and medicine. The eicosanoids comprise the prostaglandins, thromboxanes and leukotrienes and are products of arachidonic acid, an essential polyunsaturated fatty acid stored in tissue phospholipids. Disturbances of eicosanoids and their metabolic products play a regulatory role in many types of cell injuries and diseases. One of the most exciting areas of eicosanoid research pinpoints their participation in the control of cell proliferation and differentiation. Eicosanoids form a link between different fields of research into such areas as cancer, inflammation and radiation-induced injury. This link provided the impetus for the development of the conference series of which the present volume represents the proceedings of the Second International Conference, held in Berlin in October 1991.

COX-2 Inhibitors

Author : Michel Pairet,Joanne van Ryn
Publisher : Springer Science & Business Media
Page : 264 pages
File Size : 53,9 Mb
Release : 2004-03-29
Category : Medical
ISBN : 3764369019

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COX-2 Inhibitors by Michel Pairet,Joanne van Ryn Pdf

COX-2 inhibitors are important drugs with analgesic and anti-inflammatory effects. The discovery of COX-2, the evolution of drug development in this field and the implications of these developments in patient therapy are topics of this volume. This book presents both pre-clinical and clinical information and is important for clinicians interested in the latest information about this class of drugs, for researchers and for students in the field.

COX-2 Inhibitors

Author : Michel Pairet,Joanne van Ryn
Publisher : Birkhäuser
Page : 255 pages
File Size : 42,8 Mb
Release : 2012-12-06
Category : Medical
ISBN : 9783034878791

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COX-2 Inhibitors by Michel Pairet,Joanne van Ryn Pdf

COX-2 inhibitors are important drugs with analgesic and anti-inflammatory effects. The discovery of COX-2, the evolution of drug development in this field and the implications of these developments in patient therapy are topics of this volume. This book presents both pre-clinical and clinical information and is important for clinicians interested in the latest information about this class of drugs, for researchers and for students in the field.

Eicosanoids and Other Bioactive Lipids in Cancer, Inflammation, and Radiation Injury, 5

Author : Kenneth V. Honn,Lawrence J. Marnett,Santosh Nigam,Charles N. Serhan,Edward A. Dennis
Publisher : Springer Science & Business Media
Page : 592 pages
File Size : 41,8 Mb
Release : 2012-12-06
Category : Science
ISBN : 9781461501930

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Eicosanoids and Other Bioactive Lipids in Cancer, Inflammation, and Radiation Injury, 5 by Kenneth V. Honn,Lawrence J. Marnett,Santosh Nigam,Charles N. Serhan,Edward A. Dennis Pdf

This volume represents a collection of contributions from the 6th International Conference on Eicosanoids and Other Bioactive Lipids in Cancer, Inflammation, and Related Diseases held in Boston from September 12-15, 1999. The mission of this meeting was to bring together senior and junior investigators to both announce and examine their recent advancements in cutting-edge research on the roles and actions of lipid mediators and their impact in human physiology and disease pathogenesis. The meeting focused on new concepts in these areas of interest to both clinicians and researchers. The program included several outstanding plenary lectures and presentations by leading experts in the fields of cancer and inflammation. In addition, the Boston meeting presented three Young Investigator awards, one in each of the major focus areas. The meeting was exciting and proved to be very memorable. The program was developed with an emphasis on recent advances in molecular and of lipid mediators relevant in cellular mechanisims involved in the formation and actions inflammation and cancer. Plenary lectures were presented by Prof. Bengt Sammuelsson (Karolinska Institute, Stockholm; 1982 Nobel Laureate in Physiology or Medicine) and Prof. E. 1. Corey (Harvard University; 1990 Nobel Laureate in Chemistry). Both of these plenary lectures were held on Day 1, which set an exciting tone for this meeting. Immediately following these plenary lectures, three simultaneous breakout sessions were held, one of inflammation, a second on cancer and synthesis of novel inhibitors, and a third on enzymes-lipoxygenases/cyclooxygenases and inhibitors.

The Essence of Analgesia and Analgesics

Author : Raymond S. Sinatra,Jonathan S. Jahr,J. Michael Watkins-Pitchford
Publisher : Cambridge University Press
Page : 551 pages
File Size : 47,5 Mb
Release : 2010-10-14
Category : Medical
ISBN : 9781139491983

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The Essence of Analgesia and Analgesics by Raymond S. Sinatra,Jonathan S. Jahr,J. Michael Watkins-Pitchford Pdf

The Essence of Analgesia and Analgesics is an invaluable practical resource for clinicians giving pain relief in any clinical setting, describing the pharmacologic principles and clinical use of all available pain medications. As well as detailed overviews of pain processing and analgesic theory, sections are dedicated to oral and panteral opioid analgesics, neuraxial opioids, NSAIDs, local anesthetics, anticonvulsant type analgesics, NMDA antagonists, alpha adrenergic analgesics, antidepressant analgesics, muscle relaxants, adjuvant medications, and new and emerging analgesics. The concise format of the chapters allows for quick and easy reading and assimilation of information. Enhanced by summary tables and figures, each chapter provides an overview of a particular drug, covering chemical structure, mode of activity, indications, contraindications, common doses and uses, advantages and disadvantages, and drug related adverse events. Key references are also provided. Edited by leading experts in pain management, this is essential reading for any clinician involved in pain management.

Primes of the Form x2 + ny2

Author : David A. Cox
Publisher : John Wiley & Sons
Page : 372 pages
File Size : 40,9 Mb
Release : 2011-10-24
Category : Mathematics
ISBN : 9781118031001

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Primes of the Form x2 + ny2 by David A. Cox Pdf

Modern number theory began with the work of Euler and Gauss to understand and extend the many unsolved questions left behind by Fermat. In the course of their investigations, they uncovered new phenomena in need of explanation, which over time led to the discovery of field theory and its intimate connection with complex multiplication. While most texts concentrate on only the elementary or advanced aspects of this story, Primes of the Form x2 + ny2 begins with Fermat and explains how his work ultimately gave birth to quadratic reciprocity and the genus theory of quadratic forms. Further, the book shows how the results of Euler and Gauss can be fully understood only in the context of class field theory. Finally, in order to bring class field theory down to earth, the book explores some of the magnificent formulas of complex multiplication. The central theme of the book is the story of which primes p can be expressed in the form x2 + ny2. An incomplete answer is given using quadratic forms. A better though abstract answer comes from class field theory, and finally, a concrete answer is provided by complex multiplication. Along the way, the reader is introduced to some wonderful number theory. Numerous exercises and examples are included. The book is written to be enjoyed by readers with modest mathematical backgrounds. Chapter 1 uses basic number theory and abstract algebra, while chapters 2 and 3 require Galois theory and complex analysis, respectively.

Beneficial Effects of Fish Oil on Human Brain

Author : Akhlaq A. Farooqui
Publisher : Springer Science & Business Media
Page : 409 pages
File Size : 53,8 Mb
Release : 2009-07-14
Category : Medical
ISBN : 9781441905437

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Beneficial Effects of Fish Oil on Human Brain by Akhlaq A. Farooqui Pdf

It is becoming increasingly evident that the deficiency of n-3 fatty acids in diet is not only associated with cardiovascular diseases, but also involved in stroke, epilepsy and other neurological and neurodegenerative diseases, such as Alzheimer disease, Parkinson disease, and peroxisomal diseases. In his newest book, Beneficial Effects of Fish Oil on Human Brain, Dr. Akhlaq A. Farooqui expands on the status and therapeutic importance of n-3 fatty acids (major components of fish oil) and their mediators in normal brain and those with neurodegenerative and neuropsychiatric diseases. Farooqui presents the benefits of n-3 fatty acids on Western diet, which is enriched in n-6 fatty acids (major components of vegetable oil) and may promote the above neurological disorders. The book will present readers with cutting edge and comprehensive information on metabolism and roles of neural membrane n-3 fatty acids.

Inflammation in the Pathogenesis of Chronic Diseases

Author : Randall E. Harris
Publisher : Springer
Page : 0 pages
File Size : 54,9 Mb
Release : 2010-11-22
Category : Medical
ISBN : 9048174295

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Inflammation in the Pathogenesis of Chronic Diseases by Randall E. Harris Pdf

In this book, a worldwide panel of leading experts discuss the role of inflammation in the pathogenesis of major chronic diseases and the current controversy regarding risk versus benefit of selective cyclooxygenase-2 (COX-2) inhibitors. The authors provide exciting and enlightening perspectives on COX-2 and related molecular targets in the future of medicine, including historical perspectives.