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Multivalency To Inhibit and Discriminate Hexosaminidases
Dimitri Alvarez-Dorta1, Dustin T King2, Thibaut Legigan3
1LUNAM Université, CEISAM, Chimie Et Interdisciplinarité, Synthèse, Analyse, Modélisation, UMR CNRS 6230, UFR des Sciences et des Techniques, 2, rue de la Houssinière, BP 92208, 44322, Nantes Cedex 3, France.
Chemistry (Weinheim an Der Bergstrasse, Germany)
|May 27, 2017
Summary
Researchers developed multivalent polyhydroxylated acetamidoazepanes. These compounds showed enhanced potency and selectivity against hexosaminidases, offering potential therapeutic benefits.
Area of Science:
- Carbohydrate Chemistry
- Enzyme Inhibition
- Medicinal Chemistry
Background:
- Hexosaminidases are crucial enzymes involved in various biological processes.
- Dysregulation of hexosaminidases is linked to several diseases.
- Developing selective inhibitors is important for therapeutic intervention.
Purpose of the Study:
- To synthesize novel multivalent polyhydroxylated acetamidoazepanes.
- To evaluate the inhibitory activity of these compounds against a range of hexosaminidases.
- To explore the impact of multimerization on inhibitor potency and selectivity.
Main Methods:
- Synthesis of multivalent compounds utilizing ethylene glycol, glucoside, and cyclodextrin scaffolds.
- Enzyme inhibition assays against plant, mammalian, and therapeutically relevant hexosaminidases.
- Structure-activity relationship analysis to understand the effect of multimerization.
Main Results:
- Successful preparation of a diverse set of multivalent polyhydroxylated acetamidoazepanes.
- Demonstrated significant inhibitory potency against various hexosaminidases.
- Observed synergistic effects of multimerization, leading to enhanced inhibitory activity.
- Achieved fine-tuning of selectivity profiles between closely related hexosaminidases.
Conclusions:
- Multivalent polyhydroxylated acetamidoazepanes represent a promising class of hexosaminidase inhibitors.
- Multimerization is a viable strategy to improve inhibitor potency and selectivity.
- These findings could pave the way for developing new therapeutics targeting hexosaminidase-related disorders.
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