Download or read book In Vitro and in Vivo Pharmacologic Evaluation of Novel Lysophospholipid Analogs as Anticancer Agents written by and published by . This book was released on 2005 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt: Lysophospholipids are phospholipid growth factors that promote tumor cell proliferation, survival, and invasion by binding to a family of G protein-coupled receptors. Due to their involvement in cancer progression and overexpression of their receptors in cancer, novel agents that inhibit molecules in the lysophospholipid signal transduction pathways hold promise as potential chemotherapeutic agents. Prostate cancer presents a unique disease model to study the role of lysophospholipid growth factor signaling pathways. Different human prostate cancer cell lines represent a wide range of clinically relevant prostate tumor types demonstrating various stages of the disease, different sites of metastasis, and differences in androgen dependence for cell growth. Moreover, these cell lines demonstrate differential expression and activity profiles of the LPL receptors and downstream mediators including PTEN lipid phosphatase and AKT and MAPK. Three classes of lysophospholipid analogs were synthesized and tested in prostate cancer cell lines and a negative control cell line that lacks lysophospholipid receptors. Active serine amide derivatives showed potency similar to that of 5-fluorouracil, but they also affected growth of the negative control cell line. Thiazolidinone analogs were equipotent to serine amides with improved selectivity. Thiazolidine analogs were the most potent and selective of all three groups of lysophospholipid analogs examined. Further, thiazolidine analogs almost completely inhibited AKT phosphorylation, consequently inducing apoptosis. However, these analogs failed to interact directly with lysophosphatidic acid receptors as proven by absence of inhibitory action on lysophosphatidic acid-driven calcium mobilization. Two thiazolidine analogs were chosen for assessment of in vivo anticancer activity. Daily intraperitoneal doses of these analogs significantly delayed PC-3 xenograft tumor growth, validating the importance of LPL receptor and/or downstream signal transduction pathways in growth and progression of prostate tumors. Thiazolidine analogs also enhanced bicalutamide activity in vitro by 2- to 30-fold in both androgen-dependent and androgen-independent prostate cancer cell lines. In conclusion, lysophospholipid signal transduction pathways can be exploited to provide a novel modality for prostate cancer treatment. Identification of target proteins and improvement of intrinsic activity, selectivity profile, and pharmacokinetic properties will hopefully lead to an increase in the in vivo efficacy of this series of lysophospholipid analogs.

Download or read book Dissertation Abstracts International written by and published by . This book was released on 2006 with total page 860 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Download or read book Index Medicus written by and published by . This book was released on 2004 with total page 1938 pages. Available in PDF, EPUB and Kindle. Book excerpt: Vols. for 1963- include as pt. 2 of the Jan. issue: Medical subject headings.

Download or read book Cumulated Index Medicus written by and published by . This book was released on 1992 with total page 1444 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Download or read book Chagas disease novel drug targets and treatments written by Vilma G. Duschak and published by Frontiers Media SA. This book was released on 2023-06-22 with total page 129 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Download or read book Exocytosis and Endocytosis written by Andrei I. Ivanov and published by Springer Science & Business Media. This book was released on 2008 with total page 407 pages. Available in PDF, EPUB and Kindle. Book excerpt: In this book, skilled experts provide the most up-to-date, step-by-step laboratory protocols for examining molecular machinery and biological functions of exocytosis and endocytosis in vitro and in vivo. The book is insightful to both newcomers and seasoned professionals. It offers a unique and highly practical guide to versatile laboratory tools developed to study various aspects of intracellular vesicle trafficking in simple model systems and living organisms.

Download or read book Autophagy Cancer Other Pathologies Inflammation Immunity Infection and Aging written by M. A. Hayat and published by Academic Press. This book was released on 2016-12-28 with total page 431 pages. Available in PDF, EPUB and Kindle. Book excerpt: Autophagy: Cancer, Other Pathologies, Inflammation, Immunity, Infection, and Aging is an eleven volume series that discusses in detail all aspects of autophagy machinery in the context of health, cancer, and other pathologies. Autophagy maintains homeostasis during starvation or stress conditions by balancing the synthesis of cellular components and their deregulation by autophagy. This series discusses the characterization of autophagosome-enriched vaccines and its efficacy in cancer immunotherapy. Autophagy serves to maintain healthy cells, tissues, and organs, but also promotes cancer survival and growth of established tumors. Impaired or deregulated autophagy can also contribute to disease pathogenesis. Understanding the importance and necessity of the role of autophagy in health and disease is vital for the studies of cancer, aging, neurodegeneration, immunology, and infectious diseases. Comprehensive and forward-thinking, these books offer a valuable guide to cellular processes while also inciting researchers to explore their potentially important connections. Presents the most advanced information regarding the role of the autophagic system in life and death Examines whether autophagy acts fundamentally as a cell survivor or cell death pathway or both Introduces new, more effective therapeutic strategies in the development of targeted drugs and programmed cell death, providing information that will aid in preventing detrimental inflammation Features recent advancements in the molecular mechanisms underlying a large number of genetic and epigenetic diseases and abnormalities, including atherosclerosis and CNS tumors, and their development and treatment Includes chapters authored by leaders in the field around the globe—the broadest, most expert coverage available

Download or read book Diversity Oriented Synthesis written by Andrea Trabocchi and published by John Wiley & Sons. This book was released on 2013-06-17 with total page 550 pages. Available in PDF, EPUB and Kindle. Book excerpt: Discover an enhanced synthetic approach to developing and screening chemical compound libraries Diversity-oriented synthesis is a new paradigm for developing large collections of structurally diverse small molecules as probes to investigate biological pathways. This book presents the most effective methods in diversity-oriented synthesis for creating small molecule collections. It offers tested and proven strategies for developing diversity-oriented synthetic libraries and screening methods for identifying ligands. Lastly, it explores some promising new applications based on diversity-oriented synthesis that have the potential to dramatically advance studies in drug discovery and chemical biology. Diversity-Oriented Synthesis begins with an introductory chapter that explores the basics, including a discussion of the relationship between diversity-oriented synthesis and classic combinatorial chemistry. Divided into four parts, the book: Offers key chemical methods for the generation of small molecules using diversity-oriented principles, including peptidomimetics and macrocycles Expands on the concept of diversity-oriented synthesis by describing chemical libraries Provides modern approaches to screening diversity-oriented synthetic libraries, including high-throughput and high-content screening, small molecule microarrays, and smart screening assays Presents the applications of diversity-oriented synthetic libraries and small molecules in drug discovery and chemical biology, reporting the results of key studies and forecasting the role of diversity-oriented synthesis in future biomedical research This book has been written and edited by leading international experts in organic synthesis and its applications. Their contributions are based on a thorough review of the current literature as well as their own firsthand experience developing synthetic methods and applications. Clearly written and extensively referenced, Diversity-Oriented Synthesis introduces novices to this highly promising field of research and serves as a springboard for experts to advance their own research studies and develop new applications.

Download or read book Targeted Intracellular Drug Delivery by Receptor Mediated Endocytosis written by Padma V. Devarajan and published by Springer Nature. This book was released on 2019-11-09 with total page 560 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book elaborates on drug delivery targeting via intracellular delivery, specifically through the Receptor Mediated Endocytosis (RME) approach, due to the involvement of cellular receptors in various grave diseases. Targeted delivery relies on two basic approaches, passive and active targeting. While passive targeting approaches have shown great promise, the improved selectivity achieved with active targeting approaches has resulted in significantly higher efficacy. Interestingly there are numerous strategies for active targeting, many of which are already highlighted in , Targeted Drug Delivery: Concepts and Applications. Nevertheless an exciting and practical strategy for active targeting, which could enable high intracellular delivery, is through exploitation of RME. Cells in the body express receptors to enable various physiological and biochemical processes. As a result, many of these receptors are overexpressed in pathological conditions, or newer receptors expressed due to defective cellular functioning. RME is based on exploitation of such receptors to achieve intracellular delivery. While targeted delivery can have manifold applications, in this book we focus on two major and challenging therapeutic areas; i) Cancer and ii) Infectious Diseases. Targeted Intracellular Drug Delivery by Receptor Medicated Endocytosis discusses the major receptors that are useful for targeted delivery for these afflictions. A major section of this book is dedicated to details regarding their occurrence and location, the recognition domain of the receptor, structure activity relationship of substrate /ligand for selective binding, ligands explored, antagonists for ligand binding and relevance of these aspects for therapy of cancer and infectious diseases. These facets are elucidated with the help of specific examples from academic research and also emphasize commercial products, wherever relevant. In vitro cellular models relied on for assessing receptor mediated cellular targeting and in vivo models depicting clinical efficacy are focused on in a separate section. Finally, we briefly discuss the regulatory and toxicity issues that may be associated specifically with the RME approach of intracellular drug delivery.

Download or read book Fragment Based Drug Discovery written by Edward R. Zartler and published by John Wiley & Sons. This book was released on 2008-11-20 with total page 296 pages. Available in PDF, EPUB and Kindle. Book excerpt: Fragment-based drug discovery (FBDD) is a new paradigm in drug discovery that utilizes very small molecules - fragments of larger molecules. It is a faster, cheaper, smarter way to do drug discovery, as shown by the number of pharmaceutical companies that have embraced this approach and the biotechnology companies who use fragments as their sole source of drug discovery. Fragment-Based Drug Discovery: A Practical Approach is a guide to the techniques and practice of using fragments in drug screening. The emphasis is on practical guidance, with procedures, case studies, practical tips, and contributions from industry. Topics covered include: an introduction to fragment based drug discovery, why using fragments is a more efficient process than predominant models, and what it means to have a successful FBDD effort. setting up an FBDD project library building and production NMR in fragment screening and follow up application of protein-ligand NOE matching to the rapid evaluation of fragment binding poses target immobilized NMR screening: validation and extension to membrane proteins in situ fragment-based medicinal chemistry: screening by mass spectrometry computational approaches to fragment and substructure discovery and evaluation virtual fragment scanning: current trends, applications and web based tools fragment-based lead discovery using covalent capture methods case study from industry: the identification of high affinity beta-secretase inhibitors using fragment-based lead generation With contributions from industry experts who have successfully set up an industrial fragment-based research program, Fragment-Based Drug Discovery: A Practical Approach offers essential advice to anyone embarking on drug discovery using fragments and those looking for a new approach to screening for drugs.

Download or read book Phytonanotechnology written by N. Thajuddin and published by Elsevier. This book was released on 2020-05-31 with total page 354 pages. Available in PDF, EPUB and Kindle. Book excerpt: Phytonanotechnology: Challenges and Prospects consolidates information on the use of phytonanoparticles for biomedical, environmental and agricultural applications, covering recent advances in experimental and theoretical studies on various properties of nanoparticles derived from plant sources. The book deals with various attributes of phytonanoparticles, discussing their current and potential applications. In addition, it explores the development of phytonanoparticles, synthesis techniques, characterization techniques, environmental remediation applications, anti-microbial properties, miscellaneous applications, and multi-functional applications. Risks associated with nanoparticles are also discussed. This book is an important reference for materials scientists, engineers, environmental scientists, food scientists and biomedical scientists who want to learn more about the applications of nanoparticles derived from plant sources. Explores synthesis methods of phytonanoparticles from a variety of plant groups Discusses the major biological reactions of phytonanoparticles Outlines the major opportunities and challenges of using phytonanoparticles in biomedical, environmental and agricultural applications

Download or read book Handbook of Marine Natural Products written by Ernesto Fattorusso and published by Springer. This book was released on 2012-04-21 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: "Handbook of Marine Natural Products" takes a fresh approach to describing the major themes of research in this rapidly developing field. This two volume reference work begins with a section that provides a taxonomic survey of the secondary metabolites of diverse marine life including microbes, algae, and invertebrates. This is followed by a demonstration of the techniques and strategies employed in modern structure elucidation of complex natural products. The natural roles of marine natural products are then explored in a series of focused chapters which include the topics of symbiosis, anti-predation and antifouling, chemical interactions, and defence against UV stress. Various routes which facilitate the understanding of marine natural product biosynthesis are subsequently explained and these are followed by an extensive set of chapters on the biomedical potential of marine natural products. The latter portion of this section considers the technologies and scientific disciplines necessary for advancing bioactive marine natural product lead compounds into actual pharmaceuticals. The reference work finishes with a selection of chapters describing marine toxins and their impact on public health and seafood resources. Final thoughts presented at the end of the second volume focus on the future of this field of investigation and discovery research. This publication is presented as a reference handbook and general concepts are emphasized and illustrated with numerous interesting examples, graphical information, and a comprehensive index. "Handbook of Marine Natural Products" introduces students who are at advanced undergraduate and entry graduate student levels to this fascinating multidisciplinary field. It is an ideal desk companion for courses focusing on this contemporary area.

Download or read book Sphingolipids as Signaling and Regulatory Molecules written by Charles Chalfant and published by Springer Science & Business Media. This book was released on 2011-01-12 with total page 311 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book attempts to analyze the latest discoveries in sphingolipid biology and how the alteration of their metabolism leads to altered signaling events and to the development of pathobiological disorders, such as cancer, cardiovascular diseases, asthma, diabetes, inflammation and infectious diseases.

Download or read book Kucers The Use of Antibiotics written by M. Lindsay Grayson and published by CRC Press. This book was released on 2017-10-02 with total page 5390 pages. Available in PDF, EPUB and Kindle. Book excerpt: Kucers’ The Use of Antibiotics is the definitive, internationally-authored reference, providing everything that the infectious diseases specialist and prescriber needs to know about antimicrobials in this vast and rapidly developing field. The much-expanded Seventh Edition comprises 4800 pages in 3 volumes in order to cover all new and existing therapies, and emerging drugs not yet fully licensed. Concentrating on the treatment of infectious diseases, the content is divided into four sections - antibiotics, anti-fungal drugs, anti-parasitic drugs, and anti-viral drugs - and is highly structured for ease of reference. Each chapter is organized in a consistent format, covering susceptibility, formulations and dosing (adult and pediatric), pharmacokinetics and pharmacodynamics, toxicity, and drug distribution, with detailed discussion regarding clinical uses - a feature unique to this title. Compiled by an expanded team of internationally renowned and respected editors, with expert contributors representing Europe, Africa, Asia, Australia, South America, the US, and Canada, the Seventh Edition adopts a truly global approach. It remains invaluable for anyone using antimicrobial agents in their clinical practice and provides, in a systematic and concise manner, all the information required when prescribing an antimicrobial to treat infection.

Download or read book Carotenoids written by John T. Landrum and published by CRC Press. This book was released on 2009-12-21 with total page 562 pages. Available in PDF, EPUB and Kindle. Book excerpt: Carotenoids are of great interest due to their essential biological functions in both plants and animals. However, the properties and functions of carotenoids in natural systems are surprisingly complex. With an emphasis on the chemical aspects of these compounds, Carotenoids: Physical, Chemical, and Biological Functions and Properties presents a b

Download or read book Matricellular Receptors as Potential Targets in Anti Cancer Therapeutic Strategies written by Hervé Emonard and published by Frontiers Media SA. This book was released on 2016-11-22 with total page 131 pages. Available in PDF, EPUB and Kindle. Book excerpt: The invasive character of a primary cancer is greatly dependent on numerous interactions between tumor cells and their extracellular surroundings. Matricellular receptors are defined as (cell-surface) receptors that bind extracellular matrix (ECM) structural proteins and soluble factors dynamically acting on ECM homeostasis. Matricellular receptors mediate numerous signalings from the extracellular environment to cell nucleus and drive main biological functions that are cell growth, survival and migration. Numerous data from the last decade evidence that matricellular receptors are biosensors that allow to a tumor cell answering to microenvironmental variations, and in this sense they are important contributors to tumor cell malignancy. Matricellular receptors represent thus valuable targets for the development of original anti-cancer strategies. Original reports, bibliographic reviews or hypotheses are welcome to improve the basic knowledge of matricellular receptor properties, their spatio-temporal regulation, the dynamic formation of complex receptors and the impact of such interactions on the invasive properties of tumor cells. Biological, biophysical and pharmacological, as well as in silico contributions will be appreciated.

Download or read book Edible Oil Processing written by Wolf Hamm and published by John Wiley & Sons. This book was released on 2013-08-05 with total page 360 pages. Available in PDF, EPUB and Kindle. Book excerpt: Oils and fats are almost ubiquitous in food processing, whether naturally occurring in foods or added as ingredients that bring functional benefits. Whilst levels of fat intake must be controlled in order to avoid obesity and other health problems, it remains the fact that fats (along with proteins and carbohydrates) are one of the three macronutrients and therefore an essential part of a healthy diet. The ability to process oils and fats to make them acceptable as part of our food supplies is a key component in our overall knowledge of them. Without this ability, the food that we consume would be totally different, and much of the flexibility available to us as a result of the application of processing techniques would be lost. Obviously we need to know how to process fatty oils, but we also need to know how best to use them once they have been processed. This second edition of Edible Oil Processing presents a valuable overview of the technology and applications behind the subject. It covers the latest technologies which address new environmental and nutritional requirements as well as the current state of world edible oil markets. This book is intended for food scientists and technologists who use oils and fats in food formulations, as well as chemists and technologists working in edible oils and fats processing.