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- Volume 2, Issue 3, 2005
Drug Design Reviews - Online (Discontinued) - Volume 2, Issue 3, 2005

Volume 2, Issue 3, 2005
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Protein-Protein Interactions in Drug Discovery
More LessAlthough the regulation of cellular processes is mediated to a large extent by posttranslational modification of proteins, the target specificity of enzymatic, e.g. protein kinase and phosphatase, activities derives in large part from protein-protein interactions (PPIs) rather than enzyme substrate specificity. Similarly, signal transduction through interaction of biological effectors such as hormones and cytokines with their r Read More
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Therapeutic Antibodies
Authors: J. R. Adair and A. D. G. LawsonSince the time of the earliest jawed fish, some 400 million years ago, evolution has been honing the design of antibody molecules to function as specific markers, alerting immune defences to the presence of pathogenic antigens, and recruiting effector function in the form of complement and Fc receptor-bearing cells. For the last twenty-five years, the biopharmaceutical industry has been applying the versatility of antibodi Read More
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The Mast Cell: A Potential Therapeutic Target in Myocardial Infarction
Authors: Pawel Zymek, Porur Somasundaram, Anna Cieslak and Nikolaos G. FrangogiannisMast cells are multifunctional effector cells of the immune system, capable of producing a variety of vasoactive mediators, cytokines and growth factors. The presence of resident mast cells in the myocardium has been established; however, their exact role in cardiac pathology remains unclear. The current review presents evidence suggesting the importance of mast cells in the infarcted myocardium. Myocardial ischemi Read More
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Computational Design, Organic Synthesis, and Biological Evaluation of Polyphenol Proteasome Inhibitors: Significance in Drug Discovery and Cancer Prevention
Authors: K. G. Daniel, T. H. Chan and Q. P. DouHuman tumor cell growth depends on the ubiquitin/proteasome degradation pathway. This pathway is essential in promotion of tumor cellular proliferation, inhibition of programmed cell death (apoptosis), and development of drug resistance, suggesting that proteasome inhibitors could be developed as potential novel anticancer drugs. This hypothesis has been supported by both experimental and clinical results. Most recen Read More
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Treatment of CNS Malignancies with a Recombinant Oncolytic Poliovirus
Authors: Stephanie A. Campbell, Melinda K. Merrill and Matthias GromeierSpread to the central nervous system (CNS) and the leptomeninges is a frequent complication of systemic cancers that is associated with serious morbidity and high mortality. We have developed a novel therapeutic approach against primary CNS tumors and secondary CNS malignancy complicating systemic cancer based on the human neuropathogen poliovirus. Susceptibility to poliovirus infection and ensuing rapid cell Read More
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Pentavalent Antimonials: From Chemistry to the Design of New Drugs
Authors: C. Demicheli and F. FrezardPentavalent antimonials, including meglumine antimoniate and sodium stibogluconate, have been used for more than half a century in the therapy of the parasitic disease leishmaniasis. Even though antimonials are still the firstline drugs, they exhibit several limitations, including severe side effects, the need for daily parenteral administration and drug resistance. The molecular structure of antimonials, their metabolism and Read More
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β-Glucans: Old Molecules with Newly Discovered Immunological Activities
Authors: L. Amati, D. Leogrande, M. E. Passeri, M. L. Mastronardi, L. Passantino, P. Venezia and E. Jirilloβ-glucans (BG) are polysaccharides contained in the cell wall of fungi but also present in nature as normal constituents of oats, barley and yeast. The recent discovery of the major receptor for BG on antigen-presenting cells, dectin-1, has given a strong impetus to a series of researches on BG immunobiological activities. In particular, BG possess antimicrobial activity by exerting a direct effect on monocytes and neutrophils. At t Read More
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