title: A peripheral benzodiazepine receptor targeted agent for in vitro imaging and screening.
abstract: We developed a molecular imaging agent (MIA), a conjugable form of PK11195 (conPK11195) coupled to a lissamine dye (Liss-ConPK11195), which targets the peripheral benzodiazepine receptor (PBR). To determine that our compound specifically binds to this 18 kDa protein, primarily expressed on the mitochondria, we performed classic binding studies on live MDA-MB-231 breast cancer cells and measured fluorescence in cell fractions of C6 glioma cells. We found that conPK11195 conjugated to the fluorophore retained significant binding to its target. Here we demonstrate the utility of the agent for in vitro imaging of live cells by specific binding to the protein of interest.
authors.affiliation: Department of Chemistry, Vanderbilt University, Nashville, Tennessee 37235, USA.
authors.forename: H Charles
authors.initials: HC
authors.lastname: Manning
authors.forename: Sarah M
authors.initials: SM
authors.lastname: Smith
authors.forename: Michelle
authors.initials: M
authors.lastname: Sexton
authors.forename: Sarah
authors.initials: S
authors.lastname: Haviland
authors.forename: Mingfeng
authors.initials: M
authors.lastname: Bai
authors.forename: Kristin
authors.initials: K
authors.lastname: Cederquist
authors.forename: Nephi
authors.initials: N
authors.lastname: Stella
authors.forename: Darryl J
authors.initials: DJ
authors.lastname: Bornhop
mesh_terms: D000818:Animals; D002460:Cell Line; D006801:Humans; D007546:Isoquinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D008928:Mitochondria / Q000187:drug effects / Q000201:enzymology; D015394:Molecular Structure; D051381:Rats; D018079:Receptors, GABA / Q000378:metabolism*; D013385:Succinate Dehydrogenase / Q000378:metabolism
chemical_list: D007546:Isoquinolines; D018079:Receptors, GABA; D013385:Succinate Dehydrogenase; C037850:PK 11195