Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 48, Issue 17, Pages 5404-5407Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm050008p
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Funding
- NCI NIH HHS [P50 CA94056, CA83841] Funding Source: Medline
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To image apoptosis in vivo with a small, membrane-permeant probe, TcapQ(647) was synthesized comprising a Tat-peptide-based permeation peptide sequence, an effector caspase recognition sequence, DEVD, and a flanking optically activatable pair comprising a far-red quencher, QSY 21, and a fluorophore, Alexa Fluor 647. Under baseline conditions, high quenching efficiencies were observed resulting in low background fluorescence. Upon exposure to executioner caspases, TcapQ(647) was specifically cleaved, thereby releasing the fluorophore from the quencher and enabling imaging of apoptosis.
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