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A kinase-independent function of AKT promotes cancer cell survival.
(ELIFE SCIENCES PUBLICATIONS LTD, 2014-12-31)
The serine-threonine kinase AKT regulates proliferation and survival by phosphorylating a network of protein substrates. In this study, we describe a kinase-independent function of AKT. In cancer cells harboring gain-of-function ...
Targeting molecular addictions in cancer.
(NATURE PUBLISHING GROUP, 2014-11-25)
Cancer cells depend on a finite number of critical signals for their survival. Oncogene addiction, that is, the acquired dependence of a cancer cell on the activity of a single oncogenic gene product, has been the basis ...
A systematic molecular and pharmacologic evaluation of AKT inhibitors reveals new insight into their biological activity.
(SPRINGERNATURE, 2020-08-18)
BACKGROUND: AKT, a critical effector of the phosphoinositide 3-kinase (PI3K) signalling cascade, is an intensely pursued therapeutic target in oncology. Two distinct classes of AKT inhibitors have been in clinical development, ...
Inhibitors in AKTion: ATP-competitive vs allosteric.
(PORTLAND PRESS LTD, 2020-06-30)
Aberrant activation of the PI3K pathway is one of the commonest oncogenic events in human cancer. AKT is a key mediator of PI3K oncogenic function, and thus has been intensely pursued as a therapeutic target. Multiple AKT ...
Mathematical modeling identifies optimum lapatinib dosing schedules for the treatment of glioblastoma patients.
(PUBLIC LIBRARY SCIENCE, 2018-01-01)
Human primary glioblastomas (GBM) often harbor mutations within the epidermal growth factor receptor (EGFR). Treatment of EGFR-mutant GBM cell lines with the EGFR/HER2 tyrosine kinase inhibitor lapatinib can effectively ...
Orally bioavailable CDK9/2 inhibitor shows mechanism-based therapeutic potential in MYCN-driven neuroblastoma.
(AMER SOC CLINICAL INVESTIGATION INC, 2020-11-02)
The undruggable nature of oncogenic Myc transcription factors poses a therapeutic challenge in neuroblastoma, a pediatric cancer in which MYCN amplification is strongly associated with unfavorable outcome. Here, we show ...
EGFR feedback-inhibition by Ran-binding protein 6 is disrupted in cancer.
(NATURE PUBLISHING GROUP, 2017-12-11)
Transport of macromolecules through the nuclear pore by importins and exportins plays a critical role in the spatial regulation of protein activity. How cancer cells co-opt this process to promote tumorigenesis remains ...