A peripheral benzodiazepine receptor targeted agent for in vitro imaging and screening

H. Charles Manning; Sarah M. Smith; Michelle Sexton; Sarah Haviland; Mingfeng Bai; Kristin Cederquist; Nephi Stella; Darryl J. Bornhop

doi:10.1021/bc060020b

A peripheral benzodiazepine receptor targeted agent for in vitro imaging and screening

H. Charles Manning, Sarah M. Smith, Michelle Sexton, Sarah Haviland, Mingfeng Bai, Kristin Cederquist, Nephi Stella, Darryl J. Bornhop

Research output: Contribution to journal › Article › peer-review

34 Scopus citations

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.

Original language	English (US)
Pages (from-to)	735-740
Number of pages	6
Journal	Bioconjugate Chemistry
Volume	17
Issue number	3
DOIs	https://doi.org/10.1021/bc060020b
State	Published - 2006
Externally published	Yes

ASJC Scopus subject areas

Biotechnology
Bioengineering
Biomedical Engineering
Pharmacology
Pharmaceutical Science
Organic Chemistry

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10.1021/bc060020b

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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.",

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AU - Manning, H. Charles

AU - Smith, Sarah M.

AU - Sexton, Michelle

AU - Haviland, Sarah

AU - Bai, Mingfeng

AU - Cederquist, Kristin

AU - Stella, Nephi

AU - Bornhop, Darryl J.

PY - 2006

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AB - 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.

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A peripheral benzodiazepine receptor targeted agent for in vitro imaging and screening

Abstract

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