肿瘤多药耐药蛋白抑制剂

肿瘤细胞产生多药耐药性是肿瘤化疗失败的主要原因之一，肿瘤多药耐药性（ｍｕｌｉｄｒｕｇｒｅｓｉｓａｎｃｅ，ＭＤＲ）的产生主要与肿瘤细胞的膜蛋白，Ｐ－糖蛋白（ＰＧ－１７０）多药耐药蛋白（ＭＲＰ－１９０）和肺耐药蛋白（ＬＲＰ）的过多表达有关。在发现维拉帕米，奎尼丁和环孢菌素等药物具有逆转ＭＤＲ作用的基础上，发展了一些新的能够逆转ＭＤＲ现象的多药耐药蛋白抑制剂，如环孢菌素的类似物ＳＤＺＰＳＣ８３３和奎民丁

Tumor multidrug resistance protein inhibitor

The acquired multidrug resistance remains a major challenge to successful chemotherapy of neoplastic disorders. Three kinds of protein showing to cause this type of multidrug resistance in human tumor cells are P glycoprotein(PG 170), multidrug resistance protein(MRP 190) and lung resistance protein(LRP). Based on the multidrug resistance reversal activity of chemosensitizers such as verapamil, quinidine and cyclosporin A , many novel multidrug resistance protein inhibitors have been developed. Novel cyclosporins analog SDZ PSC833 , quinidine analog MS 209 , other novel compounds such as S 9788, GF 120918, VX 710, and a natural product Hapalosin and its analogs are among these developed agents. Future investigations will lead to successful development of selective inhibitors of multidrug resistance protein, which would combat the development of resistance when given concurrently with chemotherapeutic agents.