Design of a doxorubicin-peptidomimetic conjugate that targets HER2-positive cancer cells

详细信息    查看全文

• 作者：Sandeep Pallerla^a ; Ted Gauthier^b ; Rushikesh Sable^a ; Seetharama D. Jois^a ; ^jois@ulm.edu
• 关键词：HER2 ; Lung cancer ; Breast cancer ; Doxorubicin ; Peptidomimetic ; Conjugate
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：5 January 2017
• 年：2017
• 卷：125
• 期：Complete
• 页码：914-924
• 全文大小：1382 K
• 卷排序：125

文摘

A conjugate of DOX-peptidomimetic synthesized was shown to exhibit antiproliferative activity in HER2 positive cancer cells. The peptidomimetic is highly specific for HER2 protein overexpressed cancer cell lines. The conjugate was shown to bind to HER2 protein domain IV by surface plasmon resonance. The conjugate binds to HER2 positive cancer cells and doxorubicin internalizes after 4 h as shown by confocal microscopy.