Hight MR, Cheung YY, Nickels ML, Dawson ES, Zhao P, Saleh S, Buck JR, Tang D, Washington MK, Coffey RJ, Manning HC. A peptide-based positron emission tomography probe for in vivo detection of caspase activity in apoptotic cells. Clinical cancer research : an official journal of the American Association for Cancer Research. 2014 Apr 15;20(20). 2126-35. PMID: 24573549 [PubMed] PMCID: PMC3989451 NIHMSID: NIHMS571532.
Apoptosis, or programmed cell death, can be leveraged as a surrogate measure of response to therapeutic interventions in medicine. Cysteine aspartic acid-specific proteases, or caspases, are essential determinants of apoptosis signaling cascades and represent promising targets for molecular imaging. Here, we report development and in vivo validation of [(18)F]4-fluorobenzylcarbonyl-Val-Ala-Asp(OMe)-fluoromethylketone ([(18)F]FB-VAD-FMK), a novel peptide-based molecular probe suitable for quantification of caspase activity in vivo using positron emission tomography (PET).