Discovery of an orally effective double-stapled peptide for reducing ovariectomy-induced bone loss in mice

Stapled peptides with significantly enhanced pharmacological profiles have emerged as promising therapeutic molecules due to their remarkable resistance to proteolysis and performance to penetrate cells. The all-hydrocarbon peptide stapling technique has already widely adopted with great success, yielding numerous potent peptide-based molecules. Based on our prior efforts, we conceived and prepared a double-stapled peptide in this study, termed FRNC-1, which effectively attenuated the bone resorption capacity of mature osteoclasts in vitro through specific inhibition of phosphorylated GSK-3β. The double-stapled peptide FRNC-1 displayed notably improved helical contents and resistance to proteolysis than its linear form. Additionally, FRNC-1 effectively prevented osteoclast activation and improved bone density for ovariectomized (OVX) mice after intravenous injection and importantly, after oral (intragastric) administration. The double-stapled peptide FRNC-1 is the first orally effective peptide that has been validated to date as a therapeutic candidate for postmenopausal osteoporosis (PMOP).

Design of ultrahigh-affinity and dual-specificity peptide antagonists of MDM2 and MDMX for P53 activation and tumor suppression

Peptide inhibition of the interactions of the tumor suppressor protein P53 with its negative regulators MDM2 and MDMX activates P53

Research progress of inhibitors of peptides and peptidomimetic acting on P 53-MDM2 i nte rf ace / 药学实践杂志

Tumor diseases have attracted great attention of the society because of the increasing morbidity in recent years .To inhibit the P53-MDM2 interaction has become an important target for design of cancer drug ,and a lot of peptide and small molecule inhibitors have been found with various kinds of drug screening and research tools .This paper summarized the recent progress of the peptide and peptidomimetic inhibitors of P53-MDM2 at home and abroad lately .

Solid-phase synthesis of the antifungal tetrapeptide from the culture of penicilli-um canescens / 药学实践杂志

Objective To synthesize the antifungal tetrapetide by solid-phase synthesis method .Methods The solid-phase peptide synthesis was chosen for getting the desired target tetrapeptide and its structure was confirmed by MS and 1 H NMR.Results The synthesis of the D-Phe-Val-D-Val-Tyr-OH was realized with yield of 47%.Conclusion The synthetic method was feasible and practical.The desired target tetrapeptide could be used for screening of antifungal activity .

Progress of Research on Nanopore-macromolecule Detection / 分析化学

After Human Gene Project, studying the kinetics of DNA translocation through a nanopore, and developing a novel fast DNA sequencing technology by using nanopore have become one of the hot in gene-research). This contribution provides an overview of nanopore macromolecular identification,including bionanopore and solid-state nanopore, while the perspective of these research are also summarized.