(6R,7R)-7-[[2-[2-(氨基甲基)苯基]乙酰]氨基]-3-[[1-(羧甲基)四唑-5-基]硫甲基]-8-氧代-5-硫杂-1-氮杂双环[4.2.0]辛-2-烯-2-羧酸

Zosuquidar (LY335979)是P-糖蛋白(P-gp)介导的多药抗性负调节剂,Ki为60 nM。

信号通路 >> 跨膜转运 >> P-糖蛋白

研究领域 >> 癌症

[1]. Dantzig AH, et al. Reversal of P-glycoprotein-mediated multidrug resistance by a potent cyclopropyldibenzosuberane modulator, LY335979. Cancer Res. 1996 Sep 15;56(18):4171-9.

[2]. Marcelletti JF, Multani PS, Lancet JE et al. Leukemic blast and natural killer cell P-glycoprotein function and inhibition in a clinical trial of zosuquidar infusion in acute myeloid leukemia. Leuk Res. 2009 Jun;33(6):769-74.

[3]. Ruff P, Vorobiof DA, Jordaan JP et al. A randomized, placebo-controlled, double-blind phase 2 study of docetaxel compared to docetaxel plus zosuquidar (LY335979) in women with metastatic or locally recurrent breast cancer who have received one prior chemotherapy regimen. Cancer Chemother Pharmacol. 2009 Sep;64(4):763-8.

[4]. Cripe LD, Uno H, Paietta EM et al. Zosuquidar, a novel modulator of P-glycoprotein, does not improve the outcome of older patients with newly diagnosed acute myeloid leukemia: a randomized, placebo-controlled trial of the Eastern Cooperative Oncology Group 3999. Blood. 2010 Nov 18;116(20):4077-85.

[5]. Abu Ajaj K, Graeser R, Kratz F. Zosuquidar and an albumin-binding prodrug of zosuquidar reverse multidrug resistance in breast cancer cells of doxorubicin and an albumin-binding prodrug of doxorubicin. Breast Cancer Res Treat. 2012 Jul;134(1):117-29.

依克立达 | 伐司扑达 | Tariquidar | 唑喹达三盐酸盐 | 利培酮 | 芥子碱硫氰酸盐 | 胡椒碱 | HM30181 | 20(S)-原人参二醇 | Dofequidar富马酸盐 | 2-(4-甲氧基苯基)-alpha-2-哌啶基-4-喹啉甲醇二盐酸盐 | 泽泻醇F | 聚乙二醇硬脂酸酯 | 比立考达 | MCI826