title: Novel (64)Cu-radiolabeled bile acid conjugates for targeted PET imaging.
abstract: A promising bifunctional chelate (N-NE3TA) was conjugated to bile acids, cholic acid (CA), deoxycholic acid (DCA), and chenodeoxycholic acid (CDCA) as tumor targeting vectors. Bile acid conjugates of N-NE3TA (CA-N-NE3TA, DCA-N-NE3TA, and CDCA-N-NE3TA) were comparatively evaluated for complexation with (64)Cu, an imaging probe for positron emission tomography (PET). N-NE3TA-bile acid conjugates were evaluated for radiolabeling kinetics with (64)Cu, and the corresponding (64)Cu-radiolabeled conjugates were screened for complex stability in human serum and EDTA solution. The NE3TA-bile acid conjugates instantly bound to (64)Cu with excellent radiolabeling efficiency at room temperature. All NE3TA-bile acid conjugates radiolabeled with (64)Cu remained inert in human serum for 2days without releasing a considerable amount of the radioactivity. The (64)Cu-radiolabeled complexes were further challenged by EDTA in a 100-fold molar excess. Bile acid-N-NE3TA conjugates radiolabeled with (64)Cu were quite stable with a minimal transfer of (64)Cu to EDTA at 4h time point. The in vitro data indicate that the bile acid-N-NE3TA conjugates deserve further biological evaluation for (64)Cu-based targeted PET imaging applications.
authors: Chemistry Division, Department of Biological and Chemical Sciences, Illinois Institute of Technology, 3101 S. Dearborn St., LS 182, Chicago, IL 60616, United States. Electronic address: Chong@iit.edu.
authors: Hyun-Soon
authors: HS
authors: Chong
authors: Chemistry Division, Department of Biological and Chemical Sciences, Illinois Institute of Technology, 3101 S. Dearborn St., LS 182, Chicago, IL 60616, United States.
authors: Yunwei
authors: Y
authors: Chen
authors: Chemistry Division, Department of Biological and Chemical Sciences, Illinois Institute of Technology, 3101 S. Dearborn St., LS 182, Chicago, IL 60616, United States.
authors: Chi Soo
authors: CS
authors: Kang
authors: Chemistry Division, Department of Biological and Chemical Sciences, Illinois Institute of Technology, 3101 S. Dearborn St., LS 182, Chicago, IL 60616, United States.
authors: Xiang
authors: X
authors: Sun
authors: Chemistry Division, Department of Biological and Chemical Sciences, Illinois Institute of Technology, 3101 S. Dearborn St., LS 182, Chicago, IL 60616, United States.
authors: Ningjie
authors: N
authors: Wu
mesh_terms: D001647:Bile Acids and Salts / Q000097:blood / Q000737:chemistry*; D056831:Coordination Complexes / Q000097:blood / Q000737:chemistry*; D003301:Copper Radioisotopes / Q000097:blood / Q000737:chemistry*; D006801:Humans; D049268:Positron-Emission Tomography / Q000379:methods*; D019275:Radiopharmaceuticals / Q000097:blood / Q000737:chemistry
chemical_list: D001647:Bile Acids and Salts; D056831:Coordination Complexes; D003301:Copper Radioisotopes; D019275:Radiopharmaceuticals
keywords: Bifunctional chelator; Bile acid; Cu-64; PET imaging; Polyaminocarboxylate; Radiolabeling; Serum stability