FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2054165089> ?p ?o ?g. }

• W2054165089 endingPage "1782" @default.
• W2054165089 startingPage "1771" @default.
• W2054165089 abstract "The embodiment of 4-aminoproline residues (Amp) into the arginine-glycine-aspartate (RGD) sequence led to the discovery of a novel class of high-affinity αVβ3/αVβ5 integrin binders [IC50h(αVβ3) 0.03–5.12 nM; IC50h(αVβ5) 0.88–154 nM]. A total of eight cyclopeptides of type cyclo-[-Arg-Gly-Asp-Amp-], 5−12, were assembled by a standard solid-phase peptide synthesis protocol that involved the C2-carboxyl and C4-amino functionalities of the proline scaffolds, leaving the Nα-nuclear site untouched. Functionalization of this vacant proline site with either alkyl or acyl substituents proved feasible, with significant benefit to the integrin binding capabilities of the ligands. Notably, six out of eight cyclopeptide inhibitors, 5−7 and 9−11, showed moderate yet significant selectivity toward the αVβ3 receptor. The three-dimensional structure in water was determined by NMR techniques and molecular dynamics calculations. Docking studies to the X-ray crystal structure of the extracellular segment of integrin αVβ3 complexed with reference compound 1 were also performed on selected analogues to highlight the structural features required for potent ligand binding affinity." @default.
• W2054165089 created "2016-06-24" @default.
• W2054165089 creator A5015241973 @default.
• W2054165089 creator A5015765747 @default.
• W2054165089 creator A5015882421 @default.
• W2054165089 creator A5016774025 @default.
• W2054165089 creator A5022701055 @default.
• W2054165089 creator A5029082625 @default.
• W2054165089 creator A5030927398 @default.
• W2054165089 creator A5031073405 @default.
• W2054165089 creator A5031983959 @default.
• W2054165089 creator A5035973591 @default.
• W2054165089 creator A5050471753 @default.
• W2054165089 creator A5064278106 @default.
• W2054165089 creator A5082424642 @default.
• W2054165089 date "2008-02-28" @default.
• W2054165089 modified "2023-10-18" @default.
• W2054165089 title "Discovery of Subnanomolar Arginine-Glycine-Aspartate-Based α_Vβ₃/α_Vβ₅ Integrin Binders Embedding 4-Aminoproline Residues" @default.
• W2054165089 cites W1141074930 @default.
• W2054165089 cites W1514050185 @default.
• W2054165089 cites W1576773659 @default.
• W2054165089 cites W1586022877 @default.
• W2054165089 cites W1586238324 @default.
• W2054165089 cites W1594038744 @default.
• W2054165089 cites W1938388466 @default.
• W2054165089 cites W1973662849 @default.
• W2054165089 cites W1981937465 @default.
• W2054165089 cites W1982117697 @default.
• W2054165089 cites W1984673823 @default.
• W2054165089 cites W1987955781 @default.
• W2054165089 cites W1988001328 @default.
• W2054165089 cites W1992221074 @default.
• W2054165089 cites W2000305302 @default.
• W2054165089 cites W2000440264 @default.
• W2054165089 cites W2003306565 @default.
• W2054165089 cites W2010320204 @default.
• W2054165089 cites W2011217812 @default.
• W2054165089 cites W2011552652 @default.
• W2054165089 cites W2013381560 @default.
• W2054165089 cites W2014776038 @default.
• W2054165089 cites W2015128434 @default.
• W2054165089 cites W2015769593 @default.
• W2054165089 cites W2016750917 @default.
• W2054165089 cites W2017252248 @default.
• W2054165089 cites W2019241564 @default.
• W2054165089 cites W2022574738 @default.
• W2054165089 cites W2024012070 @default.
• W2054165089 cites W2025240607 @default.
• W2054165089 cites W2029231027 @default.
• W2054165089 cites W2030388689 @default.
• W2054165089 cites W2036055423 @default.
• W2054165089 cites W2039317622 @default.
• W2054165089 cites W2043610973 @default.
• W2054165089 cites W2050426579 @default.
• W2054165089 cites W2051200797 @default.
• W2054165089 cites W2053183574 @default.
• W2054165089 cites W2055452115 @default.
• W2054165089 cites W2059102232 @default.
• W2054165089 cites W2059790617 @default.
• W2054165089 cites W2063330553 @default.
• W2054165089 cites W2065097700 @default.
• W2054165089 cites W2067836657 @default.
• W2054165089 cites W2074787208 @default.
• W2054165089 cites W2080109954 @default.
• W2054165089 cites W2083182472 @default.
• W2054165089 cites W2085560654 @default.
• W2054165089 cites W2090343380 @default.
• W2054165089 cites W2091462162 @default.
• W2054165089 cites W2094469836 @default.
• W2054165089 cites W2096377687 @default.
• W2054165089 cites W2096868396 @default.
• W2054165089 cites W2098438673 @default.
• W2054165089 cites W2099768941 @default.
• W2054165089 cites W2108059110 @default.
• W2054165089 cites W2108713158 @default.
• W2054165089 cites W2116063661 @default.
• W2054165089 cites W2132995754 @default.
• W2054165089 cites W2138986195 @default.
• W2054165089 cites W2158065054 @default.
• W2054165089 cites W2158534713 @default.
• W2054165089 cites W2166407135 @default.
• W2054165089 cites W2169337864 @default.
• W2054165089 cites W2327877667 @default.
• W2054165089 cites W2949250147 @default.
• W2054165089 cites W2952658233 @default.
• W2054165089 cites W3021421549 @default.
• W2054165089 cites W4213141530 @default.
• W2054165089 doi "https://doi.org/10.1021/jm701214z" @default.
• W2054165089 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/18303826" @default.
• W2054165089 hasPublicationYear "2008" @default.
• W2054165089 type Work @default.
• W2054165089 sameAs 2054165089 @default.
• W2054165089 citedByCount "47" @default.
• W2054165089 countsByYear W20541650892012 @default.
• W2054165089 countsByYear W20541650892013 @default.
• W2054165089 countsByYear W20541650892014 @default.
• W2054165089 countsByYear W20541650892015 @default.
• W2054165089 countsByYear W20541650892016 @default.

• next