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Human Hydroxyacid Oxidase (HAO1); A Target Enabling Package

Lookup NU author(s): Dr Sabrina MackinnonORCiD

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Abstract

This project provides the tools and data to develop small molecule inhibitors for an inherited metabolic disorder (Primary hyperoxaluria type 1) due to the defective enzyme (AGXT), by targeting the enzyme (HAO1) upstream of the glyoxylate metabolic pathway to mitigate the defect (i.e. substrate reduction approach). This TEP package includes recombinant human HAO1 purification protocols, structures of the HAO1 in different states, in vitro assays to detect ligand/inhibitor binding (DSF, SPR) and enzyme activity (amplex red assay) of human HAO1, as well as initial chemical matters identified from crystallography-based fragment screening.

Publication metadata

Author(s): MacKinnon S, Arruda Bezerra G, Krojer T, Bradley AR, Talon R, Brandao-Neto J, Douangamath A, Oppermann U, von Delft F, Brennan PE, Yue WW

Publication type: Online Publication

Publication status: Published

Series Title:

Year: 2018

Access Year: 2022

Acceptance date: 30/06/2018

Publisher: Zenodo

Place Published: Geneva

Access Date: 8 April

URL: https://doi.org/10.5281/zenodo.4153603

DOI: 10.5281/zenodo.4153603

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