Drug-like properties in macrocycles above MW 1000: Backbone rigidity vs. side-chain lipophilicity

Large, macrocyclic peptides can achieve surprisingly high membrane permeability, although the properties that govern permeability in this chemical space are only beginning to come into focus. We generated two libraries of cyclic decapeptides with stable, cross-β conformations, and found that peptoid...

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Bibliografiska uppgifter
I publikationen:Angew Chem Int Ed Engl
Huvudupphovsmän: Furukawa, Akihiro, Schwochert, Joshua, Pye, Cameron R., Asano, Daigo, Edmondson, Quinn D., Turmon, Alexandra C., Klein, Victoria G., Ono, Satoshi, Okada, Okimasa, Lokey, R. Scott
Materialtyp: Artigo
Språk:Inglês
Publicerad: 2020
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Article
Länkar:https://ncbi.nlm.nih.gov/pmc/articles/PMC7719619/
https://ncbi.nlm.nih.gov/pubmed/32789999
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1002/anie.202004550
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