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G protein-coupled receptors (GPCRs)

 

G protein-coupled receptors (GPCRs) sense molecules outside the cell and activate inside signal transduction pathways and, ultimately, cellular responses. They are called seven-transmembrane receptors because they pass through the cell membrane seven times.

Figure 1 ASSET™ plan and detail Copyright: The Automation Partnership
Figure 1 ASSET™ plan and detail Copyright: The Automation Partnership
article

High content cell based primary screening for oncology targets – a perspective

25 June 2010 | By Peter Alcock, Colin Bath, Carolyn Blackett & Peter B. Simpson, Screening & Assay Sciences, Cancer Bioscience, AstraZeneca Alderley Park

Over the last 15 years, vendors have offered microscope-based instruments capable of producing images of fluorescent labelled components of cells grown in microtitre plates. These instruments are typically bundled with analysis software capable of defining the relative distribution of several fluorescent markers on a cell by cell basis1,2. As the…

Figure 1 MD simulation model of the opsin-transducin complex in a POPC lipid bilayer. Opsin and transducin are drawn in ribbon format and post-translational modification on opsin and transducin are represented in space-fill style. Opsin is oriented in the bilayer such that helix 4 (H4) is perpendicular to the plane of the bilayer. The extracellular surface is oriented toward the top of the figure.
Figure 1 MD simulation model of the opsin-transducin complex in a POPC lipid bilayer. Opsin and transducin are drawn in ribbon format and post-translational modification on opsin and transducin are represented in space-fill style. Opsin is oriented in the bilayer such that helix 4 (H4) is perpendicular to the plane of the bilayer. The extracellular surface is oriented toward the top of the figure.
article

Examining receptor activation: New technologies reveal how G protein-coupled receptors recognise ligands and talk to intracellular partners

24 June 2010 | By Thomas P. Sakmar, Laboratory of Molecular Biology & Biochemistry, Rockefeller University

Heptahelical G protein-coupled receptors (GPCRs) are arguably the most important single class of pharmaceutical drug targets in the human genome. According to Overington, of the 266 human targets for approved drugs, a remarkable 27 per cent correspond to rhodopsin-like, or Family A, GPCRs. Despite recent dramatic advances in targeting of…