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Single Photon Emission Computed Tomography Imaging Agents for Formyl Peptide Receptors 1 and 2
Author(s) -
stasiuk graeme J,
long nicholas,
gavins felicity
Publication year - 2012
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.26.1_supplement.679.3
Subject(s) - receptor , inflammation , peptide , antagonist , single photon emission computed tomography , chemistry , g protein coupled receptor , molecular imaging , emission computed tomography , microbiology and biotechnology , pharmacology , cancer research , medicine , biology , biochemistry , positron emission tomography , neuroscience , in vivo , genetics
Formyl Peptide Receptors (FPR) 1 and 2 are key in the signalling pathway of inflammation, and are found on leucocytes in particular neutrophils. Inflammation is a major marker of many disease states in particular Ischaemia‐reperfusion injury and atherosclerosis. 1 Identifying cells with high expression of FPR1 and FPR2 is important in the diagnosis and therapy of these diseases. Single Photon Emission Computed Tomography (SPECT) is an incredibly sensitive imaging modality and ideal for imaging receptors on the surface of cells as they are only present in extremely low concentrations. Two peptides have been identified as targets for FPR1 and FPR2, cFLFLFK 2 and WKYMVm 3 respectively. cFLFLFK is a hexapeptide with cinnamoyl group at the c‐terminus, which acts as an antagonist for FPR1. WKYMVm has been shown to have agonistic effect on FPR2. These two peptides have been modified with 99m Tc chelates to give SPECT imaging agents for FPR1 and FPR2. The biological properties of the agents have been investigated so that they maintain specific binding to the FPR. The results obtain demonstrate that the FPRs (in particular FPR1 and FPR2) provide potential targets for visualising inflammation in disease. The research has been supported by the BBSRC and GE Healthcare.