Allosteric binding sites on cell-surface receptors: novel targets for drug discovery

@article{Christopoulos2002AllostericBS,
  title={Allosteric binding sites on cell-surface receptors: novel targets for drug discovery},
  author={A. Christopoulos},
  journal={Nature Reviews Drug Discovery},
  year={2002},
  volume={1},
  pages={198-210}
}
  • A. Christopoulos
  • Published 2002
  • Chemistry, Medicine
  • Nature Reviews Drug Discovery
  • Cell-surface receptors are the targets for more than 60% of current drugs. Traditionally, optimizing the interaction of lead molecules with the binding site for the endogenous agonist (orthosteric site) has been viewed as the best means of achieving selectivity of action. However, recent developments have highlighted the fact that drugs can interact with binding sites on the receptor molecule that are distinct from the orthosteric site, known as allosteric sites. Allosteric modulators could… CONTINUE READING
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    References

    SHOWING 1-10 OF 148 REFERENCES
    G Protein-Coupled Receptor Allosterism and Complexing
    • 820
    • PDF
    Positive allosteric modulators of metabotropic glutamate 1 receptor: Characterization, mechanism of action, and binding site
    • F. Knoflach, V. Mutel, +5 authors J. Kemp
    • Biology, Medicine
    • Proceedings of the National Academy of Sciences of the United States of America
    • 2001
    • 220
    • PDF
    Antagonists with negative intrinsic activity at delta opioid receptors coupled to GTP-binding proteins.
    • T. Costa, A. Herz
    • Chemistry, Medicine
    • Proceedings of the National Academy of Sciences of the United States of America
    • 1989
    • 474
    • PDF
    Structural and functional aspects of G protein-coupled receptor oligomerization.
    • 112
    Inverse, protean, and ligand‐selective agonism: matters of receptor conformation
    • T. Kenakin
    • Biology, Medicine
    • FASEB journal : official publication of the Federation of American Societies for Experimental Biology
    • 2001
    • 394