Metabolic Soft Spot and Pharmacokinetics: Functionalization of C-3 Position of an Eph–Ephrin Antagonist Featuring a Bile Acid Core as an Effective Strategy to Obtain Oral Bioavailability in Mice

UniPR129, an L-β-homotryptophan conjugate of the secondary bile acid lithocholic acid (LCA), acts as an effective protein-protein interaction (PPI) inhibitor of the Eph–ephrin system but suffers from a poor oral bioavailability in mice. To improve UniPR129 bioavailability, a metabolic soft spot, i.e...

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Detalles Bibliográficos
Autores principales: Ferlenghi, Francesca, Giorgio, Carmine, Incerti, Matteo, Guidetti, Lorenzo, Chiodelli, Paola, Rusnati, Marco, Tognolini, Massimiliano, Vacondio, Federica, Mor, Marco, Lodola, Alessio
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8779995/
https://www.ncbi.nlm.nih.gov/pubmed/35056098
http://dx.doi.org/10.3390/ph15010041

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8779995/
https://www.ncbi.nlm.nih.gov/pubmed/35056098
http://dx.doi.org/10.3390/ph15010041

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