1,2,3-Triazoles as Biomimetics in Peptide Science DOI Creative Commons
Naima Agouram, El Mestafa El Hadrami,

Abdeslem Bentama

et al.

Molecules, Journal Year: 2021, Volume and Issue: 26(10), P. 2937 - 2937

Published: May 14, 2021

Natural peptides are an important class of chemical mediators, essential for most vital processes. What limits the potential use as drugs is their low bioavailability and enzymatic degradation in vivo. To overcome this limitation, development new molecules mimicking great importance biologically active molecules. Therefore, replacing amide bond a peptide with heterocyclic bioisostere, such 1,2,3-triazole ring, can be considered effective solution synthesis relevant peptidomimetics. These 1,2,3-triazoles may have interesting biological activity, because they behave rigid link units, which mimic electronic properties bonds show bioisosteric effects. Additionally, triazole used linker moiety to other functional groups.

Language: Английский

Combating Antibiotic-Resistant Bacterial Infection Using Coassembled Dimeric Antimicrobial Peptide-Based Nanofibers DOI

Guoyu Li,

Haoran Deng, Wanying Xu

et al.

ACS Nano, Journal Year: 2025, Volume and Issue: unknown

Published: Jan. 13, 2025

The emergence of multidrug-resistant (MDR) pathogens, coupled with the limited effectiveness existing antibiotics in eradicating biofilms, presents a significant threat to global health care. This critical situation underscores urgent need for discovery and development antimicrobial agents. Recently, peptide-derived nanomaterials have shown promise combating such infections. Amino acid noncovalent forces, notably π–π stacking electrostatic interactions, remain underutilized guiding coassembly peptides into bacteriostatic nanomaterials. Thus, we constructed dimeric nanopeptide system using disulfide bonds cysteine. self-assembly nanofibers was realized by interaction aromatic amino acids (Trp, Phe, Pyr) attraction between oppositely charged (Asp Arg). optimal peptide 2D2W exhibits potent antibacterial activity against resistant bacteria is nontoxic. Mechanistically, penetrated outer membrane after adsorption, resulting plasma depolarization, homeostatic disruption, ultimately bacterial death. In mouse model peritonitis, demonstrated efficacy vivo treatment conclusion, design nanopeptides co-driven intermolecular forces provides promising avenue high-performance These advances may also facilitate application advancement peptide-based agents clinical practice.

Language: Английский

Citations

3
Metal‐Protein Hybrid Materials: Unlocking New Frontiers in Biomedical Applications DOI Open Access
Yong Pan, Han Zhao, Wenyong Huang

et al.

Advanced Healthcare Materials, Journal Year: 2025, Volume and Issue: unknown

Published: Jan. 7, 2025

Abstract Metal‐protein hybrid materials represent a novel class of functional that exhibit exceptional physicochemical properties and tunable structures, rendering them remarkable applications in diverse fields, including engineering, biocatalysis, biosensing, biomedicine. The design development multifunctional biocompatible metal‐protein have been the subject extensive research key aspiration for practical clinical settings. This review provides comprehensive analysis strategies, intrinsic properties, biomedical these materials, with specific emphasis on their potential cancer therapy, drug vaccine delivery, antibacterial treatments, tissue regeneration. Through rational design, stable can be synthesized using straightforward methods, enabling therapeutic, immunomodulatory, other desired functionalities. Finally, outlines existing limitations challenges associated evaluates translation, providing insights into implementation within applications.

Language: Английский

Citations

2
Antimicrobial Peptides and Their Mimetics: Promising Candidates of Next‐Generation Therapeutic Agents Combating Multidrug‐Resistant Bacteria DOI Open Access
Tianyi Zhang, Qiao Jin,

Jian Ji

et al.

Advanced Biology, Journal Year: 2025, Volume and Issue: unknown

Published: Feb. 6, 2025

Abstract The increasing morbidity and mortality caused by multidrug‐resistant bacteria alerts human beings to the fact that conventional antibiotics are no longer reliable effective alternatives imperatively needed. Owing wide range of sources, diverse structures, unique mode action, antimicrobial peptides have been highly anticipated extensively studied in recent years. Besides, integration artificial intelligence helps researchers gain access vast unexplored chemical space, which opens more opportunities for optimization design novel structures. Moreover, Due advances chemistry synthetic biology, also begun focus on potential mimetics peptides. In this review, a comprehensive discussion about natural synthesized as well their is made, so provide summary field inspire follow‐up research.

Language: Английский

Citations

2
The emergence of the C–H functionalization strategy in medicinal chemistry and drug discovery DOI
Ranjan Jana, Hasina Mamataj Begam,

Enakshi Dinda

et al.

Chemical Communications, Journal Year: 2021, Volume and Issue: 57(83), P. 10842 - 10866

Published: Jan. 1, 2021

Owing to the market competitiveness and urgent societal need, an optimum speed of drug discovery is important criterion for successful implementation. Despite rapid ascent artificial intelligence computational bioanalytical techniques accelerate in big pharma, organic synthesis privileged scaffolds predicted silico vitro vivo studies still considered as rate-limiting step. C-H activation latest technology added into chemist's toolbox construction late-stage modification functional molecules achieve desired chemical physical properties. Particularly, elimination prefunctionalization steps, exceptional group tolerance, complexity-to-diversity oriented synthesis, functionalization medicinal expand space. It has immense potential a library molecules, structural required pharmacological properties such absorption, distribution, metabolism, excretion, toxicology (ADMET) attachment reporters proteome profiling, metabolite etc. preclinical studies. Although heterocycle modification, 18F labelling, methylation, via have been reviewed from synthetic standpoint, general overview these protocols aspects not reviewed. In this feature article, we will discuss recent trends methodologies through activation/annulation cascade; arylation sp2-sp2 sp2-sp3 cross-coupling; borylation/silylation introduce linchpin further manipulation; amination N-heterocycles hydrogen bond acceptors; fluorination/fluoroalkylation tune polarity lipophilicity; methylation: methyl magic discovery; peptide macrocyclization therapeutics biologics; fluorescent labelling radiolabelling bioimaging; bioconjugation biology studies; drug-metabolite biodistribution excretion diversification drug-molecules increase efficacy safety; cutting-edge DNA encoded improved chemistry discovery.

Language: Английский

Citations

92
1,2,3-Triazoles as Biomimetics in Peptide Science DOI Creative Commons
Naima Agouram, El Mestafa El Hadrami,

Abdeslem Bentama

et al.

Molecules, Journal Year: 2021, Volume and Issue: 26(10), P. 2937 - 2937

Published: May 14, 2021

Natural peptides are an important class of chemical mediators, essential for most vital processes. What limits the potential use as drugs is their low bioavailability and enzymatic degradation in vivo. To overcome this limitation, development new molecules mimicking great importance biologically active molecules. Therefore, replacing amide bond a peptide with heterocyclic bioisostere, such 1,2,3-triazole ring, can be considered effective solution synthesis relevant peptidomimetics. These 1,2,3-triazoles may have interesting biological activity, because they behave rigid link units, which mimic electronic properties bonds show bioisosteric effects. Additionally, triazole used linker moiety to other functional groups.

Language: Английский

Citations

65