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- Volume 19, Issue 6, 2013
Current Pharmaceutical Design - Volume 19, Issue 6, 2013
Volume 19, Issue 6, 2013
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Selective Inhibitors of Human Neutrophil Proteinase 3
More LessHuman neutrophil proteinase 3 (PR3) and elastase (HNE) are homologous serine proteinases involved in the proteolytic events associated with inflammation and infection. Their close structural and functional resemblance makes it difficult to understand their respective biological functions. Thus, all natural inhibitors of PR3 identified to date preferentially target HNE, and only recently have inhibitors that target PR3 selectivel Read More
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HtrA Protease Family as Therapeutic Targets
The HtrA proteases degrade damaged proteins and thus control the quality of proteins and protect cells against the consequences of various stresses; they also recognize specific protein substrates and in this way participate in regulation of many pathways. In many pathogenic bacteria strains lacking the HtrA function lose virulence or their virulence is decreased. This is due to an increased vulnerability of bacteria to stre Read More
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The Proteasome in Health and Disease
Authors: Elzbieta Jankowska, Julia Stoj, Przemyslaw Karpowicz, Pawel A. Osmulski and Maria GaczynskaThe giant proteolytic factory called the proteasome came a long way from a biochemical curio to a major regulator of cellular physiology and a renowned drug target within the ubiquitin proteasome pathway (UPP). Thanks to availability of highly specific inhibitors of the proteasome, in less than twenty years it was possible to identify major transcription factors, cyclins, and products of oncogenes as crucial substrates for the Read More
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Processing and Regulation Mechanisms within Antigen Presenting Cells: A Possibility for Therapeutic Modulation
By Timo BursterProcessing of antigens within antigen presenting cells (APCs) is necessary for an immune response. Two pathways exist to present antigens to T cells: the major histocompatibility complex class I (MHC I) pathway to activate cytotoxic T cells (CTLs) and the MHC II route to stimulate T helper cells (Ths). Prior to efficient antigen presentation to MHC II, antigens have to be proteolytically degraded by proteases, the cathepsins, in Read More
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Dynorphin Convertases and their Functions in CNS
Authors: Joanna Ner and Jerzy SilberringNeuropeptides play crucial, mediatory roles in many processes that occur in both CNS and PNS. The commonly accepted dogma for the release of bioactive peptides involves cleavage of inactive precursor by sequential action of proteinases recognizing dibasic stretches, followed by truncation of C-terminal Arg/Lys by the carboxypeptidase-like enzyme(s). Dynorphin convertases play an important role in CNS by regulating dynor Read More
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Matriptase-2, a Regulatory Protease of Iron Homeostasis: Possible Substrates, Cleavage Sites and Inhibitors
Authors: Marit Stirnberg and Michael GutschowMatriptase-2 is a cell surface serine protease with a modular structure. The exploration of its function in iron homeostasis was of significance for the understanding of the regulation of hepcidin expression, the master protein in iron control. Mutations in matriptase- 2 cause iron-refractory iron deficiency anemia (IRIDA), an iron deficiency disorder where the level of hepcidin is inappropriately high. Matriptase-2 controls hepcidin Read More
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Future of Protease Activity Assays
Authors: Magdalena Wysocka and Adam LesnerProteolysis is doubtlessly the most widespread mechanism of biological regulation. By controlling protein synthesis, turnover and activity, it is involved in fundamental physiological processes including apoptosis, cell differentiation, growth and signaling, fertilization, immune response, blood coagulation and digestion. Yet, uncontrolled proteolysis can be harmful for organisms, causing - amongst others - such diseases as canc Read More
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Natural Proteinaceous Inhibitors of Serine Proteases
More LessThe deregulated proteolysis is associated with various diseases in humans. Proteases are commonly regarded as the therapeutic targets. Almost one-third of all proteolytic enzymes in humans are serine proteases. This work provides a brief characteristic of the proteinaceous natural inhibitors, mostly of serine proteases. The examples of some classical and recently identified canonical and noncanonical inhibitors as w Read More
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MMP-9 Inhibitors in the Brain: Can Old Bullets Shoot New Targets?
More LessMatrix metalloproteinases (MMPs) are either secreted or membrane-bound proteases, capable to degrade extracellular matrix (ECM) proteins as well as a large number of non-ECM proteins, such as growth factors, cytokines, chemokines, cell surface receptors, serine proteinase inhibitors and other MMPs. MMPs play major physiological roles in reproduction, growth, development, angiogenesis, immune response, wound healing Read More
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Bacterial Proteases in Disease – Role in Intracellular Survival, Evasion of Coagulation/ Fibrinolysis Innate Defenses, Toxicoses and Viral Infections
Authors: Grzegorz Dubin, Joanna Koziel, Krzysztof Pyrc, Benedykt Wladyka and Jan PotempaPathogenic bacteria have evolved multiple mechanisms aimed to evade host defenses. This review summarizes selected examples of how bacteria utilize proteolytic enzymes to efficiently establish and spread infection systemically. First, the role of proteases in intracellular survival and persistence – the primary means used by bacteria to endure phagocytosis and/or avoid the vigilance of the immune system – is discusse Read More
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Mast Cell Chymase and Tryptase as Targets for Cardiovascular and Metabolic Diseases
Authors: Aina He and Guo-Ping ShiMast cells are critical effectors in inflammatory diseases, including cardiovascular and metabolic diseases and their associated complications. These cells exert their physiological and pathological activities by releasing granules containing histamine, cytokines, chemokines, and proteases, including mast cell-specific chymases and tryptases. Several recent human and animal studies have shown direct or indirect participatio Read More
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Viral Proteases as Targets for Drug Design
Authors: Marcin Skorenski and Marcin SienczykIn order to productively infect a host, viruses must enter the cell and force host cell replication mechanisms to produce new infectious virus particles. The success of this process unfortunately results in disease progression and, in the case of infection with many viral species, may cause mortality. The discoveries of Louis Pasteur and Edward Jenner led to one of the greatest advances in modern medicine - the developme Read More
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Phosphonic Esters and their Application of Protease Control
Authors: Renata Grzywa and Marcin Sienczykα-Aminoalkylphosphonate diaryl esters are potent, irreversible, and highly selective site-directed inhibitors of serine proteases. The structure of the phosphonate group resembles the transition state observed during a peptide bond hydrolysis and therefore phosphonates are referred as transition state analogues. They react with the hydroxyl group of the active site serine residue leading to formation of a stable enzyme-inhibitor co 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)
- Issue 42
- Issue 41
- Issue 40
- Issue 39
- Issue 38
- Issue 37
- Issue 36
- Issue 35
- Issue 34
- Issue 33
- Issue 32
- Issue 31
- Issue 30
- Issue 29
- Issue 27
- Issue 26
- Issue 25
- Issue 24
- Issue 23
- Issue 22
- Issue 21
- Issue 20
- Issue 19
- Issue 18
- Issue 17
- Issue 16
- Issue 15
- Issue 28
- Issue 14
- Issue 13
- 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 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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