This article describes the structure-guided optimisation of a screening hit against the pro-survival protein BCL-XL, which is often overexpressed in solid tumors and results in malignant tumor cells showing resistance to anticancer treatments.
Structure-guided design of a selective BCL-XL inhibitor
Guillaume Lessene, Peter E Czabotar, Brad E Sleebs, Kerry Zobel, Kym N Lowes, Jerry M Adams, Jonathan B Baell, Peter M Colman, Kurt Deshayes, Wayne J Fairbrother, John A Flygare, Paul Gibbons, Wilhelmus J A Kersten, Sanji Kulasegaram, Rebecca M Moss, John P Parisot, Brian J Smith, Ian P Street, Hong Yang, David C S Huang and Keith G Watson
Nature Chemical Biology, 9, 390–397, (2013)
Editors’ Choice articles are articles identified as being of high potential interest to medicinal chemists, selected from the wider literature by members of the Editorial Board.