Publication: Development of [18F]ICMT-11 for Imaging Caspase-3/7 Activity during Therapy-Induced Apoptosis
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Date
2020-08-06
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MDPI
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Abstract
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.
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Medical Subject Headings::Chemicals and Drugs::Enzymes and Coenzymes::Enzymes::Hydrolases::Peptide Hydrolases::Cysteine Proteases::Cysteine Endopeptidases::Caspases::Caspases, Effector::Caspase 3
Medical Subject Headings::Chemicals and Drugs::Heterocyclic Compounds::Heterocyclic Compounds, 2-Ring::Indoles::Isatin
Medical Subject Headings::Analytical, Diagnostic and Therapeutic Techniques and Equipment::Diagnosis::Diagnostic Techniques and Procedures::Diagnostic Techniques, Radioisotope::Radionuclide Imaging::Tomography, Emission-Computed::Positron-Emission Tomography
Medical Subject Headings::Chemicals and Drugs::Enzymes and Coenzymes::Enzymes::Oxidoreductases::NADH, NADPH Oxidoreductases::Apoptosis Inducing Factor
Medical Subject Headings::Chemicals and Drugs::Organic Chemicals::Amides::Sulfonamides
Medical Subject Headings::Diseases::Neoplasms
Medical Subject Headings::Analytical, Diagnostic and Therapeutic Techniques and Equipment::Investigative Techniques::Drug Discovery
Medical Subject Headings::Organisms::Eukaryota::Animals::Chordata::Vertebrates::Mammals::Primates::Haplorhini::Catarrhini::Hominidae::Humans
Medical Subject Headings::Chemicals and Drugs::Heterocyclic Compounds::Heterocyclic Compounds, 2-Ring::Indoles::Isatin
Medical Subject Headings::Analytical, Diagnostic and Therapeutic Techniques and Equipment::Diagnosis::Diagnostic Techniques and Procedures::Diagnostic Techniques, Radioisotope::Radionuclide Imaging::Tomography, Emission-Computed::Positron-Emission Tomography
Medical Subject Headings::Chemicals and Drugs::Enzymes and Coenzymes::Enzymes::Oxidoreductases::NADH, NADPH Oxidoreductases::Apoptosis Inducing Factor
Medical Subject Headings::Chemicals and Drugs::Organic Chemicals::Amides::Sulfonamides
Medical Subject Headings::Diseases::Neoplasms
Medical Subject Headings::Analytical, Diagnostic and Therapeutic Techniques and Equipment::Investigative Techniques::Drug Discovery
Medical Subject Headings::Organisms::Eukaryota::Animals::Chordata::Vertebrates::Mammals::Primates::Haplorhini::Catarrhini::Hominidae::Humans
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Keywords
Positron emission tomography, Apoptosis, Caspase-3, [18F]ICMT-11, Pyrimidoindolone, Michael acceptor, Neoplasms, Isatin, Tomografía de emisión de positrones, Caspasa-3, Neoplasias, Isatina
Citation
García-Argüello SF, Lopez-Lorenzo B, Cornelissen B, Smith G. Development of [18F]ICMT-11 for Imaging Caspase-3/7 Activity during Therapy-Induced Apoptosis. Cancers. 2020 Aug 6;12(8):2191