Two mutations in extracellular loop 2 of the human GnRH receptor convert an antagonist to an agonist

Molecular Endocrinology

Volumn 16, Issue 5, 2002, Pages 1079-1088

  Ott, Thomas R ^a   Troskie, Brigitte E ^b   Roeske, Roger W ^c   Illing, Nicola ^d   Flanagan, Colleen A ^e   Millar, Robert P ^a  

^a MRC Reproductive Biology Unit   (United Kingdom)

^b Laboratory Science   (United States)

^c UNIVERSITY OF CAPE TOWN   (South Africa)

^d INDIANA UNIVERSITY SCHOOL OF MEDICINE   (United States)

^e UNIVERSITY OF CAPE TOWN   (South Africa)

Author keywords

[No Author keywords available]

Indexed keywords

ALANINE; G PROTEIN COUPLED RECEPTOR; GONADORELIN RECEPTOR; HISTIDINE; INOSITOL PHOSPHATE; TRYPTOPHAN; VALINE;

ARTICLE; CARBOXY TERMINAL SEQUENCE; CHICKEN; CONTROLLED STUDY; HUMAN; HUMAN TISSUE; HYDROGEN BOND; LIGAND BINDING; MOLECULAR STABILITY; POINT MUTATION; PRIORITY JOURNAL; PROTEIN CONFORMATION; PROTEIN DOMAIN; PROTEIN STRUCTURE; RECEPTOR DOWN REGULATION; RECEPTOR UPREGULATION; SIGNAL TRANSDUCTION; SITE DIRECTED MUTAGENESIS; STRUCTURE ACTIVITY RELATION; TITRIMETRY; XENOPUS LAEVIS;

GALLUS GALLUS; MAMMALIA; VERTEBRATA; XENOPUS LAEVIS;

EID: 0036256986     PISSN: 08888809     EISSN: None     Source Type: Journal    
DOI: 10.1210/mend.16.5.0824     Document Type: Article

References (48)

1. Molecular mechanisms of ligand interaction with the gonadotropin-releasing hormone receptor
2. GnRH and GnRH analogues: Structure, actions and clinical applications
3. Cloning and functional expression of a mouse gonadotropin-releasing hormone receptor
4. Isolation and characterization of cDNAs encoding the rat pituitary gonadotropin-releasing hormone receptor
5. G protein-coupled receptors. I. Diversity of receptor-ligand interactions
6. 2.61(98) side chain of the gonadotropin-releasing hormone receptor contribute differentially to ligand interaction
7. Asn102 of the gonadotropin-releasing hormone receptor is a critical determinant of potency for agonists containing C-terminal glycinamide
8. A locus of the gonadotropin-releasing hormone receptor that differentiates agonist and antagonist binding sites
9. Glutamate 301 of the mouse gonadotropin-releasing hormone receptor confers specificity for arginine 8 of mammalian gonadotropin-releasing hormone
10. Functional importance of transmembrane helix 6 Trp(279) and exoloop 3 Val(299) of rat gonadotropin-releasing hormone receptor
11. Residues within transmembrane helices 2 and 5 of the human gonadotropin-releasing hormone receptor contribute to agonist and antagonist binding
12. Integrated methods for the construction of three-dimensional models and computational probing of structure-function relations in G protein coupled receptors
13. A new photoreactive antagonist cross-links to the N-terminal domain of the gonadotropin-releasing hormone receptor
14. Identification of Phe313 of the gonadotropin-releasing hormone (GnRH) receptor as a site critical for the binding of nonpeptide GnRH antagonists
15. Functional microdomains in G-protein-coupled receptors. The conserved arginine-cage motif in the gonadotropin-releasing hormone receptor
16. Distinct efficacies for two endogenous ligands on a single cognate gonadoliberin receptor
17. Two gonadotropin-releasing hormone receptor subtypes with distinct ligand selectivity and differential distribution in brain and pituitary in the goldfish (Carassius auratus)
18. mRNA expression of gonadotropin-releasing hormones (GnRHs) and GnRH receptor in goldfish
19. 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
20. Three distinct types of gonadotropin-releasing hormone receptor characterized in a single diploid species
21. 6 in the ligand and extracellular loop two of the receptor as determinants
22. Efficient site-directed mutagenesis using uracil-containing DNA
23. Specific synthesis of DNA in vitro via a polymerase-catalyzed chain reaction
24. 11-coupled neuropeptide receptors: The GnRH receptor
25. 5-Hydroxytryptamine type 2A receptors regulate cyclic AMP accumulation in a neuronal cell line by protein kinase C-dependent and calcium/calmodulin-dependent mechanisms
26. 2-Adrenoceptor regulation of adenylyl cyciase in CHO cells: Dependence on receptor density, receptor subtype and current activity of adenylyl cyclase
27. Effects of varying the expression level of recombinant human mGlu1 α receptors on the pharmacological properties of agonists and antagonists
28. 4.4 receptors expressed in CHO cells
29. Partial agonist activity of 11-cis-retinal in rhodopsin mutants
30. A single amino acid substitution in the β-adrenergic receptor promotes partial agonist activity from antagonists
31. 2-vasopressin receptor induces a constitutive activity which permits discrimination between antagonists with partial agonist and inverse agonist activities
32. 1 angiotensin receptor is generated by angiotensin II induction
33. 1A angiotensin II receptor induces its constitutive activation
34. Mutation of a conserved serine in TM4 of opioid receptors confers full agonistic properties to classical antagonists
35. 1-dopamine receptor binding and signal transduction
36. 2A adrenergic receptors
37. 1-adrenergic receptors in patients with malignant hypertension
38. 1-adrenoceptor with positive chronotropic effect
39. 2-adrenoceptor
40. 1) in the heart with anti-peptide antibodies showing a positive chronotropic effect
41. 2 receptor involved in ligand binding and agonist sensing defined by anti-peptide antibodies
42. 1-muscarinic acetylcholine receptor activation
43. Functionally active cardiac antibodies in chronic Chagas' disease are specifically blocked by Trypanosoma cruzi antigens
44. G protein-coupled receptors. II. Mechanism of agonist activation
45. The conformational switch in 7-transmembrane receptors: The muscarinic receptor paradigm
46. Crystal structure of rhodopsin: A G protein-coupled receptor
47. 1-muscarinic receptor
48. Dissection of the structure and activity of the tyrosyl-tRNA synthetase by site-directed mutagenesis