Published September 13, 2018
| Version 0
Dataset
Open
Human Poly (ADP-ribose) Polymerase Family Member 14 (PARP14); A Target Enabling Package
Authors/Creators
- Marion Schuller1
- Christian Sieg1
- Kristein Uth1
- Kerstin Riedel2
- Franz Bracher2
- Ian Gibbs-Seymour3
- Ivan Ahel3
- Xianning Lai4
- Madalena Tarsounas4
- Stefan Knapp1
- Benedikt Kessler1
- Moses Moustakim1
- Paul Brennan1
- Romain Talon1
- Tobias Krojer1
- Octovia Monteiro1
- Sarah Martin1
- Oleg Fedorov1
- Kilian Huber1
- Pavel Savitsky1
- Jon Elkins1
- 1. Structural Genomics Consortium
- 2. Department of Pharmacy, Centre for Drug Research, Ludwig-Maximilians University of Munich
- 3. Sir William Dunn School of Pathology, University of Oxford
- 4. Oxford Institute for Radiation Oncology, Nuffield Department of Medicine, University of Oxford
Description
This work provides reagents to develop specific inhibitors of the macrodomains of PARP14, for potential use for cancer and/or inflammation. Targeting the macrodomains of PARP14 is an alternative targeting strategy to PARP catalytic domain inhibitors that may allow greater inhibitor selectivity, and an alternative cellular effect.
This package includes protein purification protocols, crystal structures of the 2nd and 3rd macrodomain of PARP14 in complex with small molecule chemical starting points, in vitro assays to measure ligand binding to the macrodomains, as well as validation of a PARP14 antibody and reagents to generate PARP14 knock-out cell lines (CRISPR-Cas9).
Notes
Future versions of this document will contain experimental data on the PARP14 TEP.
Files
PARP14_TEP.pdf
Additional details
Related works
- Is part of
- https://www.thesgc.org/tep (URL)
Funding
- Wellcome Trust
- A UK Hub to Catalyse Open Target Discovery. 106169