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...
Modification of the cross-linker of constrained peptides has recently received considerable attention. Here, we present a versatile approach to modify the cross-linking tether of chiral center-induced helical (CIH) peptides via S-alkylation reac-tion. The alkylation process displayed high conversion efficiency,...
As a novel semiconducting material, the inherent, direct, and appreciable band gap endows BP with preferable optical and electronic properties other than graphene and transition metal dichalcogenides. In addition, bio-related applications with equal importance also attract great attention thanks...
A chirality induced helicity method has been developed to modulate the peptide’s biophysical and biochemical properties. We report herein a novel approach for reversibly switching the conformation of short constraint α-helical peptides through alkylation of the in-tether thioether and...
Cytolytic peptides are an emerging class of promising cancer therapeutics shown to overcome drug resistance. They eliminate cancer cells via disruption of the phospholipid bilayer of cell membranes, a mechanism that differentiates it from traditional treatments. However, applications of...
A fluorescent dye, FEB, with high fluorescence quantum yield for tumour imaging is reported. FEB dyes can be efficiently synthesized in three steps and then easily modified with either PEG or PEG-iRGD to yield FEB-2000 or FEB-2000-iRGD, respectively. Both...
The helical peptide KLA (KLAKLAKKLAKLAK) is a well known inducer of cellular apoptosis, acting to disrupt the mitochondrial membrane. However, its weak cellular uptake impedes developing any further applications. Here, we have utilized a novel in-tether chiral center induced...
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...
Due to their enhanced stability and cell permeablity, cyclic cell penetrating peptides have been widely used as delivery vectors for transporting cell-impermeable cargos into cells. In this study, we synthesized a panel of conformationally constrained peptides with either α-helix...
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...
In some cases, helical peptides stabilized by an i, i + 7 tether exhibit bettertargetbindingandcellularfunctionscomparedtotheiri, i+4 analogues. Herein, we carried out a systematic study of the effects of an in-tether chiral center on the i, i + 7 system....
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...
The preS antigen of hepatitis B virus (HBV) corresponds to the N-terminal polypeptide in the large (L) antigen in addition to the small (S) antigen. The virus-like particle (VLP) of the S antigen is widely used as a vaccine...
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...
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...