FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2015451804> ?p ?o ?g. }

• W2015451804 endingPage "339" @default.
• W2015451804 startingPage "328" @default.
• W2015451804 abstract "The novel cyclic analogues cyclo(Phe-Leu-Leu-Arg-epsilonLys-Dap) (1) and cyclo(D-Phe-Leu-Leu-Arg-epsilonLys-Dap) (2), which differ only in the absolute conformation of Phe, have been designed and synthesized based upon the minimal peptide sequence Phe-Leu-Leu-Arg which has been found to exhibit biological activity for the thrombin receptor. Compound 1, in which all amino acids have the L-configuration, exhibited higher activity in the rat aorta relaxation and rat longitudinal muscle bioassays compared to compound 2, in which the Phe residue is in the D-configuration. This is attributed to the spatial proximity of the Phe and Arg in compound 1 which does not exist in its diastereomeric compound 2, as is depicted from a combination of NMR studies and computational analysis. Structure-activity studies (SAR) showed that the Phe and Arg side chains along with a primary amino group form an active recognition motif that is augmented by the presence of a second primary amino group in the cyclic peptide. We suggest that a comparable cyclic conformation may be responsible for the interaction of linear TRAPs with the thrombin receptor. The validity of this proposition was tested by the synthesis of four active nonpeptide thrombin receptor mimetics. Substance (S)-N-(6-guanidohexanoyl)-N'-(2-amino-3-phenylpropionyl)piperazine (3), in which the pharmacophoric phenyl, guanidino, and amino groups were incorporated onto a piperazine template, was found to be the most active compared to the other synthesized compounds which lack the amino pharmacophoric group." @default.
• W2015451804 created "2016-06-24" @default.
• W2015451804 creator A5009553458 @default.
• W2015451804 creator A5032749978 @default.
• W2015451804 creator A5049009149 @default.
• W2015451804 creator A5053153114 @default.
• W2015451804 creator A5054817512 @default.
• W2015451804 creator A5057892922 @default.
• W2015451804 creator A5072960254 @default.
• W2015451804 creator A5076188669 @default.
• W2015451804 date "2000-12-29" @default.
• W2015451804 modified "2023-10-02" @default.
• W2015451804 title "Design, Synthesis, and Modeling of Novel Cyclic Thrombin Receptor-Derived Peptide Analogues of the Ser⁴²-Phe-Leu-Leu-Arg⁴⁶ Motif Sequence with Fixed Conformations of Pharmacophoric Groups: Importance of a Phe/Arg/NH₂ Cluster for Receptor Activation and Implications in the Design of Nonpeptide Thrombin Receptor Mimetics" @default.
• W2015451804 cites W1487725726 @default.
• W2015451804 cites W1489529085 @default.
• W2015451804 cites W1495307817 @default.
• W2015451804 cites W1668651547 @default.
• W2015451804 cites W1847187734 @default.
• W2015451804 cites W1969738964 @default.
• W2015451804 cites W1987934518 @default.
• W2015451804 cites W1990500910 @default.
• W2015451804 cites W1991741054 @default.
• W2015451804 cites W1996052275 @default.
• W2015451804 cites W1998899308 @default.
• W2015451804 cites W2001285955 @default.
• W2015451804 cites W2006849546 @default.
• W2015451804 cites W2016969337 @default.
• W2015451804 cites W2026680735 @default.
• W2015451804 cites W2044080127 @default.
• W2015451804 cites W2071435247 @default.
• W2015451804 cites W2074384162 @default.
• W2015451804 cites W2093175816 @default.
• W2015451804 cites W2095481288 @default.
• W2015451804 cites W2153444599 @default.
• W2015451804 cites W228010362 @default.
• W2015451804 doi "https://doi.org/10.1021/jm0001525" @default.
• W2015451804 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/11462974" @default.
• W2015451804 hasPublicationYear "2000" @default.
• W2015451804 type Work @default.
• W2015451804 sameAs 2015451804 @default.
• W2015451804 citedByCount "17" @default.
• W2015451804 countsByYear W20154518042012 @default.
• W2015451804 countsByYear W20154518042014 @default.
• W2015451804 countsByYear W20154518042015 @default.
• W2015451804 countsByYear W20154518042018 @default.
• W2015451804 countsByYear W20154518042021 @default.
• W2015451804 crossrefType "journal-article" @default.
• W2015451804 hasAuthorship W2015451804A5009553458 @default.
• W2015451804 hasAuthorship W2015451804A5032749978 @default.
• W2015451804 hasAuthorship W2015451804A5049009149 @default.
• W2015451804 hasAuthorship W2015451804A5053153114 @default.
• W2015451804 hasAuthorship W2015451804A5054817512 @default.
• W2015451804 hasAuthorship W2015451804A5057892922 @default.
• W2015451804 hasAuthorship W2015451804A5072960254 @default.
• W2015451804 hasAuthorship W2015451804A5076188669 @default.
• W2015451804 hasConcept C116073593 @default.
• W2015451804 hasConcept C138716334 @default.
• W2015451804 hasConcept C178790620 @default.
• W2015451804 hasConcept C185592680 @default.
• W2015451804 hasConcept C202751555 @default.
• W2015451804 hasConcept C203014093 @default.
• W2015451804 hasConcept C2776201271 @default.
• W2015451804 hasConcept C2777292125 @default.
• W2015451804 hasConcept C2778886182 @default.
• W2015451804 hasConcept C2779281246 @default.
• W2015451804 hasConcept C2779809887 @default.
• W2015451804 hasConcept C515207424 @default.
• W2015451804 hasConcept C55493867 @default.
• W2015451804 hasConcept C57002609 @default.
• W2015451804 hasConcept C60984968 @default.
• W2015451804 hasConcept C71240020 @default.
• W2015451804 hasConcept C86803240 @default.
• W2015451804 hasConcept C89560881 @default.
• W2015451804 hasConceptScore W2015451804C116073593 @default.
• W2015451804 hasConceptScore W2015451804C138716334 @default.
• W2015451804 hasConceptScore W2015451804C178790620 @default.
• W2015451804 hasConceptScore W2015451804C185592680 @default.
• W2015451804 hasConceptScore W2015451804C202751555 @default.
• W2015451804 hasConceptScore W2015451804C203014093 @default.
• W2015451804 hasConceptScore W2015451804C2776201271 @default.
• W2015451804 hasConceptScore W2015451804C2777292125 @default.
• W2015451804 hasConceptScore W2015451804C2778886182 @default.
• W2015451804 hasConceptScore W2015451804C2779281246 @default.
• W2015451804 hasConceptScore W2015451804C2779809887 @default.
• W2015451804 hasConceptScore W2015451804C515207424 @default.
• W2015451804 hasConceptScore W2015451804C55493867 @default.
• W2015451804 hasConceptScore W2015451804C57002609 @default.
• W2015451804 hasConceptScore W2015451804C60984968 @default.
• W2015451804 hasConceptScore W2015451804C71240020 @default.
• W2015451804 hasConceptScore W2015451804C86803240 @default.
• W2015451804 hasConceptScore W2015451804C89560881 @default.
• W2015451804 hasIssue "3" @default.
• W2015451804 hasLocation W20154518041 @default.
• W2015451804 hasLocation W20154518042 @default.
• W2015451804 hasOpenAccess W2015451804 @default.
• W2015451804 hasPrimaryLocation W20154518041 @default.
• W2015451804 hasRelatedWork W1983723018 @default.
• W2015451804 hasRelatedWork W1987608813 @default.

• next