Synthesis of an Uncharged Tetra-cyclopeptide Acting as a Transmembrane Carrier: Enhanced Cellular and Nuclear Uptake

Org Lett. 2017 Feb 3;19(3):612-615. doi: 10.1021/acs.orglett.6b03776. Epub 2017 Jan 20.


A small uncharged cyclopeptide scaffold inspired by a natural product and designed to undergo postfunctionalizations was used as a new transmembrane vector. A bioactive and fluorescent triazole aminocoumarin was bound to this carrier to facilitate its moving across cell and subcellular membranes, and this led to an increase in its cell toxicity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Membrane
  • Molecular Structure
  • Peptides, Cyclic / chemistry*


  • Peptides, Cyclic