Page last updated: 2024-08-07 13:41:54
KiSS-1 receptor
A KiSS-1 receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q969F8]
Synonyms
KiSS-1R;
G-protein coupled receptor 54;
G-protein coupled receptor OT7T175;
hOT7T175;
Hypogonadotropin-1;
Kisspeptins receptor;
Metastin receptor
Research
Bioassay Publications (10)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 2 (20.00) | 29.6817 |
| 2010's | 7 (70.00) | 24.3611 |
| 2020's | 1 (10.00) | 2.80 |
Compounds (4)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Identification of an Journal of medicinal chemistry, , 06-10, Volume: 64, Issue:11, 2021
A new class of pentapeptide KISS1 receptor agonists with hypothalamic-pituitary-gonadal axis activation.Bioorganic & medicinal chemistry letters, , 02-15, Volume: 29, Issue:4, 2019
Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-d-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NHJournal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.Journal of medicinal chemistry, , Jul-24, Volume: 57, Issue:14, 2014
Design, synthesis, and biological evaluation of novel investigational nonapeptide KISS1R agonists with testosterone-suppressive activity.Journal of medicinal chemistry, , Nov-14, Volume: 56, Issue:21, 2013
Serum stability of selected decapeptide agonists of KISS1R using pseudopeptides.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 22, Issue:20, 2012
Trypsin resistance of a decapeptide KISS1R agonist containing an Nω-methylarginine substitution.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 22, Issue:20, 2012
Activation of Neuropeptide FF Receptors by Kisspeptin Receptor Ligands.ACS medicinal chemistry letters, , Jan-13, Volume: 2, Issue:1, 2011
Development of novel G-protein-coupled receptor 54 agonists with resistance to degradation by matrix metalloproteinase.Journal of medicinal chemistry, , Dec-11, Volume: 51, Issue:23, 2008
Metastin (KiSS-1) mimetics identified from peptide structure-activity relationship-derived pharmacophores and directed small molecule database screening.Journal of medicinal chemistry, , Feb-08, Volume: 50, Issue:3, 2007
Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-d-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NHJournal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.Journal of medicinal chemistry, , Jul-24, Volume: 57, Issue:14, 2014
Enables
This protein enables 3 target(s):
| Target | Category | Definition |
|---|
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| neuropeptide receptor activity | molecular function | Combining with a neuropeptide to initiate a change in cell activity. [GOC:ai] |
| G protein-coupled peptide receptor activity | molecular function | Combining with a peptide and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. [GOC:dph, GOC:tb] |
Located In
This protein is located in 5 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] |
| cilium | cellular component | A specialized eukaryotic organelle that consists of a filiform extrusion of the cell surface and of some cytoplasmic parts. Each cilium is largely bounded by an extrusion of the cytoplasmic (plasma) membrane, and contains a regular longitudinal array of microtubules, anchored to a basal body. [GOC:cilia, GOC:curators, GOC:kmv, GOC:vw, ISBN:0198547684, PMID:16824949, PMID:17009929, PMID:20144998] |
| cell surface | cellular component | The external part of the cell wall and/or plasma membrane. [GOC:jl, GOC:mtg_sensu, GOC:sm] |
| 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] |
| intracellular membrane-bounded organelle | cellular component | Organized structure of distinctive morphology and function, bounded by a single or double lipid bilayer membrane and occurring within the cell. Includes the nucleus, mitochondria, plastids, vacuoles, and vesicles. Excludes the plasma membrane. [GOC:go_curators] |
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 2 target(s):
| Target | Category | Definition |
|---|
| 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] |
| neuropeptide signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by a neuropeptide binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process. [GOC:mah, ISBN:0815316194] |