@article{oai:nagasaki-u.repo.nii.ac.jp:00001339, author = {Wang, Wei and Suga, Tadaharu and Hagimori, Masayori and Kuroda, Naotaka and Fuchigami, Yuki and Kawakami, Shigeru}, issue = {9}, journal = {Biological and Pharmaceutical Bulletin}, month = {Sep}, note = {Oligoarginines (Rn) are becoming promising tools for the intracellular delivery of biologically active molecules. NuBCP-9, a peptide that induces apoptosis in B-cell lymphoma 2 (Bcl-2)-expressing cancer cells, has been reported to promote the uptake and non-specific cytotoxicity of R8, also called octaarginine. However, it is unknown whether a similar synergistic effect can be seen with other Rn. In this study, we conjugated NuBCP-9 with various Rn (n=8, 10, 12, 14) to investigate and compare their cellular uptake characteristics. In addition, their non-specific cytotoxicity and apoptosis-inducing abilities were evaluated. We found that NuBCP-9 conjugated with Rn enhanced cellular uptake mainly through clathrin-mediated endocytosis and macropinocytosis, and that the uptake pathways were not different from those used by unconjugated Rn. However, the cytotoxicity study showed that NuBCP-9-R12 and NuBCP-9-R14 conjugates enhanced nonspecific cytotoxicity. We found that NuBCP-9-R10 conjugate had the highest uptake efficiency and induced correspondingly high levels of apoptosis, while resulting in a tolerable degree of non-specific toxicity., Biological and Pharmaceutical Bulletin, 41(9), pp.1448-1455; 2018}, pages = {1448--1455}, title = {Investigation of Intracellular Delivery of NuBCP-9 by Conjugation with Oligoarginines Peptides in MDA-MB-231 Cells}, volume = {41}, year = {2018} }