Published January 7, 2021 | Version 1
Dataset Open

Artemis (DCLRE1C, SNM1C): A Target Enabling Package

  • 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

This document represents version 1 of the TEP datasheet and includes all updates on the project as of November 2020. For more information about TEPs and the TEP Programme, please visit https://thesgc.org/tep.

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Artemis TEP_v1.pdf

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Additional details

Related works

Funding

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