Structural basis for prodrug recognition by the SLC15 family of proton-coupled peptide transporters.

ABSTRACT: A major challenge in drug development is the optimization of intestinal absorption and cellular uptake. A successful strategy has been to develop prodrug molecules, which hijack solute carrier (SLC) transporters for active transport into the body. The proton-coupled oligopeptide transporters, PepT1 and PepT2, have been successfully targeted using this approach. Peptide transporters display a remarkable capacity to recognize a diverse library of di- and tripeptides, making them extremely promiscuous and major contributors to the pharmacokinetic profile of several important drug classes, including beta-lactam antibiotics and antiviral and antineoplastic agents. Of particular interest has been their ability to recognize amino acid and peptide-based prodrug molecules, thereby providing a ratio

SUBMITTER: Minhas GS 

PROVIDER: S-EPMC6338836 | biostudies-literature | 2019 Jan

REPOSITORIES: biostudies-literature