Demmer A, Dunn T, Hoof T, Kubesch P, Tümmler B
Klinische Forschergruppe Molekulare Pathologie, Medizinischen Hochschule Hannover, Germany.
Eur J Pharmacol. 1996 Nov 21;315(3):339-43. doi: 10.1016/s0014-2999(96)00616-4.
The affinity of the multidrug resistance modulator S9788 to interact with P-glycoprotein was characterized by its ability to inhibit the photoaffinity labelling of plasma membranes of multidrug resistant chinese hamster ovary B30 cells by iodomycin. This iodinated analogue of daunomycin specifically photolabels P-glycoprotein in membrane vesicles as well as in intact cells. The multidrug resistance reversing agents verapamil and cyclosporin and the cytotoxic drugs vinblastine and daunomycin which are known to be recognized by P-glycoprotein competed with iodomycin for its binding site on P-glycoprotein. Vinblastine and cyclosporin bound with high affinity, S9788 and verapamil with medium affinity to P-glycoprotein.
多药耐药调节剂S9788与P-糖蛋白相互作用的亲和力，通过其抑制碘霉素对多药耐药中国仓鼠卵巢B30细胞膜的光亲和标记的能力来表征。柔红霉素的这种碘化类似物可特异性地对膜囊泡以及完整细胞中的P-糖蛋白进行光标记。已知被P-糖蛋白识别的多药耐药逆转剂维拉帕米和环孢菌素，以及细胞毒性药物长春碱和柔红霉素，与碘霉素竞争其在P-糖蛋白上的结合位点。长春碱和环孢菌素以高亲和力结合，S9788和维拉帕米以中等亲和力结合到P-糖蛋白上。
