Cellular internalization of a cell-penetrating peptide conjugated gastrin-releasing peptide receptor antagonist
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This research aims to develop a gastrin-releasing peptide receptor (GRP-R) antagonist that can internalize into the tumor cells by conjugation a cell-penetrating peptide (CPP) to the GRP-R antagonist RM26. Firstly, the side effects of agonist can be avoided. Secondly, cellular internalization allows longer retention in the tumor cells. After the peptides were radiolabeled with 99mTc, cellular uptake and internalization as well as blocking tests were performed to evaluate the cell-penetrating and targeting property of the CPP-conjugated GRP-R antagonist. This study demonstrates the opportunity to modify antagonists with CCPs to enhance their cellular internalization and therapeutic efficacy.
KeywordsCell-penetrating GRP-R Antagonist Agonist Internalization Peptide
This research is financially supported by Science and Technology Development of Foundation of China Academy of Engineering Physics (2014A0301011) and China National Natural Science Foundation (21571164).
Compliance with ethical standards
Conflict of interest
No conflict of interest exits in this research
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