1020536-48-4Relevant academic research and scientific papers
Evaluation of Enzyme Substrate Radiotracers as PET/MRS Hybrid Imaging Agents
Brooks, Allen F.,Drake, Lindsey R.,Shao, Xia,Zhao, Austin,Scott, Peter J. H.,Kilbourn, Michael R.
, p. 1140 - 1143 (2018)
The development of a positron emission tomography (PET)/magnetic resonance spectroscopy (MRS) hybrid imaging agent allows for functional imaging by both methods with a single imaging agent. Enzyme substrates that are cleaved to form two metabolites present an interesting opportunity, as the unique metabolites generated might each be detected by a different modality. To be successful, such enzyme substrates would require administration of doses that (a) reach the in vivo target tissue at concentrations necessary for MRS imaging, (b) do not show substrate inhibition of tissue uptake or enzymatic activity, and (c) provide PET images that still reflect the action of the enzyme. We report in vitro and in vivo proof-of-concept studies of a carbon-11 small molecule substrate for brain monoamine oxidases that, upon enzyme-mediated cleavage, produces two metabolites, one detectable by PET and the other by MRS.
KINASE INHIBITORS AND USES THEREOF
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Page/Page column 146-147, (2008/12/05)
The present invention relates to compounds of the general formula (A) and pharmaceutical compositions thereof that inhibit protein tyrosine activity. In particular the invention relates to said compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signalling, for example, the inhibition of VEGF receptor signalling and HGF receptor signalling. Said compounds and compositions are useful for the treatment of cell proliferative diseases and conditions.
