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Title | Structure-Guided Design of EED Binders Allosterically Inhibiting the Epigenetic Polycomb Repressive Complex 2 (PRC2) Methyltransferase. |
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Journal, issue, pages | J. Med. Chem., Vol. 60, Page 415-427, Year 2017 |
Publish date | Dec 6, 2016 (structure data deposition date) |
Authors | Lingel, A. / Sendzik, M. / Huang, Y. / Shultz, M.D. / Cantwell, J. / Dillon, M.P. / Fu, X. / Fuller, J. / Gabriel, T. / Gu, J. ...Lingel, A. / Sendzik, M. / Huang, Y. / Shultz, M.D. / Cantwell, J. / Dillon, M.P. / Fu, X. / Fuller, J. / Gabriel, T. / Gu, J. / Jiang, X. / Li, L. / Liang, F. / McKenna, M. / Qi, W. / Rao, W. / Sheng, X. / Shu, W. / Sutton, J. / Taft, B. / Wang, L. / Zeng, J. / Zhang, H. / Zhang, M. / Zhao, K. / Lindvall, M. / Bussiere, D.E. |
External links | J. Med. Chem. / PubMed:27992714 |
Methods | X-ray diffraction |
Resolution | 1.6 - 2.33 Å |
Structure data | PDB-5u5h: PDB-5u5k: PDB-5u5t: PDB-5u62: |
Chemicals | ChemComp-7VV: ChemComp-GOL: ChemComp-HOH: ChemComp-FMT: ChemComp-7VY: ChemComp-7W7: ChemComp-YT3: ChemComp-7WD: |
Source |
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Keywords | TRANSCRIPTION / EED / fragment-based generation / oncology / Transcription/Transferase / Transcription-Transferase complex |