Article
Mutations in UBA3 confer resistance to the NEDD8-activating enzyme inhibitor MLN4924 in human leukemic cells.
PloS one - 1 Jan 2014
Xu G Wei, Toth Julia I, da Silva Sara R, Paiva Stacey-Lynn, Lukkarila Julie L, Hurren Rose, Maclean Neil, Sukhai Mahadeo A, Bhattacharjee Rabindra N, Goard Carolyn A, Medeiros Bruno, Gunning Patrick T, Dhe-Paganon Sirano, Petroski Matthew D, Schimmer Aaron D
Abstract excerpt
The NEDD8-activating enzyme (NAE) initiates neddylation, the cascade of post-translational NEDD8 conjugation onto target proteins. MLN4924, a selective NAE inhibitor, has displayed preclinical anti-tumor activity in vitro and in vivo, and promising clinical activity has been reported in patients with refractory hematologic malignancies. Here, we sought to understand the mechanisms of resistance to MLN4924. K562...
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