Back Cover: Discovery of a PCAF Bromodomain Chemical Probe (Angew. Chem. Int. Ed. 3/2017)

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• 作者：Moses Moustakim ; Dr. Peter G. K. Clark ; Laura Trulli ; Dr. Angel L. Fuentes de Arriba ; Dr. Matthias T. Ehebauer ; Dr. Apirat Chaikuad ; Dr. Emma J. Murphy ; Jacqui Mendez-Johnson ; Dr. Danette Daniels ; Dr. Chun-Feng D. Hou ; Yu-Hui Lin ; Dr. John R. Walker ; Dr. Raymond Hui ; Dr. Hongbing Yang ; Prof. Dr. Lucy Dorrell ; Dr. Catherine M. Rogers ; Octovia P. Monteiro ; Dr. Oleg Fedorov ; Dr. Kilian V. M. Huber ; Prof. Dr. Stefan Knapp ; Dr. Jag Heer ; Prof. Dr. Darren J. Dixon and Prof. Dr. Paul E. Brennan
• 刊名：Angewandte Chemie International Edition
• 出版年：2017
• 出版时间：January 16, 2017
• 年：2017
• 卷：56
• 期：3
• 页码：908
• 全文大小：3707K
• ISSN：1521-3773

文摘

Epigenetic drug discovery has now witnessed the emergence of a new target class of proteins, the bromodomains. In their Communication on page 827 ff., D. J. Dixon, P. E. Brennan et al. report the first potent, selective, cell-permeable, and cell-active chemical probe for the p300/CBP associated factor (PCAF) bromodomain. A combination of computational docking studies, inhibitor design, and asymmetric synthesis furnished their probe, L-Moses, for use as a chemical tool for this epigenetic target to interrogate its role in associated diseases.