Current Drug Targets - Infectious Disorders - Volume 3, Issue 1, 2003

Volume 3, Issue 1, 2003
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Mode of Action of Plant Defensins Suggests Therapeutic Potential
Authors: B.P.H.J. Thomma, B.P.A. Cammue and K. ThevissenHigher vertebrates can rely both on an innate as well as an adaptive immune system for defense against invading pathogens. In contrast, plants can only employ an innate immune system that largely depends on the production of antimicrobial compounds such as plant defensins and other pathogenesis-related proteins. Plant defensins are ubiquitous, cationic, cysteine-rich plant peptides and have a folding pattern that shar Read More
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β-Lactamases: A Survey of Protein Diversity
Authors: M.S. Helfand and R.A. BonomoBacterial resistance to β-lactam antibiotics and β-lactamase inhibitors is an ever increasing problem that threatens the clinical utility of drugs that form the cornerstone of the antibiotic armamentarium. Especially among Gram-negative pathogens, elaboration of structurally and mechanistically novel β-lactamase enzymes is the most important means by which resistance occurs. An appreciation of the tremendous diversity of the Read More
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Therapy of Chronic Hepatitis C: A Critical Review
Authors: G. Saracco, A. Olivero, A. Ciancio, S. Carenzi and M. RizzettoCombination therapy (Interferon plus ribavirin) is the current therapeutic gold standard for naive Hepatitis C Virus (HCV)-positive patients and with the recent advent of pegylated (PEG) IFN the rate of the sustained virological response (HCV-RNA clearance 6 months after the end of treatment) is about 54%-56%with a therapeutical gain mainly among patients with unfavourable HCV genotype (1a, 1b); in this subset of patients, a 4 Read More
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Strategy of Computer-Aided Drug Design
Authors: A.V. Veselovsky and A.S. IvanovModern strategies of computer-aided drug design (CADD) are reviewed. The task of CADD in the pipeline of drug discovery is accelerating of finding the new lead compounds and their structure optimization for the following pharmacological tests. The main directions in CADD are based on the availability of the experimentally determined three-dimensional structure of the target macromolecule. If spatial structure is known the Read More
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Antivirals at the Mirror: The Lack of Stereospecificity of Some Viral and Human Enzymes Offers Novel Opportunities in Antiviral Drug Development
Authors: F. Focher, S. Spadari and G. MagaThe enantioselectivity of enzymes, namely the property of enzymes to recognise and metabolise only one of the two enantiomers of chiral molecules, is related to the chiral structure of the enzymes, reflecting the three-dimensional folding of the polypeptide backbone and the orientation of the amino acid side chains in the folded molecule. Because of the chirality of the amino acids (L), the chemistry of life sho Read More
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A Review of Macrolide Treatment of Atherosclerosis and Abdominal Aortic Aneurysms
Authors: J.S. Lindholt, J. Stovring, P. Andersen, E.W. Henneberg and L. OstergaardSeroepidemiological studies have shown an association between Chlamydia pneumoniae and atherosclerosis, the risk of acute myocardial infarction and abdominal aortic aneurysms (AAA).Several studies have detected C. pneumoniae in atherosclerotic lesions from coronary and carotid arteries, in AAA, and in sclerotic aortic valves. However, culturing of C. pneumoniae is difficult and has seldomly succeeded from Read More
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New Approaches for Anti-Infective Drug Discovery: Antibiotics, Vaccines and Beyond
Authors: Q. Cheng, S. Wang and A.A. SalyersInfectious disease is the leading cause of death worldwide, and billions of dollars are invested every year in developing anti-infective drugs. In the meantime, resistant bacteria are on the steady rise and render many once effective drugs useless. The tremendous funding and the urgent need to treat the resistant bacterial infections lead to the rapid progress on development of new drugs and potential new drug targets. New disc Read More
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Chitin Synthesis as a Target for Antifungal Drugs
Authors: J. Ruiz-Herrera and G. San-BlasHuman mycoses have become a threat to health world-wide. Unfortunately there are only a limited number of antimycotic drugs in use. Promising targets for drugs specific against fungi are those affecting chitin synthesis. Chitin is absent in vertebrates, and is essential for fungal wall integrity. A thorough knowledge of the mechanism of chitin synthesis is required to design specific inhibitors. We review here our current understan Read More
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