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Mostrando ítems 1-10 de 68
Artículo
Stable Pyrrole-Linked Bioconjugates through Tetrazine-Triggered Azanorbornadiene Fragmentation
(Wiley-Blackwell, 2020)
An azanorbornadiene bromovinyl sulfone reagent for cysteine-selective bioconjugation has been developed. Subsequent reaction with dipyridyl tetrazine leads to bond cleavage and formation of a pyrrole-linked conjugate. The ...
Artículo
Masked Phenolic-Selenium Conjugates: Potent and Selective Antiproliferative Agents Overcoming P-gp Resistance
(MDPI, 2020)
Cancer accounts for one of the most complex diseases nowadays due to its multifactorial nature. Despite the vast number of cytotoxic agents developed so far, good therapeutic approaches are not always reached. In recent ...
Artículo
Self-acetylation at the active site of phosphoenolpyruvate carboxykinase (PCK1) controls enzyme activity
(American Society for Biochemistry and Molecular Biology Inc., 2021)
Acetylation is known to regulate the activity of cytosolic phosphoenolpyruvate carboxykinase (PCK1), a key enzyme in gluconeogenesis, by promoting the reverse reaction of the enzyme (converting phosphoenolpyruvate to ...
Artículo
Piperidine Azasugars Bearing Lipophilic Chains: Stereoselective Synthesis and Biological Activity as Inhibitors of Glucocerebrosidase (GCase)
(American Chemical Society, 2021)
We report a straightforward synthetic strategy for the preparation of trihydroxypiperidine azasugars decorated with lipophilic chains at both the nitrogen and the adjacent carbon as potential inhibitors of the lysosomal ...
Artículo
Tuning the activity of iminosugars: novel N-alkylated deoxynojirimycin derivatives as strong BuChE inhibitors
(Taylor & Francis Open Access, 2021)
We have designed unprecedented cholinesterase inhibitors based on 1-deoxynojirimycin as potential anti-Alzheimer’s agents. Compounds are comprised of three key structural motifs: the iminosugar, for interaction with ...
Artículo
Multienzymatic processes involving baeyer–villiger monooxygenases
(Multidisciplinary Digital Publishing Institute (MDPI), 2021)
Baeyer–Villiger monooxygenases (BVMOs) are flavin-dependent oxidative enzymes capable of catalyzing the insertion of an oxygen atom between a carbonylic Csp2 and the Csp3 at the alpha position, therefore transforming linear ...
Artículo
Uncovering a novel molecular mechanism for scavenging sialic acids in bacteria
(American Society for Biochemistry and Molecular Biology, 2020)
The human gut symbiont Ruminococcus gnavus scavenges host-derived N-acetylneuraminic acid (Neu5Ac) from mucins by converting it to 2,7-anhydro-Neu5Ac. We previously showed that 2,7-anhydro-Neu5Ac is transported into R. ...
Artículo
Cyclodextrin-Based Functional Glyconanomaterials
(MDPI, 2020-12)
Cyclodextrins (CDs) have long occupied a prominent position in most pharmaceutical laboratories as “off-the-shelve” tools to manipulate the pharmacokinetics of a broad range of active principles, due to their unique ...
Artículo
Influence of the surfactant degree of oligomerization on the formation of cyclodextrin: surfactant inclusion complexes
(Elsevier, 2020)
Supramolecular complexation is an attractive strategy to modulate the performance of surfactants, e.g., by host-guest interactions. Here, we investigate the interaction of single-chained, di-, tri-, and tetrameric cationic ...
Artículo
Inhibitory effect of olive phenolic compounds isolated from olive oil by-product on melanosis of shrimps
(Multidisciplinary Digital Publishing Institute (MDPI), 2021)
Melanosis is an unsolved problem of the crustacean industry and the cause of great loss of value. This study investigates the effect of two potent, natural antioxidants isolated from olive waste (hydroxytyrosol, HT and ...