Quantity and accessibility for specific targeting of receptors in tumours.
Quantity and accessibility for specific targeting of receptors in tumours.
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DOI：
10.1038/srep05232
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发表时间：
2014-06-10
影响因子：
4.6
通讯作者：
Ruoslahti E
中科院分区：
文献类型：
--
作者：
Hussain S;Rodriguez-Fernandez M;Braun GB;Doyle FJ 3rd;Ruoslahti E
Synaphic (ligand-directed) targeting of drugs is an important potential new approach to drug delivery, particularly in oncology. Considerable success with this approach has been achieved in the treatment of blood-borne cancers, but the advances with solid tumours have been modest. Here, we have studied the number and availability for ligand binding of the receptors for two targeting ligands. The results show that both paucity of total receptors and their poor availability are major bottlenecks in drug targeting. A tumour-penetrating peptide greatly increases the availability of receptors by promoting transport of the drug to the extravascular tumour tissue, but the number of available receptors still remains low, severely limiting the utility of the approach. Our results emphasize the importance of using drugs with high specific activity to avoid exceeding receptor capacity because any excess drug conjugate would lose the targeting advantage. The mathematical models we describe make it possible to focus on those aspects of the targeting mechanism that are most likely to have a substantial effect on the overall efficacy of the targeting.
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DOI：
10.1083/jcb.200910104
发表时间：
2010-03-22
期刊：
The Journal of cell biology
影响因子：
--
作者：
Ruoslahti E;Bhatia SN;Sailor MJ
通讯作者：
Sailor MJ
影响因子：
10.3
作者：
Dreher, MR;Liu, WG;Chilkoti, A
通讯作者：
Chilkoti, A
影响因子：
--
作者：
Shi, Yining;Huang, Weidong;Winslow, John
通讯作者：
Winslow, John
影响因子：
3.4
作者：
Strassberger, Verena;Truessel, Sabrina;Roesli, Christoph
通讯作者：
Roesli, Christoph
影响因子：
3.1
作者：
WU, NZ;KLITZMAN, B;DEWHIRST, MW
通讯作者：
DEWHIRST, MW