the phosphodiesterase-5 inhibitor vardenafil is a potent inhibitor of abcb1p-glycoprotein transporterphosphodiesterase-5抑制剂伐地那非是一个abcb1p-glycoprotein运输车的有效抑制剂.pdfVIP
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the phosphodiesterase-5 inhibitor vardenafil is a potent inhibitor of abcb1p-glycoprotein transporterphosphodiesterase-5抑制剂伐地那非是一个abcb1p-glycoprotein运输车的有效抑制剂
The Phosphodiesterase-5 Inhibitor Vardenafil Is a Potent
Inhibitor of ABCB1/P-Glycoprotein Transporter
1,2,3 1 4 1 1,2,5
Pei-Rong Ding , Amit K. Tiwari , Shinobu Ohnuma , Jeferson W. K. K. Lee , Xin An , Chun-Ling
1 1¤ 1 6 1 4
Dai , Qi-Si Lu , Satyakam Singh , Dong-Hua Yang , Tanaji T. Talele , Suresh V. Ambudkar , Zhe-Sheng
Chen1*
1 Department of Pharmaceutical Sciences, College of Pharmacy and Allied Health Professions, St. John’s University, Jamaica, New York, United States of America, 2 State
Key Laboratory of Oncology in South China, Cancer Center, Sun Yat-Sen University, Guangzhou, China, 3 Department of Colorectal Surgery, Cancer Center, Sun Yat-Sen
University, Guangzhou, China, 4 Laboratory of Cell Biology, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, Maryland, United
States of America, 5 Department of Medical Oncology, Cancer Center, Sun Yat-Sen University, Guangzhou, China, 6 Biosample Repository, Fox Chase Cancer Center,
Philadelphia, Pennsylvania, United States of America
Abstract
One of the major causes of chemotherapy failure in cancer treatment is multidrug resistance (MDR) which is mediated by
the ABCB1/P-glycoprotein. Previously, through the use of an extensive screening process, we found that vardenafil, a
phosphodiesterase 5 (PDE-5) inhibitor significantly reverses MDR in ABCB1 overexpressing cancer cells, and its efficacy was
greater than that of tadalafil, another PDE-5 inhibitor. The present study was designed to determine the reversal
mechanism
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