title: Evaluation and comparison of a new DOTA and DTPA-bombesin agonist in vitro and in vivo in low and high GRPR expressing prostate and breast tumor models.
abstract: We evaluated and compared a new bombesin analog [Tyr-Gly5, Nle(14)]-BBN(6-14) conjugated to DOTA or DTPA and radiolabeled with In-111 in low and high GRPR expressing tumor models. Both peptides were radiolabeled with high radiochemical purity and specific activity. In vitro assays on T-47D, LNCaP and PC-3 cells showed that the affinity of peptides is similar and a higher binding and internalization of DOTA-peptide to PC-3 cells was observed. Both peptides could target PC-3 and LNCaP tumors in vivo and both tumor types could be visualized by microSPECT/CT.
authors.affiliation: Centre for Molecular Oncology, Barts Cancer Institute, Queen Mary University of London, London EC1M 6BQ, United Kingdom; Nuclear and Energy Research Institute (IPEN), University of Sao Paulo, Sao Paulo, Brazil. Electronic address: pujatti.pb@gmail.com.
authors.forename: Priscilla B
authors.initials: PB
authors.lastname: Pujatti
authors.affiliation: Centre for Molecular Oncology, Barts Cancer Institute, Queen Mary University of London, London EC1M 6BQ, United Kingdom.
authors.forename: Julie M
authors.initials: JM
authors.lastname: Foster
authors.affiliation: InviCRO LLC, 27 Drydock Ave, Boston, MA 02210, United States.
authors.forename: Ciara
authors.initials: C
authors.lastname: Finucane
authors.affiliation: Centre for Molecular Oncology, Barts Cancer Institute, Queen Mary University of London, London EC1M 6BQ, United Kingdom.
authors.forename: Chantelle D
authors.initials: CD
authors.lastname: Hudson
authors.affiliation: Biospace Lab, 13 rue Georges Auric, 75011 Paris, France.
authors.forename: Jerome C
authors.initials: JC
authors.lastname: Burnet
authors.affiliation: Laboratory of Biochemistry and Biphysics, Butantan Institute, Sao Paulo, Brazil.
authors.forename: Kerly F M
authors.initials: KFM
authors.lastname: Pasqualoto
authors.affiliation: Nuclear and Energy Research Institute (IPEN), University of Sao Paulo, Sao Paulo, Brazil.
authors.forename: Jair
authors.initials: J
authors.lastname: Mengatti
authors.affiliation: Centre for Molecular Oncology, Barts Cancer Institute, Queen Mary University of London, London EC1M 6BQ, United Kingdom.
authors.forename: Stephen J
authors.initials: SJ
authors.lastname: Mather
authors.affiliation: Nuclear and Energy Research Institute (IPEN), University of Sao Paulo, Sao Paulo, Brazil.
authors.forename: Elaine B
authors.initials: EB
authors.lastname: de Araújo
authors.affiliation: Centre for Molecular Oncology, Barts Cancer Institute, Queen Mary University of London, London EC1M 6BQ, United Kingdom.
authors.forename: Jane K
authors.initials: JK
authors.lastname: Sosabowski
mesh_terms: D000818:Animals; D001839:Bombesin / Q000031:analogs & derivatives* / Q000737:chemistry; D001943:Breast Neoplasms / Q000000981:diagnostic imaging* / Q000378:metabolism*; D045744:Cell Line, Tumor; D004355:Drug Stability; D005260:Female; D006573:Heterocyclic Compounds, 1-Ring; D064593:Heterografts; D006801:Humans; D066298:In Vitro Techniques; D007205:Indium Radioisotopes; D008297:Male; D016513:Mice, SCID; D009368:Neoplasm Transplantation; D004369:Pentetic Acid / Q000031:analogs & derivatives*; D011471:Prostatic Neoplasms / Q000000981:diagnostic imaging* / Q000378:metabolism*; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000737:chemistry; D018004:Receptors, Bombesin / Q000378:metabolism*; D014018:Tissue Distribution
chemical_list: D006573:Heterocyclic Compounds, 1-Ring; D007205:Indium Radioisotopes; D019275:Radiopharmaceuticals; D018004:Receptors, Bombesin; C071349:1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid; D004369:Pentetic Acid; D001839:Bombesin
keywords: Bombesin; Comparison; DOTA; DTPA; GRPR