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Gastroresistant oral peptide for fluorescence imaging of colonic inflammation

Luciani, Paola and Estella-Hermoso de Mendoza, Ander and Casalini, Tommaso and Lang, Silvia and Atrott, Kirstin and Spalinger, Marianne R. and Pratsinis, Anna and Sobek, Jens and Frey-Wagner, Isabelle and Schumacher, Jens and Leroux, Jean-Christophe and Rogler, Gerhard. (2017) Gastroresistant oral peptide for fluorescence imaging of colonic inflammation. Journal of controlled release, 262. pp. 118-126.

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Official URL: https://edoc.unibas.ch/64195/

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Abstract

The use of molecular markers for inflammation in the gastrointestinal tract could empower optical imaging modalities for early diagnosis and eventually personalized timely treatments. A major hurdle to the widespread use of functional fluorescence imaging is the absence of suitable contrast agents, in particular to be administered via the oral route due to the usual proteolytic susceptibility of the biomarkers. By designing a retro-inverso peptide, starting from a previously described sequence specific for N-cadherin, we achieved resistance to gastrointestinal degradation and even slightly improved specificity towards the target, both in ex vivo and in vivo experimental colitis. Simulations at fundamental molecular level suggested that the introduced retro-inverso modifications did not affect the folding of the peptide, leaving its ability to interact with the binding pocket of the monomeric N-cadherin unaltered, even when fluorescently labeled. Possible further derivatization of this sequence could be envisaged to further extend the potential of the designed retro-inverso peptide as diagnostic or theranostic agent for the oral route.
Faculties and Departments:05 Faculty of Science > Departement Pharmazeutische Wissenschaften > Pharmazie > Pharmazeutische Technologie (Huwyler)
UniBasel Contributors:Pratsinis, Anna
Item Type:Article, refereed
Article Subtype:Research Article
ISSN:1873-4995
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:23 Feb 2019 13:07
Deposited On:23 Feb 2019 13:07

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