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  • Peptide density targets and impedes triple negative breast cancer metastasis.

Peptide density targets and impedes triple negative breast cancer metastasis.

Nature communications (2018-07-06)
Daxing Liu, Peng Guo, Craig McCarthy, Biran Wang, Yu Tao, Debra Auguste
ABSTRACT

The C-X-C chemokine receptor type 4 (CXCR4, CD184) pathway is a key regulator of cancer metastasis. Existing therapeutics that block CXCR4 signaling are dependent on single molecule-receptor interactions or silencing CXCR4 expression. CXCR4 localizes in lipid rafts and forms dimers therefore CXCR4 targeting and signaling may depend on ligand density. Herein, we report liposomes presenting a CXCR4 binding peptide (DV1) as a three-dimensional molecular array, ranging from 9k to 74k molecules μm-2, target triple negative breast cancer (TNBC). TNBC cells exhibit a maxima in binding and uptake of DV1-functionalized liposomes (L-DV1) in vitro at a specific density, which yields a significant reduction in cell migration. This density inhibits metastasis from a primary tumor for 27 days, resulting from peptide density dependent gene regulation. We show that complementing cell membrane receptor expression may be a strategy for targeting cells and regulating signaling.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Creatine Kinase Activity Assay Kit, sufficient for 100 tests (Ultraviolet)
Sigma-Aldrich
NanoFabTx - Azide Lipid Mix, for synthesis of azide-functionalized liposomes