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Design Of Anti Aids Drugs
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Book Synopsis Design of Anti-AIDS Drugs by : Erik De Clercq
Download or read book Design of Anti-AIDS Drugs written by Erik De Clercq and published by Elsevier Publishing Company. This book was released on 1990 with total page 392 pages. Available in PDF, EPUB and Kindle. Book excerpt: There are several steps in the replicative cycle of human immunodeficiency virus (HIV) that could be considered as adequate targets for chemotherapeutic intervention, e.g., virus attachment to the cells, virus penetration and uncoating, transcription of the viral (RNA) genome to proviral DNA, integration of the proviral DNA into host cell DNA, transcription of the proviral precursor proteins to mature viral proteins, assembly and release ('budding') of the viral particles. These processes depend on, and are regulated by, specific viral proteins. This makes many of these processes and proteins plausible targets for the design of selective inhibitors. The contributions assembled in this book are aimed at presenting what is known anno 1990 about (1) the different steps in the HIV replicative cycle that could be considered as targets for anti-HIV agents, (2) the compounds that interact with these targets and offer promise as candidate drugs for the treatment of HIV infection, and (3) to the extent that it has been resolved, the mechanism of interaction of the anti-HIV agents with their putative targets.
Book Synopsis Introduction to Biological and Small Molecule Drug Research and Development by : Arun K. Ghosh
Download or read book Introduction to Biological and Small Molecule Drug Research and Development written by Arun K. Ghosh and published by Elsevier Inc. Chapters. This book was released on 2013-05-07 with total page 43 pages. Available in PDF, EPUB and Kindle. Book excerpt: The development of HIV protease inhibitors (PIs) and their inclusion in highly active antiretroviral therapies (HAARTs) marked the beginning of a treatment breakthrough in the management of human immunodeficiency virus (HIV)/acquired immunodeficiency syndrome (AIDS). The HAART treatment regimen can cut HIV viral load to undetectable levels. Nonetheless, the rapid emergence of HIV drug resistance has continued to seriously compromise long-term treatment options for HIV-infected patients. Our structure-based design strategy to develop PIs that specifically target the enzyme's backbone atoms has resulted in a number of very potent inhibitors with superior drug resistance profiles. Of particular note, our development of stereochemically defined bis(tetrahydrofuranyl) urethane as a high-affinity P2 ligand has led to the development of exceedingly potent inhibitors. One of these inhibitors, darunavir, has shown exceptional potency against the HIV-1 virus and superior activity against multi-PI-resistant viral strains. Our backbone binding strategy was corroborated with detailed crystal structure analyses of darunavir-bound protease complexes which revealed a series of conserved interactions between the inhibitor and key backbone atoms of HIV-1 protease. Darunavir first received accelerated US Food and Drug Administration approval in 2006 for highly treatment-experienced patients with little therapeutic options. It has now become a leading PI in the fight against HIV infection and drug resistance.
Book Synopsis Anti-AIDS Drug Development by : Prem Mohan
Download or read book Anti-AIDS Drug Development written by Prem Mohan and published by CRC Press. This book was released on 1995-03-01 with total page 312 pages. Available in PDF, EPUB and Kindle. Book excerpt: Curative anti-AIDS drug therapy still remains as an unconquered hurdle to drug research. This book covers significant aspects that are involved in the search, design and development of potential anti-AIDS agents with emphasis on areas related to drug development. These include enzyme inhibitors (reverse transcriptase, protease, glucosidase), inhibitors of gene expression (oligonucleotides), viral-binding inhibitors (anionic compounds and CD4 mimetics) and various plant derived products. A focus of this book is the medicinal chemistry of these classes of compounds. In addition, other areas that are pertinent to drug development are also addressed. These include HIV regulatory proteins, the development of anti-HIV-1 assays and resistance to anti-HIV-1 agents.
Book Synopsis Advances in Antiviral Drug Design by : E. De Clercq
Download or read book Advances in Antiviral Drug Design written by E. De Clercq and published by Elsevier. This book was released on 2007-07-30 with total page 265 pages. Available in PDF, EPUB and Kindle. Book excerpt: Regularly reviewing the "state-of-the-art" developments in the antiviral drug research field, this latest volume spans the conceptual design and chemical synthesis of new antiviral compounds. It discusses their structure-activity relationship, mechanism and targets of action, pharmacological behavior, antiviral activity spectrum, and therapeutic potential for clinical use.
Book Synopsis Advances in Antiviral Drug Design by : E. De Clercq
Download or read book Advances in Antiviral Drug Design written by E. De Clercq and published by Elsevier. This book was released on 1996-04-23 with total page 249 pages. Available in PDF, EPUB and Kindle. Book excerpt: The purpose of the series on Advances in Antiviral Drug Design is to regularly review the "state of the art" on emerging new developments in the antiviral drug research field, thereby spanning the conceptual design and chemical synthesis of new antiviral compounds, their structure-activity relationship, mechanism and target(s) of action, pharmacological behavior, antiviral activity spectrum, and therapeutic potential for clinical use. Volume 2 begins with a description of the antiviral potential of antisense oligonucleotides by J. Temsamani and S. Agrawal. According to the aims of the anitsense technology, these oligonucleotides should be targeted at specific viral antisense technology, these oligonucleotides should be targeted at specific viral mRNA sequences so that translation to the virus-specified proteins is blocked; this has been achieved for a number of oligomers, some of which are now in clinical trials for the treatment of HIV, HCMV, and human papilloma virus (HPV) infections. Then C.-S. Yuan, S. Liu, S.F. Wnuk, M.J. Robins and R.T. Borchardt assess the role of S-adenosylhornocysteine (AdoHcy) hydrolase as target for the design of antiviral agents with broad-spectrum antiviral activity. This is followed by an in-depth account on the design and synthesis of a number of first-, second- and third-generation AdoHcy hydrolase inhibitors and their mode of action at the enzyme level.V.E. Marquez provides a comprehensive description of the various carbocyclic (carba) nucleosides that have been synthesized and evaluated for antiviral activity. Although the number and diversity of the carba-nucleosides that have been found to be antivirally active (or inactive) is astonishingly high, there is no limit to further expansion of this fascinating class of molecules. For the various nucleoside analogues that have to be intracellularly phosphorylated to the 5'-triphosphate stage, to interact with their target enzyme (i.e., herpesviral DNA polymerase or retroviral revers transcriptase) the first phosphorylation step is often the rate-limiting step, and thus various strategies are envisaged by C. Perigoud, J.-L. Girardet, G. Gosselin and J.-L. Bach on how to bypass this initial phosphorylation and to deliver the nucleoside 5'-monophophate directly inside the cells.The HIV protease has been considered as a paradigm for rational drug design. The enzyme is among the best understood in terms of both structure and action, and because of its crucial role in the maturation of HIV, it has been vigorously pursued as a target for anti-HIV chemotherapy. In their comprehensive review of the multidisciplinary approach towards the development of HIV protease inhibitors A.G. Tomasselli, S. Thaisrivongs and R.L. Heinrikson highlight those protease inhibitors which have been brought forward to clinical trials.
Book Synopsis The Social Impact of AIDS in the United States by : National Research Council
Download or read book The Social Impact of AIDS in the United States written by National Research Council and published by National Academies Press. This book was released on 1993-02-01 with total page 337 pages. Available in PDF, EPUB and Kindle. Book excerpt: Europe's "Black Death" contributed to the rise of nation states, mercantile economies, and even the Reformation. Will the AIDS epidemic have similar dramatic effects on the social and political landscape of the twenty-first century? This readable volume looks at the impact of AIDS since its emergence and suggests its effects in the next decade, when a million or more Americans will likely die of the disease. The Social Impact of AIDS in the United States addresses some of the most sensitive and controversial issues in the public debate over AIDS. This landmark book explores how AIDS has affected fundamental policies and practices in our major institutions, examining: How America's major religious organizations have dealt with sometimes conflicting values: the imperative of care for the sick versus traditional views of homosexuality and drug use. Hotly debated public health measures, such as HIV antibody testing and screening, tracing of sexual contacts, and quarantine. The potential risk of HIV infection to and from health care workers. How AIDS activists have brought about major change in the way new drugs are brought to the marketplace. The impact of AIDS on community-based organizations, from volunteers caring for individuals to the highly political ACT-UP organization. Coping with HIV infection in prisons. Two case studies shed light on HIV and the family relationship. One reports on some efforts to gain legal recognition for nonmarital relationships, and the other examines foster care programs for newborns with the HIV virus. A case study of New York City details how selected institutions interact to give what may be a picture of AIDS in the future. This clear and comprehensive presentation will be of interest to anyone concerned about AIDS and its impact on the country: health professionals, sociologists, psychologists, advocates for at-risk populations, and interested individuals.
Download or read book HIV-1 Integrase written by Nouri Neamati and published by John Wiley & Sons. This book was released on 2011-08-10 with total page 710 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book comprehensively covers the mechanisms of action and inhibitor design for HIV-1 integrase. It serves as a resource for scientists facing challenging drug design issues and researchers in antiviral drug discovery. Despite numerous review articles and isolated book chapters dealing with HIV-1 integrase, there has not been a single source for those working to devise anti-AIDS drugs against this promising target. But this book fills that gap and offers a valuable introduction to the field for the interdisciplinary scientists who will need to work together to design drugs that target HIV-1 integrase.
Book Synopsis Nutrition and HIV by : Saurabh Mehta
Download or read book Nutrition and HIV written by Saurabh Mehta and published by CRC Press. This book was released on 2018-05-15 with total page 326 pages. Available in PDF, EPUB and Kindle. Book excerpt: The world continues to lose more than a million lives each year to the HIV epidemic, and nearly two million individuals were infected with HIV in 2017 alone. The new Sustainable Development Goals, adopted by countries of the United Nations in September 2015, include a commitment to end the AIDS epidemic by 2030. Considerable emphasis on prevention of new infections and treatment of those living with HIV will be needed to make this goal achievable. With nearly 37 million people now living with HIV, it is a communicable disease that behaves like a noncommunicable disease. Nutritional management is integral to comprehensive HIV care and treatment. Improved nutritional status and weight gain can increase recovery and strength of individuals living with HIV/AIDS, improve dietary diversity and caloric intake, and improve quality of life. This book highlights evidence-based research linking nutrition and HIV and identifies research gaps to inform the development of guidelines and policies for the United Nations’ Sustainable Development Goals. A comprehensive approach that includes nutritional interventions is likely to maximize the benefit of antiretroviral therapy in preventing HIV disease progression and other adverse outcomes in HIV-infected men and women. Modification of nutritional status has been shown to enhance the quality of life of those suffering HIV/AIDS, both physically in terms of improved body mass index and immunological markers, and psychologically, by improving symptoms of depression. While the primary focus for those infected should remain on antiretroviral treatment and increasing its availability and coverage, improvement of nutritional status plays a complementary role in the management of HIV infection.
Book Synopsis Advances in Antiviral Drug Design by : E. De Clercq
Download or read book Advances in Antiviral Drug Design written by E. De Clercq and published by Elsevier. This book was released on 2003-12-17 with total page 231 pages. Available in PDF, EPUB and Kindle. Book excerpt: The fourth volume of Advances in Antiviral Drug Design is keeping up with the recent progress made in the broad field of antiviral drug research and encompasses six specific directions that have opened new avenues for the treatment of HIV and other virus infections.First, as the introductory chapter, the different new anti-HIV agents that are now in preclinical or clinical development are reviewed by E. De Clercq. This includes new NRTIs, NNRTIs and PIs, but also HIV entry/fusion inhibitors as well as integrase inhibitors, and some of these agents, such as the NRTI emtricitabine [(-)FTC] and the PI atazanavir, may soon be licensed for clinical use.Second, high expectations are vested in the potential therapeutic usefulness of inhibitors of HIV integration, a point of no return in the life cycle of HIV, and this approach is highlighted by D.J. Hazuda and S.D. Young.Third, as all currently available PIs can be described as "peptidomimetic", and, therefore, expected to demonstrate overlapping virus-drug resistance and side effect profiles, it would be interesting to see how a non-peptidic protease inhibitor such as tipranavir behaves, and this is covered by D. Mayers, K. Curry, V. Kohlbrenner and S. McCallister.Fourth, neuraminidase inhibitors such as zanamivir (that has to be inhaled) and oseltamivir (that can be administered via the oral route) have gained a definitive status as antiviral drugs useful for both therapy and prophylaxis of influenza A and B virus infections; as they target a specific influenza viral enzyme, neuraminidase (or sialidase), they may be expected to block newly emerging influenza viruses as well, and the design of neuraminidase inhibitors has received due attention of H. Jin and C.U. Kim.Fifth, while the major current efforts in antiviral drug development have shifted from herpesviruses towards HIV and hepatitis viruses [hepatitis B virus (HBV), hepatitis C virus (HCV)], it is interesting to note that by switching from the classical five-membered sugar or acyclic nucleoside strategy, J. Wang, M. Froeyen and P. Herdewijn have gone "upstream" in designing six-membered carbocyclic nucleosides as potential anti-herpesvirus agents.Sixth, following up on the nucleotide prodrug strategy introduced above under ix, to deliver the biologically active nucleotides inside the cells, C. Meier has elaborated on a particular class of such pronucleotides, namely that of the cyclosaligenyl pronucleotides, an approach that should have far reaching implications for compounds effective against HIV, HBV and other viruses.The six topics covered in this fourth volume of Advances in Antiviral Drug Design are in the front line of the present endeavors towards the design and development of new therapeutic agents for virus infections. They pertain to the combat against three of the most important viral pathogens of current times: HIV, HBV, influenza virus and herpesviruses.
Book Synopsis Structure-based Design of Drugs and Other Bioactive Molecules by : Arun K. Ghosh
Download or read book Structure-based Design of Drugs and Other Bioactive Molecules written by Arun K. Ghosh and published by John Wiley & Sons. This book was released on 2014-08-11 with total page 474 pages. Available in PDF, EPUB and Kindle. Book excerpt: Drug design is a complex, challenging and innovative research area. Structure-based molecular design has transformed the drug discovery approach in modern medicine. Traditionally, focus has been placed on computational, structural or synthetic methods only in isolation. This one-of-akind guide integrates all three skill sets for a complete picture of contemporary structure-based design. This practical approach provides the tools to develop a high-affinity ligand with drug-like properties for a given drug target for which a high-resolution structure exists. The authors use numerous examples of recently developed drugs to present "best practice" methods in structurebased drug design with both newcomers and practicing researchers in mind. By way of a carefully balanced mix of theoretical background and case studies from medicinal chemistry applications, readers will quickly and efficiently master the basic skills of successful drug design. This book is aimed at new and active medicinal chemists, biochemists, pharmacologists, natural product chemists and those working in drug discovery in the pharmaceutical industry. It is highly recommended as a desk reference to guide students in medicinal and chemical sciences as well as to aid researchers engaged in drug design today.
Book Synopsis Novel Approaches for the Delivery of Anti-HIV Drugs by : José das Neves
Download or read book Novel Approaches for the Delivery of Anti-HIV Drugs written by José das Neves and published by MDPI. This book was released on 2020-05-20 with total page 208 pages. Available in PDF, EPUB and Kindle. Book excerpt: HIV/AIDS continues to be one of the most challenging individual and public health concerns of the present day. According to the UNAIDS, nearly 38 million individuals were living with the infection by the end of 2018, while 1.7 million new cases occurred during that same year. In spite of the numerous advances in the development and delivery of antiretroviral agents, both for treatment and prevention, several challenges remain. This book includes original research and review articles on innovative strategies and approaches for the formulation and delivery of anti-HIV drugs, including genetic material and other biopharmaceuticals. Different local and systemic delivery strategies are addressed based on different technologies intended for oral, transdermal, subcutaneous, vaginal, or rectal administration. Authored by eminent scientists in academia and nonprofit organizations involved in the development of antiretroviral drug products, this collection provides useful information for all those involved in HIV/AIDS treatment and prevention.
Book Synopsis The Ups and Downs in Drug Design by : Victor E. Marquez
Download or read book The Ups and Downs in Drug Design written by Victor E. Marquez and published by CRC Press. This book was released on 2021-11-15 with total page 566 pages. Available in PDF, EPUB and Kindle. Book excerpt: The Ups and Downs in Drug Design: Adventures in Medicinal Chemistry highlights the necessity for an integrative approach in medicinal chemistry and chemical biology. As medicinal chemistry is not a monolithic science, it is important to emphasize the other various disciplines that are required for successful drug design. This book presents the author’s own personal experience in this field and describes the "ups" and "downs" that come with drug discovery. It is an excellent companion text for graduate and postgraduate students who would like further insight into the parameters of drug design, including the challenges that come with the project. Key Features Illustrates "real-life" examples in medicinal chemistry Integrates the use of physical, chemical, and biological concepts that are important in drug design Highlights the "ups" and "downs" that come with drug discovery Aims to inspire students who may be struggling with the challenges and thought process in drug design Intends to be an excellent companion text for graduate and postgraduate students
Book Synopsis Evolution of Anti-HIV Drug Resistance by : Lutz Gürtler
Download or read book Evolution of Anti-HIV Drug Resistance written by Lutz Gürtler and published by S. Karger AG (Switzerland). This book was released on 2012-01-24 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: Despite recent advances in antiretroviral therapy treating HIV drug resistance remains a challenge. With the growing number of anti-HIV drugs and the enormous variant space accessible by viral evolution, manual selection of effective anti-HIV therapies has become complex. This publication represents a recent update on the determination of antiretroviral drug resistance determination, its computer program-assisted interpretation and beneficial effect on the treatment of HIV-1- and HIV-2-infected patients. Starting with the description of the human immunodeficiency viruses and their mutation frequency it goes on to discuss methods of resistance determination and bioinformatic-guided algorithm of interpretation, the fate of patients in large cohorts benefitting from improved therapeutic interventions and limitations in individual patients and HIV-2 infection. Furthermore Pyro 454 sequencing and interpretation of single amino acids in the context of all involved mutations in antiretroviral drug resistance are described and R5 and X4 differentiation by nucleic acid sequencing and susceptibility of HIV to a maraviroc treatment regimen are specified. This special issue of Intervirology will be of benefit to medical doctors involved in the treatment of HIV-infected patients as well as to pharmacologists, bioinformaticians and laboratory personnel working in the field of drug resistance analysis, drug design and antivirals. Furthermore it is a valuable resource for researchers involved in the confection of new drugs and interactions of old drugs as well as in assays of antiviral drug resistance.
Book Synopsis Design and Synthesis of HIV-1 Protease Inhibitors by : Mathias Alterman
Download or read book Design and Synthesis of HIV-1 Protease Inhibitors written by Mathias Alterman and published by . This book was released on 2001 with total page 70 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Book Synopsis Frontiers in Clinical Drug Research: HIV by : Atta-ur-Rahman
Download or read book Frontiers in Clinical Drug Research: HIV written by Atta-ur-Rahman and published by Bentham Science Publishers. This book was released on 2015-04-02 with total page 300 pages. Available in PDF, EPUB and Kindle. Book excerpt: Frontiers in Clinical Drug Research – HIV is an eBook series that brings updated reviews to readers interested in learning about advances in the development of pharmaceutical agents for the treatment of acquired immune deficiency syndrome (AIDS) and other disorders associated with human immunodeficiency virus (HIV) infection. The scope of the eBook series covers a range of topics including the medicinal chemistry and pharmacology of natural and synthetic drugs employed in the treatment of AIDS (including HAART) and resulting complications, and the virology and immunological study of HIV and related viruses. Frontiers in Clinical Drug Research – HIV is a valuable resource for pharmaceutical scientists, clinicians and postgraduate students seeking updated and critically important information for developing clinical trials and devising research plans in HIV/AIDS research. The first volume of this series features 7 chapters that cover a variety of topics including: -Antiretroviral drug development -HIV-1 genomics -HIV drug targets such as ribosomes and HIV Integrase -HAART associated nephrotoxicity
Book Synopsis Consolidated Guidelines on the Use of Antiretroviral Drugs for Treating and Preventing HIV Infection by : World Health Organization
Download or read book Consolidated Guidelines on the Use of Antiretroviral Drugs for Treating and Preventing HIV Infection written by World Health Organization and published by . This book was released on 2016 with total page 429 pages. Available in PDF, EPUB and Kindle. Book excerpt: These guidelines provide guidance on the diagnosis of human immunodeficiency virus (HIV) infection, the use of antiretroviral (ARV) drugs for treating and preventing HIV infection and the care of people living with HIV. They are structured along the continuum of HIV testing, prevention, treatment and care. This edition updates the 2013 consolidated guidelines on the use of antiretroviral drugs following an extensive review of evidence and consultations in mid-2015, shared at the end of 2015, and now published in full in 2016. It is being published in a changing global context for HIV and for health more broadly.
Author :National Research Council and Institute of Medicine Publisher :National Academies Press ISBN 13 :0309176212 Total Pages :352 pages Book Rating :4.3/5 (91 download)
Book Synopsis Preventing HIV Transmission by : National Research Council and Institute of Medicine
Download or read book Preventing HIV Transmission written by National Research Council and Institute of Medicine and published by National Academies Press. This book was released on 1995-09-14 with total page 352 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume addresses the interface of two major national problems: the epidemic of HIV-AIDS and the widespread use of illegal injection drugs. Should communities have the option of giving drug users sterile needles or bleach for cleaning needs in order to reduce the spread of HIV? Does needle distribution worsen the drug problem, as opponents of such programs argue? Do they reduce the spread of other serious diseases, such as hepatitis? Do they result in more used needles being carelessly discarded in the community? The panel takes a critical look at the available data on needle exchange and bleach distribution programs, reaches conclusions about their efficacy, and offers concrete recommendations for public policy to reduce the spread of HIV/AIDS. The book includes current knowledge about the epidemiologies of HIV/AIDS and injection drug use; characteristics of needle exchange and bleach distribution programs and views on those programs from diverse community groups; and a discussion of laws designed to control possession of needles, their impact on needle sharing among injection drug users, and their implications for needle exchange programs.
