title: Imaging human melanoma using a novel Tc-99m-labeled lactam bridge-cyclized alpha-MSH peptide.
abstract: In this study, the human melanoma targeting property of (99m)Tc(EDDA)-HYNIC-AocNle-CycMSHhex {hydrazinonicotinamide-8-aminooctanoic acid-Nle-c[Asp-His-DPhe-Arg-Trp-Lys]-CONH2} was determined in M21 human melanoma-xenografts to demonstrate its potential for human melanoma imaging. The IC50 value of HYNIC-AocNle-CycMSHhex was 0.48±0.01nM in M21 human melanoma cells (1281receptors/cell). The M21 human melanoma uptake of (99m)Tc(EDDA)-HYNIC-AocNle-CycMSHhex was 4.03±1.25, 3.26±1.23 and 3.36±1.48%ID/g at 0.5, 2 and 4h post-injection, respectively. Approximately 92% of injected dose cleared out the body via urinary system at 2h post-injection. (99m)Tc(EDDA)-HYNIC-AocNle-CycMSHhex showed high tumor/blood, tumor/muscle and tumor/skin uptake ratios after 2h post-injection. The M21 human melanoma-xenografted tumor lesions were clearly visualized by SPECT/CT using (99m)Tc(EDDA)-HYNIC-AocNle-CycMSHhex as an imaging probe at 2h post-injection. Overall, (99m)Tc(EDDA)-HYNIC-AocNle-CycMSHhex exhibited favorable human melanoma imaging property, highlighting its potential as an imaging probe for human metastatic melanoma detection.
authors: School of Chemistry and Biological Engineering, University of Science and Technology Beijing, Beijing 100083, PR China.
authors: Liqin
authors: L
authors: Liu
authors: Department of Radiology, School of Medicine, University of Colorado Denver, Aurora, CO 80045, USA.
authors: Jingli
authors: J
authors: Xu
authors: Department of Radiology, School of Medicine, University of Colorado Denver, Aurora, CO 80045, USA.
authors: Jianquan
authors: J
authors: Yang
authors: College of Pharmacy, University of New Mexico, Albuquerque, NM 87131, USA.
authors: Changjian
authors: C
authors: Feng
authors: Department of Radiology, School of Medicine, University of Colorado Denver, Aurora, CO 80045, USA. Electronic address: yubin.miao@ucdenver.edu.
authors: Yubin
authors: Y
authors: Miao
mesh_terms: D000818:Animals; D045744:Cell Line, Tumor; D003500:Cyclization; D064593:Heterografts; D006801:Humans; D007769:Lactams / Q000737:chemistry*; D008546:Melanoma, Experimental / Q000473:pathology; D015609:Organotechnetium Compounds / Q000737:chemistry*; D000521:alpha-MSH / Q000737:chemistry*
chemical_list: D007769:Lactams; D015609:Organotechnetium Compounds; D000521:alpha-MSH
keywords: (99m)Tc-labeled lactam bridge-cyclized peptide; Alpha-melanocyte stimulating hormone; Human melanoma targeting; SPECT/CT