β-Aminoalkylboronic acids are capable of binding to carbohydrate derivatives through reversible covalent interactions. An anthracene-bearing β-aminoboronic acid has been synthesized, enabling determinations of association constants for binding of sugars by fluorescence spectroscopy. The diol-binding properties of β-aminoboronic acids are also useful in catalysis: one such compound displays remarkably high activity for regioselective O-acylation of a pyranoside derivative.
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http://dx.doi.org/10.1039/c6cc09640a | DOI Listing |
ACS Med Chem Lett
January 2025
Sustainable Chemistry for Metals and Molecules, Department of Chemistry, KU Leuven, Leuven 3000, Belgium.
Cruzipain (CZP) is an essential cysteine protease of , the etiological agent of Chagas disease, and a promising druggable target. To date, no CZP inhibitors have reached clinical use, with research efforts mostly hampered by insufficient potency, limited target selectivity or lack of bioactivity translation from the isolated enzyme to the parasite in cellular environments. In this study, we report the design of , a 1,2,3-triazole-based targeted covalent inhibitor with nanomolar potency (IC = 28 nM) and null inhibition of human cathepsin L.
View Article and Find Full Text PDFMater Horiz
January 2025
Key Laboratory of Functional Inorganic Material Chemistry (MOE), School of Chemistry and Materials Science, Heilongjiang University, Harbin 150080, China.
In such an era of information explosion, improving the level of information security is still a challenging task. Self-erasing luminescent hydrogels are becoming ideal candidates for improving the level of information security with simple encryption and decryption methods. Herein, a lanthanide-polyoxometalate-based self-erasing luminescent hydrogel with time-dependent and resilient properties was constructed through a covalent crosslinked network constructed with polyacrylamide and a non-covalent crosslinked network constructed with [2-(methacryloyloxy)ethyl]trimethyl ammonium chloride/NaDyWO, along with doping urease.
View Article and Find Full Text PDFThe coronavirus main protease (MPro) plays a pivotal role in viral replication and is the target of several antivirals against SARS-CoV-2. In some species, CRCs of MPro enzymatic activity can exhibit biphasic behavior in which low ligand concentrations activate the enzyme whereas higher ones inhibit it. While this behavior has been attributed to ligand-induced dimerization, quantitative enzyme kinetics models have not been fit to it.
View Article and Find Full Text PDFAnal Cell Pathol (Amst)
January 2025
Department of General Practice, Renji Hospital, Shanghai JiaoTong University School of Medicine, Shanghai, China.
Circular RNAs (circRNAs), covalently closed single-stranded RNAs, have been implicated in cancer progression. A previous investigation revealed that circ-ZEB1 is expressed abnormally in liver cancer. However, the roles of circ-ZEB1 in non-small cell lung cancer (NSCLC) are unknown.
View Article and Find Full Text PDFAngew Chem Int Ed Engl
January 2025
Westlake University, School of Engineering, 18 Shilongshan Road, 310024, Hangzhou, CHINA.
The Friedel-Crafts reaction has been extensively applied to the preparation of various porous organic polymers because of its simple operation and abundant building blocks. However, due to its poor reversibility and excessive random reactive sites, the synthesis of crystalline organic polymers/frameworks by Friedel-Crafts reaction has never been realized so far. Herein, we develop a molecular confined Friedel-Crafts reaction strategy to achieve rapid preparation (within only 30 minutes) of highly crystalline covalent triazine frameworks (CTFs) with tailorable functionality for the first time.
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