摘要
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（ｍｕｌｔｉｄｒｕｇｒｅｓｉｓｔａｎｃｅ，ＭＤＲ）的产生主要与肿瘤细胞中的膜蛋白：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和奎尼丁的类似物ＭＳ－２０９，新结构的化合物Ｓ－９７８８、ＧＦ－１２０９１８和ＶＸ－７１０，以及天然产物Ｈａｐａｌｏｓｉｎ等。有效的多药耐药蛋白抑制剂有望发展成为与化疗药物配伍使用的一类药物，以减少ＭＤＲ的产生，提高肿瘤化疗药物的敏感性。本文对ＭＤＲ研究的进展。
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.
出处
《军事医学科学院院刊》
CSCD
北大核心
1999年第1期67-69,共3页
Bulletin of the Academy of Military Medical Sciences
关键词
肿瘤
多药耐药性
P-糖蛋白
MDR
LRP
药物疗法
multidrug resistance
P glycoprotein(PG 170)
multidrug resistance protein(MRP 190)
lung resistance protein(LRP)
multidrug resistance protein inhibitors
