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- Volume 10, Issue 30, 2004
Current Pharmaceutical Design - Volume 10, Issue 30, 2004
Volume 10, Issue 30, 2004
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Virus Attachment and Entry Offer Numerous Targets for Antiviral Therapy
More LessIn 2003 the first virus entry inhibitor, the anti-HIV peptide T20 (Fuzeon®, enfuvirtide®), was approved for treatment of advanced Human Immunodeficiency Virus Type 1 infection. T20 is an unconventional antiviral drug, as it does not target a viral replicase or protease but a conformational transition within the HIV1 fusion protein gp41 required for virus-cell membrane fusion. Beyond membrane fusion, numer Read More
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Closely Related Antiretroviral Agents as Inhibitors of Two HIV-1 Enzymes, Ribonuclease H and Integrase: “Killing Two Birds with One Stone”
More LessThe structures of the catalytic core of two HIV-1 encoded enzymes play a crucial role in the retroviral cycle: integrase and RNase H exhibit striking similarities. These enzymes also share a similar mechanism of catalysis. The homologies between RNase H and integrase led to studying the effect of the RNase H inhibitors on integrase. ODNs aptamers active on RNase H were shown to be strong IN inhibitors. On the contrary, comp Read More
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Targeting the Assembly of the Human Immunodeficiency Virus Type I
Authors: D. Muriaux, J. L. Darlix and A. CimarelliIn the rush to develop anti-viral drugs against the human immunodeficiency virus type I (HIV-1), all the steps of the viral life cycle are potential targets of therapeutic intervention. In this review, we will explore the recent advances on strategies that aim at obstructing the formation, the release and the infectivity of newly formed virion particles from HIV-1 infected cells.
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Three Properties of the Hepatitis C Virus RNA Genome Related to Antiviral Strategies Based on RNA-Therapeutics: Variability, Structural Conformation and tRNA Mimicry
Authors: Jordi Gomez, Anna Nadal, Rosario Sabariegos, Nerea Beguiristain, Maria Martell and Maria PironThe concept of using RNA molecules as therapeutic agents is receiving increasing attention by basic science and pharmaceutical research. Over the past five years, a number of clinical trials have been initiated to evaluate the efficacy and safety of several RNA agents for the treatment of a range of conditions from cancer to infectious disease. From a molecular biology perspective, two main factors are implicated in RNA the Read More
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Picornavirus IRES: Structure Function Relationship
Authors: Encarnacion Martinez-Salas and Olga Fernandez-MiragallPicornavirus infections have been a challenging problem in human health. Genome organisation of picornavirus is unique in having a long, heavily-structured, multifunctional 5'untranslated region, preceding a single open reading frame from which all viral proteins are produced. Within the 5'leader, an internal region termed ribosome entry site (IRES) regulates viral protein synthesis in a 5'-independent manner. The IRES ele Read More
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Replication and Transcription of the Rotavirus Genome
Authors: John T. Patton, Rodrigo Vasquez-Del Carpio and Eugenio SpencerRotaviruses are an important cause of human morbidity and mortality, representing the primary pathogens responsible for acute dehydrating diarrhea in children under the age of 3. The infectious rotavirus particle is made up of three concentric layers of protein, and contains a genome consisting of eleven segments of double-stranded (ds)RNA. Upon infection, RNA polymerases associated with double-layered virus partic Read More
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Coumarin and Isocoumarin as Serine Protease Inhibitors
Authors: Lionel Pochet, Raphael Frederick and Bernard MasereelSerine proteases are attractive targets for the design of enzyme inhibitors since they are involved in the etiology of several diseases. Within the class of serine proteases, HLE is one of the most destructive enzymes in the body. It is implicated in the promotion or exacerbation of a number of diseases including pancreatitis, acute respiratory syndrome, rheumatoid arthritis, atherosclerosis, pulmonary emphysema, and cystic fib Read More
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Studies on Coumarins and Coumarin-Related Compounds to Determine their Therapeutic Role in the Treatment of Cancer
Authors: Aoife Lacy and Richard O'KennedyThe Benzopyrones are a group of compounds whose members include coumarins and flavonoids. Dietary exposure to benzopyrones is quite significant, as these compounds are found in vegetables, fruit, seeds, nuts, coffee, tea and wine. It is estimated that the average western diet contains approximately 1g / day of mixed benzopyrones. It is, therefore, not difficult to see why extensive research into their pharmacol Read More
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Natural and Synthetic Coumarin Derivatives with Anti-Inflammatory / Antioxidant Activities
Several natural products with a coumarinic moiety have been reported to have multiple biological activities. It is to be expected that, in a similar way to isomeric flavonoids, coumarins might affect the formation and scavenging of reactive oxygen species (ROS) and influence processes involving free radical-mediated injury. Coumarin can reduce tissue edema and inflammation. Moreover coumarin and its 7-hydroxy-deri Read More
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The Coumarin Moiety as Chromophore of Fluorescent Ion Indicators in Biological Systems
More LessFluorescent probes have evolved into an extremely useful tool for the detection of ions in biological systems. The design of ion indicators is based in the proper choice of the ion chelating group as well as the chromophore moiety. The chromophores of choice should fulfill a number of requirements concerning the photostability of the group, the range of the excitation and emission wavelengths of the indicators, the Sto Read More
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Volumes & issues
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Volume 31 (2025)
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Volume 30 (2024)
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Volume 29 (2023)
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Volume 28 (2022)
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Volume 27 (2021)
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Volume 26 (2020)
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Volume 25 (2019)
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Volume 24 (2018)
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Volume 23 (2017)
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Volume 22 (2016)
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Volume 21 (2015)
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Volume 20 (2014)
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Volume 19 (2013)
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Volume 18 (2012)
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Volume 17 (2011)
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Volume 16 (2010)
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Volume 15 (2009)
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Volume 14 (2008)
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Volume 13 (2007)
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Volume 12 (2006)
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Volume 11 (2005)
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Volume 10 (2004)
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Volume 9 (2003)
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Volume 8 (2002)
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Volume 7 (2001)
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Volume 6 (2000)
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