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Li group published article on Chembiochem about a study of effect of stapling architecture on physiochemical properties and cell permeability of stapled – helical peptides

Stapled peptides emerged as a new class of targeting molecules of high binding affinity and specificity for intracellular undruggable targets. Their ability to penetrate cell membranes were exceptionally intriguing to the field, yet elusively and controversially discussed. To understand...

Li group published article on Chemical Science about a study of reversible stapling of unprotected peptides via chemoselective methionine bis-alkylation/dealkylation

We have developed a general peptide macrocyclization strategy that involves a facile and chemoselective methionine bis-alkylation/dealkylation process. This method provides a straightforward and easy approach to generate cyclic peptides with tolerances of all amino acids (including Cys), variable loop...

Li group published article on Chemical Communication about a study of N terminal N-methylation modulates chiral centre induced helical (CIH) peptides’ biophysical properties

The N-methylation effects on CIH peptides’ biophysical properties were systematically studied. The N-methylation at the N terminal NH could help improve the peptides’ cellular uptakes with retained helical conformation. This Nmethylation strategy could also be applied to longer peptides...

Li group published article on Acs Chemical Biology about a study of development of stabilized peptide-based PROTACs against estrogen receptor α

Peptide modulators targeting protein-protein interactions (PPIs) exhibit greater potential than small-molecule drugs in several important aspects including facile modification and relative large contact surface area. Stabilized peptides constructed by variable chemistry methods exhibit improved peptide stability and cell permeability...

Li group published cover paper on Theranostics

Link: http://www.thno.org/v07p4566.pdf Abstract: Inhibition of the interaction between p53 and MDM2/MDMX has attracted significant attention in anticancer therapy development. We designed a series of in-tether chiral center-induced helical stabilized peptides, among which MeR/PhR effectively reactivated p53. The activation of p53...

Li group published article on Journal of Medicinal Chemistry about a study of structural basis of inhibition of ERα-coactivator interaction by high affinity N‑terminus isoaspartic acid tethered helical peptides

Direct inhibition of the protein−protein interaction of ERα and its endogenous coactivators with a cell permeable stabilized peptide may offer a novel, promising strategy for combating ERα positive breast cancers. Here, we report the cocrystal structure of a helical...

Li group published article on Theranostics about a study of In-tether chiral center induced helical peptide modulators target p53-MDM2/MDMX and inhibit tumor growth in stem-like cancer cell

Inhibition of the interaction between p53 and MDM2/MDMX has attracted significant attention in anticancer therapy development. We designed a series of in-tether chiral center-induced helical stabilized peptides, among which MeR/PhR effectively reactivated p53. The activation of p53 inhibits cell...