Proteins > Gonadotropin-releasing hormone receptor
Page last updated: 2024-08-07 16:27:16
Gonadotropin-releasing hormone receptor
A gonadotropin-releasing hormone I receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:P30968]
Synonyms
GnRH receptor;
GnRH-R
Research
Bioassay Publications (26)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 1 (3.85) | 18.2507 |
| 2000's | 17 (65.38) | 29.6817 |
| 2010's | 7 (26.92) | 24.3611 |
| 2020's | 1 (3.85) | 2.80 |
Compounds (15)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Design, synthesis, and structure-activity relationships of thieno[2,3-b]pyridin-4-one derivatives as a novel class of potent, orally active, non-peptide luteinizing hormone-releasing hormone receptor antagonists.Journal of medicinal chemistry, , Jun-29, Volume: 49, Issue:13, 2006
Discovery of a novel, potent, and orally active nonpeptide antagonist of the human luteinizing hormone-releasing hormone (LHRH) receptor.Journal of medicinal chemistry, , Oct-22, Volume: 41, Issue:22, 1998
Discovery of 1-{4-[1-(2,6-difluorobenzyl)-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl]phenyl}-3-methoxyurea (TAK-385) as a potent, orally active, non-peptide antagonist of the human gonadotJournal of medicinal chemistry, , Jul-28, Volume: 54, Issue:14, 2011
Non-peptide gonadotropin-releasing hormone receptor antagonists.Journal of medicinal chemistry, , Jun-26, Volume: 51, Issue:12, 2008
Determination of the binding mode of thienopyrimidinedione antagonists to the human gonadotropin releasing hormone receptor using structure-activity relationships, site-directed mutagenesis, and homology modeling.Journal of medicinal chemistry, , Oct-19, Volume: 49, Issue:21, 2006
Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor.Journal of medicinal chemistry, , Jan-26, Volume: 49, Issue:2, 2006
Synthesis and structure-activity relationships of thieno[2,3-d]pyrimidine-2,4-dione derivatives as potent GnRH receptor antagonists.Bioorganic & medicinal chemistry letters, , Oct-20, Volume: 13, Issue:20, 2003
Discovery of a thieno[2,3-d]pyrimidine-2,4-dione bearing a p-methoxyureidophenyl moiety at the 6-position: a highly potent and orally bioavailable non-peptide antagonist for the human luteinizing hormone-releasing hormone receptor.Journal of medicinal chemistry, , Jan-02, Volume: 46, Issue:1, 2003
Small molecule piperazinyl-benzimidazole antagonists of the gonadotropin-releasing hormone (GnRH) receptor.MedChemComm, , Oct-01, Volume: 8, Issue:10, 2017
Non-peptide gonadotropin-releasing hormone receptor antagonists.Journal of medicinal chemistry, , Jun-26, Volume: 51, Issue:12, 2008
Design, synthesis, and structure-activity relationships of thieno[2,3-b]pyridin-4-one derivatives as a novel class of potent, orally active, non-peptide luteinizing hormone-releasing hormone receptor antagonists.Journal of medicinal chemistry, , Jun-29, Volume: 49, Issue:13, 2006
3-[(2R)-Amino-2-phenylethyl]-1-(2,6-difluorobenzyl)-5-(2-fluoro-3-methoxyphenyl)- 6-methylpyrimidin-2,4-dione (NBI 42902) as a potent and orally active antagonist of the human gonadotropin-releasing hormone receptor. Design, synthesis, and in vitro and inJournal of medicinal chemistry, , Feb-24, Volume: 48, Issue:4, 2005
Synthesis and structure-activity relationships of thieno[2,3-d]pyrimidine-2,4-dione derivatives as potent GnRH receptor antagonists.Bioorganic & medicinal chemistry letters, , Oct-20, Volume: 13, Issue:20, 2003
Synthesis and initial structure-activity relationships of a novel series of imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists.Bioorganic & medicinal chemistry letters, , Aug-19, Volume: 12, Issue:16, 2002
Initial structure-activity relationship studies of a novel series of pyrrolo[1,2-a]pyrimid-7-ones as GnRH receptor antagonists.Bioorganic & medicinal chemistry letters, , Feb-11, Volume: 12, Issue:3, 2002
Small molecule piperazinyl-benzimidazole antagonists of the gonadotropin-releasing hormone (GnRH) receptor.MedChemComm, , Oct-01, Volume: 8, Issue:10, 2017
Synthesis and in vitro evaluation of small-molecule [18F] labeled gonadotropin-releasing hormone (GnRH) receptor antagonists as potential PET imaging agents for GnRH receptor expression.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 24, Issue:7, 2014
[no title available]Journal of medicinal chemistry, , 10-22, Volume: 63, Issue:20, 2020
Discovery of 1-{4-[1-(2,6-difluorobenzyl)-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl]phenyl}-3-methoxyurea (TAK-385) as a potent, orally active, non-peptide antagonist of the human gonadotJournal of medicinal chemistry, , Jul-28, Volume: 54, Issue:14, 2011
Synthesis and biological evaluation of 3-(2-aminoethyl) uracil derivatives as gonadotropin-releasing hormone (GnRH) receptor antagonists.European journal of medicinal chemistry, , Feb-10, Volume: 145, 2018
Discovery of an Orally Bioavailable Gonadotropin-Releasing Hormone Receptor Antagonist.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
5-Aryluracils as potent GnRH antagonists-Characterization of atropisomers.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 18, Issue:11, 2008
Non-peptide gonadotropin-releasing hormone receptor antagonists.Journal of medicinal chemistry, , Jun-26, Volume: 51, Issue:12, 2008
Discovery of sodium R-(+)-4-{2-[5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (elagolix), a potent and orally available nonpeptide antagonist of the human Journal of medicinal chemistry, , Dec-11, Volume: 51, Issue:23, 2008
Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor.Journal of medicinal chemistry, , Jan-26, Volume: 49, Issue:2, 2006
3-[(2R)-Amino-2-phenylethyl]-1-(2,6-difluorobenzyl)-5-(2-fluoro-3-methoxyphenyl)- 6-methylpyrimidin-2,4-dione (NBI 42902) as a potent and orally active antagonist of the human gonadotropin-releasing hormone receptor. Design, synthesis, and in vitro and inJournal of medicinal chemistry, , Feb-24, Volume: 48, Issue:4, 2005
Uracils as potent antagonists of the human gonadotropin-releasing hormone receptor without atropisomers.Bioorganic & medicinal chemistry letters, , May-16, Volume: 15, Issue:10, 2005
Synthesis and biological evaluation of piperazinyl heterocyclic antagonists of the gonadotropin releasing hormone (GnRH) receptor.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 20, Issue:8, 2010
Discovery of 6-({4-[2-(4-tert-butylphenyl)-1H-benzimidazol-4-yl]piperazin-1-yl}methyl)quinoxaline (WAY-207024): an orally active antagonist of the gonadotropin releasing hormone receptor (GnRH-R).Journal of medicinal chemistry, , Apr-09, Volume: 52, Issue:7, 2009
Novel analogues of degarelix incorporating hydroxy-, methoxy-, and pegylated-urea moieties at positions 3, 5, 6 and the N-terminus. Part III.Journal of medicinal chemistry, , Jun-15, Volume: 49, Issue:12, 2006
Iterative approach to the discovery of novel degarelix analogues: substitutions at positions 3, 7, and 8. Part II.Journal of medicinal chemistry, , Jul-28, Volume: 48, Issue:15, 2005
GnRH antagonists: a new generation of long acting analogues incorporating p-ureido-phenylalanines at positions 5 and 6.Journal of medicinal chemistry, , Feb-01, Volume: 44, Issue:3, 2001
Structure-activity relationship studies of gonadotropin-releasing hormone antagonists containing S-aryl/alkyl norcysteines and their oxidized derivatives.Journal of medicinal chemistry, , May-03, Volume: 50, Issue:9, 2007
Novel analogues of degarelix incorporating hydroxy-, methoxy-, and pegylated-urea moieties at positions 3, 5, 6 and the N-terminus. Part III.Journal of medicinal chemistry, , Jun-15, Volume: 49, Issue:12, 2006
GnRH antagonists: a new generation of long acting analogues incorporating p-ureido-phenylalanines at positions 5 and 6.Journal of medicinal chemistry, , Feb-01, Volume: 44, Issue:3, 2001
[no title available]Journal of medicinal chemistry, , 10-22, Volume: 63, Issue:20, 2020
GnRH antagonists: a new generation of long acting analogues incorporating p-ureido-phenylalanines at positions 5 and 6.Journal of medicinal chemistry, , Feb-01, Volume: 44, Issue:3, 2001
Enables
This protein enables 2 target(s):
| Target | Category | Definition |
|---|
| peptide binding | molecular function | Binding to a peptide, an organic compound comprising two or more amino acids linked by peptide bonds. [GOC:jl] |
| gonadotropin-releasing hormone receptor activity | molecular function | Combining with gonadotropin-releasing hormone to initiate a change in cell activity. Gonadotropin-releasing hormone (GnRH) is a peptide hormone responsible for the release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) from the anterior pituitary. GnRH is synthesized and released by the hypothalamus. [GOC:mah] |
Located In
This protein is located in 2 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Involved In
This protein is involved in 4 target(s):
| Target | Category | Definition |
|---|
| gonadotropin secretion | biological process | The regulated release of a gonadotropin, any hormone that stimulates the gonads, especially follicle-stimulating hormone and luteinizing hormone. [GOC:mah, ISBN:0721662544] |
| cellular response to gonadotropin-releasing hormone | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a gonadotropin-releasing hormone stimulus. Gonadotropin-releasing hormone (GnRH) is a peptide hormone responsible for the release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) from the anterior pituitary. GnRH is synthesized and released by the hypothalamus. [GOC:yaf, PMID:15976007] |
| G protein-coupled receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor] |
| cellular response to hormone stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a hormone stimulus. [GOC:mah] |