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Uptake of of branched polypeptides with poly[L-Lys] backbone by bone-marrow derived murine macrophages: The role of the class A scavenger |
Tartalom: | http://real.mtak.hu/3490/ |
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Archívum: | MTA Könyvtár |
Gyűjtemény: |
Status = Published
Type = Article |
Cím: |
Uptake of of branched polypeptides with poly[L-Lys] backbone by bone-marrow derived murine macrophages: The role of the class A scavenger
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Létrehozó: |
Peiser, Leanne
Heinsbroek, Sigrid
Gordon, Siamon
Hudecz, Ferenc
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Kiadó: |
American Chemical Society
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Dátum: |
2005
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Tartalmi leírás: |
Selective delivery of antiparasitic or antibacterial drugs into infected macrophages could be a promising approach for improved therapies. Methotrexate conjugate with branched chain polypeptides exhibited pronounced anti-Leishmania activity in vitro and in vivo as reported here earlier. To identify structural requirements for efficient uptake of branched polypeptides, we have studied murine bone marrow
culture-derived macrophages (BMMphi) from 129/ICR mice. We report on the translocation characteristics of structurally closely related compounds labeled with 5(6)- carboxyfluorescein. We found that this process is dependent on experimental conditions (e.g. polypeptide concentration, incubation time, and temperature). Using specific inhibitors as well as macrophages from wild-type and class-A scavenger receptor knockout (SR-A -/-) mice, we demonstrated that SR-A was involved in the endocytosis of some polypeptides depending on their charge. Uptake could be blocked by unlabeled polypeptide, by SR-A inhibitors, and by specific anti-SR-A monoclonal antibody. The polyanionic polypeptide poly[Lys(Succ-Glu1.0-DL-Ala3.8)] (SuccEAK) with high charge density translocated more efficiently than poly[Lys(Ac-Glu1.0-DL-Ala3.8)] (AcEAK), which had a lower anionic charge density. On the basis of experimental data presented, SuccEAK can be considered as a potential candidate for the design of a macromolecular carrier for specific drug delivery of bioactive entities into macrophages via SR-A. |
Nyelv: |
magyar
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Típus: |
Article
PeerReviewed
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Formátum: |
application/pdf
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Azonosító: | |
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