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- Volume 18, Issue 9, 2011
Current Medicinal Chemistry - Volume 18, Issue 9, 2011
Volume 18, Issue 9, 2011
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Editorial [Hot Topic:Protein targets for development of drugs against Mycobacterium tuberculosis (Guest Editor: Walter Filgueira de Azevedo)]
More LessThe bacterium Mycobacterium tuberculosis remains a major challenge to public health systems worldwide, especially affecting developing countries in Asia, Africa, Latin America and Eastern Europe. Tuberculosis (TB) is one the most common bacterial diseases of humans, and World Health Organization estimates that nearly thirty percent of the world's population is infected with M. tuberculosis in a latent form and, as a resu Read More
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Purine Salvage Pathway in Mycobacterium tuberculosis
Authors: R. G. Ducati, A. Breda, L. A. Basso and D. S. SantosMillions of deaths worldwide are caused by the aetiological agent of tuberculosis, Mycobacterium tuberculosis. The increasing prevalence of this disease, the emergence of drug-resistant strains, and the devastating effect of human immunodeficiency virus coinfection have led to an urgent need for the development of new and more efficient antimycobacterial drugs. The modern approach to the development of new chemic Read More
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Analysis of Molecular Targets of Mycobacterium tuberculosis by Analytical Ultracentrifugation
Authors: J. C. Borges and C. H.I. RamosThe interest in analytical ultracentrifugation (AUC) to analyze protein structural parameters and interactions has increased in the past decades as a result of several developments on new generation instrumentation and data analysis tools. In this article, we review AUC principles and applications to study proteins, emphasizing molecular targets of Mycobacterium tuberculosis.
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Pyrimidine Salvage Pathway in Mycobacterium tuberculosis
Authors: A. D. Villela, Z. A. Sanchez-Quitian, R. G. Ducati, D. S. Santos and L. A. BassoThe causative agent of tuberculosis (TB), Mycobacterium tuberculosis, infects one-third of the world population. TB remains the leading cause of mortality due to a single bacterial pathogen. The worldwide increase in incidence of M. tuberculosis has been attributed to the high proliferation rates of multi and extensively drug-resistant strains, and to co-infection with the human immunodeficiency virus. There is thus a continu Read More
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Shikimate Kinase (EC 2.7.1.71) from Mycobacterium tuberculosis: Kinetics and Structural Dynamics of a Potential Molecular Target for Drug Development
Authors: D. M. Saidemberg, A. W. Passarelli, A. V. Rodrigues, L. A. Basso, D. S. Santos and M. S. PalmaThe enzymes of the shikimate pathway represent potential molecular targets for the development of non-toxic antimicrobial agents and anti-parasite drugs. One of the most promising of these enzymes is shikimate kinase (EC 2.7.1.71), which is responsible for the fifth step in the shikimate pathway. This enzyme phosphorylates shikimic acid to yield shikimate-3-phosphate, using ATP as a substrate. In this work, the conformat Read More
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Understanding the Structure, Activity and Inhibition of Chorismate Synthase from Mycobacterium tuberculosis
Authors: H. A. Arcuri and M. S. PalmaTuberculosis is considered a worldwide health problem mainly due to co-infection with HIV and proliferation of multi-drugresistant strains. The enzymes of the shikimate pathway are potential targets for the development of new therapies because they are essential for bacteria, but absent from mammals. The last step in this pathway is performed by chorismate synthase (CS), which catalyzes the conversion of 5-enolpyruvy Read More
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The β-Ketoacyl-ACP Synthase from Mycobacterium tuberculosis as Potential Drug Targets
Authors: V. Singh, I. Mani, D. K. Chaudhary and P. SomvanshiThe continuous preventive measures and control of tuberculosis are often hampered by re-emergence of multi-drug-resistant (MDR) strains of Mycobacterium tuberculosis. A novel drug approach is desperately needed to combat the global threat posed by MDR strains. In spite of current advancement in biological techniques viz. microarray and proteomics data for tuberculosis, no such potent drug has been developed in t Read More
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The Methylerythritol Phosphate (MEP) Pathway for Isoprenoid Biosynthesis as a Target for the Development of New Drugs Against Tuberculosis
Authors: C. Obiol-Pardo, J. Rubio-Martinez and S. ImperialTuberculosis remains a major infectious disease to humans. It accounts for approximately 8-9 million new cases worldwide and an estimated 1.6 million deaths annually. Effective treatments for tuberculosis consist of a combination of several drugs administered over long periods of time. Since Mycobacterium tuberculosis often acquires multiple drug resistant mechanisms, development of new drugs with innovative action Read More
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Bio-Inspired Algorithms Applied to Molecular Docking Simulations
Authors: G. Heberle and W. F. de AzevedoNature as a source of inspiration has been shown to have a great beneficial impact on the development of new computational methodologies. In this scenario, analyses of the interactions between a protein target and a ligand can be simulated by biologically inspired algorithms (BIAs). These algorithms mimic biological systems to create new paradigms for computation, such as neural networks, evolutionary computing, and s Read More
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Molecular Dynamics Simulations of Protein Targets Identified in Mycobacterium tuberculosis
More LessApplication of molecular dynamics simulation technique has become a conventional computational methodology to calculate significant processes at the molecular level. This computational methodology is particularly useful for analyzing the dynamics of proteinligand systems. Several uses of molecular dynamics simulation makes possible evaluation of important structural features found at interface between a ligand and a pr Read More
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Tumor Physiology and Charge Dynamics of Anticancer Drugs: Implications for Camptothecin-based Drug Development
Authors: D. J. Adams and L. R. MorganCharge is an important characteristic of drug molecules, since ionization sites determine the pKa at a particular pH. The pKa in turn can affect many parameters, including solubility, dissolution rate, reaction kinetics, formulation, cell permeability, tissue distribution, renal elimination, metabolism, protein binding and receptor interactions. The impact of charge dynamics is amplified in human solid tumors that exhibit th Read More
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The Delivery of Biologically Active (Therapeutic) Peptides and Proteins into Cells
By M. GrdisaBiologically active peptides and proteins have a great potential to act as targeted drug therapies in the treatment of a variety of diseases, including cancer. However, their use in vivo is limited by their low stability and cell permeability. Thus, it is necessary to develop efficient and safe peptide/protein delivery systems that can overcome these problems and increase a therapy's bioavailability. The search for promising v Read More
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Schizophrenia: A Systematic Review of the Disease State, Current Therapeutics and their Molecular Mechanisms of Action
Authors: J. K. Shin, D. T. Malone, I. T. Crosby and B. CapuanoThe treatment of schizophrenia, one of the most debilitating mental illnesses, began by the serendipitous discovery of chlorpromazine. Since then, researchers have endeavored to find the cause of the illness but it remains unresolved. As a result, literature on the etiology of schizophrenia is littered with hypotheses and theories that are constantly reviewed, modified and rejected. Two hypotheses, however, have withstood the Read More
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Regulation of Gene Expression by Retinoids
Authors: P. M. Amann, S. B. Eichmuller, J. Schmidt and A. V. BazhinVitamin A serves as substrate for the biosynthesis of several derivates (retinoids) which are important for cell growth and cell differentiation as well as for vision. Retinoic acid is the major physiologically active form of vitamin A regulating the expression of different genes. At present, hundreds of genes are known to be regulated by retinoic acid. This regulation is very complex and is, in turn, regulated on many levels. To date, two Read More
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Volumes & issues
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Volume 32 (2025)
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Volume 31 (2024)
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Volume 30 (2023)
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Volume 29 (2022)
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Volume 28 (2021)
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Volume 27 (2020)
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Volume 26 (2019)
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Volume 25 (2018)
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Volume 24 (2017)
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Volume 23 (2016)
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Volume 22 (2015)
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Volume 21 (2014)
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Volume 20 (2013)
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Volume 19 (2012)
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Volume 18 (2011)
- Issue 36
- Issue 35
- Issue 34
- Issue 33
- Issue 32
- Issue 31
- Issue 30
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- Issue 12
- Issue 11
- Issue 10
- Issue 9
- Issue 8
- Issue 7
- Issue 6
- Issue 5
- Issue 4
- Issue 3
- Issue 2
- Issue 1
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Volume 17 (2010)
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Volume 16 (2009)
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Volume 15 (2008)
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Volume 14 (2007)
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Volume 13 (2006)
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Volume 12 (2005)
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Volume 11 (2004)
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Volume 10 (2003)
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Volume 9 (2002)
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Volume 8 (2001)
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Volume 7 (2000)
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