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Titlebook: GPCRs: From Deorphanization to Lead Structure Identification; H. Bourne,R. Horuk,H. Michel Conference proceedings 2007 Springer-Verlag Ber

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Modulation of GPCR Conformationsby Ligands, G-Proteins, and Arrestins,f GPCRs, G-proteins, arrestins, and ligands in solubilized systems, where the concentration of each component can be defined. Here we summarize results of these studies as they pertain to the regulation of GPCR conformations and affinities for interacting species.
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High Content Screening to Monitor G Protein-Coupled Receptor Internalisation,n, resulting in the termination of receptor signalling and the seclusion of the GPCR from further extracellular stimulation. Complementary to other functional GPCR drug discovery assays, GPCR internalisation assays enable a desensitisation-focussed pharmacological analysis of test compounds.
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Modeling GPCRs,ase of the structure of bovine rhodopsin in August 2000 enabled us to analyze models built before that period to learn things for the models we build today. We conclude that the GPCR modeling field is riddled with “common knowledge”. Several characteristics of the bovine rhodopsin structure came as
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QSAR Modeling of GPCR Ligands: Methodologies and Examples of Applications,se 3D structures of GPCRs as determined by experimental techniques are still unavailable, ligand-based drug discovery methods remain the major computational molecular modeling approaches to the analysis of growing data sets of tested GPCR ligands. This paper presents an overview of modern Quantitati
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Privileged Structures in GPCRs, structures. In seeking an explanation for this phenomenon, it is observed that the privileged structure represents a generic substructure that matches commonly recurring conserved structural motifs in the target proteins, which may otherwise be quite diverse in sequence and function. Using sequence
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Designing Compound Libraries Targeting GPCRs,ors and the herewith linked dominant place in the discovery portfolios. In the present symposium chapter, we outline GPCR compound library design strategies recently followed by our group and discuss them in a more general context.
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Orphan Seven Transmembrane Receptor Screening,g them. However, it is clear that there remains an undefined potential within this protein family for successful drugs of the future. The human genome sequencing project identified approximately 720 genes that belong to the 7TMR superfamily. Around half of these genes encode sensory receptors, while
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