FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2024846876> ?p ?o ?g. }

• W2024846876 endingPage "2426" @default.
• W2024846876 startingPage "2417" @default.
• W2024846876 abstract "Two tripeptide analogues (N-[3-methyl-1-S[[2-S-[(methyl-amino)carbonyl]-1-pyrrolidinyl]carbonyl]butyl-d-analine) (SC40476) and N-[3-methyl-S-(1-pyrrolidinylcarbonyl)butyl]-d-alanine, ethyl ester, hydrochloride (SC42619)), inhibit aggregation of, and secretion from, human platelets induced by thrombin but cause no significant inhibition of esterolysis or fibrin formation catalysed by this enzyme. Inhibition by SC40476 of the aggregatory response induced by thrombin is incomplete. Neither peptide analogue inhibits aggregation induced by ADP, collagen, vasopressin or 11,9-epoxymethanoprostaglandin H2 (U-46619). Enhancement of the response is observed when non-saturating concentrations of these agonists are employed. SC42619 causes a parallel shift to the right in the concentration-response curve describing aggregation induced by thrombin. The Schild plot of these data has a slope of 1.05 and the pA2 is 2.9 ± 0.1. Both SC40476 and SC42619 induce a small but significant decrease in the single platelet content of platelet suspensions. Neither peptide analogue increases platelet cytosolic [Ca2+] measured using quin 2 or Fura 2. Both analogues cause inhibition of the increase in cytosolic [Ca2+] induced by thrombin. Inhibition by SC42619 is competitive with respect to thrombin when the extracellular [Ca2+] is reduced to < 0.1 μM but is non-competitive in the presence of 1 mM Ca2+. SC42619 also inhibits the increase in cytosolic [Ca2+] induced by ADP in the presence of 1 mM Ca2+ but not the smaller increase caused by this agonist when the medium contains < 0.1 μM Ca2+. SC42619 inhibits Mn2+ influx induced by thrombin and ADP. SC40476 and SC42619 inhibit the enhanced incorporation of [32P] into phosphatidic acid observed on stimulation by thrombin of platelets pre-labelled with [32P]-phosphate. Addition of the peptide analogues alone fails to increase significantly the 32P content of phosphatidate, phosphatidylcholine, phosphatidylserine or phosphatidylethanolamine. SC40476 causes no detectable hydrolysis of glycoprotein V as detected by release of the proteolytic product (glycoprotein Vfr). The results indicate that SC40476 and SC42619 interact selectively with the platelet thrombin receptor. Both peptide analogues act as effective antagonists for this receptor but also possess weak agonist activity which may also result from interaction with the thrombin receptor. The molecular basis for this latter activity has not been defined. SC42619 non-selectively inhibits Ca2+ influx induced by several agonists but this effect does not appear to contribute to the observed inhibition of the aggregatory and secretory responses." @default.
• W2024846876 created "2016-06-24" @default.
• W2024846876 creator A5010882295 @default.
• W2024846876 creator A5013829081 @default.
• W2024846876 creator A5022285894 @default.
• W2024846876 creator A5087076378 @default.
• W2024846876 creator A5087581579 @default.
• W2024846876 date "1988-06-01" @default.
• W2024846876 modified "2023-09-27" @default.
• W2024846876 title "Identification of small peptide analogues having agonist and antagonist activity at the platelet thrombin receptor" @default.
• W2024846876 cites W1007473445 @default.
• W2024846876 cites W150011782 @default.
• W2024846876 cites W1533339726 @default.
• W2024846876 cites W1538720735 @default.
• W2024846876 cites W1568858788 @default.
• W2024846876 cites W1577793849 @default.
• W2024846876 cites W1578415899 @default.
• W2024846876 cites W1593048150 @default.
• W2024846876 cites W1596637835 @default.
• W2024846876 cites W174426101 @default.
• W2024846876 cites W1964620148 @default.
• W2024846876 cites W1964925994 @default.
• W2024846876 cites W1970038583 @default.
• W2024846876 cites W1974228025 @default.
• W2024846876 cites W1993489267 @default.
• W2024846876 cites W1997882330 @default.
• W2024846876 cites W2002154893 @default.
• W2024846876 cites W2012138617 @default.
• W2024846876 cites W2015432612 @default.
• W2024846876 cites W2019295772 @default.
• W2024846876 cites W2023355277 @default.
• W2024846876 cites W2031387417 @default.
• W2024846876 cites W2038147870 @default.
• W2024846876 cites W2038510313 @default.
• W2024846876 cites W2056812477 @default.
• W2024846876 cites W2060131985 @default.
• W2024846876 cites W2064483070 @default.
• W2024846876 cites W2065993385 @default.
• W2024846876 cites W2070206012 @default.
• W2024846876 cites W2070598525 @default.
• W2024846876 cites W2082857015 @default.
• W2024846876 cites W2091156380 @default.
• W2024846876 cites W2102217061 @default.
• W2024846876 cites W2158081554 @default.
• W2024846876 cites W2196351397 @default.
• W2024846876 cites W2212590994 @default.
• W2024846876 cites W2314347700 @default.
• W2024846876 cites W2437313923 @default.
• W2024846876 cites W2465111858 @default.
• W2024846876 cites W2473230978 @default.
• W2024846876 cites W33385424 @default.
• W2024846876 cites W4233375127 @default.
• W2024846876 cites W4233524361 @default.
• W2024846876 doi "https://doi.org/10.1016/0006-2952(88)90369-3" @default.
• W2024846876 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/2839193" @default.
• W2024846876 hasPublicationYear "1988" @default.
• W2024846876 type Work @default.
• W2024846876 sameAs 2024846876 @default.
• W2024846876 citedByCount "8" @default.
• W2024846876 countsByYear W20248468762012 @default.
• W2024846876 countsByYear W20248468762016 @default.
• W2024846876 crossrefType "journal-article" @default.
• W2024846876 hasAuthorship W2024846876A5010882295 @default.
• W2024846876 hasAuthorship W2024846876A5013829081 @default.
• W2024846876 hasAuthorship W2024846876A5022285894 @default.
• W2024846876 hasAuthorship W2024846876A5087076378 @default.
• W2024846876 hasAuthorship W2024846876A5087581579 @default.
• W2024846876 hasConcept C12554922 @default.
• W2024846876 hasConcept C126322002 @default.
• W2024846876 hasConcept C167392928 @default.
• W2024846876 hasConcept C170493617 @default.
• W2024846876 hasConcept C181199279 @default.
• W2024846876 hasConcept C185592680 @default.
• W2024846876 hasConcept C2776885963 @default.
• W2024846876 hasConcept C2777292125 @default.
• W2024846876 hasConcept C2778886182 @default.
• W2024846876 hasConcept C2778938600 @default.
• W2024846876 hasConcept C2779281246 @default.
• W2024846876 hasConcept C28406088 @default.
• W2024846876 hasConcept C55493867 @default.
• W2024846876 hasConcept C71240020 @default.
• W2024846876 hasConcept C71924100 @default.
• W2024846876 hasConcept C86803240 @default.
• W2024846876 hasConcept C89560881 @default.
• W2024846876 hasConcept C98539663 @default.
• W2024846876 hasConceptScore W2024846876C12554922 @default.
• W2024846876 hasConceptScore W2024846876C126322002 @default.
• W2024846876 hasConceptScore W2024846876C167392928 @default.
• W2024846876 hasConceptScore W2024846876C170493617 @default.
• W2024846876 hasConceptScore W2024846876C181199279 @default.
• W2024846876 hasConceptScore W2024846876C185592680 @default.
• W2024846876 hasConceptScore W2024846876C2776885963 @default.
• W2024846876 hasConceptScore W2024846876C2777292125 @default.
• W2024846876 hasConceptScore W2024846876C2778886182 @default.
• W2024846876 hasConceptScore W2024846876C2778938600 @default.
• W2024846876 hasConceptScore W2024846876C2779281246 @default.
• W2024846876 hasConceptScore W2024846876C28406088 @default.
• W2024846876 hasConceptScore W2024846876C55493867 @default.

• next