Applying the Retro-Enantio Approach To Obtain a Peptide Capable of Overcoming the Blood-Brain Barrier
The blood–brain barrier (BBB) is a formidable physical and enzymatic barrier that tightly controls the passage of molecules from the blood to the brain. In fact, less than 2 % of all potential neurotherapeutics are able to cross it. Here, by applying the retro‐enantio approach to a peptide that targ...
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| Veröffentlicht in: | Angewandte Chemie International Edition 2015-03, Vol.54 (13), p.3967-3972 |
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| creator | Prades, Roger Oller-Salvia, Benjamí Schwarzmaier, Susanne M. Selva, Javier Moros, María Balbi, Matilde Grazú, Valeria de La Fuente, Jesus M. Egea, Gustavo Plesnila, Nikolaus Teixidó, Meritxell Giralt, Ernest |
| description | The blood–brain barrier (BBB) is a formidable physical and enzymatic barrier that tightly controls the passage of molecules from the blood to the brain. In fact, less than 2 % of all potential neurotherapeutics are able to cross it. Here, by applying the retro‐enantio approach to a peptide that targets the transferrin receptor, a full protease‐resistant peptide with the capacity to act as a BBB shuttle was obtained and thus enabled the transport of a variety of cargos into the central nervous system.
Jumping hurdles: The retro‐enantio approach has been applied to a peptide that targets the transferrin receptor. The stability and permeability of the peptide across the blood–brain barrier (BBB) were notably increased. This new protease‐resistant peptide was tested as a BBB shuttle, and it does facilitate the transport of cargo across the BBB, both in vitro and in vivo, as demonstrated by intravital microscopy in living mice. |
| doi_str_mv | 10.1002/anie.201411408 |
| format | Article |
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Jumping hurdles: The retro‐enantio approach has been applied to a peptide that targets the transferrin receptor. The stability and permeability of the peptide across the blood–brain barrier (BBB) were notably increased. This new protease‐resistant peptide was tested as a BBB shuttle, and it does facilitate the transport of cargo across the BBB, both in vitro and in vivo, as demonstrated by intravital microscopy in living mice.</description><edition>International ed. in English</edition><identifier>ISSN: 1433-7851</identifier><identifier>EISSN: 1521-3773</identifier><identifier>DOI: 10.1002/anie.201411408</identifier><identifier>PMID: 25650865</identifier><identifier>CODEN: ACIEAY</identifier><language>eng</language><publisher>Weinheim: WILEY-VCH Verlag</publisher><subject>Animals ; Biological Transport ; Blood ; Blood-brain barrier ; Blood-Brain Barrier - metabolism ; Cattle ; Central nervous system ; Central Nervous System Agents - pharmacokinetics ; Coculture Techniques ; enantioselectivity ; Endothelial Cells - metabolism ; membranes ; Mice ; Microscopy ; Peptide Hydrolases - chemistry ; Peptides ; Peptides - chemical synthesis ; Peptides - pharmacokinetics ; Permeability ; Rats ; Receptors ; Receptors, Transferrin - drug effects ; Stereoisomerism ; Transferrin ; Transport</subject><ispartof>Angewandte Chemie International Edition, 2015-03, Vol.54 (13), p.3967-3972</ispartof><rights>2015 WILEY‐VCH Verlag GmbH & Co. KGaA, Weinheim</rights><rights>2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.</rights><rights>2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c6508-b05757c3f1c6b9b2f6986a8768e238e83d3383318d6b571cae104b5af3a43d3c3</citedby><cites>FETCH-LOGICAL-c6508-b05757c3f1c6b9b2f6986a8768e238e83d3383318d6b571cae104b5af3a43d3c3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://onlinelibrary.wiley.com/doi/pdf/10.1002%2Fanie.201411408$$EPDF$$P50$$Gwiley$$H</linktopdf><linktohtml>$$Uhttps://onlinelibrary.wiley.com/doi/full/10.1002%2Fanie.201411408$$EHTML$$P50$$Gwiley$$H</linktohtml><link.rule.ids>314,776,780,1411,27901,27902,45550,45551</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/25650865$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Prades, Roger</creatorcontrib><creatorcontrib>Oller-Salvia, Benjamí</creatorcontrib><creatorcontrib>Schwarzmaier, Susanne M.</creatorcontrib><creatorcontrib>Selva, Javier</creatorcontrib><creatorcontrib>Moros, María</creatorcontrib><creatorcontrib>Balbi, Matilde</creatorcontrib><creatorcontrib>Grazú, Valeria</creatorcontrib><creatorcontrib>de La Fuente, Jesus M.</creatorcontrib><creatorcontrib>Egea, Gustavo</creatorcontrib><creatorcontrib>Plesnila, Nikolaus</creatorcontrib><creatorcontrib>Teixidó, Meritxell</creatorcontrib><creatorcontrib>Giralt, Ernest</creatorcontrib><title>Applying the Retro-Enantio Approach To Obtain a Peptide Capable of Overcoming the Blood-Brain Barrier</title><title>Angewandte Chemie International Edition</title><addtitle>Angew. Chem. Int. Ed</addtitle><description>The blood–brain barrier (BBB) is a formidable physical and enzymatic barrier that tightly controls the passage of molecules from the blood to the brain. In fact, less than 2 % of all potential neurotherapeutics are able to cross it. Here, by applying the retro‐enantio approach to a peptide that targets the transferrin receptor, a full protease‐resistant peptide with the capacity to act as a BBB shuttle was obtained and thus enabled the transport of a variety of cargos into the central nervous system.
Jumping hurdles: The retro‐enantio approach has been applied to a peptide that targets the transferrin receptor. The stability and permeability of the peptide across the blood–brain barrier (BBB) were notably increased. This new protease‐resistant peptide was tested as a BBB shuttle, and it does facilitate the transport of cargo across the BBB, both in vitro and in vivo, as demonstrated by intravital microscopy in living mice.</description><subject>Animals</subject><subject>Biological Transport</subject><subject>Blood</subject><subject>Blood-brain barrier</subject><subject>Blood-Brain Barrier - metabolism</subject><subject>Cattle</subject><subject>Central nervous system</subject><subject>Central Nervous System Agents - pharmacokinetics</subject><subject>Coculture Techniques</subject><subject>enantioselectivity</subject><subject>Endothelial Cells - metabolism</subject><subject>membranes</subject><subject>Mice</subject><subject>Microscopy</subject><subject>Peptide Hydrolases - chemistry</subject><subject>Peptides</subject><subject>Peptides - chemical synthesis</subject><subject>Peptides - pharmacokinetics</subject><subject>Permeability</subject><subject>Rats</subject><subject>Receptors</subject><subject>Receptors, Transferrin - drug effects</subject><subject>Stereoisomerism</subject><subject>Transferrin</subject><subject>Transport</subject><issn>1433-7851</issn><issn>1521-3773</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2015</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqN0c1v0zAYBnALgdgYXDkiS1y4pPjbzrEtZUwa7UBDHC0necM80jjYKdD_HkfdKsRlnGzJv_fRaz0IvaRkRglhb13vYcYIFZQKYh6hUyoZLbjW_HG-C84LbSQ9Qc9Sus3eGKKeohMmlSRGyVME82Ho9r7_hscbwJ9hjKFY9a4ffcD5KQZX3-DrgDfV6HyPHb6CYfQN4KUbXNUBDi3e_IRYh-19yKILoSkWcfILF6OH-Bw9aV2X4MXdeYa-vF9dLz8Ul5vzi-X8sqinfYqKSC11zVtaq6qsWKtKo5zRygDjBgxvODecU9OoSmpaO6BEVNK13In8VvMz9OaQmxf_sYM02q1PNXSd6yHskqWaUMJZWZqHqVKGCUmV_B8qhKBM6Exf_0Nvwy72-c-TyrVQIVhWs4OqY0gpQmuH6Lcu7i0ldqrVTrXaY6154NVd7K7aQnPk9z1mUB7AL9_B_oE4O19frP4OLw6zPo3w-zjr4nerNNfSfl2f23drptiV-mg_8T8pUrqD</recordid><startdate>20150323</startdate><enddate>20150323</enddate><creator>Prades, Roger</creator><creator>Oller-Salvia, Benjamí</creator><creator>Schwarzmaier, Susanne M.</creator><creator>Selva, Javier</creator><creator>Moros, María</creator><creator>Balbi, Matilde</creator><creator>Grazú, Valeria</creator><creator>de La Fuente, Jesus M.</creator><creator>Egea, Gustavo</creator><creator>Plesnila, Nikolaus</creator><creator>Teixidó, Meritxell</creator><creator>Giralt, Ernest</creator><general>WILEY-VCH Verlag</general><general>WILEY‐VCH Verlag</general><general>Wiley Subscription Services, Inc</general><scope>BSCLL</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>7TM</scope><scope>K9.</scope><scope>7X8</scope><scope>7TK</scope><scope>7SR</scope><scope>8BQ</scope><scope>8FD</scope><scope>JG9</scope></search><sort><creationdate>20150323</creationdate><title>Applying the Retro-Enantio Approach To Obtain a Peptide Capable of Overcoming the Blood-Brain Barrier</title><author>Prades, Roger ; Oller-Salvia, Benjamí ; Schwarzmaier, Susanne M. ; Selva, Javier ; Moros, María ; Balbi, Matilde ; Grazú, Valeria ; de La Fuente, Jesus M. ; Egea, Gustavo ; Plesnila, Nikolaus ; Teixidó, Meritxell ; Giralt, Ernest</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c6508-b05757c3f1c6b9b2f6986a8768e238e83d3383318d6b571cae104b5af3a43d3c3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2015</creationdate><topic>Animals</topic><topic>Biological Transport</topic><topic>Blood</topic><topic>Blood-brain barrier</topic><topic>Blood-Brain Barrier - metabolism</topic><topic>Cattle</topic><topic>Central nervous system</topic><topic>Central Nervous System Agents - pharmacokinetics</topic><topic>Coculture Techniques</topic><topic>enantioselectivity</topic><topic>Endothelial Cells - metabolism</topic><topic>membranes</topic><topic>Mice</topic><topic>Microscopy</topic><topic>Peptide Hydrolases - chemistry</topic><topic>Peptides</topic><topic>Peptides - chemical synthesis</topic><topic>Peptides - pharmacokinetics</topic><topic>Permeability</topic><topic>Rats</topic><topic>Receptors</topic><topic>Receptors, Transferrin - drug effects</topic><topic>Stereoisomerism</topic><topic>Transferrin</topic><topic>Transport</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Prades, Roger</creatorcontrib><creatorcontrib>Oller-Salvia, Benjamí</creatorcontrib><creatorcontrib>Schwarzmaier, Susanne M.</creatorcontrib><creatorcontrib>Selva, Javier</creatorcontrib><creatorcontrib>Moros, María</creatorcontrib><creatorcontrib>Balbi, Matilde</creatorcontrib><creatorcontrib>Grazú, Valeria</creatorcontrib><creatorcontrib>de La Fuente, Jesus M.</creatorcontrib><creatorcontrib>Egea, Gustavo</creatorcontrib><creatorcontrib>Plesnila, Nikolaus</creatorcontrib><creatorcontrib>Teixidó, Meritxell</creatorcontrib><creatorcontrib>Giralt, Ernest</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>Nucleic Acids Abstracts</collection><collection>ProQuest Health & Medical Complete (Alumni)</collection><collection>MEDLINE - Academic</collection><collection>Neurosciences Abstracts</collection><collection>Engineered Materials Abstracts</collection><collection>METADEX</collection><collection>Technology Research Database</collection><collection>Materials Research Database</collection><jtitle>Angewandte Chemie International Edition</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Prades, Roger</au><au>Oller-Salvia, Benjamí</au><au>Schwarzmaier, Susanne M.</au><au>Selva, Javier</au><au>Moros, María</au><au>Balbi, Matilde</au><au>Grazú, Valeria</au><au>de La Fuente, Jesus M.</au><au>Egea, Gustavo</au><au>Plesnila, Nikolaus</au><au>Teixidó, Meritxell</au><au>Giralt, Ernest</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Applying the Retro-Enantio Approach To Obtain a Peptide Capable of Overcoming the Blood-Brain Barrier</atitle><jtitle>Angewandte Chemie International Edition</jtitle><addtitle>Angew. 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Jumping hurdles: The retro‐enantio approach has been applied to a peptide that targets the transferrin receptor. The stability and permeability of the peptide across the blood–brain barrier (BBB) were notably increased. This new protease‐resistant peptide was tested as a BBB shuttle, and it does facilitate the transport of cargo across the BBB, both in vitro and in vivo, as demonstrated by intravital microscopy in living mice.</abstract><cop>Weinheim</cop><pub>WILEY-VCH Verlag</pub><pmid>25650865</pmid><doi>10.1002/anie.201411408</doi><tpages>6</tpages><edition>International ed. in English</edition></addata></record> |
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| subjects | Animals Biological Transport Blood Blood-brain barrier Blood-Brain Barrier - metabolism Cattle Central nervous system Central Nervous System Agents - pharmacokinetics Coculture Techniques enantioselectivity Endothelial Cells - metabolism membranes Mice Microscopy Peptide Hydrolases - chemistry Peptides Peptides - chemical synthesis Peptides - pharmacokinetics Permeability Rats Receptors Receptors, Transferrin - drug effects Stereoisomerism Transferrin Transport |
| title | Applying the Retro-Enantio Approach To Obtain a Peptide Capable of Overcoming the Blood-Brain Barrier |
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