 | Acta Crystallographica Section D Acta Crystallographica Section D BIOLOGICAL CRYSTALLOGRAPHY |
journal menu
![[Figure 1]](cb5079fig1mag.jpg)
|
|
Figure 1
Structure and function of selenium-labelled homotrimeric cyclopeptides. (a) The chemical structures of the cyclopeptide series bear an identical backbone but with side chains systematically increasing in size and hydrophobicity (from left to right). (b) Stimulation of the basal ATPase activity of purified P-gp. QZ-Ala (green) conferred the highest degree of stimulation (∼16-fold) relative to the basal activity, with an EC50 value of 0.92 µM, followed by QZ-Val (blue; ∼7-fold). Data for verapamil (black), QZ-Leu (yellow) and QZ-Phe (red) are shown. (c) Inhibition of calcein-AM transport in P-gp-overexpressing CR1R12 cells. The same color scheme is applied for each compound as in (b) and the data were fitted using the Hill equation. The mean and SD of triple and quadruplet experiments are shown in (b) and (c), respectively. |
![[Figure 1]](cb5079fig1.jpg)
| BIOLOGICAL CRYSTALLOGRAPHY |
ISSN: 1399-0047
