Glycosidase-targeting small molecules for biological and therapeutic applications

Y Kim, H Li, J Choi, J Boo, H Jo, JY Hyun… - Chemical Society …, 2023 - pubs.rsc.org
Glycosidases are ubiquitous enzymes that catalyze the hydrolysis of glycosidic linkages in
oligosaccharides and glycoconjugates. These enzymes play a vital role in a wide variety of …

From Mechanism-Based Retaining Glycosidase Inhibitors to Activity-Based Glycosidase Profiling

M Artola, JMFG Aerts, GA van der Marel… - Journal of the …, 2024 - ACS Publications
Activity-based protein profiling (ABPP) is an effective technology for the identification and
functional annotation of enzymes in complex biological samples. ABP designs are normally …

Enzymatic assemblies of thiophosphopeptides instantly target Golgi apparatus and selectively kill cancer cells

W Tan, Q Zhang, J Wang, M Yi, H He… - Angewandte Chemie …, 2021 - Wiley Online Library
Changing an oxygen atom of the phosphoester bond in phosphopeptides by a sulfur atom
enables instantly targeting Golgi apparatus (GA) and selectively killing cancer cells by …

Chemical toolkit for PARK7: potent, selective, and high-throughput

Y Jia, RQ Kim, R Kooij, H Ovaa, A Sapmaz… - Journal of Medicinal …, 2022 - ACS Publications
The multifunctional human Parkinson's disease protein 7 (PARK7/DJ1) is an attractive
therapeutic target due to its link with early-onset Parkinson's disease, upregulation in …

Molecular basis for inhibition of heparanases and β-glucuronidases by siastatin B

Y Chen, AMCH van den Nieuwendijk… - Journal of the …, 2023 - ACS Publications
Siastatin B is a potent and effective iminosugar inhibitor of three diverse glycosidase
classes, namely, sialidases, β-d-glucuronidases, and N-acetyl-glucosaminidases. The mode …

Activity-based protein profiling of retaining α-amylases in complex biological samples

Y Chen, Z Armstrong, M Artola, BI Florea… - Journal of the …, 2021 - ACS Publications
Amylases are key enzymes in the processing of starch in many kingdoms of life. They are
important catalysts in industrial biotechnology where they are applied in, among others, food …

Harnessing natural-product-inspired combinatorial chemistry and computation-guided synthesis to develop N-glycan modulators as anticancer agents

WA Chen, YH Chen, CY Hsieh, PF Hung, CW Chen… - Chemical …, 2022 - pubs.rsc.org
Modulation of N-glycosylation using human Golgi α-mannosidase II (α-hGMII) inhibitors is a
potential anticancer approach, but the clinical utility of current α-hGMII inhibitors is limited by …

Selectivity aspects of activity-based (chemical) probes

S Heinzlmeir, S Müller - Drug Discovery Today, 2022 - Elsevier
Highlights•Activity-based probes are versatile tools to study protein function and biological
context.•Selective and non-selective ABPs are used for target evaluation.•Proteomic …

1, 4-Dideoxy-1, 4-imino-d-and l-lyxitol-based inhibitors bind to Golgi α-mannosidase II in different protonation forms

J Kóňa, S Šesták, IBH Wilson… - Organic & biomolecular …, 2022 - pubs.rsc.org
The development of effective inhibitors of Golgi α-mannosidase II (GMII, EC 3.2. 1.114) with
minimal off-target effects on phylogenetically-related lysosomal α-mannosidase (LMan, EC …

Cyclisations and strategies for stereoselective synthesis of piperidine iminosugars

D Dhara, A Dhara, J Bennett… - The Chemical Record, 2021 - Wiley Online Library
This personal account focuses on synthesis of polyhydroxylated piperidines, a subset of
compounds within the iminosugar family. Cyclisations to form the piperidine ring include …