Conformational Adaptation Drives Potent, Selective and Durable Inhibition of the Human Protein Methyltransferase DOT1L
Version of Record online: 9 OCT 2012
© 2012 John Wiley & Sons A/S
Chemical Biology & Drug Design
Volume 80, Issue 6, pages 971–980, December 2012
How to Cite
Basavapathruni, A., Jin, L., Daigle, S. R., Majer, C. R. A., Therkelsen, C. A., Wigle, T. J., Kuntz, K. W., Chesworth, R., Pollock, R. M., Scott, M. P., Moyer, M. P., Richon, V. M., Copeland, R. A. and Olhava, E. J. (2012), Conformational Adaptation Drives Potent, Selective and Durable Inhibition of the Human Protein Methyltransferase DOT1L. Chemical Biology & Drug Design, 80: 971–980. doi: 10.1111/cbdd.12050
- Issue online: 25 OCT 2012
- Version of Record online: 9 OCT 2012
- Accepted manuscript online: 15 SEP 2012 02:40AM EST
- Received 20 April 2012, revised 3 July 2012 and accepted for publication 3 August 2012
Figure S1. (A–C) 2Fo-Fc maps for compounds EPZ00004, EPZ003696 and EPZ004777. All maps were contoured at 1σ.
Table S1. Summary of the diffraction data, refinement, and structure statistics for crystal structures.
Appendix S1. Details on the preparation of EPZ000004, EPZ002446, EPZ003144, EPZ003647, EPZ003696, EPZ004450 and EPZ004777.
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