[Updated on Apr. 18] Integration of CiNii Articles into CiNii Research

A Stable and Cleavable <i>O</i>-Linked Spacer for Drug Delivery Systems

  • Ito Kei
    Graduate School of Pharmaceutical Sciences, The University of Tokyo
  • Tatsumi Toshifumi
    Graduate School of Pharmaceutical Sciences, The University of Tokyo
  • Takahashi Kazuki
    Graduate School of Pharmaceutical Sciences, The University of Tokyo
  • Shimizu Yohei
    Graduate School of Pharmaceutical Sciences, The University of Tokyo
  • Yamatsugu Kenzo
    Graduate School of Pharmaceutical Sciences, The University of Tokyo
  • Kanai Motomu
    Graduate School of Pharmaceutical Sciences, The University of Tokyo

Bibliographic Information

Other Title
  • Communications to the Editor : A Stable and Cleavable O-Linked Spacer for Drug Delivery Systems

Search this article

Abstract

<p>Anti-cancer chemotherapy with good efficacy and fewer side effects is highly desirable. A drug delivery system comprising a cancer-targeting module and a cytotoxic agent connected with a cleavable linker is promising for reducing side effects. The development of a cleavable linker satisfying the requirements of both stability and cleavability, however, is difficult, especially when a carbonate moiety is used for conjugating the linker to a hydroxy group in a drug of interest. We herein report a new stable linker comprising carbamate and ester spacers, which can be introduced on a hydroxy group of a drug. This linker is more stable in aqueous neutral buffer than a corresponding carbonate-type linker, and releases a payload anti-cancer drug, SN-38, through a two-step sequence upon cathepsin B treatment. This linker may have potential use in other drug delivery systems to lower side effects by selectively transporting cytotoxic drugs to tumor cells.</p>

Journal

Citations (0)*help

See more

References(23)*help

See more

Related Articles

See more

Related Data

See more

Related Books

See more

Related Dissertations

See more

Related Projects

See more

Related Products

See more

Details

Report a problem

Back to top