Photoaffinity substrates for P-glycoprotein
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Cited by (117)
Radiosynthesis of a <sup>18</sup>F-labeled 2,3-diarylsubstituted indole via McMurry coupling for functional characterization of cyclooxygenase-2 (COX-2) in vitro and in vivo
2012, Bioorganic and Medicinal ChemistryCitation Excerpt :The specificity of the radiotracer uptake was further tested by performing blocking experiments with all cells after preincubation with a 100 μmol/L solution of the corresponding nonradioactive reference compound 3 for 30 min (Fig. 3). Moreover, the possible interaction with the P-glycoprotein (P-gp) efflux pump was examined in the presence of P-gp inhibitor cyclosporine A and the calcium blocker verapamil, respectively.14,33,34 Therefore, cells were incubated with cyclosporine A and verapamil for 60 min before [18F]-3 was added to the loading buffer.
Fluorescent cyclin-dependent kinase inhibitors block the proliferation of human breast cancer cells
2011, Bioorganic and Medicinal ChemistryCitation Excerpt :In order to evaluate the MDR effect on VMY-1-103, we tested the effect of VMY-1-103 on the proliferation in CL 10.3 (MDR-positive) cells, which over express P-glycoprotein,29 and compare with MDR-negative MCF-7 cells. Paclitaxel, a known P-glycoprotein substrate30 was included as a positive control. In Table 3, the IC50 of the compounds are represented along with the ratio of difference between MDR-positive and MDR-negative cell lines.
1-[4-(2-Aminoethoxy)phenylcarbonyl]-3,5-bis-(benzylidene)-4-oxopiperidin es: A novel series of highly potent revertants of P-glycoprotein associated multidrug resistance
2008, Bioorganic and Medicinal Chemistry LettersMechanisms underlying the anticancer activities of the angucycline landomycin E
2007, Biochemical PharmacologyCitation Excerpt :Numerous researchers have worked on identifying chemical modifications of anthracyclines that would decrease drug efflux by P-gp [31–35]. Beck and Qian [36] proposed that P-gp substrate drugs often contain at least two planar groups and a tertiary nitrogen charged at physiological pH. Regarding ADR, distinct modifications of the sugar moiety [34] (often regarding the nitrogen group [31–33]) were in the focus of interest. Results of these approaches suggest that neutral charge and enhanced lipophilicity prevent anthracyclines from being transported by P-gp.
A simplified model to predict P-glycoprotein interacting drugs from 3D molecular interaction field
2006, International Journal of PharmaceuticsA high-throughput screening microplate test for the interaction of drugs with P-glycoprotein
2002, Analytical Biochemistry
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