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 mitoc...
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| Veröffentlicht in: | Bioconjugate chemistry 2006-05, Vol.17 (3), p.735-740 |
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| container_end_page | 740 |
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| container_issue | 3 |
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| container_title | Bioconjugate chemistry |
| container_volume | 17 |
| creator | Manning, H. Charles Smith, Sarah M Sexton, Michelle Haviland, Sarah Bai, Mingfeng Cederquist, Kristin Stella, Nephi Bornhop, Darryl J |
| description | 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. |
| doi_str_mv | 10.1021/bc060020b |
| format | Article |
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Charles ; Smith, Sarah M ; Sexton, Michelle ; Haviland, Sarah ; Bai, Mingfeng ; Cederquist, Kristin ; Stella, Nephi ; Bornhop, Darryl J</creator><creatorcontrib>Manning, H. Charles ; Smith, Sarah M ; Sexton, Michelle ; Haviland, Sarah ; Bai, Mingfeng ; Cederquist, Kristin ; Stella, Nephi ; Bornhop, Darryl J</creatorcontrib><description>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.</description><identifier>ISSN: 1043-1802</identifier><identifier>EISSN: 1520-4812</identifier><identifier>DOI: 10.1021/bc060020b</identifier><identifier>PMID: 16704212</identifier><language>eng</language><publisher>United States: American Chemical Society</publisher><subject>Animals ; Binding sites ; Breast cancer ; Cell Line ; Cells ; Humans ; Isoquinolines - chemical synthesis ; Isoquinolines - chemistry ; Isoquinolines - pharmacology ; Medical imaging ; Mitochondria - drug effects ; Mitochondria - enzymology ; Molecular Structure ; Proteins ; Rats ; Receptors, GABA - metabolism ; Succinate Dehydrogenase - metabolism</subject><ispartof>Bioconjugate chemistry, 2006-05, Vol.17 (3), p.735-740</ispartof><rights>Copyright © 2006 American Chemical Society</rights><rights>Copyright American Chemical Society May 2006</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-a475t-2140671577d700222dbd1b7cec7c8b5a59a2f861a71d7926a709faeeeee824e83</citedby><cites>FETCH-LOGICAL-a475t-2140671577d700222dbd1b7cec7c8b5a59a2f861a71d7926a709faeeeee824e83</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://pubs.acs.org/doi/pdf/10.1021/bc060020b$$EPDF$$P50$$Gacs$$H</linktopdf><linktohtml>$$Uhttps://pubs.acs.org/doi/10.1021/bc060020b$$EHTML$$P50$$Gacs$$H</linktohtml><link.rule.ids>314,780,784,2763,27075,27923,27924,56737,56787</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/16704212$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Manning, H. Charles</creatorcontrib><creatorcontrib>Smith, Sarah M</creatorcontrib><creatorcontrib>Sexton, Michelle</creatorcontrib><creatorcontrib>Haviland, Sarah</creatorcontrib><creatorcontrib>Bai, Mingfeng</creatorcontrib><creatorcontrib>Cederquist, Kristin</creatorcontrib><creatorcontrib>Stella, Nephi</creatorcontrib><creatorcontrib>Bornhop, Darryl J</creatorcontrib><title>A Peripheral Benzodiazepine Receptor Targeted Agent for In Vitro Imaging and Screening</title><title>Bioconjugate chemistry</title><addtitle>Bioconjugate Chem</addtitle><description>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.</description><subject>Animals</subject><subject>Binding sites</subject><subject>Breast cancer</subject><subject>Cell Line</subject><subject>Cells</subject><subject>Humans</subject><subject>Isoquinolines - chemical synthesis</subject><subject>Isoquinolines - chemistry</subject><subject>Isoquinolines - pharmacology</subject><subject>Medical imaging</subject><subject>Mitochondria - drug effects</subject><subject>Mitochondria - enzymology</subject><subject>Molecular Structure</subject><subject>Proteins</subject><subject>Rats</subject><subject>Receptors, GABA - metabolism</subject><subject>Succinate Dehydrogenase - metabolism</subject><issn>1043-1802</issn><issn>1520-4812</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2006</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqF0UtvEzEQAGALUdEHHPgDyEKiEoeFGWdtr4-hgjZSVQINETfL650NWxLvYm8k6K-vq0StBAd88evTPDSMvUR4hyDwfe1BAQion7AjlAKKskLxNJ-hnBRYgThkxyndAIDBSjxjh6g0lALFEVtO-ZxiN_yg6Nb8A4XbvuncLQ1dIP6VPA1jH_nCxRWN1PDpisLI2_w0C3zZjbHns41bdWHFXWj4tY9EId-es4PWrRO92O8n7Nunj4uzi-Ly8_nsbHpZuFLLsRBYgtIotW50bkCIpm6w1p689lUtnTROtJVCp7HRRiinwbSO7lclSqomJ-x0F3eI_a8tpdFuuuRpvXaB-m2yShutJar_QtTKGDBlhq__gjf9NobchBWosJLSyIze7pCPfUqRWjvEbuPiH4tg70diH0aS7at9wG29oeZR7meQQbEDXRrp98O_iz9z-RMt7WJ-bb-I70uF51d2nv2bnXc-PRb3b-I7mUGffw</recordid><startdate>200605</startdate><enddate>200605</enddate><creator>Manning, H. 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Charles</creatorcontrib><creatorcontrib>Smith, Sarah M</creatorcontrib><creatorcontrib>Sexton, Michelle</creatorcontrib><creatorcontrib>Haviland, Sarah</creatorcontrib><creatorcontrib>Bai, Mingfeng</creatorcontrib><creatorcontrib>Cederquist, Kristin</creatorcontrib><creatorcontrib>Stella, Nephi</creatorcontrib><creatorcontrib>Bornhop, Darryl J</creatorcontrib><collection>Istex</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Biotechnology Research Abstracts</collection><collection>Nucleic Acids Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Bioconjugate chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Manning, H. Charles</au><au>Smith, Sarah M</au><au>Sexton, Michelle</au><au>Haviland, Sarah</au><au>Bai, Mingfeng</au><au>Cederquist, Kristin</au><au>Stella, Nephi</au><au>Bornhop, Darryl J</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>A Peripheral Benzodiazepine Receptor Targeted Agent for In Vitro Imaging and Screening</atitle><jtitle>Bioconjugate chemistry</jtitle><addtitle>Bioconjugate Chem</addtitle><date>2006-05</date><risdate>2006</risdate><volume>17</volume><issue>3</issue><spage>735</spage><epage>740</epage><pages>735-740</pages><issn>1043-1802</issn><eissn>1520-4812</eissn><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). 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| identifier | ISSN: 1043-1802 |
| ispartof | Bioconjugate chemistry, 2006-05, Vol.17 (3), p.735-740 |
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| language | eng |
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| source | MEDLINE; ACS Publications |
| subjects | Animals Binding sites Breast cancer Cell Line Cells Humans Isoquinolines - chemical synthesis Isoquinolines - chemistry Isoquinolines - pharmacology Medical imaging Mitochondria - drug effects Mitochondria - enzymology Molecular Structure Proteins Rats Receptors, GABA - metabolism Succinate Dehydrogenase - metabolism |
| title | A Peripheral Benzodiazepine Receptor Targeted Agent for In Vitro Imaging and Screening |
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