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

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 the amide...

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Detalles Bibliográficos
Autores principales: Ghosh, Pritha, Raj, Nishant, Verma, Hitesh, Patel, Monika, Chakraborti, Sohini, Khatri, Bhavesh, Doreswamy, Chandrashekar M., Anandakumar, S. R., Seekallu, Srinivas, Dinesh, M. B., Jadhav, Gajanan, Yadav, Prem Narayan, Chatterjee, Jayanta
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group UK 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10539501/
https://www.ncbi.nlm.nih.gov/pubmed/37770425
http://dx.doi.org/10.1038/s41467-023-41748-y