Binding and transport of PAMAM-RGD in a tumor spheroid model: the effect of RGD targeting ligand density.
Binding and transport of PAMAM-RGD in a tumor spheroid model: the effect of RGD targeting ligand density.
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PAMAM-RGD在肿瘤球体模型中的结合和转运：RGD靶向配体密度的影响。
DOI：
10.1002/bit.23255
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发表时间：
2011-12
影响因子：
3.8
通讯作者：
Roth, Charles M.
中科院分区：
文献类型：
--
作者：
Waite, Carolyn L.;Roth, Charles M.
在这项工作中，有效的肿瘤球状体的渗透和运输的机制进行了评估，显示不同数量的环状RGD靶向肽（2，3，7，或10）的聚（酰胺胺）（PAMAM）树枝状大分子。实验测定PAMAM-RGD缀合物与恶性胶质瘤细胞的无细胞结合亲和力和细胞内化动力学，并将结果纳入数学模型以预测这些材料通过多细胞肿瘤球体的运输。理论分析表明，更大的RGD交联可能会改善运输通过肿瘤球体，由于其降低整合素结合亲和力。这项研究提供的证据表明，改变药物递送平台的肿瘤靶向配体的密度是优化抗癌剂的肿瘤渗透效率的可行方法，并提供了对这些缀合物的相对有效性的物理化学机制的见解。
The mechanisms governing the efficient tumor spheroid penetration and transport by poly(amidoamine) (PAMAM) dendrimers displaying varying numbers of cyclic RGD targeting peptides (2, 3, 7, or 10) were evaluated in this work. The cell-free binding affinities and cellular internalization kinetics of PAMAM-RGD conjugates to malignant glioma cells were determined experimentally, and the results were incorporated into a mathematical model to predict the transport of these materials through a multicellular tumor spheroid. The theoretical analysis demonstrated that greater RGD crosslinking may improve transport through tumor spheroids due to their decreased integrin-binding affinity. This study provides evidence that altering the density of tumor-targeting ligands from a drug delivery platform is a feasible way to optimize the tumor-penetration efficiency of an anticancer agent, and provides insight into the physicochemical mechanisms governing the relative effectiveness of these conjugates.
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影响因子：
4.7
作者：
Liu S
通讯作者：
Liu S
影响因子：
4.4
作者：
Kostarelos, K;Emfietzoglou, D;Sgouros, G
通讯作者：
Sgouros, G
DOI：
10.1073/pnas.92.19.8999
发表时间：
1995-09-12
影响因子：
11.1
作者：
SAGA, T;NEUMANN, RD;WEINSTEIN, JN
通讯作者：
WEINSTEIN, JN
影响因子：
10.8
作者：
Han, Muri;Bae, Younsoo;Kataoka, Kazurlori
通讯作者：
Kataoka, Kazurlori
影响因子：
7.3
作者：
Montet, Xavier;Funovics, Martin;Josephson, Lee
通讯作者：
Josephson, Lee