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...
Congratulations to our lab members who won the awards during the last year! Link: http://scbb.pkusz.edu.cn/index.php? =content&c=index&a=show&catid=862&id=1359
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...
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...
Prof. Benzhong Tang from Hong Kong University of Science and Technology visited our school and gave an interesting lecture titled “Biomedical Applications of AIEgens” Link:http://scbb.pkusz.edu.cn/2017/schoolnews_0922/1534.html
Prof. Xiaoyuan Chen from NIH visited our school and gave an interesting lecture titled “Cancer Nanotheranostics” Link:http://scbb.pkusz.edu.cn/2017/schoolnews_1030/1568.html
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...
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...
We have developed a facile N-terminus helix-nucleating strategy using an unnaturally tethered aspartic acid (TD strategy). Relatively weak nuclear translocation efficiency of TD PERM limits its further biological applications. A potent peptide inhibitor of estrogen receptor α (ER-α) with...
The eukaryotic-like Ser/Thr kinase Stk1 is crucial for virulence, cell wall biosynthesis, and drug susceptibility in methicillin-resistant Staphylococcus aureus (S. aureus) (MRSA). Importantly, MRSA lacking Stk1 become sensitive to β-lactam antibiotics, implying that Stk1 could be an alternative target...
