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)

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-affi...

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Udgivet i:Cell Death Dis
Main Authors: Leverson, J D, Zhang, H, Chen, J, Tahir, S K, Phillips, D C, Xue, J, Nimmer, P, Jin, S, Smith, M, Xiao, Y, Kovar, P, Tanaka, A, Bruncko, M, Sheppard, G S, Wang, L, Gierke, S, Kategaya, L, Anderson, D J, Wong, C, Eastham-Anderson, J, Ludlam, M J C, Sampath, D, Fairbrother, W J, Wertz, I, Rosenberg, S H, Tse, C, Elmore, S W, Souers, A J
Format: Artigo
Sprog:Inglês
Udgivet: Nature Publishing Group 2015
Fag:
Original Article
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC4669759/
https://ncbi.nlm.nih.gov/pubmed/25590800
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1038/cddis.2014.561
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