Literature DB >> 18164781

The design of guanidinium-rich transporters and their internalization mechanisms.

Paul A Wender1, Wesley C Galliher, Elena A Goun, Lisa R Jones, Thomas H Pillow.   

Abstract

The ability of a drug or probe to cross a biological barrier has historically been viewed to be a function of its intrinsic physical properties. This view has largely restricted drug design and selection to agents within a narrow log P range. Molecular transporters offer a strategy to circumvent these restrictions. In the case of guanidinium-rich transporters (GRTs), a typically highly water-soluble conjugate is found to readily pass through the non-polar membrane of a cell and for some across tissue barriers. This activity opens a field of opportunities for the use of GRTs to enable delivery of polar and non-polar drugs or probes as well as to enhance uptake of those of intermediate polarity. The field of transporter enabled or enhanced uptake has grown dramatically in the last decade. Some GRT drug conjugates have been advanced into clinical trials. This review will provide an overview of recent work pertinent to the design and mechanism of uptake of GRTs.

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Year:  2007        PMID: 18164781      PMCID: PMC2533582          DOI: 10.1016/j.addr.2007.10.016

Source DB:  PubMed          Journal:  Adv Drug Deliv Rev        ISSN: 0169-409X            Impact factor:   15.470


  106 in total

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