Access
To read this story in full you will need to login or make a payment (see right).
Technical Report
Nature Medicine 13, 1114 - 1119 (2007)
Published online: 12 August 2007 | doi:10.1038/nm1608
Molecular imaging of Akt kinase activity
Limin Zhang1, Kuei C Lee2, Mahaveer S Bhojani1, Amjad P Khan1, Alla Shilman1, Eric C Holland3, Brian D Ross2,4 & Alnawaz Rehemtulla1,4
Abstract
The serine/threonine kinase Akt mediates mitogenic and anti-apoptotic responses that result from activation of multiple signaling cascades. It is considered a key determinant of tumor aggressiveness and is a major target for anticancer drug development. Here, we describe a new reporter molecule whose bioluminescence activity within live cells and in mice can be used to measure Akt activity. Akt activity in cultured cells and tumor xenografts was monitored quantitatively and dynamically in response to activation or inhibition of receptor tyrosine kinase, inhibition of phosphoinositide 3-kinase, or direct inhibition of Akt. The results provide unique insights into the pharmacokinetics and pharmacodynamics of agents that modulate Akt activity, revealing the usefulness of this reporter for rapid dose and schedule optimization in the drug development process.
To read this story in full you will need to login or make a payment (see right).
MORE ARTICLES LIKE THIS
These links to content published by NPG are automatically generated.
RESEARCH
Akt phosphorylation of La regulates specific mRNA translation in glial progenitorsOncogene Original Article
Differential response to gefitinib of cells expressing normal EGFR and the mutant EGFRvIIIBritish Journal of Cancer Original Article
Dual EGFR and mTOR targeting in squamous cell carcinoma models, and development of early markers of efficacyBritish Journal of Cancer Original Article
Structure-guided development of affinity probes for tyrosine kinases using chemical geneticsNature Chemical Biology Article (01 Apr 2007)
See all 60 matches for Research