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Vol. 60, Issue 1, 1-19, July 2001
Novasite Pharmaceuticals, Inc. (J.A.B.), San Diego, California;
Center for Molecular Recognition (L.S., J.A.J.) and Departments of
Psychiatry (J.A.J.) and Pharmacology (L.S., J.A.J.), Columbia
University College of Physicians and Surgeons, New York, New York
The availability of a high-resolution structure of rhodopsin now allows
us to reconsider research attempts to understand structure-function relationships in other G protein-coupled receptors (GPCRs). A comparison of the rhodopsin structure with the results of previous sequence analysis and molecular modeling that incorporated experimental results demonstrates a high degree of success for these methods in
predicting the helix ends and protein-protein interface of GPCRs.
Moreover, the amino acid residues inferred to form the surface of the
binding-site crevice based on our application of the
substituted-cysteine accessibility method in the dopamine D2 receptor are in remarkable agreement with the rhodopsin
structure, with the notable exception of some residues in the fourth
transmembrane segment. Based on our analysis of the data reviewed, we
propose that the overall structures of rhodopsin and of amine receptors are very similar, although we also identified localized regions where
the structure of these receptors may diverge. We further propose that
several of the highly unusual structural features of rhodopsin are also
present in amine GPCRs, despite the absence of amino acids that might
have thought to have been critical to the adoption of these features.
Thus, different amino acids or alternate microdomains can support
similar deviations from regular 
-helical structure, thereby
resulting in similar tertiary structure. Such structural mimicry is a
mechanism by which a common ancestor could diverge sufficiently to
develop the selectivity necessary to interact with diverse signals,
while still maintaining a similar overall fold. Through this process,
the core function of signaling activation through a conformational
change in the transmembrane segments that alters the conformation of
the cytoplasmic surface and subsequent interaction with G proteins is
presumably shared by the entire Class A family of receptors, despite
their selectivity for a diverse group of ligands.
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M. L. Lopez-Rodriguez, B. Vicente, X. Deupi, S. Barrondo, M. Olivella, M. J. Morcillo, B. Behamu, J. A. Ballesteros, J. Salles, and L. Pardo Design, Synthesis and Pharmacological Evaluation of 5-Hydroxytryptamine1a Receptor Ligands to Explore the Three-Dimensional Structure of the Receptor Mol. Pharmacol., July 1, 2002; 62(1): 15 - 21. [Abstract] [Full Text] [PDF]
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R. L. Papke Enhanced Inhibition of a Mutant Neuronal Nicotinic Acetylcholine Receptor by Agonists: Protection of Function by (E)-N-Methyl-4-(3-pyridinyl)-3-butene-1-amine (TC-2403) J. Pharmacol. Exp. Ther., May 1, 2002; 301(2): 765 - 773. [Abstract] [Full Text] [PDF]
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V. Vlaeminck-Guillem, S.-C. Ho, P. Rodien, G. Vassart, and S. Costagliola Activation of the cAMP Pathway by the TSH Receptor Involves Switching of the Ectodomain from a Tethered Inverse Agonist to an Agonist Mol. Endocrinol., April 1, 2002; 16(4): 736 - 746. [Abstract] [Full Text] [PDF]
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M. Yang, W. Wang, M. Zhong, A. Philippi, O. Lichtarge, and B. M. Sanborn Lysine 270 in the Third Intracellular Domain of the Oxytocin Receptor is an Important Determinant for G{alpha}q Coupling Specificity Mol. Endocrinol., April 1, 2002; 16(4): 814 - 823. [Abstract] [Full Text] [PDF]
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 S. Panicker, H. Cruz, C. Arrabit, and P. A. Slesinger Evidence for a Centrally Located Gate in the Pore of a Serotonin-Gated Ion Channel J. Neurosci., March 1, 2002; 22(5): 1629 - 1639. [Abstract] [Full Text] [PDF]
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