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- Volume 18, Issue 30, 2012
Current Pharmaceutical Design - Volume 18, Issue 30, 2012
Volume 18, Issue 30, 2012
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Pharmacophore Modelling as a Virtual Screening Tool for the Discovery of Small Molecule Protein-protein Interaction Inhibitors
Authors: Arnout Voet and Kam Y.J. ZhangPharmacophore searches have become a popular tool for virtual screening of libraries to identify novel active substances that can be potentially developed into drugs. While they have been applied for years on common drug targets, their application in the discovery of protein-protein interaction inhibitors remains limited. This review describes current pharmacophore modelling methods applied in the discovery of novel Read More
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Druggability of Dynamic Protein-protein Interfaces
Authors: Ozlem Ulucan, Susanne Eyrisch and Volkhard HelmsThe conformational flexibility of protein targets is being increasingly recognized in the drug discovery and design processes. When working on a particular disease-related biochemical pathway, it is of crucial importance to carefully select druggable protein binding pockets among all those cavities that may appear transiently or permanently on the respective protein surface. In this review, we will focus on the conformation Read More
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Protein-protein Docking and Hot-spot Prediction for Drug Discovery
Authors: Solene Grosdidier and Juan Fernandez-RecioMost processes in living organisms occur through an intricate network of protein-protein interactions, in which any malfunctioning can lead to pathological situations. Therefore, current research in biomedicine is starting to focus on protein interaction networks. A detailed structural knowledge of these interactions at molecular level will be necessary for drug discovery targeting protein-protein interactions. The challe Read More
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Protein-protein Interactions: Network Analysis and Applications in Drug Discovery
Authors: Jennyfer Bultinck, Sam Lievens and Jan TavernierPhysical interactions among proteins constitute the backbone of cellular function, making them an attractive source of therapeutic targets. Although the challenges associated with targeting protein-protein interactions (PPIs) -in particular with small molecules - are considerable, a growing number of functional PPI modulators is being reported and clinically evaluated. An essential starting point for PPI inhibitor scree Read More
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Modulating Protein-Protein Interactions: From Structural Determinants of Binding to Druggability Prediction to Application
Authors: Alexander Metz, Emanuele Ciglia and Holger GohlkeDuring the last decades, a large amount of evidence has been gathered on the importance of protein-protein interactions in tuning and regulating most important biological processes. Since many of these pathways are deeply involved in diseases, extensive research efforts have been undertaken towards the modulation of protein-protein interactions. At the early stage of this challenge most of the attention was drawn Read More
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A Leap into the Chemical Space of Protein-Protein Interaction Inhibitors
Authors: B. O. Villoutreix, C. M. Labbe, D. Lagorce, G. Laconde and O. SperandioProtein-protein interactions (PPI) are involved in vital cellular processes and are therefore associated to a growing number of diseases. But working with them as therapeutic targets comes with some major hurdles that require substantial mutations from our way to design drugs on historical targets such as enzymes and G-Protein Coupled Receptor (GPCR). Among the numerous ways we could improve our methodologies to Read More
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P53 Mdm2 Inhibitors
Authors: Kareem Khoury and Alex DomlingThe protein-protein interaction (PPI) between p53 and its negative regulator MDM2 comprises one of the most important and intensely studied PPI's involved in preventing the initiation of cancer. The interaction between p53 and MDM2 is conformation-based and is tightly regulated on multiple levels. Due to the Angstrom level structural insight there is a reasonable understanding of the structural requirements needed for a mol Read More
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Small-Molecule Inhibitors of Protein-Protein Interactions: How to Mimic a Protein Partner
By David C. FryThis systematic review describes successful examples of small-molecule inhibitors of protein-protein interactions, and compares their binding strategies to those employed by the natural protein partners. It extends and updates an earlier survey of this type (Fry DC, Curr Prot Pep Sci 2008; 9: 240-7). From analysis of these systems, common themes and lessons are presented that may assist future drug discovery efforts invo Read More
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Using Fragment-Based Technologies to Target Protein-Protein Interactions
Authors: Justin F. Bower and Andrew PanniferWhilst fragment-based screening has found significant utility in aiding the discovery of high quality hits against a range of targets, the use of this technology in the protein-protein interaction inhibitor field is very much in its infancy. This review aims to highlight the key technologies used to identify fragment hits, such as NMR, SPR, X-ray crystallography and biochemical screening, the fragmentbased protein-protein interacti Read More
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Protein-protein Interfaces Integrated into Interaction Networks: Implications on Drug Design
Authors: Gozde Kar, Guray Kuzu, Ozlem Keskin and Attila GursoyThe growing perception that diseases are often consequences of multiple molecular abnormalities rather than being the result of a single defect highlights the importance of network-centric view in therapeutic approaches. Protein interaction networks may contribute to understanding of disease, assist in drug design and discovery. Here, we review some recent advances in disease-associated protein interaction networks t Read More
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Bioactive Peptides - Are There More Antihypertensive Mechanisms Beyond ACE Inhibition?
Diet has a high relevance in health. Hypertension is a major risk factor for cardiovascular diseases and has an important impact on public health, and consequently on countries economy. Scientific research gathered strong evidence about the role of several dietary factors either in etiology or in treatment/prevention of these diseases. Peptides from different food matrices have been studied, and indicated as compounds with p Read More
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Vasopressin Secretion Control: Central Neural Pathways, Neurotransmitters and Effects of Drugs
Vasopressin (AVP) secretion and release are regulated by a number of central nervous system sites that receive peripheral signals from the osmoreceptors and baroreceptors. Aim of this paper is to review anatomical pathways and neurotransmitters involved as well as drugs affecting AVP secretion.
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Protein Kinase C-theta Inhibitors: A Novel Therapy for Inflammatory Disorders
Authors: Sukhvir Chand, Nisha Mehta, Malkeet Singh Bahia, Anshuman Dixit and Om SilakariPKC- is a serine/threonine specific protein kinase and its activation depends upon the concentration of diacylglycerol (DAG) and phospholipids (phosphatidylserine). PKC- phosphorylates a variety of proteins that are known to be involved in the diverse cellular signaling pathways. It is predominantly expressed in the T-cells and localized in the center of immunological synapse upon T-cell receptor (TCR) and CD28 signali 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)
- Issue 38
- Issue 37
- Issue 36
- Issue 35
- Issue 34
- Issue 33
- Issue 32
- Issue 31
- Issue 30
- Issue 29
- Issue 28
- 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 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 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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