Identification of Phe313 of the gonadotropin-releasing hormone (GnRH) receptor as a site critical for the binding of nonpeptide GnRH antagonists

Molecular Endocrinology

Volumn 14, Issue 5, 2000, Pages 671-681

  Cui, Jisong ^a   Smith, Roy G ^b   Mount, George R ^c   Lo, Jane L ^a   Yu, Jinghua ^a   Walsh, Thomas F ^a   Singh, Suresh B ^a   DeVita, Robert J ^a   Goulet, Mark T ^a   Schaeffer, James M ^a   Cheng, Kang ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

^b Huffington Center on Aging   (United States)

^c TEMPLE UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

GONADORELIN; GONADORELIN AGONIST; LEUCINE; PHENYLALANINE; QUINOLONE DERIVATIVE; GONADORELIN RECEPTOR; HORMONE ANTAGONIST; HYBRID PROTEIN; OLIGOPEPTIDE;

AMINO ACID SEQUENCE; AMINO ACID SUBSTITUTION; ANIMAL TISSUE; ARTICLE; DOG; DRUG EFFECT; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; HUMAN; LIGAND BINDING; NONHUMAN; NUCLEOTIDE SEQUENCE; PRIORITY JOURNAL; REACTION ANALYSIS; RECEPTOR AFFINITY; RECEPTOR INTRINSIC ACTIVITY; SEQUENCE ANALYSIS; SEQUENCE HOMOLOGY; SITE DIRECTED MUTAGENESIS; STRUCTURE ACTIVITY RELATION; ANIMAL; BINDING SITE; CHEMICAL STRUCTURE; CHEMISTRY; COMPARATIVE STUDY; DRUG ANTAGONISM; GENETICS; METABOLISM; MOLECULAR CLONING; MOLECULAR GENETICS; PROTEIN BINDING; SEQUENCE ALIGNMENT; SPECIES DIFFERENCE; SYNTHESIS;

ANIMALIA; CANIS FAMILIARIS;

AMINO ACID SEQUENCE; AMINO ACID SUBSTITUTION; ANIMALS; BINDING SITES; CLONING, MOLECULAR; DOGS; GONADOTROPIN-RELEASING HORMONE; HORMONE ANTAGONISTS; HUMANS; LEUCINE; MODELS, MOLECULAR; MOLECULAR SEQUENCE DATA; MOLECULAR STRUCTURE; MUTAGENESIS, SITE-DIRECTED; OLIGOPEPTIDES; PHENYLALANINE; PROTEIN BINDING; QUINOLONES; RECEPTORS, LHRH; RECOMBINANT FUSION PROTEINS; SEQUENCE ALIGNMENT; SEQUENCE HOMOLOGY, AMINO ACID; SPECIES SPECIFICITY; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 85047684169     PISSN: 08888809     EISSN: None     Source Type: Journal    
DOI: 10.1210/mend.14.5.0464     Document Type: Article

References (28)

1. Gonadotropin secretion and its control
2. Molecular mechanisms of ligand interaction with the gonadotropin-releasing hormone receptor
3. Cloning and functional expression of a mouse gonadotropinreleasing hormone receptor
4. Cloning, sequencing, and expression of human gonadotropin releasing hormone (GnRH) receptor
5. Cloning and characterization of the human GnRH receptor
6. Cloning and sequencing of the sheep pituitary gonadotropin-releasing hormone receptor and changes in expression of its mRNA during the estrous cycle
7. Molecular cloning, sequencing, and characterizing the bovine receptor for gonadotropin releasing hormone (GnRH)
8. Rapid communication: Nucleotide sequence of luteinizing hormone-releasing hormone (LHRH) receptor cDNA in the pig pituitary
9. Isolation and characterization of cDNAs encoding the rat pituitary gonadotropin-releasing hormone receptor
10. Gonadotropin-releasing hormone and its analogs
11. Clinical applications of gonadotropin-releasing hormones in reproductive disorders
12. Inhibition of luteinizing hormone, follicle-stimulating hormone and sex-steroid levels in men and women with a potent antagonist analog of luteinizing hormone-releasing hormone, Cetrorelix (SB-75)
13. LHRH antagonists
14. Identification and initial structure-activity relationships of a novel non-peptide quinolone GnRH receptor antagonist
15. Investigation of the 4-alkylamine substituent of non-peptide quinolone GnRH receptor antagonists
16. Potent antagonists of gonadotropin releasing hormone receptors derived from quinolone-6-carboxamides
17. Differential sensitivity of agonist- and antagonist-occupied gonadotropin-releasing hormone receptors to protein kinase C activators. A marker for receptor activation
18. A locus of the gonadotropin-releasing hormone receptor that differentiates agonist and antagonist binding sites
19. Asn102 of the gonadotropin-releasing hormone receptor is a critical determinant of potency for agonists containing C-terminal glycinamide
20. Glutamate 301 of the mouse gonadotropin-releasing hormone receptor confers specificity for arginine 8 of mammalian gonadotropin-releasing hormone
21. Role of Asp2.61(198) in agonist complexing with the human gonadotropin-releasing hormone receptor
22. Influence of a species-specific extracellular amino acid on expression and function of the human gonadotropin-releasing hormone receptor
23. Discovery of a novel, potent, and orally active nonpeptide antagonist of the human luteinizing hormone-releasing hormone (LHRH) receptor
24. Pharmacological endocrine characterization of A-198401, an orally-active GnRH antagonist, in intact and castrate male rats, dogs and cynomolagous monkeys
25. Non-peptide LH-RH antagonists
26. Structure and function of G protein-coupled receptors
27. Accurate modeling of protein conformation by automatic segment matching
28. Protein folding by restrained energy minimization and molecular dynamics