RESUMO
Peptides are fragments of proteins that carry out biological functions. They act as signaling entities via all domains of life and interfere with protein-protein interactions, which are indispensable in bio-processes. Short peptides include fundamental molecular information for a prelude to the symphony of life. They have aroused considerable interest due to their unique features and great promise in innovative bio-therapies. This work focusing on the current state-of-the-art short peptide-based therapeutical developments is the first global review written by researchers from all continents, as a celebration of 100 years of peptide therapeutics since the commencement of insulin therapy in the 1920s. Peptide "drugs" initially played only the role of hormone analogs to balance disorders. Nowadays, they achieve numerous biomedical tasks, can cross membranes, or reach intracellular targets. The role of peptides in bio-processes can hardly be mimicked by other chemical substances. The article is divided into independent sections, which are related to either the progress in short peptide-based theranostics or the problems posing challenge to bio-medicine. In particular, the SWOT analysis of short peptides, their relevance in therapies of diverse diseases, improvements in (bio)synthesis platforms, advanced nano-supramolecular technologies, aptamers, altered peptide ligands and in silico methodologies to overcome peptide limitations, modern smart bio-functional materials, vaccines, and drug/gene-targeted delivery systems are discussed.
Assuntos
Anti-Infecciosos/farmacologia , Antivirais/farmacologia , Peptídeos/química , Peptídeos/farmacologia , Peptídeos/uso terapêutico , Aminoácidos/química , Anti-Infecciosos/química , Antivirais/química , Simulação por Computador , Cosmecêuticos/química , Cosmecêuticos/uso terapêutico , Suplementos Nutricionais , Técnicas de Transferência de Genes , Humanos , Lactoferrina/química , Bicamadas Lipídicas , Nanoestruturas/administração & dosagem , Nanoestruturas/química , Peptídeos/administração & dosagem , Células-Tronco , Vacinas de Subunidades Antigênicas/química , Vacinas de Subunidades Antigênicas/farmacologia , Tratamento Farmacológico da COVID-19RESUMO
Starting from xanthatin, the biomimetic synthesis of 4ß,5ß-epoxyxanthatin-1α,4α-endoperoxide, a novel monomeric xanthanolide, has been achieved. Moreover, four unprecedented xanthanolide dimers were synthesized by three different dimerizations of xanthatin, either in a head-to-head or head-to-tail fashion. Notably, these dimeric compounds were firstly identified as artifacts in the laboratory, and two of them, mogolidesâ A and B, proved to be natural products present in the Xanthium mogolium Kitag plant.
Assuntos
Materiais Biomiméticos/síntese química , Furanos/química , Lactonas/síntese química , Peróxidos/síntese química , Produtos Biológicos/síntese química , Produtos Biológicos/química , Materiais Biomiméticos/química , Cristalografia por Raios X , Reação de Cicloadição , Dimerização , Isomerismo , Lactonas/química , Conformação Molecular , Peróxidos/química , Xanthium/química , Xanthium/metabolismoRESUMO
Let's swap: a scalable, atom-economic, enantio-, and diastereoselective synthetic route to trisubstituted γ-butyrolactones based on a Wagner-Meerwein-type dyotropic rearrangement of cis-ß-lactones is described. This methodology was applied in efficient and protecting-group-free formal syntheses and total syntheses of various xanthanolide natural products.
Assuntos
4-Butirolactona/química , Produtos Biológicos/síntese química , Lactonas/química , Sesquiterpenos/síntese química , Xanthium/química , Estrutura Molecular , EstereoisomerismoRESUMO
The functionalized FGH ring system of micrandilactone A was successfully constructed in high selectivity and good yields. The key reactions in our strategy are the Co-thiourea-catalyzed stereoselective, intramolecular Pauson-Khand reaction and Pd-thiourea-catalyzed stereoselective, intramolecular annulation. [structure: see text]