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Review
. 2006 Mar;11(5-6):191-202.
doi: 10.1016/S1359-6446(05)03689-5.

Keynote review: allosterism in membrane receptors

Zhan-Guo Gao  1 , Kenneth A Jacobson
Affiliations
Review

Keynote review: allosterism in membrane receptors

Zhan-Guo Gao et al. Drug Discov Today. 2006 Mar.

Abstract

Allosteric modulation of membrane receptors has been intensively studied in the past three decades and is now considered to be an important indirect mechanism for the control of receptor function. The allosteric site on the GABA(A) receptor is the target for the most widely prescribed sleep medicines, the benzodiazepines. Cinacalcet, an allosteric enhancer of the calcium-sensing receptor, is used to treat secondary hyperparathyroidism. Allosteric ligands might be especially valuable to control receptors for which the design of selective orthosteric agonists or antagonists has been elusive, such as muscarinic acetylcholine receptors.

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Figures

FIGURE 1
FIGURE 1
Structures of representative allosteric modulators for class A GPCRs that are in clinical trials or used as research tools.
FIGURE 2
FIGURE 2
Structures of representative allosteric modulators for class B GPCRs that are in clinical trials or used as research tools.
FIGURE 3
FIGURE 3
Structures of representative allosteric modulators for class C GPCRs (GABAB and mGlu) that are in clinical trials or used as research tools.
FIGURE 4
FIGURE 4
Structures of representative allosteric modulators for class C GPCRs (CaR) that are used in the clinic or as research tools.
FIGURE 5
FIGURE 5
Structures of representative allosteric modulators for LGICs,Trk and guanylate cyclase receptors that are used in the clinic or as research tools.
See this image and copyright information in PMC

References

    1. Monod J et al. (1965) On the nature of allosteric transitions: a plausible model. J. Mol. Biol 12, 88–118 - PubMed
    1. Christopoulos A (2002) Allosteric binding sites on cell-surface receptors: novel targets for drug discovery. Nat. Rev. Drug Discov 1, 198–210 - PubMed
    1. Changeux JP and Edelstein SJ (2005) Allosteric mechanisms of signal transduction. Science 308, 1424–1428 - PubMed
    1. Bohr C et al. (1904) Ubereinen in biologischen Beziehung wichtigen Einfluss, den die Kohlen-sauerspannung des Blütes auf dessen Sauerstoffbindung ubt. Skand. Arch. Physiol 15, 401–412
    1. Changeux JP et al. (1967) On the cooperativity of biological membranes. Proc. Natl. Acad. Sci. U. S. A 57, 335–341 - PMC - PubMed

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