Reference - Detail
| RRC ID | 68578 |
|---|---|
| Author | Yamasaki T, Kawamura K, Hatori A, Yui J, Yanamoto K, Yoshida Y, Ogawa M, Nengaki N, Wakisaka H, Fukumura T, Zhang MR. |
| Title | PET study on mice bearing human colon adenocarcinoma cells using [11C]GF120918, a dual radioligand for P-glycoprotein and breast cancer resistance protein. |
| Journal | Nucl Med Commun |
| Abstract |
OBJECTIVE:To evaluate the functions of P-glycoprotein (Pgp) and breast cancer resistance protein (BCRP) in human colon adenocarcinoma (Caco-2), we carried out an in-vitro study and a small animal positron emission tomography (PET) study using [C]GF120918 (elacridar). METHODS:[C]GF120918 was synthesized by reacting the desmethyl precursor with [C]CH3I. An in-vitro study using [C]GF120918 was carried out in Caco-2 and Madin-Darby canine kidney cells in the presence or absence of a transporter inhibitor (cyclosporine A and unlabeled GF120918). The biodistribution of radioactivity after the injection of [C]GF120918 was determined in Caco-2-bearing mice using a small animal PET scanner. RESULTS:In Caco-2 cells expressing Pgp and BCRP, coincubation with unlabeled GF120918 caused an approximately two-fold increase in [C]GF120918 uptake compared with that of the control ([C]GF120918 only). In Caco-2-bearing mice, PET results indicated that [C]GF120918 uptake in the tumor was low, but was significantly increased by treatment with unlabeled GF120918. In metabolite analysis, the radioactive component in the tumor almost corresponded to intact [C]GF120918. CONCLUSION:A PET study combining the administration of [C]GF120918 with unlabeled GF120918 may be a useful tool for evaluating the functions of Pgp and BCRP in tumors. |
| Volume | 31(11) |
| Pages | 985-93 |
| Published | 2010-11-1 |
| DOI | 10.1097/MNM.0b013e32833fbf87 |
| PMID | 20859232 |
| MeSH | ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism* ATP Binding Cassette Transporter, Subfamily G, Member 2 ATP-Binding Cassette Transporters / metabolism* Acridines / metabolism* Adenocarcinoma / pathology* Animals Biological Transport Blotting, Western Caco-2 Cells Carbon Radioisotopes Colonic Neoplasms / pathology* Dogs Humans Ligands Male Mice Neoplasm Proteins / metabolism* Positron-Emission Tomography / methods* Tetrahydroisoquinolines / metabolism* Tomography, Emission-Computed, Single-Photon |
| IF | 1.334 |
| Resource | |
| Human and Animal Cells | CACO-2(RCB0988) MDCK(RCB0995) |