The state of GPCR research in 2004

@article{Ellis2004TheSO,
  title={The state of GPCR research in 2004},
  author={Clare Udras Ellis},
  journal={Nature Reviews Drug Discovery},
  year={2004},
  volume={3},
  pages={577-626}
}
  • C. Ellis
  • Published 1 July 2004
  • Biology
  • Nature Reviews Drug Discovery
G-protein-coupled receptors (GPCRs) comprise the largest single class of cell-surface receptors, and have a history of being excellent therapeutic targets for a number of diseases. Yet several fundamental questions remain regarding their underlying biology, and many GPCRs that could be promising targets for drug discovery are still uncharacterized at the level of identified ligand or biological function. In an attempt to find some answers, we posed 20 questions of fundamental importance to the… 
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The role of membrane cholesterol in GPCR function is discussed with specific example of the receptor and an emerging and important concept is oligomerization of GPCRs and its role in G PCR function and signaling.
The function of G-protein coupled receptors and membrane cholesterol: specific or general interaction?
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The nature of cholesterol dependence of GPCR function is highlighted by taking a few known examples and suggesting alterations in the membrane physical properties induced by cholesterol.
Sphingolipids in the function of G protein-coupled receptors.
Receptors as Drug Targets
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Concepts such as receptor constitutive activity, internalization and dimerization add additional complexity to the role of receptors in tissue function and in precisely characterizing their role in homeostasis and disease.
An improved classification of G-protein-coupled receptors using sequence-derived features
TLDR
High accuracies are achieved when predicting GPCRs at all the five levels with the proposed PCA-GPCR method, believed to be capable of capturing information about amino acid composition, sequence order as well as various physicochemical properties of proteins.
G-protein-coupled receptor signalling through protein networks.
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This short review provides a broad, and therefore necessarily incomplete and personal, overview of G-protein-coupled receptors, which are often targets for a wide range of important drugs: their structure, function and interactions with associated proteins.
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  • T. Kenakin
  • Biology
    Nature Reviews Drug Discovery
  • 2002
TLDR
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TLDR
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