Potent and selective small-molecule MCL-1 inhibitors demonstrate on-target cancer cell killing activity as single agents and in combination with ABT-263 (navitoclax)

@inproceedings{Leverson2015PotentAS,
  title={Potent and selective small-molecule MCL-1 inhibitors demonstrate on-target cancer cell killing activity as single agents and in combination with ABT-263 (navitoclax)},
  author={Joel D Leverson and Haichao Zhang and Jun Chen and Stephen K. Tahir and Darren Charles Phillips and John Xue and Paul M. Nimmer and Sha Jin and Morey L. Smith and Yu Xiao and Peter J Kovar and Azusa Tanaka and Milan Bruncko and George S Sheppard and Leyu Wang and Sarah Gierke and Lorna S. Kategaya and David J. Anderson and Chihunt Wong and Jeff Eastham-Anderson and Mary J. C. Ludlam and Deepak Sampath and Wayne J. Fairbrother and Ingrid E. Wertz and Saul H. Rosenberg and C. -M. Tse and Steven W. Elmore and Andrew J. Souers},
  booktitle={Cell Death and Disease},
  year={2015}
}
The anti-apoptotic protein MCL-1 is a key regulator of cancer cell survival and a known resistance factor for small-molecule BCL-2 family inhibitors such as ABT-263 (navitoclax), making it an attractive therapeutic target. However, directly inhibiting this target requires the disruption of high-affinity protein–protein interactions, and therefore designing small molecules potent enough to inhibit MCL-1 in cells has proven extremely challenging. Here, we describe a series of indole-2-carboxylic… CONTINUE READING
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