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Type of information: TECHNICAL ARTICLES

In this section, you can access to the latest technical information related to the PISA project topic.

Synthesis and evaluation of a [18F]formylâ??Metâ??Leuâ??Phe derivative: A positron emission tomography imaging probe for bacterial infections

The tripeptide formylâ??Metâ??Leuâ??Phe (fMLF) is a prototype of N-formylated chemotactic peptides for neutrophils owing to its ability to bind and activate the G protein-coupled formyl peptide receptor (FPR). Here, we developed an 18F-labeled fMLF derivative targeting FPR as a positron emission tomography (PET) imaging probe for bacterial infections. The study demonstrates that the fMLF derivative fMLFXYk(FB)k (X = Nle) has a high affinity for FPR (Ki = 0.62 ± 0.13 nM). The radiochemical yield and purity of [18F]fMLFXYk(FB)k were 16% and >96%, respectively. The in vivo biodistribution study showed that [18F]fMLFXYk(FB)k uptake was higher in the bacterial infected region than in the non-infected region. We observed considerably higher infection-to-muscle ratio of 4.6 at 60 min after [18F]fMLFXYk(FB)k injection. Furthermore, small-animal PET imaging studies suggested that [18F]fMLFXYk(FB)k uptake in the bacterial infected region was clearly visualized 60 min after injection.

» Author: Hiroyuki Kimura, Saki Yamauchi, Hidekazu Kawashima, Kenji Arimitsu, Yusuke Yagi, Yuji Nakamoto, Kaori Togashi, Masahiro Ono, Hideo Saji

» Reference: Bioorganic & Medicinal Chemistry Letters

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