On guanidinium and cellular uptake.

On guanidinium and cellular uptake.
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DOI:
10.1021/jo501101s
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发表时间:
2014-08-01
期刊:
The Journal of organic chemistry
影响因子:
--
通讯作者:
Tor Y
Tor Y
中科院分区:
其他
文献类型:
--
作者:
Wexselblatt E;Esko JD;Tor Y

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富含胍的支架有助于细胞移位和生物活性物质通过生物屏障的递送。虽然在细胞培养和动物模型中已经证明了非寡聚体和非pept(o)胍基化支架的显著吸收,但缺乏对这些过程的基本理解。已经提出了与细胞表面对应物的电荷配对和氢键,但它们的确切作用仍然是假定的。胍基的数量和空间关系对递送和细胞器/器官定位的影响尚未确定。
Guanidinium-rich scaffolds facilitate cellular translocation and delivery of bioactive cargos through biological barriers. Although impressive uptake has been demonstrated for nonoligomeric and nonpept(o)idic guanidinylated scaffolds in cell cultures and animal models, the fundamental understanding of these processes is lacking. Charge pairing and hydrogen bonding with cell surface counterparts have been proposed, but their exact role remains putative. The impact of the number and spatial relationships of the guanidinium groups on delivery and organelle/organ localization is yet to be established.
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