Synlett 2017; 28(15): 1897-1900
DOI: 10.1055/s-0036-1588807
© Georg Thieme Verlag Stuttgart · New York

Lipid–Cell-Penetrating-Peptide Conjugates as Effective Delivery Systems

Yan-Hong Jianga, Hui Zhaoa, Yuan Tianb, Zi-Gang Li*a
  • aSchool of Chemical Biology and Biotechnology, Peking University Shenzhen Graduate School, Shenzhen, 518055, P. R. of China
  • bSchool of Life Science and Engineering, Southwest Jiaotong University, Chengdu, 611756, P. R. of China   Email:
Supported by: National Natural Science Foundation of China (21102007, 21372023)
Supported by: MOST (2015DFA31590)
Supported by: Shenzhen Science and Technology Innovation Committee (SW201110018, SGLH20120928095602764, ZDSY20130331145112855, JSGG20140519105550503)
Supported by: Shenzhen Peacock Program (KQTD201103)
Further Information

Publication History

Received: 18 February 2017

Accepted after revision: 02 April 2017

Publication Date:
20 April 2017 (eFirst)

Published as part of the Cluster Recent Advances in Protein and Peptide Synthesis


A lipid–cell-penetrating-peptide (CPP) conjugate was designed to deliver cargoes with poor cellular permeability, including peptides or small-molecule therapeutics, into cells. The lipid–CPP conjugate facilitated the cellular uptake of cargoes noncovalently through an ATP-dependent micropinocytosis mechanism. This delivery system is simple, efficient, has minimal cellular toxicity, and might be useful in a wide range of biological research.

Supporting Information