Molecular imaging of protein kinases.
Protein kinases are important regulators of signal-transduction pathways. Dysregulated kinase activity is observed in a variety of human diseases such as cancer, making them targets for the development of molecular therapies. Identification of new drugs is greatly aided by molecular imaging tools which enable real time, non-invasive, dynamic and quantitative imaging of kinase activity in vivo. We have recently described a new reporter platform based on conformation dependent complementation of firefly luciferase to monitor serine/threonine kinase (Akt) activity. The reporter system provides unique insights into the pharmacokinetics and pharmacodynamics of drugs that modulate kinase activity in living subjects and also provide a platform for cell based high-throughput drug screening for modulators of kinase activity.
Zhang
Limin
L
Department of Radiation Oncology, University of Michigan School of Medicine, Ann Arbor, Michigan 48109, USA.
Bhojani
Mahaveer S
MS
Ross
Brian D
BD
Rehemtulla
Alnawaz
A
D000818:Animals; D031541:Fluorescence Resonance Energy Transfer / Q000379:methods*; D006801:Humans; D019906:Nuclear Magnetic Resonance, Biomolecular / Q000379:methods; D011494:Protein Kinases / Q000032:analysis* / Q000235:genetics / Q000378:metabolism*; D015398:Signal Transduction / Q000502:physiology
D011494:Protein Kinases