Abstract
Recently, peptides have been validated to address intracellular targets and/or to be orally bioavailable. This review describes some of these scaffolds, offers insight in new cyclization methodologies thought to be beneficial to enhance permeability, and highlights modification on peptides thought to improve oral bioavailability. In this context, side chains and back-bone derivatization beneficial to encourage cellular uptake are presented. In addition, new methodologies supporting the assessment of permeability are discussed.
Acknowledgements
The excellent support of the author's Novartis colleague M Schaefer for providing figures is gratefully acknowledged.
Financial & competing interests disclosure
The author has no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.
No writing assistance was utilized in the production of this manuscript.