ArticleChemistry (Weinheim an der Bergstrasse, Germany)2016
A Modular Approach to Phosphoglycosyltransferase Inhibitors Inspired by Nucleoside Antibiotics.
Article in Chemistry (Weinheim an der Bergstrasse, Germany), 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 29 citations in OpenAlex.
- Uridine Bisphosphonates Differentiate Phosphoglycosyl Transferase Superfamilies.Journal of the American Chemical Society · 2024Article
- Defining Early Steps inbioRxiv : the preprint server for biology · 2023Article
- Probing Monotopic Phosphoglycosyl Transferases from Complex Cellular Milieu.ACS chemical biology · 2022Article
- Backbone-Anchoring, Solid-Phase Synthesis Strategy To Access a Library of Peptidouridine-Containing Small Molecules.Organic letters · 2022Article
- Dismantling the bacterial glycocalyx: Chemical tools to probe, perturb, and image bacterial glycans.Bioorganic & medicinal chemistry · 2021Review
- Uridine natural products: Challenging targets and inspiration for novel small molecule inhibitors.Bioorganic & medicinal chemistry · 2020Review
- Engineering nucleoside antibiotics toward the development of novel antimicrobial agents.The Journal of antibiotics · 2019Review
- Mechanism of action of nucleoside antibacterial natural product antibiotics.The Journal of antibiotics · 2019Review
- Coordination of capsule assembly and cell wall biosynthesis in Staphylococcus aureus.Nature communications · 2019Article
- Facile Solid-Phase Synthesis and Assessment of Nucleoside Analogs as Inhibitors of Bacterial UDP-Sugar Processing Enzymes.ACS chemical biology · 2018Article
- GlcNAc-1-P-transferase-tunicamycin complex structure reveals basis for inhibition of N-glycosylation.Nature structural & molecular biology · 2018Article
- Article
- Design, Modeling and Synthesis of 1,2,3-Triazole-Linked Nucleoside-Amino Acid Conjugates as Potential Antibacterial Agents.Molecules (Basel, Switzerland) · 2017Article
- Bacterial phosphoglycosyl transferases: initiators of glycan biosynthesis at the membrane interface.Glycobiology · 2017Review
- Analysis of a dual domain phosphoglycosyl transferase reveals a ping-pong mechanism with a covalent enzyme intermediate.Proceedings of the National Academy of Sciences of the United States of America · 2017Article
- A Rapid and Efficient Luminescence-based Method for Assaying Phosphoglycosyltransferase Enzymes.Scientific reports · 2016Article
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
Phosphoglycosyltransferases (PGTs) represent "gatekeeper" enzymes in complex glycan assembly pathways by catalyzing transfer of a phosphosugar from an activated nucleotide diphosphosugar to a membrane-resident polyprenol phosphate. The unique structures of selected nucleoside antibiotics, such as tunicamycin and mureidomycin A, which are known to inhibit comparable biochemical transformations, are exploited as the foundation for the development of modular synthetic inhibitors of PGTs. Herein we present the design, synthesis, and biochemical evaluation of two readily manipulatable modular scaffolds as inhibitors of monotopic bacterial PGTs. Selected compounds show IC50 values down to the 40 μm range, thereby serving as lead compounds for future development of selective and effective inhibitors of diverse PGTs of biological and medicinal interest.
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Registered trials
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