title: Synthesis and evaluation of 18F-labeled carbonic anhydrase IX inhibitors for imaging with positron emission tomography.
abstract: Two carbonic anhydrase IX (CA IX) inhibitors were radiolabeled with (18)F, and evaluated for imaging CA IX expression. Despite good affinity for CA IX and excellent plasma stability, uptake of both tracers in CA IX-expressing HT-29 tumor xenografts in mice was low. (18)F-FEC accumulated predominately in the liver and nasal cavity, whereas a significant amount of (18)F-U-104 was retained in blood. Due to minimal uptake in HT-29 tumors compared to other organs/tissues, these two tracers are not suitable for use for CA IX-targeted imaging.
authors: Department of Molecular Oncology, BC Cancer Agency , Vancouver, BC , Canada .
authors: Jinhe
authors: J
authors: Pan
authors: Joseph
authors: J
authors: Lau
authors: Felix
authors: F
authors: Mesak
authors: Navjit
authors: N
authors: Hundal
authors: Maral
authors: M
authors: Pourghiasian
authors: Zhibo
authors: Z
authors: Liu
authors: François
authors: F
authors: Bénard
authors: Shoukat
authors: S
authors: Dedhar
authors: Claudiu T
authors: CT
authors: Supuran
authors: Kuo-Shyan
authors: KS
authors: Lin
mesh_terms: D000230:Adenocarcinoma / Q000000981:diagnostic imaging; D000818:Animals; D000951:Antigens, Neoplasm / Q000378:metabolism*; D000071231:Carbonic Anhydrase IX; D002257:Carbonic Anhydrase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D002256:Carbonic Anhydrases / Q000378:metabolism*; D004355:Drug Stability; D005462:Fluorine Radioisotopes; D019073:HT29 Cells; D006801:Humans; D051379:Mice; D016688:Mice, Inbred NOD; D018345:Mice, Knockout; D016513:Mice, SCID; D015394:Molecular Structure; D049268:Positron-Emission Tomography / Q000379:methods*; D019275:Radiopharmaceuticals; D015375:Receptors, Interleukin-2 / Q000235:genetics; D014018:Tissue Distribution; D023041:Xenograft Model Antitumor Assays
chemical_list: D000951:Antigens, Neoplasm; D002257:Carbonic Anhydrase Inhibitors; D005462:Fluorine Radioisotopes; D019275:Radiopharmaceuticals; D015375:Receptors, Interleukin-2; C089226:CA9 protein, human; D000071231:Carbonic Anhydrase IX; D002256:Carbonic Anhydrases