Rational design of caspase-responsive smart molecular probe for positron emission tomography imaging of drug-induced apoptosis.

ABSTRACT: Purpose: Positron emission tomography (PET) imaging of apoptosis is very important for early evaluation of tumor therapeutic efficacy. A stimuli-responsive probe based on the peptide sequence Asp-Glu-Val-Asp (DEVD), [¹⁸F]DEVD-Cys(StBu)-PPG(CBT)-AmBF₃ ([¹⁸F]1), for PET imaging of tumor apoptosis was designed and prepared. This study aimed to develop a novel smart probe using a convenient radiosynthesis method and to fully examine the sensitivity and specificity of the probe response to the tumor treatment. Methods: The radiolabelling precursor DEVD-Cys(StBu)-PPG(CBT)-AmBF₃ (1) was synthesized through multistep reactions. The reduction together with caspase-controlled macrocyclization and self-assembly of 1 was ch

SUBMITTER: Qiu L 

PROVIDER: S-EPMC6815954 | biostudies-literature | 2019

REPOSITORIES: biostudies-literature