Ontology highlight
ABSTRACT:
SUBMITTER: Leverson JD
PROVIDER: S-EPMC4669759 | biostudies-literature | 2015 Jan
REPOSITORIES: biostudies-literature
Leverson J D JD Zhang H H Chen J J Tahir S K SK Phillips D C DC Xue J J Nimmer P P Jin S S Smith M M Xiao Y Y Kovar P P Tanaka A A Bruncko M M Sheppard G S GS Wang L L Gierke S S Kategaya L L Anderson D J DJ Wong C C Eastham-Anderson J J Ludlam M J C MJ Sampath D D Fairbrother W J WJ Wertz I I Rosenberg S H SH Tse C C Elmore S W SW Souers A J AJ
Cell death & disease 20150115
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 a ...[more]