Targeting protein and peptide therapeutics to the heart via tannic acid modification View Full Text


Ontology type: schema:ScholarlyArticle     


Article Info

DATE

2018-05

AUTHORS

Mikyung Shin, Hyang-Ae Lee, Mihyun Lee, Yoomi Shin, Ji-Joon Song, Sun-Woong Kang, Dae-Hwan Nam, Eun Je Jeon, Mira Cho, Minjae Do, SunHyun Park, Moon Sue Lee, Jae-Hyung Jang, Seung-Woo Cho, Ki-Suk Kim, Haeshin Lee

ABSTRACT

Systemic injection into blood vessels is the most common method of drug administration. However, targeting drugs to the heart is challenging, owing to its dynamic mechanical motions and large cardiac output. Here, we show that the modification of protein and peptide therapeutics with tannic acid-a flavonoid found in plants that adheres to extracellular matrices, elastins and collagens-improves their ability to specifically target heart tissue. Tannic-acid-modified (TANNylated) proteins do not adsorb on endothelial glycocalyx layers in blood vessels, yet they penetrate the endothelium to thermodynamically bind to myocardium extracellular matrix before being internalized by myoblasts. In a rat model of myocardial ischaemia-reperfusion injury, TANNylated basic fibroblast growth factor significantly reduced infarct size and increased cardiac function. TANNylation of systemically injected therapeutic proteins, peptides or viruses may enhance the treatment of heart diseases. More... »

PAGES

304-317

Identifiers

URI

http://scigraph.springernature.com/pub.10.1038/s41551-018-0227-9

DOI

http://dx.doi.org/10.1038/s41551-018-0227-9

DIMENSIONS

https://app.dimensions.ai/details/publication/pub.1103690999

PUBMED

https://www.ncbi.nlm.nih.gov/pubmed/30936449


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