NUDT7_TEP_datasheet_v1 for SGC Killian.pdf (2.5 MB)
Human peroxisomal coenzyme A diphosphatase (NUDT7): a target enabling package (TEP)
journal contribution
posted on 2023-06-09, 19:26 authored by Srikannathasan Velupillai, Laura Díaz Sáez, Tobias Krojer, James Bennett, Gian Filippo Ruda, Tamas Szommer, Verena Straub, Graciela Nunez Alonso, Paulina Siejka, Anthony Bradley, Romain Talon, Michael Fairhead, Jon Elkins, Nir London, John SpencerJohn Spencer, Frank von Delft, Oleg Fedorov, Paul Brennan, Kilian HuberIn 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.
Funding
A Precompetitive Modular Peptidomimetic Toolkit for Targeting PPIs iCASE AZ; G1623; ASTRAZENECA
History
Publication status
- Published
File Version
- Published version
Journal
ZenodoExternal DOI
Page range
1-15Department affiliated with
- Chemistry Publications
Full text available
- Yes
Peer reviewed?
- No
Legacy Posted Date
2019-10-25First Open Access (FOA) Date
2019-10-25First Compliant Deposit (FCD) Date
2019-10-23Usage metrics
Categories
No categories selectedKeywords
Licence
Exports
RefWorks
BibTeX
Ref. manager
Endnote
DataCite
NLM
DC