Residues within transmembrane helices 2 and 5 of the human gonadotropin-releasing hormone receptor contribute to agonist and antagonist binding

Molecular Endocrinology

Volumn 14, Issue 7, 2000, Pages 1099-1115

  Hoffmann, Silke H ^a,b   Laak, Ton Ter ^c,d   Kühne, Ronald ^c   Reiländer, Helmut ^b   Beckers, Thomas ^a  

^a ASTA MEDICA AG   (Germany)

^b MAX PLANCK INSTITUTE OF BIOPHYSICS   (Germany)

^c LEIBNIZ INSTITUT FÜR MOLEKULARE PHARMAKOLOGIE   (Germany)

^d VU UNIVERSITY AMSTERDAM   (Netherlands)

Author keywords

[No Author keywords available]

Indexed keywords

ADENYLATE CYCLASE; ALANINE; CETRORELIX; CYCLIC AMP; GONADORELIN RECEPTOR; GUANINE NUCLEOTIDE BINDING PROTEIN; IODINE 125; LUCIFERASE; MEMBRANE PROTEIN; RECEPTOR PROTEIN; TRIPTORELIN;

AMINO ACID SUBSTITUTION; AMINO TERMINAL SEQUENCE; ANIMAL CELL; ARTICLE; BINDING AFFINITY; CONTROLLED STUDY; DRUG ANTAGONISM; DRUG POTENTIATION; ENZYME ACTIVITY; GLYCOSYLATION; HORMONE RECEPTOR INTERACTION; HUMAN; LIGAND BINDING; MOUSE; NONHUMAN; PRIORITY JOURNAL; PROTEIN CONFORMATION; RAT; REPORTER GENE; SIGNAL TRANSDUCTION; SITE DIRECTED MUTAGENESIS;

ANIMALIA; PHOTINUS PYRALIS; PYRALIS;

EID: 0034464661     PISSN: 08888809     EISSN: None     Source Type: Journal    
DOI: 10.1210/mend.14.7.0483     Document Type: Article

References (64)

1. Isolation of the luteinizing hormone and follicle-stimulating hormone-releasing hormone from porcine hypothalami
2. Primary structure of ovine hypothalamic luteinizing hormone-releasing factor (LRF)
3. Modulation of gonadotropin levels by peptides acting at the anterior pituitary gland
4. The use of a potent stimulatory LHRH analog (D-Trp6-LHRH) in the induction of ovulation
5. Long-term treatment of central precocious puberty with a long-acting analogue of luteinizing hormone-releasing hormone
6. Chemistry and molecular biology in the search for new LH-RH antagonists
7. Gonadotropin-releasing hormone and its analogues
8. The use of luteinizing hormone-releasing hormone agonists and antagonists in gynaecological cancers
9. LH-RH antagonists: State of the art and future perspectives
10. Conformation-function relationships in LHRH analogs
11. Gonadotropin-releasing hormone analog design. Structure function studies towards development of agonists and antagonists: Rational and perspective
12. Gonadotropin-releasing hormone receptors: Structure and signal transduction pathways
13. Molecular mechanisms of ligand interaction with the gonadotropin-releasing hormone receptor
14. Mechanisms mediating multiple physiological responses to gonadotropin-releasing hormone
15. 2+ and protein kinase C
16. Regulation of Gq/G11α by the GnRH receptor
17. Gonadotropin-releasing hormone receptor couples to multiple G proteins in rat gonadotrophs and in GH3 cells: Evidence from palmitoylation and overexpression of G proteins
18. Stable transfection of GH3 cells with rat gonadotropin-releasing hormone receptor complementary deoxyribonucleic acid results in expression of a receptor coupled to cyclic adenosine 3′,5′-monophosphate-dependent prolactin release via a G-protein
19. Biphasic action of cyclic adenosine 3′,5′-monophosphate in gonadotropin-releasing hormone (GnRH) analog-stimulated hormone release from GH3 cells stably transfected with GnRH receptor complementary deoxyribonucleic acid
20. Rat gonadotropin-releasing hormone receptor expressed in insect cells induces activation of adenylyl cyclase
21. Projections structure of rhodopsin
22. Low resolution structure of bovine rhodopsin determined by electron cryomicroscopy
23. Arrangement of rhodopsin transmembrane α-helices
24. Locating ligand-binding sites in 7TM receptors by protein engineering
25. Advances in understanding gonadotropin-releasing hormone receptor structure and ligand interactions
26. Molecular function of the gonadotropin-releasing hormone receptor: Insights from sitedirected mutagenesis
27. A reciprocal mutation supports helix 2 and helix 7 proximity in the gonadotropin-releasing hormone receptor
28. Effects of Asn318 and Asp87Asn318 mutations on signal transduction by the gonadotropin-releasing hormone receptor and receptor regulation
29. Effects of Asn87 and Asp318 mutations on ligand binding and signal transduction in the rat GnRH receptor
30. Rhodopsin-family receptors associate with small G proteins to activate phospholipase D
31. Mediation of cyclic AMP signaling by the first intracellular loop of the gonadotropin-releasing hormone receptor
32. Effects of second intracellular loop mutations on signal transduction and internalization of the gonadotropin-releasing hormone receptor
33. Mutations in gonadotropin-releasing hormone receptor gene cause hypogonadotropic hypogonadism
34. Dependence of agonist activation on an aromatic moiety in the DPLIY motif of the gonadotropin-releasing hormone receptor
35. Influence of a species-specific extracellular amino acid on expression and function of the human gonadotropin-releasing hormone receptor
36. The same molecular defects of the gonadotropin-releasing hormone receptor determine a variable degree of hypogonadism in affected kindred
37. Functional microdomains in G-protein-coupled receptors. The conserved arginine-cage motif in the gonadotropin-releasing hormone receptor
38. Mutations of the conserved DRS motif in the second intracellular loop of the gonadotropin-releasing hormone receptor affect expression, activation, and internalization
39. Glutamate 301 of the mouse gonadotropin-releasing hormone receptor confers specificity for arginine 8 of mammalian gonadotropin-releasing hormone
40. A locus of the gonadotropin-releasing hormone receptor that differentiates agonist and antagonist binding sites
41. Asn102 of the gonadotropin-releasing hormone receptor is a critical determinant of potency for agonists containing C-terminal glycineamide
42. Characterization of gonadotropin-releasing hormone analogs based on a sensitive cellular luciferase reporter gene assay
43. Selection and characterization of mammalian cell lines with stable over-expression of human pituitary receptors for gonadoliberin
44. Transformation of mammalian cells with genes from procaryotes and eucaryotes
45. Expression in mammalian cells of a gene from Streptomyces alboniger conferring puromycin resistance
46. A new dominant hybrid selective marker for higher eukaryotic cells
47. Highly sensitive northern hybridization of rare mRNA using a positively charged nylon membrane
48. Firefly luciferase gene: Structure and expression in mammalian cells
49. Analysis of radioligand binding experiments: A collection of computer programs for the IBM PC
50. Cloning, sequencing and expressing of human gonadotropin-releasing hormone (GnRH) receptor
51. Cloning and characterization of the human gonadotropin-releasing hormone receptor
52. An α-carbon template for the transmembrane helices in the rhodopsin family of G-protein-coupled receptors
53. Irreversible activation of the gonadotropin-releasing hormone receptor by photoaffiniity crosslinking: Localization of attachment site to cys residue in N-terminal segment
54. Bacteriorhodopsin in a periodic boundary water-vacuum-water box as an example towards stable molecular dynamics simulations of G-protein coupled receptors
55. Discovery of a novel, potent, and orally active nonpeptide antagonist of the human luteinizing hormone-releasing hormone (LHRH) receptor
56. A database of mutants and effects of site-directed mutagenesis experiments on G protein-coupled receptors
57. A high affinity gonadotropin-releasing hormone (GnRH) tracer, radioiodinated at position 6, facilitates analysis of mutant GnRH receptors
58. Stimulus-response mechanisms
59. An intramolecular disulfide bond between conserved extracellular cysteines in the gonadotropin-releasing hormone receptor is essential for binding and activation
60. Differences in structure-function relations between nonmammalian and mammalian gonadotropin-releasing hormone receptors
61. Isolation and characterization of cDNAs encoding the rat pituitary gonadotropin-releasing hormone receptor
62. Molecular cloning and expression of cDNA encoding the murine gonadotropin-releasing hormone receptor
63. Identification of N-glycosylation sites in the gonadotropin-releasing hormone receptor: Role in receptor expression but not ligand binding