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Verfasst von:Mier, Walter [VerfasserIn]   i
 Krämer, Susanne [VerfasserIn]   i
 Zitzmann, Sabine [VerfasserIn]   i
 Altmann, Annette [VerfasserIn]   i
 Leotta, Karin [VerfasserIn]   i
 Schierbaum, Ursula [VerfasserIn]   i
 Schnölzer, Martina [VerfasserIn]   i
 Eisenhut, Michael [VerfasserIn]   i
 Haberkorn, Uwe [VerfasserIn]   i
Titel:PEGylation enables the specific tumor accumulation of a peptide identified by phage display
Verf.angabe:Walter Mier, Susanne Krämer, Sabine Zitzmann, Annette Altmann, Karin Leotta, Ursula Schierbaum, Martina Schnölzer, Michael Eisenhut and Uwe Haberkorn
E-Jahr:2013
Jahr:25 Feb 2013
Umfang:6 S.
Teil:volume:11
 year:2013
 number:16
 pages:2706-2711
 extent:6
Fussnoten:Gesehen am 21.05.2021
Titel Quelle:Enthalten in: Organic & biomolecular chemistry
Ort Quelle:Cambridge : Royal Society of Chemistry, 2003
Jahr Quelle:2013
Band/Heft Quelle:11(2013), 16, Seite 2706-2711
ISSN Quelle:1477-0539
Abstract:Peptides are excellent alternatives to small molecules and proteinaceous drugs. Their high medicinal potential for diagnostic and therapeutic applications has prompted the development of tumor targeting peptides. Despite its excellent tumor binding capacity, FROP-DOTA (H-Glu-Asn-Tyr-Glu-Leu-Met-Asp-Leu-Leu-Ala-Tyr-Leu-Lys(DOTA)-NH2), a peptide that we had identified in phage display libraries, revealed slow binding kinetics. Consequently, biodistribution studies showed that its excretion forestalled a significant tumor accumulation. The aim of this study was to investigate whether the conjugation of PEG to FROP-DOTA resulted in a derivative with a prolonged residence time in the blood. A synthetic method for the PEGylation of the tumor specific peptide FROP-DOTA was developed. Thereafter, binding studies were done in vitro and a biodistribution was performed in tumor bearing animals. These were compared to the data obtained with FROP-DOTA. The binding kinetics of the PEGylated FROP-DOTA was even slower than that of FROP-DOTA. Biodistribution studies of the labeled conjugate in mice bearing human FRO82-2 tumors showed a time dependent increased uptake of the PEGylated peptide with a high retention (at 24 h p.i. 76% of the maximal activity concentration persisted in the tumor). The highest uptake values were determined at 120 min p.i. reaching 2.3%ID/g tumor as compared to 0.06%ID/g observed for the non-PEGylated derivative at 135 min p.i. Apparently, PEGylation provides a substantially improved stabilization in the circulation which allowed a stable tumor accumulation.
DOI:doi:10.1039/C3OB27475F
URL:Bitte beachten Sie: Dies ist ein Bibliographieeintrag. Ein Volltextzugriff für Mitglieder der Universität besteht hier nur, falls für die entsprechende Zeitschrift/den entsprechenden Sammelband ein Abonnement besteht oder es sich um einen OpenAccess-Titel handelt.

Volltext ; Verlag: https://doi.org/10.1039/C3OB27475F
 Volltext: https://pubs.rsc.org/en/content/articlelanding/2013/ob/c3ob27475f
 DOI: https://doi.org/10.1039/C3OB27475F
Datenträger:Online-Ressource
Sprache:eng
K10plus-PPN:1758343575
Verknüpfungen:→ Zeitschrift

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