Enhanced biological activity of antisense oligonucleotides complexed with glycosylated poly-L-lysine.
Identifieur interne : 002966 ( Main/Exploration ); précédent : 002965; suivant : 002967Enhanced biological activity of antisense oligonucleotides complexed with glycosylated poly-L-lysine.
Auteurs : A. Stewart ; Chantal Pichon [France] ; L. Meunier ; P. Midoux [France] ; M. Monsigny [France] ; A. Roche [France]Source :
- Molecular Pharmacology [ 0026-895X ] ; 1996-12.
Abstract
We sought to exploit glycosylated poly-L-lysine (pLK) to increase the uptake and biological antisense activity of a phosphorothioate oligonucleotide (pt-odn) [pt-odn complementary to the 3' noncoding region of intercellular adhesion molecule-1 (ICAM-1) (odn(ICAM-1))] complementary to the 3'-noncoding region of ICAM-1 in A549 cells. Dose-dependent inhibition of ICAM-1 expression was obtained (IC50 = 500 nM) through treatment of cells with odn(ICAM-1) complexed with pLK carrying fucose residues in the presence of 100 microM chloroquine. Alteration in the charge ratio between fucosylated pLK and pt-odn had a significant effect on the efficacy of inhibition (optimal conditions, charge ratio = 1.1). This effect was also dependent on the number of fucose moieties per pLK. Free pt-odn or pt-odn complexed with nonglycosylated pLK gave no inhibition at concentrations of < or = 2 microM. Two control pt-odn (one was targeted against an unrelated gene not present in these cells, gag(HIV), and the other had a randomized sequence) gave no inhibition of ICAM-1 expression in the presence or absence of pLK carrying fucose residues at concentrations of < or = 2 microM. When complexed with pLK carrying 100 fucose residues, the amount of cell-associated pt-odn was increased by 15-fold compared with the free pt-odn. Nongycosylated pLK also increased the amount of cell-associated pt-odn by >10 fold but did not alter the biological activity. These results demonstrate clearly the potential of glycosylated pLK as a pt-odn transporter.
Url:
Affiliations:
- France
- Centre-Val de Loire, Région Centre
- Orléans
- Centre Val de Loire Université, Université d'Orléans
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Le document en format XML
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Stewart</name></author><author><name sortKey="Pichon, Chantal" sort="Pichon, Chantal" uniqKey="Pichon C" first="Chantal" last="Pichon">Chantal Pichon</name><affiliation wicri:level="1"><hal:affiliation type="laboratory" xml:id="struct-451" status="VALID"> <idno type="IdRef">170121070</idno> <idno type="RNSR">196717612S</idno> <orgName>Centre de biophysique moléculaire</orgName> <orgName type="acronym">CBM</orgName> <date type="start">1967-01-01</date> <desc> <address> <addrLine>Rue Charles Sadron 45071 ORLEANS CEDEX 2</addrLine> <country key="FR"></country> </address> <ref type="url">http://cbm.cnrs-orleans.fr/</ref> </desc> <listRelation> <relation name="UPR4301" active="#struct-300297" type="direct"></relation> <relation name="UPR4301" active="#struct-303623" type="direct"></relation> <relation name="UPR4301" active="#struct-441569" type="direct"></relation> </listRelation> <tutelles><tutelle name="UPR4301" active="#struct-300297" type="direct"><org type="institution" xml:id="struct-300297" status="VALID"> <idno type="IdRef">026402971</idno> <idno type="ISNI">0000000121581666 </idno> <orgName>Université d'Orléans</orgName> <orgName type="acronym">UO</orgName> <desc> <address> <addrLine>Château de la Source - Avenue du Parc Floral - BP 6749 - 45067 Orléans cedex 2</addrLine> <country key="FR"></country> </address> <ref type="url">http://www.univ-orleans.fr/</ref> </desc> </org></tutelle><tutelle name="UPR4301" active="#struct-303623" type="direct"><org type="institution" xml:id="struct-303623" status="VALID"> <idno type="IdRef">026388278</idno> <orgName>Institut National de la Santé et de la Recherche Médicale</orgName> <orgName type="acronym">INSERM</orgName> <desc> <address> <addrLine>101, rue de Tolbiac, 75013 Paris </addrLine> <country key="FR"></country> </address> <ref type="url">http://www.inserm.fr</ref> </desc> </org></tutelle><tutelle name="UPR4301" active="#struct-441569" type="direct"><org type="institution" xml:id="struct-441569" status="VALID"> <idno type="IdRef">02636817X</idno> <idno type="ISNI">0000000122597504</idno> <orgName>Centre National de la Recherche Scientifique</orgName> <orgName type="acronym">CNRS</orgName> <date type="start">1939-10-19</date> <desc> <address> <country key="FR"></country> </address> <ref type="url">http://www.cnrs.fr/</ref> </desc> </org></tutelle></tutelles></hal:affiliation><country>France</country><placeName><settlement type="city">Orléans</settlement><region type="old region" nuts="2">Région Centre</region><region type="region" nuts="2">Centre-Val de Loire</region></placeName><orgName type="university">Université d'Orléans</orgName><orgName type="institution" wicri:auto="newGroup">Centre Val de Loire Université</orgName></affiliation></author><author><name sortKey="Meunier, L" sort="Meunier, L" uniqKey="Meunier L" first="L" last="Meunier">L. 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Monsigny</name><affiliation wicri:level="1"><hal:affiliation type="laboratory" xml:id="struct-451" status="VALID"> <idno type="IdRef">170121070</idno> <idno type="RNSR">196717612S</idno> <orgName>Centre de biophysique moléculaire</orgName> <orgName type="acronym">CBM</orgName> <date type="start">1967-01-01</date> <desc> <address> <addrLine>Rue Charles Sadron 45071 ORLEANS CEDEX 2</addrLine> <country key="FR"></country> </address> <ref type="url">http://cbm.cnrs-orleans.fr/</ref> </desc> <listRelation> <relation name="UPR4301" active="#struct-300297" type="direct"></relation> <relation name="UPR4301" active="#struct-303623" type="direct"></relation> <relation name="UPR4301" active="#struct-441569" type="direct"></relation> </listRelation> <tutelles><tutelle name="UPR4301" active="#struct-300297" type="direct"><org type="institution" xml:id="struct-300297" status="VALID"> <idno type="IdRef">026402971</idno> <idno type="ISNI">0000000121581666 </idno> <orgName>Université d'Orléans</orgName> <orgName type="acronym">UO</orgName> <desc> <address> <addrLine>Château de la Source - Avenue du Parc Floral - BP 6749 - 45067 Orléans cedex 2</addrLine> <country key="FR"></country> </address> <ref type="url">http://www.univ-orleans.fr/</ref> </desc> </org></tutelle><tutelle name="UPR4301" active="#struct-303623" type="direct"><org type="institution" xml:id="struct-303623" status="VALID"> <idno type="IdRef">026388278</idno> <orgName>Institut National de la Santé et de la Recherche Médicale</orgName> <orgName type="acronym">INSERM</orgName> <desc> <address> <addrLine>101, rue de Tolbiac, 75013 Paris </addrLine> <country key="FR"></country> </address> <ref type="url">http://www.inserm.fr</ref> </desc> </org></tutelle><tutelle name="UPR4301" active="#struct-441569" type="direct"><org type="institution" xml:id="struct-441569" status="VALID"> <idno type="IdRef">02636817X</idno> <idno type="ISNI">0000000122597504</idno> <orgName>Centre National de la Recherche Scientifique</orgName> <orgName type="acronym">CNRS</orgName> <date type="start">1939-10-19</date> <desc> <address> <country key="FR"></country> </address> <ref type="url">http://www.cnrs.fr/</ref> </desc> </org></tutelle></tutelles></hal:affiliation><country>France</country><placeName><settlement type="city">Orléans</settlement><region type="old region" nuts="2">Région Centre</region><region type="region" nuts="2">Centre-Val de Loire</region></placeName><orgName type="university">Université d'Orléans</orgName><orgName type="institution" wicri:auto="newGroup">Centre Val de Loire Université</orgName></affiliation></author><author><name sortKey="Roche, A" sort="Roche, A" uniqKey="Roche A" first="A." last="Roche">A. Roche</name><affiliation wicri:level="1"><hal:affiliation type="laboratory" xml:id="struct-451" status="VALID"> <idno type="IdRef">170121070</idno> <idno type="RNSR">196717612S</idno> <orgName>Centre de biophysique moléculaire</orgName> <orgName type="acronym">CBM</orgName> <date type="start">1967-01-01</date> <desc> <address> <addrLine>Rue Charles Sadron 45071 ORLEANS CEDEX 2</addrLine> <country key="FR"></country> </address> <ref type="url">http://cbm.cnrs-orleans.fr/</ref> </desc> <listRelation> <relation name="UPR4301" active="#struct-300297" type="direct"></relation> <relation name="UPR4301" active="#struct-303623" type="direct"></relation> <relation name="UPR4301" active="#struct-441569" type="direct"></relation> </listRelation> <tutelles><tutelle name="UPR4301" active="#struct-300297" type="direct"><org type="institution" xml:id="struct-300297" status="VALID"> <idno type="IdRef">026402971</idno> <idno type="ISNI">0000000121581666 </idno> <orgName>Université d'Orléans</orgName> <orgName type="acronym">UO</orgName> <desc> <address> <addrLine>Château de la Source - Avenue du Parc Floral - BP 6749 - 45067 Orléans cedex 2</addrLine> <country key="FR"></country> </address> <ref type="url">http://www.univ-orleans.fr/</ref> </desc> </org></tutelle><tutelle name="UPR4301" active="#struct-303623" type="direct"><org type="institution" xml:id="struct-303623" status="VALID"> <idno type="IdRef">026388278</idno> <orgName>Institut National de la Santé et de la Recherche Médicale</orgName> <orgName type="acronym">INSERM</orgName> <desc> <address> <addrLine>101, rue de Tolbiac, 75013 Paris </addrLine> <country key="FR"></country> </address> <ref type="url">http://www.inserm.fr</ref> </desc> </org></tutelle><tutelle name="UPR4301" active="#struct-441569" type="direct"><org type="institution" xml:id="struct-441569" status="VALID"> <idno type="IdRef">02636817X</idno> <idno type="ISNI">0000000122597504</idno> <orgName>Centre National de la Recherche Scientifique</orgName> <orgName type="acronym">CNRS</orgName> <date type="start">1939-10-19</date> <desc> <address> <country key="FR"></country> </address> <ref type="url">http://www.cnrs.fr/</ref> </desc> </org></tutelle></tutelles></hal:affiliation><country>France</country><placeName><settlement type="city">Orléans</settlement><region type="old region" nuts="2">Région Centre</region><region type="region" nuts="2">Centre-Val de Loire</region></placeName><orgName type="university">Université d'Orléans</orgName><orgName type="institution" wicri:auto="newGroup">Centre Val de Loire Université</orgName></affiliation></author></analytic><series><title level="j">Molecular Pharmacology</title><idno type="ISSN">0026-895X</idno><imprint><date type="datePub">1996-12</date></imprint></series></biblStruct></sourceDesc></fileDesc><profileDesc><textClass></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en"> <p>We sought to exploit glycosylated poly-L-lysine (pLK) to increase the uptake and biological antisense activity of a phosphorothioate oligonucleotide (pt-odn) [pt-odn complementary to the 3' noncoding region of intercellular adhesion molecule-1 (ICAM-1) (odn(ICAM-1))] complementary to the 3'-noncoding region of ICAM-1 in A549 cells. Dose-dependent inhibition of ICAM-1 expression was obtained (IC50 = 500 nM) through treatment of cells with odn(ICAM-1) complexed with pLK carrying fucose residues in the presence of 100 microM chloroquine. Alteration in the charge ratio between fucosylated pLK and pt-odn had a significant effect on the efficacy of inhibition (optimal conditions, charge ratio = 1.1). This effect was also dependent on the number of fucose moieties per pLK. Free pt-odn or pt-odn complexed with nonglycosylated pLK gave no inhibition at concentrations of < or = 2 microM. Two control pt-odn (one was targeted against an unrelated gene not present in these cells, gag(HIV), and the other had a randomized sequence) gave no inhibition of ICAM-1 expression in the presence or absence of pLK carrying fucose residues at concentrations of < or = 2 microM. When complexed with pLK carrying 100 fucose residues, the amount of cell-associated pt-odn was increased by 15-fold compared with the free pt-odn. Nongycosylated pLK also increased the amount of cell-associated pt-odn by >10 fold but did not alter the biological activity. These results demonstrate clearly the potential of glycosylated pLK as a pt-odn transporter.</p> </div></front></TEI><affiliations><list><country><li>France</li></country><region><li>Centre-Val de Loire</li><li>Région Centre</li></region><settlement><li>Orléans</li></settlement><orgName><li>Centre Val de Loire Université</li><li>Université d'Orléans</li></orgName></list><tree><noCountry><name sortKey="Meunier, L" sort="Meunier, L" uniqKey="Meunier L" first="L" last="Meunier">L. Meunier</name><name sortKey="Stewart, A" sort="Stewart, A" uniqKey="Stewart A" first="A." last="Stewart">A. Stewart</name></noCountry><country name="France"><region name="Région Centre"><name sortKey="Pichon, Chantal" sort="Pichon, Chantal" uniqKey="Pichon C" first="Chantal" last="Pichon">Chantal Pichon</name></region><name sortKey="Midoux, P" sort="Midoux, P" uniqKey="Midoux P" first="P" last="Midoux">P. Midoux</name><name sortKey="Monsigny, M" sort="Monsigny, M" uniqKey="Monsigny M" first="M." last="Monsigny">M. Monsigny</name><name sortKey="Roche, A" sort="Roche, A" uniqKey="Roche A" first="A." last="Roche">A. Roche</name></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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