pgp - publications

Predict more pgp - ligand interactions now!

1. Nucl Med Biol. 2012 Jan 18. [Epub ahead of print]

Evaluation of the relationship between [(18)F]FDG and P-glycoprotein expression:
an experimental study.

Yu C, Wan W, Zhang B, Deng S, Yen TC, Wu Y.

School of Radiation Medicine and Public Health, Soochow University, Suzhou,
215123, China; Department of Nuclear Medicine, The Fourth Affiliated Hospital of
Soochow University, Wuxi, 214062, China.

INTRODUCTION: 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-[(18)F]fluoro-2-deoxy-d-glucose ([(18)F]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
(99m)Tc-methoxyisobutylisonitrile ([(99m)Tc]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 [(99m)Tc]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 [(99m)Tc]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 [(99m)Tc]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: [(18)F]FDG combined with VER may be an
effective noninvasive method of determining P-gp expression in tumors.

Copyright © 2011 Elsevier Inc. All rights reserved.

PMID: 22264856 [PubMed - as supplied by publisher]