title: Synthesis and evaluation of a bifunctional chelate for development of Bi(III)-labeled radioimmunoconjugates.
abstract: A new bifunctional ligand C-DEPA was designed and synthesized as a component for antibody-targeted radiation therapy (radioimmunotherapy, RIT) of cancer. C-DEPA was conjugated to a tumor targeting antibody, trastuzumab, and the corresponding C-DEPA-trastuzumab conjugate was evaluated for radiolabeling kinetics with (205/6)Bi. C-DEPA-trastuzumab conjugate rapidly bound (205/6)Bi, and (205/6)Bi-C-DEPA-trastuzumab conjugate was stable in human serum for 72 h. The in vitro radiolabeling kinetics and serum stability data suggest that C-DEPA is a potential chelate for preclinical RIT applications using (212)Bi and (213)Bi.
authors: Chemistry Division, Biological, Chemical, and Physical Sciences Department, Illinois Institute of Technology, 3101 S. Dearborn St., LS 182, Chicago, IL 60616, USA.
authors: Mamta
authors: M
authors: Dadwal
authors: Chi Soo
authors: CS
authors: Kang
authors: Hyun A
authors: HA
authors: Song
authors: Xiang
authors: X
authors: Sun
authors: Anzhi
authors: A
authors: Dai
authors: Kwamena E
authors: KE
authors: Baidoo
authors: Martin W
authors: MW
authors: Brechbiel
authors: Hyun-Soon
authors: HS
authors: Chong
mesh_terms: D061067:Antibodies, Monoclonal, Humanized / Q000737:chemistry*; D001729:Bismuth / Q000737:chemistry*; D004353:Drug Evaluation, Preclinical; D004355:Drug Stability; D005998:Glycine / Q000031:analogs & derivatives* / Q000737:chemistry; D006573:Heterocyclic Compounds, 1-Ring / Q000737:chemistry*; D006801:Humans; D018796:Immunoconjugates / Q000737:chemistry* / Q000378:metabolism / Q000627:therapeutic use; D007553:Isotope Labeling; D007700:Kinetics; D009369:Neoplasms / Q000532:radiotherapy; D000068878:Trastuzumab
chemical_list: C545867:7-(2-(bis-carboxymethyl-amino)ethyl)-4,10-bis-carboxymethyl-1,4,7,10-tetraazacyclododec-1-yl-acetic acid; D061067:Antibodies, Monoclonal, Humanized; D006573:Heterocyclic Compounds, 1-Ring; D018796:Immunoconjugates; D000068878:Trastuzumab; D005998:Glycine; D001729:Bismuth