Skip to main content
. Author manuscript; available in PMC: 2014 Nov 1.
Published in final edited form as: Biochemistry (Mosc). 2013 Nov;78(11):1228–1237. doi: 10.1134/S0006297913110035

Table 2.

Therapeutic efficacies of pharmaceuticals utilizing MC1R ligands for treatment of experimental tumors

Name Active principle Maximal effect Reference
188Re-(Arg11)CCMSH 88Re – β-particle emitter 1.8-fold increase in mean life span of mice [125]
212Pb[DOTA]-Re(Arg11)CCMSH 212Pb – α-particle emitter 3.4-fold increase in mean life span of mice, 45% surviving animals [126]
177Lu-DOTA-Re(Arg11)CCMSH 177Lu – β-particle emitter 1.2-fold increase in mean life span of mice [127]
Modular nanotransporter DTox-HMP-NLS-MSH photosensitizer 2.7-fold increase in mean life span of mice [86, 87]
Polyplex PEI-PEG-MC1sp-peptide, with thymidine kinase of herpes simplex virus phosphorylated ganciclovir derivative 3.6-fold increase in mean life span of mice [128]

Note: 188Re-(Arg11)CCMSH – 188Re-[Cys3,4,10, DPhe7, Arg11]-α-MSH3–13, peptide cyclized by rhenium via 3, 4, and 10 cysteine residues, truncated (3–13), and modified by α-MSH at amino acids indicated by the upper indexes; DOTA, 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid, a chelator; PEI, polyethyleneimine; PEG, polyethylene glycol; MC1sp, peptide with sequence (SSIISHFRWGKPV) highly specific for MC1R [129].