A peripheral benzodiazepine receptor targeted agent for in vitro imaging and screening.
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.
Manning
H Charles
HC
Department of Chemistry, Vanderbilt University, Nashville, Tennessee 37235, USA.
Smith
Sarah M
SM
Sexton
Michelle
M
Haviland
Sarah
S
Bai
Mingfeng
M
Cederquist
Kristin
K
Stella
Nephi
N
Bornhop
Darryl J
DJ
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
D007546:Isoquinolines; D018079:Receptors, GABA; D013385:Succinate Dehydrogenase; C037850:PK 11195