Molecular Mechanisms of Ligand Interaction with the Gonadotropin-Releasing Hormone Receptor
Stuart C. Sealfon,
Harel Weinstein and
Robert P. Millar
Fishberg Research Center in Neurobiology (S.C.S.), Departments of
Neurology (S.C.S.), Physiology and Biophysics (H.W.), and Pharmacology
(H. W.), Mount Sinai School of Medicine, New York, New York 10029; and
Medical Research Council Regulatory Peptides Unit (R.P.M.), Departments
of Chemical Pathology (R.P.M.) and Medicine (R.P.M.), University of
Cape Town Medical School, Observatory 7925, South Africa
I. Introduction
II. Amino Acid Sequences of GnRH Receptors
A. GnRH receptor cDNAs
B. General structural features
C.Covalent modifications
D. Gene structure
III. Structure-ActivityRelations of GnRH Peptides
A. Overview
B. Comparative structuresand activities of vertebrate GnRHs
C. Roles of individualamino acids in GnRH activity at the mammalian
receptor
D.Conclusions from peptide structure-activity data
IV. Structureand Conformation of GnRH and Its Analogs
A. Early studiesof GnRH conformation
B. Integrated computational and experimentalstudies
C. Exploration of the entire conformation space ofGnRH analogs
V. Functional Structure of the Receptor and Ligand-ReceptorComplex
A. Extracellular domains
B. Helix domains
C. Intracellularloop domains
D. Computational modeling of three-dimensionalreceptor structure
VI. Conclusions
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1079 - 1088.
[Abstract][Full Text][PDF]
D. Grove-Strawser, S. A. Sower, P. M. Ronsheim, J. B. Connolly, C. G. Bourn, and B. S. Rubin Guinea Pig GnRH: Localization and Physiological Activity Reveal That It, Not Mammalian GnRH, Is the Major Neuroendocrine Form in Guinea Pigs
Endocrinology,
May 1, 2002;
143(5):
1602 - 1612.
[Abstract][Full Text][PDF]
C. Castro-Fernandez, J. A. Janovick, S. P. Brothers, R. A. Fisher, T. H. Ji, and P. M. Conn Regulation of RGS3 and RGS10 Palmitoylation by GnRH
Endocrinology,
April 1, 2002;
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D. Pati and H. R. Habibi Involvement of Protein Kinase C and Arachidonic Acid Pathways in the Gonadotropin-Releasing Hormone Regulation of Oocyte Meiosis and Follicular Steroidogenesis in the Goldfish Ovary
Biol Reprod,
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813 - 822.
[Abstract][Full Text][PDF]
B. J. Fromme, A. A. Katz, R. W. Roeske, R. P. Millar, and C. A. Flanagan Role of Aspartate7.32(302) of the Human Gonadotropin-Releasing Hormone Receptor in Stabilizing a High-Affinity Ligand Conformation
Mol. Pharmacol.,
December 1, 2001;
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[Abstract][Full Text][PDF]
H. M. Everest, J. N. Hislop, T. Harding, J. B. Uney, A. Flynn, R. P. Millar, and C. A. McArdle Signaling and Antiproliferative Effects Mediated by GnRH Receptors After Expression in Breast Cancer Cells Using Recombinant Adenovirus
Endocrinology,
November 1, 2001;
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4663 - 4672.
[Abstract][Full Text][PDF]
J. N. Hislop, H. M. Everest, A. Flynn, T. Harding, J. B. Uney, B. E. Troskie, R. P. Millar, and C. A. McArdle Differential Internalization of Mammalian and Non-mammalian Gonadotropin-releasing Hormone Receptors. UNCOUPLING OF DYNAMIN-DEPENDENT INTERNALIZATION FROM MITOGEN-ACTIVATED PROTEIN KINASE SIGNALING
J. Biol. Chem.,
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[Abstract][Full Text][PDF]
L. Wang, D. Y. Oh, J. Bogerd, H. S. Choi, R. S. Ahn, J. Y. Seong, and H. B. Kwon Inhibitory Activity of Alternative Splice Variants of the Bullfrog GnRH Receptor-3 on Wild-Type Receptor Signaling
Endocrinology,
September 1, 2001;
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[Abstract][Full Text][PDF]
F. Van Goor, Y.-X. Li, and S. S. Stojilkovic Paradoxical Role of Large-Conductance Calcium-Activated K+ (BK) Channels in Controlling Action Potential-Driven Ca2+ Entry in Anterior Pituitary Cells
J. Neurosci.,
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R. Millar, S. Lowe, D. Conklin, A. Pawson, S. Maudsley, B. Troskie, T. Ott, M. Millar, G. Lincoln, R. Sellar, et al. A novel mammalian receptor for the evolutionarily conserved type II GnRH
PNAS,
August 1, 2001;
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141048498.
[Abstract][Full Text][PDF]
R. D. Horvat, D. A. Roess, S. E. Nelson, B. G. Barisas, and C. M. Clay Binding of Agonist but Not Antagonist Leads to Fluorescence Resonance Energy Transfer between Intrinsically Fluorescent Gonadotropin-Releasing Hormone Receptors
Mol. Endocrinol.,
May 1, 2001;
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[Abstract][Full Text]
K. W. Cheon, H.-S. Lee, I. S. Parhar, and I. S. Kang Expression of the second isoform of gonadotrophin-releasing hormone (GnRH-II) in human endometrium throughout the menstrual cycle
Mol. Hum. Reprod.,
May 1, 2001;
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[Abstract][Full Text][PDF]
L. Wang, J. Bogerd, H. S. Choi, J. Y. Seong, J. M. Soh, S. Y. Chun, M. Blomenröhr, B. E. Troskie, R. P. Millar, W. H. Yu, et al. Three distinct types of GnRH receptor characterized in the bullfrog
PNAS,
December 14, 2000;
(2000)
11508498.
[Abstract][Full Text]
J. N. Hislop, M. T. Madziva, H. M. Everest, T. Harding, J. B. Uney, G. B. Willars, R. P. Millar, B. E. Troskie, J. S. Davidson, and C. A. McArdle Desensitization and Internalization of Human and XenopusGonadotropin-Releasing Hormone Receptors Expressed in {{alpha}}T4 Pituitary Cells Using Recombinant Adenovirus
Endocrinology,
December 1, 2000;
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4564 - 4575.
[Abstract][Full Text][PDF]
T. Madigou, E. Mañanos-Sanchez, S. Hulshof, I. Anglade, S. Zanuy, and O. Kah Cloning, Tissue Distribution, and Central Expression of the Gonadotropin-Releasing Hormone Receptor in the Rainbow Trout (Oncorhynchus mykiss)
Biol Reprod,
December 1, 2000;
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[Abstract][Full Text]
R. Sosnowski, P. L. Mellon, and M. A. Lawson Activation of Translation in Pituitary Gonadotrope Cells by Gonadotropin-Releasing Hormone
Mol. Endocrinol.,
November 1, 2000;
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[Abstract][Full Text]
S. H. Hoffmann, T. t. Laak, R. Kühne, H. Reiländer, and T. Beckers Residues within Transmembrane Helices 2 and 5 of the Human Gonadotropin-Releasing Hormone Receptor Contribute to Agonist and Antagonist Binding
Mol. Endocrinol.,
July 1, 2000;
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[Abstract][Full Text]
F. E. M. Rebers, P. T. Bosma, W. van Dijk, H. J. T. Goos, and R. W. Schulz GnRH stimulates LH release directly via inositol phosphate and indirectly via cAMP in African catfish
Am J Physiol Regulatory Integrative Comp Physiol,
June 1, 2000;
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[Abstract][Full Text][PDF]
J. Cui, R. G. Smith, G. R. Mount, J.-L. Lo, J. Yu, T. F. Walsh, S. B. Singh, R. J. DeVita, M. T. Goulet, J. M. Schaeffer, et al. Identification of Phe313 of the Gonadotropin-Releasing Hormone (GnRH) Receptor as a Site Critical for the Binding of Nonpeptide GnRH Antagonists
Mol. Endocrinol.,
May 1, 2000;
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671 - 681.
[Abstract][Full Text]
B. E. Troskie, J. P. Hapgood, R. P. Millar, and N. Illing Complementary Deoxyribonucleic Acid Cloning, Gene Expression, and Ligand Selectivity of a Novel Gonadotropin-Releasing Hormone Receptor Expressed in the Pituitary and Midbrain of Xenopus laevis
Endocrinology,
May 1, 2000;
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[Abstract][Full Text][PDF]
J. Carolsfeld, J. F. F. Powell, M. Park, W. H. Fischer, A. G. Craig, J. P. Chang, J. E. Rivier, and N. M. Sherwood Primary Structure and Function of Three Gonadotropin-Releasing Hormones, Including a Novel Form, from an Ancient Teleost, Herring
Endocrinology,
February 1, 2000;
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H.-O. Chung, Q. Yang, K. J. Catt, and K. K. Arora Expression and Function of the Gonadotropin-releasing Hormone Receptor Are Dependent on a Conserved Apolar Amino Acid in the Third Intracellular Loop
J. Biol. Chem.,
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M. Blomenröhr, A. Heding, R. Sellar, R. Leurs, J. Bogerd, K. A. Eidne, and G. B. Willars Pivotal Role for the Cytoplasmic Carboxyl-Terminal Tail of a Nonmammalian Gonadotropin-Releasing Hormone Receptor in Cell Surface Expression, Ligand Binding, and Receptor Phosphorylation and Internalization
Mol. Pharmacol.,
December 1, 1999;
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[Abstract][Full Text]
C. A. Flanagan, W. Zhou, L. Chi, T. Yuen, V. Rodic, D. Robertson, M. Johnson, P. Holland, R. P. Millar, H. Weinstein, et al. The Functional Microdomain in Transmembrane Helices 2 and 7 Regulates Expression, Activation, and Coupling Pathways of the Gonadotropin-releasing Hormone Receptor
J. Biol. Chem.,
October 8, 1999;
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[Abstract][Full Text][PDF]
F. P. Pralong, F. Gomez, E. Castillo, S. Cotecchia, L. Abuin, M. L. Aubert, L. Portmann, and R. C. Gaillard Complete Hypogonadotropic Hypogonadism Associated with a Novel Inactivating Mutation of the Gonadotropin-Releasing Hormone Receptor
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[Abstract][Full Text][PDF]
K. K. Arora, H.-O. Chung, and K. J. Catt Influence of a Species-Specific Extracellular Amino Acid on Expression and Function of the Human Gonadotropin-Releasing Hormone Receptor
Mol. Endocrinol.,
June 1, 1999;
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J. D. Neill, L. C. Musgrove, L. W. Duck, and J. C. Sellers High Efficiency Method for Gene Transfer in Normal Pituitary Gonadotropes: Adenoviral-Mediated Expression of G Protein-Coupled Receptor Kinase 2 Suppresses Luteinizing Hormone Secretion
Endocrinology,
June 1, 1999;
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N. Illing, B. E. Troskie, C. S. Nahorniak, J. P. Hapgood, R. E. Peter, and R. P. Millar Two gonadotropin-releasing hormone receptor subtypes with distinct ligand selectivity and differential distribution in brain and pituitary in the goldfish (Carassius auratus)
PNAS,
March 2, 1999;
96(5):
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S. Nelson, R. D. Horvat, J. Malvey, D. A. Roess, B. G. Barisas, and C. M. Clay Characterization of an Intrinsically Fluorescent Gonadotropin-Releasing Hormone Receptor and Effects of Ligand Binding on Receptor Lateral Diffusion
Endocrinology,
February 1, 1999;
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950 - 957.
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X. Lin and P. M. Conn Transcriptional Activation of Gonadotropin-Releasing Hormone (GnRH) Receptor Gene by GnRH: Involvement of Multiple Signal Transduction Pathways
Endocrinology,
January 1, 1999;
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358 - 364.
[Abstract][Full Text]
X. Lin, J. A. Janovick, and P. M. Conn Mutations at the Consensus Phosphorylation Sites in the Third Intracellular Loop of the Rat Gonadotropin-Releasing Hormone Receptor: Effects on Receptor Ligand Binding and Signal Transduction
Biol Reprod,
December 1, 1998;
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K. K. Arora, L. Z. Krsmanovic, N. Mores, H. O'Farrell, and K. J. Catt Mediation of Cyclic AMP Signaling by the First Intracellular Loop of the Gonadotropin-releasing Hormone Receptor
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October 2, 1998;
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[Abstract][Full Text][PDF]
