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

• Main Authors: Francesca Ferlenghi (Author), Carmine Giorgio (Author), Matteo Incerti (Author), Lorenzo Guidetti (Author), Paola Chiodelli (Author), Marco Rusnati (Author), Massimiliano Tognolini (Author), Federica Vacondio (Author), Marco Mor (Author), Alessio Lodola (Author)
• Format: Book
• Published: MDPI AG, 2021-12-01T00:00:00Z.
• Subjects: article
• Online Access: 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...