title: Rapid and one-step radiofluorination of bioactive peptides: potential PET radiopharmaceuticals.
abstract: In an attempt to develop a new and rapid method for labeling peptides with (18)F, we have synthesized MUC1-[(18)F]SFB and BBN-[(18)F]SFB peptide conjugates using a convenient and one-step simple reactions. Radiochemical yields for MUC1-[(18)F]SFB and BBN-[(18)F]SFB peptide conjugates were greater than 70% in less than 30 min synthesis time, thus amenable for automation for the radiofluorination of peptides. in vitro tests on T47D breast cancer cells showed that the significant amounts of the radioconjugates were associated with cell fractions and held sufficient affinities and specificities toward T47D cell line. These radioconjugates may be useful as molecular probes for detecting and staging of breast cancer and monitoring tumor response to treatment.
authors: Cyclotron and Radiopharmaceuticals Department, King Faisal Specialist Hospital and Research Centre, P.O. Box 3354, Riyadh 11211, Saudi Arabia. Electronic address: jammaz@kfshrc.edu.sa.
authors: I
authors: I
authors: AlJammaz
authors: Cyclotron and Radiopharmaceuticals Department, King Faisal Specialist Hospital and Research Centre, P.O. Box 3354, Riyadh 11211, Saudi Arabia.
authors: B
authors: B
authors: Al-Otaibi
authors: Cyclotron and Radiopharmaceuticals Department, King Faisal Specialist Hospital and Research Centre, P.O. Box 3354, Riyadh 11211, Saudi Arabia.
authors: A
authors: A
authors: Abousekhrah
authors: Cyclotron and Radiopharmaceuticals Department, King Faisal Specialist Hospital and Research Centre, P.O. Box 3354, Riyadh 11211, Saudi Arabia.
authors: S
authors: S
authors: Okarvi
mesh_terms: D001565:Benzoates / Q000737:chemistry; D001839:Bombesin / Q000031:analogs & derivatives* / Q000737:chemistry; D001943:Breast Neoplasms / Q000000981:diagnostic imaging; D045744:Cell Line, Tumor; D005260:Female; D005462:Fluorine Radioisotopes / Q000737:chemistry*; D006801:Humans; D007553:Isotope Labeling / Q000379:methods; D018396:Mucin-1 / Q000737:chemistry*; D049268:Positron-Emission Tomography / Q000379:methods; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry; D013388:Succinimides / Q000737:chemistry
chemical_list: D001565:Benzoates; D005462:Fluorine Radioisotopes; C060192:MUC1 protein, human; D018396:Mucin-1; D019275:Radiopharmaceuticals; D013388:Succinimides; C075713:N-succinimidyl-4-fluorobenzoate; D001839:Bombesin
keywords: (18)F; (18)F-peptide; Bombesin; Breast cancer; Mucine; PET radiopharmaceuticals