Published August 9, 2018 | Version 3
Dataset Open

Human Hydroxyacid Oxidase (HAO1); A Target Enabling Package

Creators

  • 1. Structural Genomics Consortium, Nuffield Department of Medicine, University of Oxford

Description

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.

Notes

This document represents version 3 of the TEP datasheet and includes all updates on the project as of October 2020. For more information about TEPs and the TEP Programme, please visit https://thesgc.org/tep.

Files

HAO1_TEP_datasheet_v3.pdf

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Additional details

Related works

Is part of
https://www.thesgc.org/tep (URL)
Is supplemented by
https://openlabnotebooks.org/category/disease-foundation/primary-hyperoxaluria/ (URL)

Funding

Wellcome Trust
A UK Hub to Catalyse Open Target Discovery. 106169