Structural study by NMR of an oxorhenium-RGD decapeptide complex for application in radiotherapy.
The decapeptide Arg-Gly-Asp-Ser-Cys-Arg-Gly-Asp-Ser-Tyr, which contains two Arg-Gly-Asp (RGD) moieties in its sequence, has been successfully labeled with radioactive rhenium (Re-188) yielding a single, stable oxorhenium complex. This complex is being evaluated for possible application in oncology as a target-specific radiotherapeutic agent, because its radioactive technetium-99m analogue has already been applied for the scintigraphic detection of malignant melanoma in humans. For structural characterization purposes, the complex of the decapeptide was synthesized at the macroscopic level using nonradioactive rhenium (Re-185/Re-187). NMR and mass spectral analysis of the nonradioactive oxorhenium complex revealed that the decapeptide coordinates to the oxorhenium core through the N(amide) of Asp3, the N(amide) of Ser4, and the N(amide) and S(thiolate) atoms of Cys5 to form a complex of the ReO[N(3)S] type.
Costopoulos
Basil
B
Institutes of Radioisotopes & Radiodiagnostic Products and Biology, National Centre for Scientific Research Demokritos, 153 10 Athens, Greece.
Benaki
Dimitra
D
Pelecanou
Maria
M
Mikros
Emmanuel
E
Stassinopoulou
Chariklia I
CI
Varvarigou
Alexandra D
AD
Archimandritis
Spyridon C
SC
D000818:Animals; D004353:Drug Evaluation, Preclinical; D009682:Magnetic Resonance Spectroscopy / Q000379:methods; D051379:Mice; D008956:Models, Chemical; D008958:Models, Molecular; D009842:Oligopeptides / Q000737:chemistry*; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D011868:Radioisotopes; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D011878:Radiotherapy; D012211:Rhenium / Q000737:chemistry*; D014018:Tissue Distribution
D009842:Oligopeptides; D009942:Organometallic Compounds; D011868:Radioisotopes; D019275:Radiopharmaceuticals; D012211:Rhenium