Published August 10, 2018
| Version 1
Dataset
Open
Human Peroxisomal Coenzyme A Diphosphatase (NUDT7); A Target Enabling Package
Authors/Creators
- Srikannathasan Velupillai1
- Laura Diaz Saez1
- Tobias Krojer1
- James Bennett1
- Gian Filippo Ruda1
- Tamas Szommer1
- Verena Straub1
- Graciela Nunez Alonso1
- Paulina Siejka1
- Anthony Bradley1
- Romain Talon1
- Michael Fairhead1
- Jon Elkins1
- Nir London2
- John Spencer3
- Frank von Delft1
- Oleg Fedorov1
- Paul Brennan1
- Kilian Huber1
- 1. Structural Genomics Consortium
- 2. Derpartment of Organic Chemistry, The Weizmann Institute of Science
- 3. Department of Chemistry, School of Life Sciences, University of Sussex
Description
In an effort to characterise the human NUDIX family SGC Oxford has expressed recombinant human NUDT7 as part of the SGC chemical probe programme and solved the first crystal structure of this enzyme. This enabled a crystallographic fragment screen which in conjunction with a separate covalent fragment approach yielded a first-in-class small molecule inhibitor of NUDT7 with activity in the single-digit micromolar range in a catalytic assay. This compound paves the way for chemical probe development and further functional exploration of NUDT7 in physiological and disease contexts.
Files
NUDT7_TEP_datasheet_v1.pdf
Files
(2.7 MB)
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Additional details
Related works
- Is part of
- https://www.thesgc.org/tep (URL)