On-resin N-methylation of cyclic peptides for discovery of orally bioavailable scaffolds

Backbone N-methylation is common among peptide natural products and has a significant impact on both the physical properties and the conformational states of cyclic peptides. However, the specific impact of N-methylation on passive membrane diffusion in cyclic peptides has not been investigated syst...

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Detalles Bibliográficos
Autores principales: White, Tina R., Renzelman, Chad M., Rand, Arthur C., Rezai, Taha, McEwen, Cayla M., Gelev, Vladimir M., Turner, Rushia A., Linington, Roger G., Leung, Siegfried S.F., Kalgutkar, Amit S., Bauman, Jonathan N., Zhang, Yizhong, Liras, Spiros, Price, David A., Mathiowetz, Alan M., Jacobson, Matthew P., Lokey, R. Scott
Formato: Online Artículo Texto
Lenguaje:English
Publicado: 2011
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3210067/
https://www.ncbi.nlm.nih.gov/pubmed/21946276
http://dx.doi.org/10.1038/nchembio.664

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