Abstract
The transmembrane peptide domains (TMs) of membrane proteins are involved in signal transduction and are crucial for receptor dimerization. Human epidermal growth factor receptor 2 (HER2 or ErbB2) promotes accelerated cancer cell proliferation and survival and is overexpressed in over 20% of all malignancies. We target ErbB2 in a set of ErbB2-positive cancer cell lines by chemically synthesized peptides mimicking the full ErbB2 TM, which inhibited downstream MAPK and PI3K/Akt signaling and drastically reduced cell viability. Loading the ErbB2 TM into surface-active ionic liquid nanocarriers demonstrated a synergic effect on cell viability via cell membrane disruption with simultaneous inhibition of the downstream signaling cascades. Thus, this proof-of-concept study demonstrates TM peptides in conjunction with surface-active ionic liquid carriers as a promising strategy for targeted cancer treatment and broad application, exemplified on ErbB2 receptor as a target here.
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