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1.
Expert Opin Drug Discov ; 19(6): 699-723, 2024 Jun.
Article En | MEDLINE | ID: mdl-38753534

INTRODUCTION: Peptide foldamers play a critical role in pharmaceutical research and biomedical applications. This review highlights recent (post-2020) advancements in novel foldamers, synthetic techniques, and their applications in pharmaceutical research. AREAS COVERED: The authors summarize the structures and applications of peptide foldamers such as α, ß, γ-peptides, hydrocarbon-stapled peptides, urea-type foldamers, sulfonic-γ-amino acid foldamers, aromatic foldamers, and peptoids, which tackle the challenges of traditional peptide drugs. Regarding antimicrobial use, foldamers have shown progress in their potential against drug-resistant bacteria. In drug development, peptide foldamers have been used as drug delivery systems (DDS) and protein-protein interaction (PPI) inhibitors. EXPERT OPINION: These structures exhibit resistance to enzymatic degradation, are promising for therapeutic delivery, and disrupt crucial PPIs associated with diseases such as cancer with specificity, versatility, and stability, which are useful therapeutic properties. However, the complexity and cost of their synthesis, along with the necessity for thorough safety and efficacy assessments, necessitate extensive research and cross-sector collaboration. Advances in synthesis methods, computational modeling, and targeted delivery systems are essential for fully realizing the therapeutic potential of foldamers and integrating them into mainstream medical treatments.


Drug Delivery Systems , Drug Development , Drug Discovery , Peptides , Humans , Drug Discovery/methods , Peptides/pharmacology , Peptides/chemistry , Peptides/administration & dosage , Drug Development/methods , Animals , Drug Design , Protein Folding
2.
Article Zh | WPRIM | ID: wpr-488939

Objective To analyze the influence of mode of delivery on post-neonatal gut microbiota using polymerase chain reaction-denaturing gradient gel electrophoresis (PCR-DGGE) technology.Methods From April to August in 2013,thirty healthy urban full-term neonates in Nanjing City were enrolled in the study,including fifteen exclusive breastfed ones (seven born of caesarean section and eight born vaginally) and fifteen mixed feeding ones (eight born of cesarean section and seven born vaginally).Stool specimens were collected on the 28th day after birth and bacterial genomic DNA was extracted and examined by PCR on 16S rDNA V3 variable region.Bacterial community profiles were obtained by DGGE.Diversity and similarity differences of the gut microbial community structures were analyzed.Two independent sample t test or Chi-square tests were used for stastistical analysis.Results (1)Diversity analysis showed that among exclusive breastfeeding infants,the Strip number and Shannon-Weaver Diversity Index of gut microbiota in infants born abdominally were significantly lower than those born vaginally [9.71 ±4.27 vs 15.12±4.19,2.13±0.39 vs 2.61±0.32,both P<0.05],but the Simpson index of gut microbiota was significantly higher [0.13 ± 0.04 vs 0.08± 0.03,P<0.05],and no significant difference was shown in Pielou Index (P>0.05).In the mixed feeding group,the Strip number and Shannon-Weaver Diversity Index of gut microbiota in infants born abdominally were significantly lower than those born vaginally [10.88±3.23 vs 16.29±5.38,2.26±0.37 vs 2.66±0.31,both P<0.05],the Simpson index was higher,but together with the Pielou Index,neither showed significant difference (both P>0.05).(2) Similarity analysis found that gut microbiota from neonates born of same mode of delivery mostly gathered together and had much more similar structures.Conclusions In the post-neonatal period,the species and numbers of gut microbiota in infants born abdominally are all behind of those born vaginally.The predominant microbiota in babies born of cesarean section are more prominent,and gut microbiota in vaginal delivered babies are more uniformly distributed.

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