2. Academic Validation
  3. Synthesis and Biological Evaluation of a Biotinylated Paclitaxel With an Extra-Long Chain Spacer Arm

Synthesis and Biological Evaluation of a Biotinylated Paclitaxel With an Extra-Long Chain Spacer Arm

  • ACS Med Chem Lett. 2012 Sep 13;3(9):745-748. doi: 10.1021/ml300149z.
Lev G Lis 1,  Mary A Smart,  Anna Luchniak,  Mohan L Gupta Jr,  Vadim J Gurvich
Affiliations

Affiliation

  • 1 Institute for Therapeutics Discovery and Development and Department of Medicinal Chemistry, University of Minnesota, Minneapolis, Minnesota 55414, United States.
PMID: 23259031 DOI: 10.1021/ml300149z
Abstract

A biotinylated paclitaxel derivative with an extra-long-chain (LC-LC-Biotin) spacer arm was synthesized using an improved synthetic reaction sequence. The biotinylated paclitaxel analogue retained excellent microtubule stabilizing activity in vitro. Furthermore, it was shown that this analogue can simultaneously engage streptavidin and the binding site on microtubules, making it suitable for localization studies or for the attachment of paclitaxel to solid substrates via a streptavidin linkage.

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