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Design of Triazolium-Grafted Peptidomimetic Macrocycles with Facial Amphipathicity to Target Pathogenic Bacteria.
Org Lett
May 2024
Université Clermont Auvergne, Clermont Auvergne INP, CNRS, ICCF, F-63000 Clermont-Ferrand, France.
Article Synopsis
- A new method was created to access 1,2,3-triazolium-grafted peptoid macrocycles through macrocyclization and postmodification of linear peptoid oligomers with specific side chains.
- X-ray and NMR studies indicated that these macrocycles tend to form stable hairpin-shaped structures, giving them a unique amphipathic character.
- Initial tests suggested that these cationic amphipathic macrocycles have potential antimicrobial properties.
A Multivalent Peptoid Conjugate Modulates Androgen Receptor Transcriptional Activity to Inhibit Therapy-resistant Prostate Cancer.
Mol Cancer Ther
October 2023
Department of Microbiology, NYU Grossman School of Medicine, New York, New York.
Prostate cancers adapt to androgen receptor (AR) pathway inhibitors and progress to castration resistance due to ongoing AR expression and function. To counter this, we developed a new approach to modulate the AR and inhibit castration-resistant prostate cancer (CRPC) using multivalent peptoid conjugates (MPC) that contain multiple copies of the AR-targeting ligand ethisterone attached to a peptidomimetic scaffold. Here, we investigated the antitumor effects of compound MPC309, a trivalent display of ethisterone conjugated to a peptoid oligomer backbone that binds to the AR with nanomolar affinity.
View Article and Find Full Text PDFDesign, synthesis and evaluation of RGD peptidomimetic - Gold nanostar conjugates as M21 cell adhesion inhibitors.
Bioorg Chem
September 2022
Department of Chemistry "Ugo Schiff", University of Florence, Via della Lastruccia 13, 50019 Sesto Fiorentino, Florence, Italy. Electronic address:
Effective targeting of αβ integrin is of high relevance in cancer research as this protein is overexpressed on several types of tumor cells, making such receptor ideal for the development of therapeutics and of diagnostic imaging agents. In this paper, the synthesis of a novel functionalized triazole-based RGD peptidomimetic and its covalent conjugation on pegylated gold nanostars is reported. These highly stable nanoconstructs showed a multivalent effect in binding αβ integrin receptors and proved to inhibit M21 cell adhesion at 25 pM concentration.
View Article and Find Full Text PDFPeptide-based supramolecular vaccine systems.
Acta Biomater
October 2021
Department of Biomedical Engineering, McKelvey School of Engineering, Washington University in St. Louis, St. Louis, MO 63130, United States. Electronic address:
Currently approved replication-competent and inactivated vaccines are limited by excessive reactogenicity and poor safety profiles, while subunit vaccines are often insufficiently immunogenic without co-administering exogenous adjuvants. Self-assembling peptide-, peptidomimetic-, and protein-based biomaterials offer a means to overcome these challenges through their inherent modularity, multivalency, and biocompatibility. As these scaffolds are biologically derived and present antigenic arrays reminiscent of natural viruses, they are prone to immune recognition and are uniquely capable of functioning as self-adjuvanting vaccine delivery vehicles that improve humoral and cellular responses.
View Article and Find Full Text PDFTargeting Galectins With Glycomimetics.
Front Chem
August 2020
CIC bioGUNE, Basque Research Technology Alliance, Derio, Spain.
Among glycan-binding proteins, galectins, β-galactoside-binding lectins, exhibit relevant biological roles and are implicated in many diseases, such as cancer and inflammation. Their involvement in crucial pathologies makes them interesting targets for drug discovery. In this review, we gather the last approaches toward the specific design of glycomimetics as potential drugs against galectins.
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