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

• Principais autores: Francesca Ferlenghi (Autor), Carmine Giorgio (Autor), Matteo Incerti (Autor), Lorenzo Guidetti (Autor), Paola Chiodelli (Autor), Marco Rusnati (Autor), Massimiliano Tognolini (Autor), Federica Vacondio (Autor), Marco Mor (Autor), Alessio Lodola (Autor)
• Formato: Livro
• Publicado em: MDPI AG, 2021-12-01T00:00:00Z.
• Assuntos: article
• Acesso em linha: Connect to this object online.

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...