An amide to thioamide substitution improves the permeability and bioavailability of macrocyclic peptides

An amide to thioamide substitution improves the permeability and bioavailability of macrocyclic peptides

Abstract Solvent shielding of the amide hydrogen bond donor (NH groups) through chemical modification or conformational control has been successfully utilized to impart membrane permeability to macrocyclic peptides. We demonstrate that passive membrane permeability can also be conferred by masking t...

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Main Authors: Pritha Ghosh, Nishant Raj, Hitesh Verma, Monika Patel, Sohini Chakraborti, Bhavesh Khatri, Chandrashekar M. Doreswamy, S. R. Anandakumar, Srinivas Seekallu, M. B. Dinesh, Gajanan Jadhav, Prem Narayan Yadav, Jayanta Chatterjee
Format: Article
Language:English
Published: Nature Portfolio 2023-09-01
Series:Nature Communications
Online Access:https://doi.org/10.1038/s41467-023-41748-y

Internet

https://doi.org/10.1038/s41467-023-41748-y

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