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Insufficient apoptosis is a recognised hallmark of cancer. A strategy to quantitatively measure apoptosis in vivo would be of immense value in both drug discovery and routine patient management. The first irreversible step in the apoptosis cascade is activation of the "executioner" caspase-3 enzyme to commence cleavage of key structural proteins. One strategy to measure caspase-3 activity is Positron Emission Tomography using isatin-5-sulfonamide radiotracers. One such radiotracer is [18F]ICMT-11, which has progressed to clinical application. This review summarises the design and development process for [18F]ICMT-11, suggesting potential avenues for further innovation.

Original publication

DOI

10.3390/cancers12082191

Type

Journal article

Journal

Cancers (Basel)

Publication Date

06/08/2020

Volume

12

Keywords

Michael acceptor, [18F]ICMT-11, apoptosis, caspase-3, positron emission tomography, pyrimidoindolone