title: Evaluation of the relationship between [18F]FDG and P-glycoprotein expression: an experimental study.
abstract: BACKGROUND
  P-glycoprotein (P-gp) is a cell-membrane-associated protein that transports a variety of drug substrates. We sought to evaluate the relationship between 2-[18F]fluoro-2-deoxy-D-glucose ([18F]FDG) and P-gp expression using breast carcinoma Bcap37/multidrug resistant (MDR1) and Bcap37 in vitro and in vivo.
  
  
  METHODS
  The function of P-gp expressed in Bcap37/MDR1 cells was evaluated using verapamil (VER), a classical inhibitor of P-gp. The accumulation of 99mTc-methoxyisobutylisonitrile ([99mTc]MIBI) in vitro was measured. In vivo imaging of severe combined immune deficiency (SCID) mice implanted with Bcap37 and Bcap37/MDR1 cells was performed by scintigraphy and micro-positron emission tomography (PET).
  
  
  RESULTS
  The uptake of [99mTc]MIBI was 0.62%±0.05% in the Bcap37/MDR1 cells and 2.02%±0.28% in the Bcap37 cells. VER significantly increased the uptake of [99mTc]MIBI in the Bcap37/MDR1 cells (1.90%±0.09%) but not in the Bcap37 cells (2.15%±0.27%). In vivo, neither the Bcap37 nor Bcap37/MDR1 tumors grown in the SCID mice could be detected by [99mTc]MIBI scintigraphy. Both the Bcap37 and Bcap37/MDR1 tumors were visible by micro-PET. The mean standardized uptake value (SUV) was significantly higher in the Bcap37 tumors (1.00±0.06) than in the Bcap37/MDR1 (0.67±0.11) tumors. VER significantly increased the mean SUV in the Bcap37/MDR1 tumors (1.02±0.16) but not in the Bcap37 tumors (1.09±0.22).
  
  
  CONCLUSIONS
  [18F]FDG combined with VER may be an effective noninvasive method of determining P-gp expression in tumors.
authors.affiliation: School of Radiation Medicine and Public Health, Soochow University, and Department of Nuclear Medicine, The First Affiliated Hospital of Soochow University, Suzhou, 215006, China.
authors.forename: Chunjing
authors.initials: C
authors.lastname: Yu
authors.forename: Weixing
authors.initials: W
authors.lastname: Wan
authors.forename: Bin
authors.initials: B
authors.lastname: Zhang
authors.forename: Shengming
authors.initials: S
authors.lastname: Deng
authors.forename: Tzu-Chen
authors.initials: TC
authors.lastname: Yen
authors.forename: Yiwei
authors.initials: Y
authors.lastname: Wu
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000037:antagonists & inhibitors / Q000378:metabolism*; D000818:Animals; D001692:Biological Transport / Q000187:drug effects; D001943:Breast Neoplasms / Q000000981:diagnostic imaging / Q000235:genetics / Q000378:metabolism / Q000473:pathology; D045744:Cell Line, Tumor; D005260:Female; D019788:Fluorodeoxyglucose F18 / Q000378:metabolism*; D015972:Gene Expression Regulation, Neoplastic / Q000187:drug effects; D006801:Humans; D051379:Mice; D049268:Positron-Emission Tomography; D000091402:Prohibitins; D020112:Rhodamine 123 / Q000378:metabolism; D017256:Technetium Tc 99m Sestamibi / Q000378:metabolism; D014700:Verapamil / Q000494:pharmacology
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; C000717331:PHB2 protein, human; C000717333:Phb2 protein, mouse; D000091402:Prohibitins; D019788:Fluorodeoxyglucose F18; D020112:Rhodamine 123; D017256:Technetium Tc 99m Sestamibi; D014700:Verapamil