title: In vitro assessment of the dual-targeting behavior of a peptide-based magnetic resonance imaging contrast agent.
abstract: In this study, a peptide-based dual-targeting magnetic resonance imaging (MRI) contrast agent (S8) was designed and synthesized. Arg-Gly-Asp (RGD) and Asn-Gly-Arg (NGR) were combined in the targeting vector so as to allow binding, on the surface of tumor cells, to integrin αvβ3 and aminopeptidase N (CD13), respectively. The longitudinal relaxivity (r1) value of S8 was 8.297 mM-1sec-1 at a magnetic field of 11.7 T, which is approximately double the r1 value (4.25 mM-1sec-1) of Magnevist, a commercially available contrast agent. MDA-MB-231 human breast cancer cells (which overexpress αvβ3) and human prostate cancer cells PC-3 (which overexpress CD13) were used to investigate the tumor‑targeting behavior of S8. The results from the present study indicate that the designed contrast agent, S8, targets both MDA-MB‑231 and PC-3 cells.
authors.affiliation: School of Chemistry and Chemical Engineering, Huazhong University of Science and Technology, Wuhan, Hubei 430007, P.R. China.
authors.forename: Yuping
authors.initials: Y
authors.lastname: Yang
authors.forename: Kaichao
authors.initials: K
authors.lastname: Yu
authors.forename: Hailu
authors.initials: H
authors.lastname: Zhang
authors.forename: Jianwu
authors.initials: J
authors.lastname: Dai
authors.forename: Zongwu
authors.initials: Z
authors.lastname: Deng
mesh_terms: D001943:Breast Neoplasms; D018826:CD13 Antigens / Q000737:chemistry; D045744:Cell Line, Tumor; D003287:Contrast Media / Q000138:chemical synthesis*; D005260:Female; D006801:Humans; D039302:Integrin alphaVbeta3 / Q000737:chemistry; D008279:Magnetic Resonance Imaging; D008297:Male; D009842:Oligopeptides / Q000737:chemistry*; D011471:Prostatic Neoplasms
chemical_list: D003287:Contrast Media; D039302:Integrin alphaVbeta3; C526428:NGR peptide; D009842:Oligopeptides; C047981:arginyl-glycyl-aspartic acid; D018826:CD13 Antigens