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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
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 ...
Artículo
Ros3 (Lem3p/CDC50) Gene Dosage Is Implicated in Miltefosine Susceptibility in Leishmania (Viannia) braziliensis Clinical Isolates and in Leishmania (Leishmania) major
(American Chemical Society, 2021)
The Ros3 protein is a component of the MT-Ros3 transporter complex, considered as the main route of miltefosine entry in Leishmania. L. braziliensis clinical isolates presenting differences in miltefosine susceptibility ...
Artículo
Synthesis of sp2-Iminosugar Selenoglycolipids as Multitarget Drug Candidates with Antiproliferative, Leishmanicidal and Anti-Inflammatory Properties
(Multidisciplinary Digital Publishing Institute (MDPI), 2021)
sp2-Iminosugar glycolipids (sp2-IGLs) represent a consolidated family of glycoconjugate mimetics encompassing a monosaccharide-like glycone moiety with a pseudoamide-type nitrogen replacing the endocyclic oxygen atom of ...
Artículo
Atroposelective transformation of axially chiral (hetero)biaryls. From desymmetrization to modern resolution strategies
(Royal Society of Chemistry, 2021)
This tutorial review provides a systematic overview of the available methodologies for the atroposelective transformation of (heterobiaryl)biaryl precursors toward the synthesis of enantiomerically enriched products and ...
Artículo
Plant Growth-Promoting Rhizobacteria Modulate the Concentration of Bioactive Compounds in Tomato Fruits
(Multidisciplinary Digital Publishing Institute (MDPI), 2021)
Background: The application of microorganisms as bioestimulants in order to increase the yield and/or quality of agricultural products is becoming a widely used practice in many countries. In this work, five plant ...
Artículo
Tacrine-sugar mimetic conjugates as enhanced cholinesterase inhibitors
(Royal Society of Chemistry, 2021-03-14)
We have used the Cu(i)-catalyzed azide-alkyne Huisgen cycloaddition reaction to obtain two families of bivalent heterodimers where tacrine is connected to an azasugar or iminosugar, respectively,vialinkers of variable ...