Novel molecular imaging platform for monitoring oncological kinases |
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| Authors: | Shyam Nyati Brian D Ross Alnawaz Rehemtulla |
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| Institution: | (1) Department of Radiation Oncology, University of Michigan, 48109 Ann Arbor, MI, USA;(2) Department of Radiology, University of Michigan, 48109 Ann Arbor, MI, USA;(3) Department of Biological Chemistry, University of Michigan, 48109 Ann Arbor, MI, USA;(4) Center for Molecular Imaging, University of Michigan, 48109 Ann Arbor, MI, USA |
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| Abstract: | Recent advances in oncology have lead to identification of a plethora of alterations in signaling pathways that are critical
to oncogenesis and propagation of malignancy. Among the biomarkers identified, dysregulated kinases and associated changes
in signaling cascade received the lion's share of scientific attention and have been under extensive investigations with goal
of targeting them for anti-cancer therapy. Discovery of new drugs is immensely facilitated by molecular imaging technology
which enables non-invasive, real time, dynamic imaging and quantification of kinase activity. Here, we review recent development
of novel kinase reporters based on conformation dependent complementation of firefly luciferase to monitor kinase activity.
Such reporter system provides unique insights into the pharmacokinetics and pharmacodynamics of drugs that modulate kinase
signaling and have a huge potential in drug discovery, validation, and drug-target interactions. |
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