FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W1993889151> ?p ?o ?g. }

• W1993889151 endingPage "1115" @default.
• W1993889151 startingPage "1099" @default.
• W1993889151 abstract "To understand the ligand binding properties of the human GnRH receptor (hGnRH-R), 24 site-specific mutants within transmembrane helices (TMH) 1, 2, and 5 and the extracellular loop 2 (E2) were generated. These mutants were analyzed by using a functional reporter gene assay, monitoring receptor signaling via adenylate cyclase to a cAMP-responsive element fused to Photinus pyralis luciferase. The functional behavior of 14 receptor mutants, capable of G-protein coupling and signaling, was studied in detail with different well described agonistic and antagonistic peptide ligands. Furthermore, the binding constants were determined in displacement binding experiments with the antagonist [125I]Cetrorelix. The substitution of residues K36, Q204, W205, H207, Q208, F20, F213, F216, and S217 for alanine had no or only a marginal effect on ligand binding and signaling. In contrast, substitution of N87, Eg9, D9, R179, W206, Y211, F214, and T215 for alanine resulted in receptor proteins neither capable of ligand binding nor signal transduction. Within those mutants affecting ligand binding and signaling to various degrees, W101A, N102A, and N212Q differentiate between agonists and antagonists. Thus, in addition to N102 already described, the residues W101 in TMH2 and N212 in TMH5 are important for the architecture of the ligand-binding pocket. Based on the experimental data, three-dimensional models for binding of the superagonist D-Trp6-GnRH (Triptorelin) and the antagonist Cetrorelix to the hGnRH-R are proposed. Both decapeptidic ligands are bound to the receptor in a bent conformation with distinct interactions within the binding pocket formed by all TMHs, E2, and E3. The antagonist Cetrorelix with bulky hydrophobic N-terminal amino acids interacts with quite different receptor residues, a hint at the failure to induce an active, G protein-coupling receptor conformation." @default.
• W1993889151 created "2016-06-24" @default.
• W1993889151 creator A5016816308 @default.
• W1993889151 creator A5038269097 @default.
• W1993889151 creator A5041145818 @default.
• W1993889151 creator A5071121260 @default.
• W1993889151 creator A5087890782 @default.
• W1993889151 date "2000-07-01" @default.
• W1993889151 modified "2023-09-25" @default.
• W1993889151 title "Residues within Transmembrane Helices 2 and 5 of the Human Gonadotropin-Releasing Hormone Receptor Contribute to Agonist and Antagonist Binding" @default.
• W1993889151 cites W120002691 @default.
• W1993889151 cites W1527506556 @default.
• W1993889151 cites W1544899066 @default.
• W1993889151 cites W1554882129 @default.
• W1993889151 cites W1579316769 @default.
• W1993889151 cites W1586407696 @default.
• W1993889151 cites W159198934 @default.
• W1993889151 cites W1616210764 @default.
• W1993889151 cites W1843552687 @default.
• W1993889151 cites W1964512812 @default.
• W1993889151 cites W1967997803 @default.
• W1993889151 cites W1970621515 @default.
• W1993889151 cites W1974170731 @default.
• W1993889151 cites W1979421949 @default.
• W1993889151 cites W1982659505 @default.
• W1993889151 cites W1985200828 @default.
• W1993889151 cites W1990205720 @default.
• W1993889151 cites W1992536794 @default.
• W1993889151 cites W1992959244 @default.
• W1993889151 cites W1993134296 @default.
• W1993889151 cites W2000469585 @default.
• W1993889151 cites W2003832016 @default.
• W1993889151 cites W2010790600 @default.
• W1993889151 cites W2013686251 @default.
• W1993889151 cites W2018132588 @default.
• W1993889151 cites W2020210419 @default.
• W1993889151 cites W2021864472 @default.
• W1993889151 cites W2023378571 @default.
• W1993889151 cites W2027411626 @default.
• W1993889151 cites W2033664346 @default.
• W1993889151 cites W2036423270 @default.
• W1993889151 cites W2042415727 @default.
• W1993889151 cites W2049197218 @default.
• W1993889151 cites W2050218326 @default.
• W1993889151 cites W2056618475 @default.
• W1993889151 cites W2057315268 @default.
• W1993889151 cites W2067674574 @default.
• W1993889151 cites W2069251863 @default.
• W1993889151 cites W2069828003 @default.
• W1993889151 cites W2073199025 @default.
• W1993889151 cites W2073295308 @default.
• W1993889151 cites W2077249532 @default.
• W1993889151 cites W2077891706 @default.
• W1993889151 cites W2078122870 @default.
• W1993889151 cites W2080932789 @default.
• W1993889151 cites W2090977762 @default.
• W1993889151 cites W2097794242 @default.
• W1993889151 cites W2109888258 @default.
• W1993889151 cites W2113606878 @default.
• W1993889151 cites W2120596322 @default.
• W1993889151 cites W2121449309 @default.
• W1993889151 cites W2132342248 @default.
• W1993889151 cites W2146209868 @default.
• W1993889151 cites W2147017397 @default.
• W1993889151 cites W2163642073 @default.
• W1993889151 cites W2177092842 @default.
• W1993889151 cites W2292879214 @default.
• W1993889151 cites W2316415325 @default.
• W1993889151 cites W2413818173 @default.
• W1993889151 cites W2418242721 @default.
• W1993889151 cites W2419282380 @default.
• W1993889151 cites W2467748439 @default.
• W1993889151 cites W2520478023 @default.
• W1993889151 doi "https://doi.org/10.1210/mend.14.7.0483" @default.
• W1993889151 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/10894158" @default.
• W1993889151 hasPublicationYear "2000" @default.
• W1993889151 type Work @default.
• W1993889151 sameAs 1993889151 @default.
• W1993889151 citedByCount "52" @default.
• W1993889151 countsByYear W19938891512014 @default.
• W1993889151 countsByYear W19938891512015 @default.
• W1993889151 countsByYear W19938891512016 @default.
• W1993889151 countsByYear W19938891512017 @default.
• W1993889151 countsByYear W19938891512019 @default.
• W1993889151 countsByYear W19938891512020 @default.
• W1993889151 crossrefType "journal-article" @default.
• W1993889151 hasAuthorship W1993889151A5016816308 @default.
• W1993889151 hasAuthorship W1993889151A5038269097 @default.
• W1993889151 hasAuthorship W1993889151A5041145818 @default.
• W1993889151 hasAuthorship W1993889151A5071121260 @default.
• W1993889151 hasAuthorship W1993889151A5087890782 @default.
• W1993889151 hasBestOaLocation W19938891511 @default.
• W1993889151 hasConcept C104317684 @default.
• W1993889151 hasConcept C107824862 @default.
• W1993889151 hasConcept C116569031 @default.
• W1993889151 hasConcept C118892022 @default.
• W1993889151 hasConcept C12554922 @default.
• W1993889151 hasConcept C135285700 @default.

• next