Kang, Rae Hyung Jang, Jeong-Eun Huh, Eugene Kang, Seong Jae Ahn, Dae-Ro Kang, Jae Seung Sailor, Michael J. Yeo, Seung Geun Oh, Myung Sook Kim, Dokyoung Kim, Hyo Young 2024-01-19T17:01:23Z 2024-01-19T17:01:23Z 2021-09-02 2020-08-01 2055-6756 https://pubs.kist.re.kr/handle/201004/118278 Organ-specific cell-penetrating peptides (CPPs) are a class of molecules that can be highly effective at delivering therapeutic cargoes, and they are currently of great interest in cancer treatment strategies. Herein, we describe a new CPP (amino acid sequence serine-isoleucine-tyrosine-valine, or SIWV) that homes to glioblastoma multiforme (GBM) brain tumor tissues with remarkable specificity in vitro and in vivo. The SIWV sequence was identified from an isoform of annexin-A3 (AA3H), a membrane-interacting human protein. The mechanism of intracellular permeation is proposed to follow a caveolin-mediated endocytotic pathway, based on in vitro and in vivo receptor inhibition and genetic knockdown studies. Feasibility as a targeting agent for therapeutics is demonstrated in a GBM xenograft mouse model, where porous silicon nanoparticles (pSiNPs) containing the clinically relevant anticancer drug SN-38 are grafted with SIWV via a poly-(ethylene glycol) (PEG) linker. The formulation shows enhanced in vivo targeting ability relative to a formulation employing a scrambled control peptide, and significant (P < 0.05) therapeutic efficacy relative to free SN-38 in the GBM xenograft animal model. English ROYAL SOC CHEMISTRY CELL-PENETRATING PEPTIDES POROUS SILICON NANOPARTICLES INHIBITORS INFECTION PATHWAYS A brain tumor-homing tetra-peptide delivers a nano-therapeutic for more effective treatment of a mouse model of glioblastoma Article 10.1039/d0nh00077a 1 NANOSCALE HORIZONS, v.5, no.8, pp.1213 - 1225 NANOSCALE HORIZONS 5 8 1213 1225 scie scopus 000553030400013 2-s2.0-85088680104 Chemistry, Physical Nanoscience & Nanotechnology Materials Science, Multidisciplinary Chemistry Science & Technology - Other Topics Materials Science Article CELL-PENETRATING PEPTIDES POROUS SILICON NANOPARTICLES INHIBITORS INFECTION PATHWAYS