Proflavine derivatives as fluorescent imaging agents of amyloid deposits
A series of proflavine derivatives for use to further image Aβ amyloid deposits were synthesized and characterized. Aged 3xTg-AD (23 months old) mice hippocampus sections incubated with these derivatives revealed preferential labeling of amyloid plaques. Furthermore an in vitro binding study showed...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2011-04, Vol.21 (8), p.2203-2206 |
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| container_title | Bioorganic & medicinal chemistry letters |
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| creator | Garin, Dominique Oukhatar, Fatima Mahon, Andrew B. Try, Andrew C. Dubois-Dauphin, Michel Laferla, Frank M. Demeunynck, Martine Sallanon, Marcelle Moulin Chierici, Sabine |
| description | A series of proflavine derivatives for use to further image Aβ amyloid deposits were synthesized and characterized. Aged 3xTg-AD (23
months old) mice hippocampus sections incubated with these derivatives revealed preferential labeling of amyloid plaques. Furthermore an in vitro binding study showed an inhibitory effect, although moderate, of these compounds on Aβ
40 fibril formation. This study highlights the potential of proflavine as a molecular scaffold for designing new Aβ imaging agents, its native fluorescence allowing in vitro neuropathological staining in AD damaged brain sections. |
| doi_str_mv | 10.1016/j.bmcl.2011.03.010 |
| format | Article |
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months old) mice hippocampus sections incubated with these derivatives revealed preferential labeling of amyloid plaques. Furthermore an in vitro binding study showed an inhibitory effect, although moderate, of these compounds on Aβ
40 fibril formation. This study highlights the potential of proflavine as a molecular scaffold for designing new Aβ imaging agents, its native fluorescence allowing in vitro neuropathological staining in AD damaged brain sections.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2011.03.010</identifier><identifier>PMID: 21435875</identifier><language>eng</language><publisher>Amsterdam: Elsevier Ltd</publisher><subject>Alzheimer Disease - pathology ; Amyloid ; Amyloid beta-Peptides - antagonists & inhibitors ; Amyloid beta-Peptides - metabolism ; Amyloid deposits imaging ; Animals ; beta -Amyloid ; Biological and medical sciences ; Brain ; Chemical Sciences ; Click chemistry ; Computed tomography ; Deposits ; Disease Models, Animal ; Fibrillogenesis ; Fluorescence ; Fluorescent Dyes - chemistry ; Fluorescent markers ; Hippocampus ; image analysis ; Medical sciences ; Mice ; Mice, Transgenic ; Microscopy, Fluorescence ; Miscellaneous ; Neuroimaging ; Peptide Fragments - antagonists & inhibitors ; Peptide Fragments - metabolism ; Pharmacology. Drug treatments ; Plaque, Amyloid - pathology ; Plaques ; Proflavine ; Proflavine - chemical synthesis ; Proflavine - chemistry ; scaffolds</subject><ispartof>Bioorganic & medicinal chemistry letters, 2011-04, Vol.21 (8), p.2203-2206</ispartof><rights>2011 Elsevier Ltd</rights><rights>2015 INIST-CNRS</rights><rights>Copyright © 2011 Elsevier Ltd. All rights reserved.</rights><rights>Distributed under a Creative Commons Attribution 4.0 International License</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c475t-b9f144bf4a8103373da7170599d97899739321b8e108b20a66f45a85bf4968363</citedby><cites>FETCH-LOGICAL-c475t-b9f144bf4a8103373da7170599d97899739321b8e108b20a66f45a85bf4968363</cites><orcidid>0000-0002-3521-0847</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.bmcl.2011.03.010$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>230,314,780,784,885,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=24091035$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/21435875$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink><backlink>$$Uhttps://hal.science/hal-01655552$$DView record in HAL$$Hfree_for_read</backlink></links><search><creatorcontrib>Garin, Dominique</creatorcontrib><creatorcontrib>Oukhatar, Fatima</creatorcontrib><creatorcontrib>Mahon, Andrew B.</creatorcontrib><creatorcontrib>Try, Andrew C.</creatorcontrib><creatorcontrib>Dubois-Dauphin, Michel</creatorcontrib><creatorcontrib>Laferla, Frank M.</creatorcontrib><creatorcontrib>Demeunynck, Martine</creatorcontrib><creatorcontrib>Sallanon, Marcelle Moulin</creatorcontrib><creatorcontrib>Chierici, Sabine</creatorcontrib><title>Proflavine derivatives as fluorescent imaging agents of amyloid deposits</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>A series of proflavine derivatives for use to further image Aβ amyloid deposits were synthesized and characterized. Aged 3xTg-AD (23
months old) mice hippocampus sections incubated with these derivatives revealed preferential labeling of amyloid plaques. Furthermore an in vitro binding study showed an inhibitory effect, although moderate, of these compounds on Aβ
40 fibril formation. This study highlights the potential of proflavine as a molecular scaffold for designing new Aβ imaging agents, its native fluorescence allowing in vitro neuropathological staining in AD damaged brain sections.</description><subject>Alzheimer Disease - pathology</subject><subject>Amyloid</subject><subject>Amyloid beta-Peptides - antagonists & inhibitors</subject><subject>Amyloid beta-Peptides - metabolism</subject><subject>Amyloid deposits imaging</subject><subject>Animals</subject><subject>beta -Amyloid</subject><subject>Biological and medical sciences</subject><subject>Brain</subject><subject>Chemical Sciences</subject><subject>Click chemistry</subject><subject>Computed tomography</subject><subject>Deposits</subject><subject>Disease Models, Animal</subject><subject>Fibrillogenesis</subject><subject>Fluorescence</subject><subject>Fluorescent Dyes - chemistry</subject><subject>Fluorescent markers</subject><subject>Hippocampus</subject><subject>image analysis</subject><subject>Medical sciences</subject><subject>Mice</subject><subject>Mice, Transgenic</subject><subject>Microscopy, Fluorescence</subject><subject>Miscellaneous</subject><subject>Neuroimaging</subject><subject>Peptide Fragments - antagonists & inhibitors</subject><subject>Peptide Fragments - metabolism</subject><subject>Pharmacology. Drug treatments</subject><subject>Plaque, Amyloid - pathology</subject><subject>Plaques</subject><subject>Proflavine</subject><subject>Proflavine - chemical synthesis</subject><subject>Proflavine - chemistry</subject><subject>scaffolds</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2011</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkcGL1DAYxYMo7jj6D3jQXkQ8tH5p0jSBvSyLOsKAgi54C1_bZMzQNmPSKex_b0rH9aa5hITfe99LHiEvKRQUqHh_LJqh7YsSKC2AFUDhEdlQLnjOOFSPyQaUgFwq_uOKPIvxCEA5cP6UXJWUs0rW1YbsvgZve5zdaLLOBDfj5GYTM4yZ7c8-mNiaccrcgAc3HjI8pFPMvM1wuO-965Lo5KOb4nPyxGIfzYvLviV3Hz98v93l-y-fPt_e7POW19WUN8pSzhvLUVJgrGYd1rSGSqlO1VKpmilW0kYaCrIpAYWwvEJZJYUSkgm2Je9W35_Y61NIwcK99uj07mavl7v0M1Va5UwT-3ZlT8H_Ops46cGl9_Q9jsafo5Z1SZkshfo_KYDWClLeLSlXsg0-xmDsQwgKeqlFH_VSi15q0cBSHkiiVxf7czOY7kHyp4cEvLkAGFvsbcCxdfEvx0Elm4V7vXIWvcZDSMzdtzSpSt0yLgRLxPVKmFTC7EzQsXVmbE3ngmkn3Xn3r6S_AfOKsZw</recordid><startdate>20110415</startdate><enddate>20110415</enddate><creator>Garin, Dominique</creator><creator>Oukhatar, Fatima</creator><creator>Mahon, Andrew B.</creator><creator>Try, Andrew C.</creator><creator>Dubois-Dauphin, Michel</creator><creator>Laferla, Frank M.</creator><creator>Demeunynck, Martine</creator><creator>Sallanon, Marcelle Moulin</creator><creator>Chierici, Sabine</creator><general>Elsevier Ltd</general><general>Elsevier</general><scope>FBQ</scope><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope><scope>7QO</scope><scope>7TK</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope><scope>1XC</scope><orcidid>https://orcid.org/0000-0002-3521-0847</orcidid></search><sort><creationdate>20110415</creationdate><title>Proflavine derivatives as fluorescent imaging agents of amyloid deposits</title><author>Garin, Dominique ; Oukhatar, Fatima ; Mahon, Andrew B. ; Try, Andrew C. ; Dubois-Dauphin, Michel ; Laferla, Frank M. ; Demeunynck, Martine ; Sallanon, Marcelle Moulin ; Chierici, Sabine</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c475t-b9f144bf4a8103373da7170599d97899739321b8e108b20a66f45a85bf4968363</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2011</creationdate><topic>Alzheimer Disease - pathology</topic><topic>Amyloid</topic><topic>Amyloid beta-Peptides - antagonists & inhibitors</topic><topic>Amyloid beta-Peptides - metabolism</topic><topic>Amyloid deposits imaging</topic><topic>Animals</topic><topic>beta -Amyloid</topic><topic>Biological and medical sciences</topic><topic>Brain</topic><topic>Chemical Sciences</topic><topic>Click chemistry</topic><topic>Computed tomography</topic><topic>Deposits</topic><topic>Disease Models, Animal</topic><topic>Fibrillogenesis</topic><topic>Fluorescence</topic><topic>Fluorescent Dyes - chemistry</topic><topic>Fluorescent markers</topic><topic>Hippocampus</topic><topic>image analysis</topic><topic>Medical sciences</topic><topic>Mice</topic><topic>Mice, Transgenic</topic><topic>Microscopy, Fluorescence</topic><topic>Miscellaneous</topic><topic>Neuroimaging</topic><topic>Peptide Fragments - antagonists & inhibitors</topic><topic>Peptide Fragments - metabolism</topic><topic>Pharmacology. Drug treatments</topic><topic>Plaque, Amyloid - pathology</topic><topic>Plaques</topic><topic>Proflavine</topic><topic>Proflavine - chemical synthesis</topic><topic>Proflavine - chemistry</topic><topic>scaffolds</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Garin, Dominique</creatorcontrib><creatorcontrib>Oukhatar, Fatima</creatorcontrib><creatorcontrib>Mahon, Andrew B.</creatorcontrib><creatorcontrib>Try, Andrew C.</creatorcontrib><creatorcontrib>Dubois-Dauphin, Michel</creatorcontrib><creatorcontrib>Laferla, Frank M.</creatorcontrib><creatorcontrib>Demeunynck, Martine</creatorcontrib><creatorcontrib>Sallanon, Marcelle Moulin</creatorcontrib><creatorcontrib>Chierici, Sabine</creatorcontrib><collection>AGRIS</collection><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><collection>Biotechnology Research Abstracts</collection><collection>Neurosciences Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>Hyper Article en Ligne (HAL)</collection><jtitle>Bioorganic & medicinal chemistry letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Garin, Dominique</au><au>Oukhatar, Fatima</au><au>Mahon, Andrew B.</au><au>Try, Andrew C.</au><au>Dubois-Dauphin, Michel</au><au>Laferla, Frank M.</au><au>Demeunynck, Martine</au><au>Sallanon, Marcelle Moulin</au><au>Chierici, Sabine</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Proflavine derivatives as fluorescent imaging agents of amyloid deposits</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2011-04-15</date><risdate>2011</risdate><volume>21</volume><issue>8</issue><spage>2203</spage><epage>2206</epage><pages>2203-2206</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>A series of proflavine derivatives for use to further image Aβ amyloid deposits were synthesized and characterized. Aged 3xTg-AD (23
months old) mice hippocampus sections incubated with these derivatives revealed preferential labeling of amyloid plaques. Furthermore an in vitro binding study showed an inhibitory effect, although moderate, of these compounds on Aβ
40 fibril formation. This study highlights the potential of proflavine as a molecular scaffold for designing new Aβ imaging agents, its native fluorescence allowing in vitro neuropathological staining in AD damaged brain sections.</abstract><cop>Amsterdam</cop><pub>Elsevier Ltd</pub><pmid>21435875</pmid><doi>10.1016/j.bmcl.2011.03.010</doi><tpages>4</tpages><orcidid>https://orcid.org/0000-0002-3521-0847</orcidid></addata></record> |
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| source | MEDLINE; Access via ScienceDirect (Elsevier) |
| subjects | Alzheimer Disease - pathology Amyloid Amyloid beta-Peptides - antagonists & inhibitors Amyloid beta-Peptides - metabolism Amyloid deposits imaging Animals beta -Amyloid Biological and medical sciences Brain Chemical Sciences Click chemistry Computed tomography Deposits Disease Models, Animal Fibrillogenesis Fluorescence Fluorescent Dyes - chemistry Fluorescent markers Hippocampus image analysis Medical sciences Mice Mice, Transgenic Microscopy, Fluorescence Miscellaneous Neuroimaging Peptide Fragments - antagonists & inhibitors Peptide Fragments - metabolism Pharmacology. Drug treatments Plaque, Amyloid - pathology Plaques Proflavine Proflavine - chemical synthesis Proflavine - chemistry scaffolds |
| title | Proflavine derivatives as fluorescent imaging agents of amyloid deposits |
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