Download or read book Structure based Drug Discovery Against a Novel Antimalarial Drug Target S adenosylmethionine Decarboxylase ornithine Decarboxylase written by Jonathan James Reynolds and published by . This book was released on 2012 with total page 208 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Download or read book Structural and Functional Validation of S adenosylmethionine Decarboxylase as a Novel Drug Target in the Malaria Parasite Plasmodium Falciparum written by Dina Coertzen and published by . This book was released on 2014 with total page 236 pages. Available in PDF, EPUB and Kindle. Book excerpt: Malaria is considered the most prevailing human parasitic disease. Despite various chemotherapeutic interventions being available, the parasite responsible for the most lethal form of malaria, Plasmodium falciparum, is continuously developing resistance towards drugs targeted against it. This, therefore, necessitates the need for validation of new antimalarial development. Polyamine biosynthetic enzymes, particularly S-adenosylmethionine-L-decarboxylase (PfAdoMetDC), has been identified as a suitable drug target for protozoan parasitic diseases due to its essential role in cell proliferation. Furthermore, in Plasmodium polyamine biosynthesis, PfAdoMetDC is organised into a unique bifunctional complex with ornithine decarboxylase (PfAdoMetDC/ODC) covalently linked by a hinge region, distinguishing this enzyme as unique a drug target. However, inhibitors targeting this pathway have not been successful in clinical assessment, creating the need for further research in identifying novel inhibitors. This study focused on the structural and functional characterisation of protein-specific properties of the AdoMetDC domain in P. falciparum parasites, as well as identifying novel inhibitors targeting this enzyme as a potential antimalarial therapeutic intervention. In order to develop novel inhibitors specifically targeting PfAdoMetDC through a structure-based drug discovery approach, the three-dimensional structure is required. However, due to a lack of structural and functional characterisation, determination of the crystal structure has been challenging. Heterologous expression of monofunctional PfAdoMetDC was achieved from a wild-type construct of the PfAdoMetDC domain including the covalently linked hinge region. In chapter 2, deletion of a large non-homologous, low-complexity parasite-specific insert (A3) in monofunctional PfAdoMetDC resulted in an increased yield, purity and sample homogeneity, whilst maintaining protein functionality and structural integrity. However, truncation of the proposed non-essential hinge region resulted in low-level expression of insoluble protein aggregates and a complete loss of protein activity, indicating that the hinge region is essential for monofunctional PfAdoMetDC. However, in the absence of the three-dimensional PfAdoMetDC crystal structure, novel derivatives of a well-known AdoMetDC inhibitor, MDL73811, were tested for their activity against heterologous PfAdoMetDC, as well as their potency against P. falciparum parasites, in chapter 3. The compound Genz-644131 was identified as a lead inhibitor of PfAdoMetDC, however, the poor membrane permeability of the compound resulted in low in vitro activity. Drug permeability of Genz-644131 into P. falciparum infected erythrocytes and its potency was significantly improved by its encapsulation into a novel immunoliposome based drug delivery system. The results presented here provide essential information for development of a unique strategy in obtaining suffiecient levels of fully active recombinant PfAdoMetDC of sufficient purity for crystallisation studies and subsequent structure-based drug design efforts. The combination of Genz-644131 with the novel drug delivery system, which markedly improved its potency against PfAdoMetDC may proof to be a viable antimalarial chemotherapeutic strategy for future investigations.

Download or read book Encyclopedia of Malaria written by and published by Springer. This book was released on 2018-07-12 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: The Encyclopedia of Malaria represents a vast databank of information about the study of malaria. It provides an overview of the historical, rapid and significant developments that have occurred in malaria research, including the 2002 genome sequencing of Plasmodium falciparum and its mosquito vector, Anopheles gambiae. This work provides a concise source of up-to-date research findings in the form of definitions and essays and present comprehensive coverage of topics from history to findings to diagnosis and treatment, written by recognized malaria researchers with practical experience. It appeals to a diverse audience, including malaria researchers, teachers, investigators and public health professionals.

Download or read book Medicinal Natural Products written by Paul M. Dewick and published by John Wiley & Sons. This book was released on 2002-01-03 with total page 524 pages. Available in PDF, EPUB and Kindle. Book excerpt: This guide covers classes of natural products in medicine, whether derived from plants, micro-organisms or animals. Structured according to biosynthetic pathway, it is written from a chemistry-based approach.

Download or read book Antituberculosis Chemotherapy written by Peter R. Donald and published by Karger Medical and Scientific Publishers. This book was released on 2011 with total page 262 pages. Available in PDF, EPUB and Kindle. Book excerpt: Tuberculosis (TB) remains one of the major infectious diseases of mankind although drugs for its treatment have been available for nearly 60 years. The standard short-course 6-month regimen used since about 1980 has helped to save millions of lives, but co-infection with HIV has had a devastating effect on the epidemic, and multidrug-resistant TB is a growing problem, particularly in communities with a high incidence of HIV. Following the declaration by the WHO in the early 1990s that TB was a 'global health emergency', interest in TB research and the development of new drugs has increased significantly. This volume reviews anti-TB chemotherapy with the emphasis on the actions and pharmacology of existing drugs and the development and evaluation of new agents. A close look is taken at new research regarding our existing drugs by some of the best-known specialists in the field, and historical aspects of these agents are reviewed from a modern perspective. The prospects for the introduction of new drugs and different approaches of how to assess them in adults and in children are discussed in detail. Several papers address the problems associated with drug resistance, its spread and diagnosis. Compiled by two editors from Cape Town, which has a particularly high incidence of TB and is a centre of tuberculosis research, this publication is an indispensable reference for anyone involved in the management of TB either as a researcher, clinician or administrator, and those working in drug development.

Download or read book Toxoplasma Gondii written by Louis M. Weiss and published by Academic Press. This book was released on 2020-02-28 with total page 1244 pages. Available in PDF, EPUB and Kindle. Book excerpt: Toxoplasma gondii: The Model Apicomplexan - Perspectives and Methods, Third Edition, reflects significant advances in the field in the last five years, including new information on the genomics, epigenomics and proteomics of T. gondii, along with a new understanding of the population biology and genetic diversity of this organism. This edition expands information on the effects of T. gondii on human psychiatric disease and new molecular techniques, such as CAS9/CSPR. T gondii remains the best model system for studying the entire Apicomplexa group of protozoans, which includes Malaria, making this new edition essential for a broad group of researchers and scientists. Presents a complete review of molecular and cellar biology and immunology of Toxoplasma gondii combined with methods and resources for working with this pathogen Provides a single source reference for a wide range of scientists and physicians working with this pathogen, including parasitologists, cell and molecular biologists, veterinarians, neuroscientists, physicians and food scientists Covers recent advances in the genomics, related bioinformatics analysis, epigenomics, gene regulation, genetic manipulation and proteomics of T. gondii Details advances in the molecular and cellular biology and immunology of Toxoplasma, and in the epidemiology, diagnosis, treatment and prevention of toxoplasmosis

Download or read book Comprehensive Analysis of Parasite Biology written by Sylke Müller and published by John Wiley & Sons. This book was released on 2016-10-10 with total page 574 pages. Available in PDF, EPUB and Kindle. Book excerpt: Written and edited by experts in the field, this book brings together the current state of the art in phenotypic and rational, target-based approaches to drug discovery against pathogenic protozoa. The chapters focus particularly on virtual compounds and high throughput screening, natural products, computer-assisted drug design, structure-based drug design, mechanism of action identification, and pathway modelling. Furthermore, state-of the art "omics" technologies are described and currently studied enzymatic drug targets are discussed. Mathematical, systems biology-based approaches are introduced as new methodologies for dissecting complex aspects of pathogen survival mechanisms and for target identification. In addition, recently developed anti-parasitic agents targeting particular pathways, which serve as lead compounds for further drug development, are presented.

Download or read book Drug Resistance in Leishmania Parasites written by Alicia Ponte-Sucre and published by Springer Science & Business Media. This book was released on 2012-09-04 with total page 458 pages. Available in PDF, EPUB and Kindle. Book excerpt: One of the main problems concerning therapeutic tools for the treatment of parasitic diseases, including leishmaniasis, is that some field parasites are naturally resistant to the classical drugs; additionally, current therapies may select parasites prone to be resistant to the applied drugs. These features are (at least partially) responsible for the disappointing persistence of the disease and resultant deaths worldwide. This book provides a comprehensive view of the pathology of the disease itself, and of parasitic drug resistance, its molecular basis, consequences and possible treatments. Scientists both from academic fields and from the industry involved in biomedical research and drug design, will find in this book a valuable and fundamental guide that conveys the knowledge needed to understand and to improve the success in combating this disease worldwide.

Download or read book Chemistry of Antibiotics and Related Drugs written by Mrinal K. Bhattacharjee and published by Springer Nature. This book was released on 2022-08-23 with total page 276 pages. Available in PDF, EPUB and Kindle. Book excerpt: This textbook builds on the success of the earlier edition, offering alternative strategies for discovering new antibiotics. It discusses how the various types of antibiotics and related drugs work to cure infections. Then it delves into the very serious matter of how bacteria are becoming resistant to these antibiotics. It also covers the global action plan on antimicrobial resistance from the World Health Organization and discusses several Antibiotic Stewardship Programs adopted by agencies at local levels. Appropriate for a one-semester course at either the graduate or advanced undergraduate level, the book is self-contained and written in accessible language. It includes all necessary background biochemistry material and a discussion of the latest developments in the field of antibiotics. Original research works are frequently cited and experimental procedures and interpretation of results are emphasized.

Download or read book Toxicoepigenetics written by Shaun D. McCullough and published by Academic Press. This book was released on 2018-11-02 with total page 430 pages. Available in PDF, EPUB and Kindle. Book excerpt: Toxicoepigenetics: Core Principles and Applications examines the core aspects of epigenetics, including chromatin biology, DNA methylation, and non-coding RNA, as well as fundamental techniques and considerations for studying each of these mechanisms of epigenetic regulation. Although its integration into the field of toxicology is in its infancy, epigenetics have taken center stage in the study of diseases such as cancer, diabetes, and neurodegeneration. Increasing the presence of epigenetics in toxicological research allows for a more in-depth understanding of important aspects of toxicology such as the role of the environment and lifestyle influencing the individual susceptibility to these effects and the trans-generational transmission of these health effects and susceptibilities. Methods chapters are included to help improve efficacy and efficiency of protocols in both the laboratory and the classroom. Toxicoepigenetics: Core Principles and Applications is an essential book for researchers and academics using epigenetics in toxicology research and study. Introduces the fundamental principles and practices for understanding the role of the epigenome in toxicology Presents the foundation of epigenetics for toxicologists with a broad range of backgrounds Discusses the incorporation of epigenetics and epigenomics into current toxicological studies and interpretation of epigenetic data in toxicological applications

Download or read book Epigenetics of Aging written by Trygve O. Tollefsbol and published by Springer Science & Business Media. This book was released on 2009-11-11 with total page 462 pages. Available in PDF, EPUB and Kindle. Book excerpt: Recent studies have indicated that epigenetic processes may play a major role in both cellular and organismal aging. These epigenetic processes include not only DNA methylation and histone modifications, but also extend to many other epigenetic mediators such as the polycomb group proteins, chromosomal position effects, and noncoding RNA. The topics of this book range from fundamental changes in DNA methylation in aging to the most recent research on intervention into epigenetic modifications to modulate the aging process. The major topics of epigenetics and aging covered in this book are: 1) DNA methylation and histone modifications in aging; 2) Other epigenetic processes and aging; 3) Impact of epigenetics on aging; 4) Epigenetics of age-related diseases; 5) Epigenetic interventions and aging: and 6) Future directions in epigenetic aging research. The most studied of epigenetic processes, DNA methylation, has been associated with cellular aging and aging of organisms for many years. It is now apparent that both global and gene-specific alterations occur not only in DNA methylation during aging, but also in several histone alterations. Many epigenetic alterations can have an impact on aging processes such as stem cell aging, control of telomerase, modifications of telomeres, and epigenetic drift can impact the aging process as evident in the recent studies of aging monozygotic twins. Numerous age-related diseases are affected by epigenetic mechanisms. For example, recent studies have shown that DNA methylation is altered in Alzheimer’s disease and autoimmunity. Other prevalent diseases that have been associated with age-related epigenetic changes include cancer and diabetes. Paternal age and epigenetic changes appear to have an effect on schizophrenia and epigenetic silencing has been associated with several of the progeroid syndromes of premature aging. Moreover, the impact of dietary or drug intervention into epigenetic processes as they affect normal aging or age-related diseases is becoming increasingly feasible.

Download or read book Essentials of Bioinformatics Volume I written by Noor Ahmad Shaik and published by Springer. This book was released on 2019-03-27 with total page 405 pages. Available in PDF, EPUB and Kindle. Book excerpt: Bioinformatics is an integrative field of computer science, genetics, genomics, proteomics, and statistics, which has undoubtedly revolutionized the study of biology and medicine in past decades. It mainly assists in modeling, predicting and interpreting large multidimensional biological data by utilizing advanced computational methods. Despite its enormous potential, bioinformatics is not widely integrated into the academic curriculum as most life science students and researchers are still not equipped with the necessary knowledge to take advantage of this powerful tool. Hence, the primary purpose of our book is to supplement this unmet need by providing an easily accessible platform for students and researchers starting their career in life sciences. This book aims to avoid sophisticated computational algorithms and programming. Instead, it mostly focuses on simple DIY analysis and interpretation of biological data with personal computers. Our belief is that once the beginners acquire these basic skillsets, they will be able to handle most of the bioinformatics tools for their research work and to better understand their experimental outcomes. Unlike other bioinformatics books which are mostly theoretical, this book provides practical examples for the readers on state-of-the-art open source tools to solve biological problems. Flow charts of experiments, graphical illustrations, and mock data are included for quick reference. Volume I is therefore an ideal companion for students and early stage professionals wishing to master this blooming field.

Download or read book Omics Technologies and Bio engineering written by Debmalya Barh and published by Academic Press. This book was released on 2017-12-01 with total page 645 pages. Available in PDF, EPUB and Kindle. Book excerpt: Omics Technologies and Bio-Engineering: Towards Improving Quality of Life, Volume 1 is a unique reference that brings together multiple perspectives on omics research, providing in-depth analysis and insights from an international team of authors. The book delivers pivotal information that will inform and improve medical and biological research by helping readers gain more direct access to analytic data, an increased understanding on data evaluation, and a comprehensive picture on how to use omics data in molecular biology, biotechnology and human health care. Covers various aspects of biotechnology and bio-engineering using omics technologies Focuses on the latest developments in the field, including biofuel technologies Provides key insights into omics approaches in personalized and precision medicine Provides a complete picture on how one can utilize omics data in molecular biology, biotechnology and human health care

Download or read book Alkaloids Secrets of Life written by Tadeusz Aniszewski and published by Elsevier. This book was released on 2007-03-22 with total page 325 pages. Available in PDF, EPUB and Kindle. Book excerpt: Alkaloids, represent a group of interesting and complex chemical compounds, produced by the secondary metabolism of living organisms in different biotopes. They are relatively common chemicals in all kingdoms of living organisms in all environments. Two hundred years of scientific research has still not fully explained the connections between alkaloids and life. Alkaloids-Chemistry, Biological Significance, Applications and Ecological Role provides knowledge on structural typology, biosynthesis and metabolism in relation to recent research work on alkaloids. Considering an organic chemistry approach to alkaloids using biological and ecological explanation. Within the book several questions that persist in this field of research are approached as are some unresearched areas. The book provides beneficial text for an academic and professional audience and serves as a source of knowledge for anyone who is interested in the fascinating subject of alkaloids. Each chapter features an abstract. Appendices are included, as are a listing of alkaloids, plants containing alkaloids and some basic protocols of alkaloid analysis. * Presents the ecological role of alkaloids in nature and ecosystems * Interdisciplinary and reader friendly approach * Up-to-date knowledge

Download or read book Approaches to Design and Synthesis of Antiparasitic Drugs written by N. Anand and published by Elsevier. This book was released on 1997-07-10 with total page 525 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book presents a comprehensive and up to date account of the chemotherapy of parasitic diseases, both human and veterinary. The book starts with an overview of parasitic diseases. The body of the book is divided into two parts: antihelminthic drugs, and antiprotozoal drugs. Both parts start with chapters highlighting the 'biochemical targets' available for chemotherapeutic interference. Individual chapters deal with one chemical class of compounds and describe their origin, structure-activity relationship, mode of action, and methods of synthesis and their status both in clinical and veterinary practice. The book will be useful to a wide spectrum of readers: students embarking on a research career in parasitic chemotherapy, clinicians (and veterinarians) and clinical pharmacologists desiring detailed information about the drugs currently in use, and pharmaceutical technologists wanting to update their knowledge of the methods of manufacture.

Download or read book CRC Handbook of Medicinal Spices written by James A. Duke and published by CRC Press. This book was released on 2002-09-27 with total page 360 pages. Available in PDF, EPUB and Kindle. Book excerpt: "Let food be your medicine, medicine your food."-Hippocrates, 2400 B.C.When the "Father of Medicine" uttered those famous words, spices were as important for medicine, embalming, preserving food, and masking bad odors as they were for more mundane culinary matters. Author James A. Duke predicts that spices such as capsicum, cinnamon, garlic, ginger

Download or read book Polyamines written by Anthony E. Pegg and published by Humana Press. This book was released on 2011-04-06 with total page 524 pages. Available in PDF, EPUB and Kindle. Book excerpt: Recently, important new findings in the polyamine field and a variety of new experimental systems have revolutionized the study of these ubiquitous cellular components, essential for normal growth and development. In Polyamines: Methods and Protocols, leading researchers contribute an extensive collection of up-to-date laboratory techniques for the further pursuit of polyamine study. The volume delves into vital subjects such as neoplasia studies with animal models and human patients, therapeutic roles for polyamine inhibitors and analogs, polyamine metabolism and oxidative damage, polyamines as regulators of critical ion channels, as well as polyamine transport systems and polyamine-responsive genes. 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 expert notes on troubleshooting and avoiding known pitfalls. Comprehensive and cutting-edge, Polyamines: Methods and Protocols provides a key resource for all scientists pursuing the study of this dynamic and significant aspect of cellular biology.