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- Volume 15, Issue 35, 2009
Current Pharmaceutical Design - Volume 15, Issue 35, 2009
Volume 15, Issue 35, 2009
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Editorial [Hot topic: In Silico Approaches in G Protein-Coupled Receptors (GPCRs) Drug Discovery: Quo Vadis? (Executive Editor: Stefano Moro)]
By Stefano MoroHow do we communicate with the outside world? How are our senses of vision, smell, taste and pain controlled at the cellular and molecular levels? What causes medical conditions like allergies, hypertension, depression, obesity and various central nervous system disorders? G protein-coupled receptors (GPCRs) provide a major part of the answer to all of these questions. GPCRs constitute the largest family of cell-surface recept Read More
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Rhodopsin and the Others: A Historical Perspective on Structural Studies of G Protein-Coupled Receptors
Authors: Stefano Costanzi, Jeffrey Siegel, Irina G. Tikhonova and Kenneth A. JacobsonThe role of rhodopsin as a structural prototype for the study of the whole superfamily of G protein-coupled receptors (GPCRs) is reviewed in an historical perspective. Discovered at the end of the nineteenth century, fully sequenced since the early 1980s, and with direct three-dimensional information available since the 1990s, rhodopsin has served as a platform to gather indirect information on the structure of the other su Read More
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Unraveling the Structure and Function of G Protein-Coupled Receptors Through NMR Spectroscopy
Authors: Irina G. Tikhonova and Stefano CostanziG protein-coupled receptors (GPCRs) are a large superfamily of signaling proteins expressed on the plasma membrane. They are involved in a wide range of physiological processes and, therefore, are exploited as drug targets in a multitude of therapeutic areas. In this extent, knowledge of structural and functional properties of GPCRs may greatly facilitate rational design of modulator compounds. Solution and solid-state nu Read More
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Progress in Elucidating the Structural and Dynamic Character of G Protein-Coupled Receptor Oligomers for Use in Drug Discovery
Authors: A. Bortolato, J. C. Mobarec, D. Provasi and M. FilizolaG Protein-Coupled Receptors (GPCRs) are the most targeted group of proteins for the development of therapeutic drugs. Until the last decade, structural information about this family of membrane proteins was relatively scarce, and their mechanisms of ligand binding and signal transduction were modeled on the assumption that GPCRs existed and functioned as monomeric entities. New crystal structures of nativ Read More
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Customizing G Protein-Coupled Receptor Models for Structure-Based Virtual Screening
Authors: Chris de Graaf and Didier RognanThis review will focus on the construction, refinement, and validation of G Protein-coupled receptor models for the purpose of structure-based virtual screening. Practical tips and tricks derived from concrete modeling and virtual screening exercises to overcome the problems and pitfalls associated with the different steps of the receptor modeling workflow will be presented. These examples will not only include rhodopsin-l Read More
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G Protein-Coupled Receptors: Target-Based In Silico Screening
Authors: Hanoch Senderowitz and Yael MarantzIn silico (or virtual) screening has become a common practice in current computer-aided drug design efforts. However, application to hit discovery in the G Protein-Coupled Receptors (GPCRs) arena was until recently hampered by the paucity of crystal structures available for this important class of pharmaceutical targets, forcing practitioners in the field to rely on GPCR models derived either ab initio or through homology modelin Read More
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Human A3 Adenosine Receptor as Versatile G Protein-Coupled Receptor Example to Validate the Receptor Homology Modeling Technology
Authors: Erika Morizzo, Stephanie Federico, Giampiero Spalluto and Stefano MoroThe development of ligands for the A3 adenosine receptor (AR) has been directed mainly by traditional medicinal chemistry, but the influence of structure-based approaches is increasing. Rhodopsin-based homology modeling had been used for many years to obtain three-dimensional models of the A3AR, and different A3AR models have been published describing the hypothetical interactions with known A3AR ligands having di 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)
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Volume 17 (2011)
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Volume 16 (2010)
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Volume 15 (2009)
- Issue 36
- Issue 35
- Issue 34
- Issue 33
- Issue 32
- Issue 31
- Issue 30
- Issue 29
- Issue 28
- Issue 27
- Issue 26
- Issue 25
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- Issue 22
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- Issue 14
- Issue 13
- Issue 12
- Issue 11
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- Issue 7
- Issue 6
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- Issue 3
- Issue 2
- Issue 1
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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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