Cyclic peptides have undergone a renaissance in medicinal chemistry, as studies into structure-property relationships have revealed that passive cell permeability can be designed into synthetic cyclic peptide scaffolds when conformational factors are considered. My group has been studying the physico-chemical properties that underlie passive membrane permeability in cyclic peptides, and we have determined a set of rules that may help to bias large, encoded libraries toward cell permeability.  I will discuss new directions for our group using high-content, image-based screening to evaluate the phenotypic diversity of libraries inspired by highly bioactive and cell permeable cyclic peptide natural products.

Onward, beyond the rule of 5! Understanding and controlling cell permeability in macrocyclic peptides

2019 Fall National Meeting

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