Artemis (DCLRE1C, SNM1C): A Target Enabling Package
Creators
- 1. Structural Genomics Consortium
- 2. Department of Oncology, Weatherall Institute of Molecular Medicine, University of Oxford
- 3. Department of Chemistry, University of Oxford
Description
Currently several radio-sensitising and chemotherapeutic agents are used in conjunction with radiotherapy to enhance the efficacy of cancer treatment. DCLRE1C/Artemis is a major player in both programmed (V(D)J) recombination and non-programmed c-NHEJ DSB repair. This makes Artemis and other DSB repair enzymes an attractive pharmacological target for the radiosensitisation of tumours. This TEP includes expression and purification methods for producing the full-length (aa 1-692), and the catalytic domain (aa 1-362) of Artemis for high-throughput activity and inhibitor assays, and a robust crystallisation method that is able to generate reproducible crystals for small molecule compound soaking. We also present an Artemis structure in complex with the β-lactam anti-bacterial compound ceftriaxone.
Notes
Files
Artemis TEP_v1.pdf
Files
(1.4 MB)
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Additional details
Related works
- Is part of
- https://www.thesgc.org/tep (URL)
Funding
- A UK Hub to Catalyse Open Target Discovery. 106169
- Wellcome Trust