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A combinatorial approach towards the synthesis of non-hydrolysable triazole–iduronic acid hybrid inhibitors of human α-L-iduronidase: discovery of enzyme stabilizers for the potential treatment of MPSI

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Abstract

Preparation of substituent-diverse, triazole–iduronic acid hybrid molecules by click reaction of an azido iduronic acid derivative with randomly chosen alkynes is described. Library members were screened for their ability to inhibit α-L-iduronidase, and hit molecules and analogues were then investigated for their ability to stabilize rh-α-IDUA in a thermal denaturation study. This work resulted in the discovery of the first small molecules that can be used to stabilize exogenous rh-α-IDUA protein in vitro.

Graphical abstract: A combinatorial approach towards the synthesis of non-hydrolysable triazole–iduronic acid hybrid inhibitors of human α-l-iduronidase: discovery of enzyme stabilizers for the potential treatment of MPSI

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Publication details

The article was received on 19 Dec 2017, accepted on 15 Feb 2018 and first published on 15 Feb 2018


Article type: Communication
DOI: 10.1039/C7CC09642A
Citation: Chem. Commun., 2018, Advance Article
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    A combinatorial approach towards the synthesis of non-hydrolysable triazole–iduronic acid hybrid inhibitors of human α-L-iduronidase: discovery of enzyme stabilizers for the potential treatment of MPSI

    W. Cheng, C. Lin, H. Li, Y. Chang, S. Lu, Y. Chen and S. Chang, Chem. Commun., 2018, Advance Article , DOI: 10.1039/C7CC09642A

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