FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2256549649> ?p ?o ?g. }

• W2256549649 endingPage "46" @default.
• W2256549649 startingPage "35" @default.
• W2256549649 abstract "Poly(ethylene glycol) (PEG) may be covalently conjugated to peptide drugs to overcome their rapid clearance but in doing so their potency can be lost. Here, a non-covalent approach was used to conjugate PEG bearing a terminal cholanic moiety (mPEG5kDa-cholane) to a 28 amino acid peptide, vasoactive intestinal peptide (VIP). Palmitoylation of the peptide was essential to facilitate physical interaction via a single binding site involving two mPEG5kDa-cholane molecules with an affinity constant of ~ 3·104 M− 1; these calorimetry data corroborating Scatchard analysis of dissolution data. The peptide/polymer complex (below 10–12 nm diameter) provided for up to 5000-fold greater solubility of the peptide at pH 7.4 (4 μg/mL) and markedly increased peptide solution stability at 25 °C over 30 days. Mannitol enabled the complex to be lyophilized to yield a freeze-dried formulation which was efficiently reconstituted albeit with an ~ 10% decrease in solubility. The predominantly α-helical conformation of the peptide alone at pH 5–6.5 was lost at pH 7.4 but fully recovered with 2 molar equivalents of mPEG5kDa-cholane. After lyophilization and reconstitution an ~ 10% loss of α-helical conformation was observed, which may reflect the equivalent decrease in solubility. Pharmacokinetic studies following subcutaneous administration of the peptide (0.1 mg/Kg) alone and with 2 molar equivalents of polymer showed that mPEG5kDa-cholane dramatically increased peptide concentration in the systemic circulation. This is the first demonstration of non-covalent PEGylation of acylated peptides, an important biologic class, which improves in vitro and in vivo properties, and thereby may prove an alternative to covalent PEGylation strategies." @default.
• W2256549649 created "2016-06-24" @default.
• W2256549649 creator A5016187996 @default.
• W2256549649 creator A5047959935 @default.
• W2256549649 creator A5050436093 @default.
• W2256549649 creator A5073154909 @default.
• W2256549649 creator A5073668447 @default.
• W2256549649 creator A5074225402 @default.
• W2256549649 creator A5075671191 @default.
• W2256549649 creator A5075879267 @default.
• W2256549649 date "2016-03-01" @default.
• W2256549649 modified "2023-09-27" @default.
• W2256549649 title "A novel combined strategy for the physical PEGylation of polypeptides" @default.
• W2256549649 cites W1047995928 @default.
• W2256549649 cites W1154718163 @default.
• W2256549649 cites W1503938975 @default.
• W2256549649 cites W1604573605 @default.
• W2256549649 cites W1722148928 @default.
• W2256549649 cites W1755903692 @default.
• W2256549649 cites W1969488119 @default.
• W2256549649 cites W1970898345 @default.
• W2256549649 cites W1977584244 @default.
• W2256549649 cites W1980141884 @default.
• W2256549649 cites W1981273187 @default.
• W2256549649 cites W1983649348 @default.
• W2256549649 cites W1983964788 @default.
• W2256549649 cites W1984548348 @default.
• W2256549649 cites W1988473687 @default.
• W2256549649 cites W1991422955 @default.
• W2256549649 cites W1992295523 @default.
• W2256549649 cites W1994125987 @default.
• W2256549649 cites W2001151797 @default.
• W2256549649 cites W2003410975 @default.
• W2256549649 cites W2003453867 @default.
• W2256549649 cites W2007527667 @default.
• W2256549649 cites W2009119064 @default.
• W2256549649 cites W2024413031 @default.
• W2256549649 cites W2031322405 @default.
• W2256549649 cites W2036042563 @default.
• W2256549649 cites W2041255666 @default.
• W2256549649 cites W2045718008 @default.
• W2256549649 cites W2047188856 @default.
• W2256549649 cites W2050061574 @default.
• W2256549649 cites W2052749821 @default.
• W2256549649 cites W2061098219 @default.
• W2256549649 cites W2062937788 @default.
• W2256549649 cites W2069002738 @default.
• W2256549649 cites W2071062403 @default.
• W2256549649 cites W2071271545 @default.
• W2256549649 cites W2084587462 @default.
• W2256549649 cites W2103768330 @default.
• W2256549649 cites W2120774566 @default.
• W2256549649 cites W2126061397 @default.
• W2256549649 cites W2155886309 @default.
• W2256549649 cites W2169791131 @default.
• W2256549649 cites W2171251826 @default.
• W2256549649 cites W2182301132 @default.
• W2256549649 cites W2280680688 @default.
• W2256549649 cites W2323190196 @default.
• W2256549649 cites W2394660565 @default.
• W2256549649 cites W38150500 @default.
• W2256549649 doi "https://doi.org/10.1016/j.jconrel.2016.02.009" @default.
• W2256549649 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/26860282" @default.
• W2256549649 hasPublicationYear "2016" @default.
• W2256549649 type Work @default.
• W2256549649 sameAs 2256549649 @default.
• W2256549649 citedByCount "17" @default.
• W2256549649 countsByYear W22565496492016 @default.
• W2256549649 countsByYear W22565496492017 @default.
• W2256549649 countsByYear W22565496492018 @default.
• W2256549649 countsByYear W22565496492019 @default.
• W2256549649 countsByYear W22565496492020 @default.
• W2256549649 countsByYear W22565496492021 @default.
• W2256549649 countsByYear W22565496492023 @default.
• W2256549649 crossrefType "journal-article" @default.
• W2256549649 hasAuthorship W2256549649A5016187996 @default.
• W2256549649 hasAuthorship W2256549649A5047959935 @default.
• W2256549649 hasAuthorship W2256549649A5050436093 @default.
• W2256549649 hasAuthorship W2256549649A5073154909 @default.
• W2256549649 hasAuthorship W2256549649A5073668447 @default.
• W2256549649 hasAuthorship W2256549649A5074225402 @default.
• W2256549649 hasAuthorship W2256549649A5075671191 @default.
• W2256549649 hasAuthorship W2256549649A5075879267 @default.
• W2256549649 hasConcept C10138342 @default.
• W2256549649 hasConcept C112613896 @default.
• W2256549649 hasConcept C134306372 @default.
• W2256549649 hasConcept C155574463 @default.
• W2256549649 hasConcept C162324750 @default.
• W2256549649 hasConcept C178790620 @default.
• W2256549649 hasConcept C180577832 @default.
• W2256549649 hasConcept C185592680 @default.
• W2256549649 hasConcept C197336794 @default.
• W2256549649 hasConcept C21951064 @default.
• W2256549649 hasConcept C2776568683 @default.
• W2256549649 hasConcept C2776964284 @default.
• W2256549649 hasConcept C2777516009 @default.
• W2256549649 hasConcept C2779149719 @default.
• W2256549649 hasConcept C2779281246 @default.

• next