PT  - JOURNAL ARTICLE
AU  - FRANK UN
AU  - BINGSEN ZHOU
AU  - YUN YEN
TI  - The Utility of Tumor-specifically Internalizing Peptides for Targeted siRNA Delivery into Human Solid Tumors
DP  - 2012 Nov 01
TA  - Anticancer Research
PG  - 4685--4690
VI  - 32
IP  - 11
4099  - http://ar.iiarjournals.org/content/32/11/4685.short
4100  - http://ar.iiarjournals.org/content/32/11/4685.full
SO  - Anticancer Res2012 Nov 01; 32
AB  - Background: Ribonucleotide reductase composed of the hRRM1 and hRRM2 subunits catalyzes the conversion of ribonucleotides to their corresponding deoxy forms for DNA replication. Anti-hRRM2 siRNA degrades hRRM2's mRNA and suppresses tumorigenesis. A Phase I clinical trial demonstrated its therapy potential. HN-1 represents a tumor-specifically internalizing peptide for targeted-drug delivery into human head and neck squamous cell carcinoma. Materials and Methods: Internalization of peptide was monitored by fluorescence microscopy. The peptide-siRNA conjugate was chemically synthesized. The hRRM2 expression was monitored by western blot analysis. Results: HN-1TYR (HN-1 with two N-terminally added tyrosines) was internalized by human head and neck or breast cancer cells. Anti-hRRM2 siRNAR (resistant to RNase degradation) was conjugated to HN-1TYR without compromising their properties. The treatment with HN-1TYR-anti-hRRM2 siRNAR partly suppressed the endogenously expressed hRRM2 in human breast cancer cells. Conclusion: Our results establish the utility of tumor-specifically internalizing peptides for targeted siRNA delivery into human cancer cells.