2. Academic Validation
  3. Lipid-peptide bioconjugation through pyridyl disulfide reaction chemistry and its application in cell targeting and drug delivery

Lipid-peptide bioconjugation through pyridyl disulfide reaction chemistry and its application in cell targeting and drug delivery

  • J Nanobiotechnology. 2019 Jun 21;17(1):77. doi: 10.1186/s12951-019-0509-8.
Diego de la Fuente-Herreruela 1 2,  Ajay K Monnappa 3,  Mónica Muñoz-Úbeda 2,  Aarón Morallón-Piña 1,  Eduardo Enciso 1,  Luis Sánchez 4,  Fabrice Giusti 5,  Paolo Natale 1 2,  Iván López-Montero 6 7
Affiliations

Affiliations

  • 1 Dto. Química Física, Universidad Complutense de Madrid, Avenida Complutense s/n, 28040, Madrid, Spain.
  • 2 Instituto de Investigación Hospital Doce de Octubre (i+12), Avenida de Córdoba s/n, 28041, Madrid, Spain.
  • 3 Department of Biological Sciences, School of Life Sciences, Ulsan National Institute of Science and Technology (UNIST), Ulsan, 689-798, Republic of Korea.
  • 4 Dto. Química Orgánica, Universidad Complutense de Madrid, Avenida Complutense s/n, 28040, Madrid, Spain.
  • 5 Institut de Chimie Séparative de Marcoule, ICSM, UMR 5257, Site de Marcoule-Bât, 426 BP 17 171, 30207, Bagnols sur Ceze, France.
  • 6 Dto. Química Física, Universidad Complutense de Madrid, Avenida Complutense s/n, 28040, Madrid, Spain. ivanlopez@quim.ucm.es.
  • 7 Instituto de Investigación Hospital Doce de Octubre (i+12), Avenida de Córdoba s/n, 28041, Madrid, Spain. ivanlopez@quim.ucm.es.
PMID: 31226993 DOI: 10.1186/s12951-019-0509-8
Abstract

Background: The design of efficient drug delivery vectors requires versatile formulations able to simultaneously direct a multitude of molecular targets and to bypass the endosomal recycling pathway of cells. Liposomal-based vectors need the decoration of the lipid surface with specific peptides to fulfill the functional requirements. The unspecific binding of peptides to the lipid surface is often accompanied with uncontrolled formulations and thus preventing the molecular mechanisms of a successful therapy.

Results: We present a simple synthesis pathway to anchor cysteine-terminal peptides to thiol-reactive lipids for adequate and quantitative liposomal formulations. As a proof of concept, we have synthesized two different lipopeptides based on (a) the truncated Fibroblast Growth Factor (tbFGF) for cell targeting and (b) the pH sensitive and fusogenic GALA peptide for endosomal scape.

Conclusions: The incorporation of these two lipopeptides in the liposomal formulation improves the fibroblast cell targeting and promotes the direct delivery of cargo molecules to the cytoplasm of the cell.

Keywords

Disulfide bonds; Endosomal escape; GALA; Smart liposomes; Targeting peptide.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-P5423C
    Cys修饰GALA肽
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