Carbohydrates are organic, multifunctional, and stereochemically rich molecules, playing important roles in biological processes relevant for health and disease

Carbohydrates are organic, multifunctional, and stereochemically rich molecules, playing important roles in biological processes relevant for health and disease. Embodying such structural features, these unique molecular entities can be transformed in a diversity of compounds applied as drugs, food supplements, as biologically active materials, in cosmetics, just to name a few of the wide uses of carbohydrates and their mimetics. Research in carbohydrates also covers a diversity of domains as highlighted in this special issue, containing contributions of experts in fields such as glycochemistry, molecular biology, computational chemistry, and materials science, that address the roles of carbohydrates to understand biological processes and to develop new approaches for disease diagnosis and treatment. Kuttel and Ravenscroft describe a molecular modeling study with the capsular polysaccharides of serotype III and serotype 14, leading to a conformational rationale for the antigenic epitopes identified for these polysaccharides. Based on their discovery they suggest a strategy for bacterial evasion of the host immune system by contamination with these bacteria. Chitosan-based films loaded with chitosan microparticles, that contain a bioactive peptide with antihypertensive properties, have been developed by Pintado and coworkers, consisting of an innovative approach to increase peptide efficiency and bioavailability. McReynolds and coworkers established a new microwave-assisted oxime-based chemoselective methodology to prepare trivalent glycoclusters. The reaction is usually completed in 30 min, with the additional advantage of using unprotected sugars, and may be a step forward for the synthesis of more complex glycoconjugates and glycoclusters, multivalent molecules relevant for a number of biomedical uses. Iminosugars are among the most relevant groups buy GW4064 of glycomimetics for therapeutic applications. Among their variety of biological properties, their ability to mimic the transition state species in glycosidase catalysis and therefore their propensity to inhibit these enzymes, which are likely involved in a number of diseases, provides resulted in some substances that are found in treatment centers for the treating diabetes or Gauchers disease. Two original articles in this special issue are devoted to the synthesis of new iminosugar derivatives and the evaluation of their glycosidase inhibitory properties. Carvalho and coworkers investigated a small library of synthesized iminosugars differing in stereochemistry, ring size, and N-substitution and found two potent -glucosidase inhibitors bearing d-and l-configurations with six-membered and seven-membered ring iminosugars, in which the endocyclic amino group was derivatized with the hydroxyethyl group. The contribution of Ramn Estevez and coworkers is based on the development of new synthetic routes to polyhydroxyoctahydroindoles, iminosugars with potential as pharmacological chaperones for lysosomal storage disorders, caused by mutations in the lysosomal -galactosidase, and frequently related to misfolding. Resulting from unusual fat burning capacity of glycosphingolipids, glycogen, glycoproteins or mucopolysaccharides, they could generate neurodegenerative disorders, amongst others. The established little substances might become ligands from the mutant enzyme, marketing the right stopping and folding its degradation on the endoplasmic reticulum, a novel approach for disease treatment. Alzheimers disease (AD) is also a neurodegenerative disorder, and medicines able to prevent disease progression are not yet available. Rauter and coworkers disclose the structure of C-glycosyl flavones as neuroprotective providers able to fully rescue human being neuroblastoma cells buy GW4064 from both H2O2 and A1-42-induced cell death, a step forward to lead constructions for further development against AD. Another approach to treat AD patients is based on the cholinergic approach. Xavier and coworkers describe elegant syntheses of fresh purine and uracil isonucleosides embodying xylosyl or glucosyl organizations, and the finding of a potent and selective acetylcholinesterase inhibitor bearing a theobromine band and an octyl string from the glucosyl group. Cell-surface glycans are named therapeutic targets, seeing that their composition adjustments in many illnesses (e.g., in cancers). The critique, authored by Rachel Hevey, addresses methods to develop glycomimetics that improve binding affinities and pharmacokinetic properties towards even more drug-like compounds handling therapies for carbohydrate-binding goals. Hossain and Andreana revised the improvement made in man made carbohydrate-based antitumor vaccines that improve immune system responses simply by targeting particular antigens, in a lovely function that also addresses various other advancements in carbohydrate-based malignancy treatments, including glycoconjugate prodrugs, glycosidase inhibitors, and early analysis. We hope the readers enjoy this Special Issue and get inspired to unveil the secrets of life with carbohydrate sciences! Author Contributions Amlia Pilar Rauter and Nuno Manuel Xavier contributed equally to this Editorial. All authors have agreed and read towards the posted version from the manuscript. Funding The authors are acknowledged to Funda gratefully??o em virtude de a Cincia e a Tecnologia for the support from the strategic task UID/MULTI/00612/2019 of Centro de Qumica e Bioqumica. Conflicts appealing The authors declare no conflicts appealing.. to build up new techniques for disease treatment and analysis. Kuttel and Ravenscroft explain a molecular modeling research using the capsular polysaccharides of serotype serotype and III 14, resulting in a conformational rationale for the antigenic epitopes determined for these polysaccharides. Predicated on their finding they suggest a technique for bacterial evasion from the host disease fighting capability by disease with these bacterias. Chitosan-based films packed with chitosan microparticles, which contain a bioactive peptide with antihypertensive properties, have already been Rabbit polyclonal to ABHD14B produced by Pintado and coworkers, comprising an innovative method of increase peptide effectiveness and bioavailability. McReynolds and coworkers founded a fresh microwave-assisted oxime-based chemoselective strategy to get ready trivalent glycoclusters. The reaction is completed in 30 min, with the additional advantage of using unprotected sugars, and may be a step forward for the synthesis of more complex glycoconjugates and glycoclusters, multivalent molecules relevant for a number of biomedical uses. Iminosugars are among the most relevant groups of glycomimetics for therapeutic applications. Among their variety of biological properties, their ability to mimic the transition state species in glycosidase catalysis and thus their propensity to inhibit these enzymes, which play a role in a variety of diseases, has led to some compounds which are used in clinics for the treatment of diabetes or Gauchers disease. Two original articles in this special issue buy GW4064 are devoted to the synthesis of new iminosugar derivatives and the evaluation of their glycosidase inhibitory properties. Coworkers and Carvalho looked into a little collection of synthesized iminosugars differing in stereochemistry, band size, and N-substitution and discovered two powerful -glucosidase inhibitors bearing d-and l-configurations with six-membered and seven-membered band iminosugars, where the endocyclic amino group was derivatized using the hydroxyethyl group. The contribution of Ramn coworkers and Estevez is dependant on the introduction of brand-new artificial routes to polyhydroxyoctahydroindoles, iminosugars with potential as pharmacological chaperones for lysosomal storage space disorders, due to mutations in the lysosomal -galactosidase, and sometimes linked to misfolding. Caused by abnormal fat burning capacity of glycosphingolipids, glycogen, mucopolysaccharides or glycoproteins, they could generate neurodegenerative disorders, and the like. The developed little molecules may become ligands from the mutant enzyme, marketing the right folding and stopping its degradation on the endoplasmic reticulum, a novel strategy for disease treatment. Alzheimers disease (Advertisement) can be a neurodegenerative disorder, and medications able to prevent disease progression are not yet available. Rauter and coworkers disclose the structure of C-glycosyl flavones as neuroprotective brokers able to fully rescue human neuroblastoma cells from both H2O2 and A1-42-induced cell death, a step forward to lead structures for further development against AD. Another approach to treat AD patients is based on the cholinergic approach. Xavier and coworkers describe elegant syntheses of new purine and uracil isonucleosides embodying xylosyl or glucosyl groups, and the discovery of a potent and selective acetylcholinesterase inhibitor bearing a theobromine ring and an octyl chain linked to the glucosyl group. Cell-surface glycans are recognized as therapeutic targets, as their composition changes in many diseases (e.g., in cancer). The review, authored by Rachel Hevey, covers approaches to develop glycomimetics that improve binding affinities and pharmacokinetic properties towards more drug-like compounds addressing therapies for carbohydrate-binding targets. Hossain and Andreana revised the progress made in synthetic carbohydrate-based antitumor vaccines that improve immune responses by targeting specific antigens, in a beautiful work that covers other.