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P-gp/BCRP-IN-2
MCE 国际站:P-gp/BCRP-IN-2
产品活性:P-gp/BCRP-IN-2 (compound 15) 是恶二唑衍生物,是 ABC 转运蛋白 P-glycoprotein (IC50: 1.6 nM) 和 BCRP (IC50: 600 nM) 的双抑制剂。P-gp/BCRP-IN-2 还能够增强 Doxorubicin (HY-15142A) 在耐药人腺癌结肠癌细胞系 HT29/DX 和 MDCK-MDR1 细胞中的抗增殖作用。
研究领域:Membrane Transporter/Ion Channel
作用靶点:P-glycoprotein | BCRP
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文献和实验, representing a built-in obstacle to therapeutic ratio. Constitutive and induced MDR activity can be detected in cellular subsets of disaggregated tissues, using the fluorescent substrates Rhodamine 123 and Hoechst 33342 for ABCB1 (also known as P-gp and MDR
In Vitro Characterization of Intestinal and Hepatic Transporters: MRP2
some overlapping substrate specificity with other ABC family members including P-glycoprotein (P-gp) and the breast cancer resistance protein (BCRP). Understanding whether investigational compounds are potential MRP2 substrates or inhibitors during drug
(glutathione s-conjugate export carrier, GS-X pump)的泵活性将这些药物泵出细胞外,从而产生耐药性。已有研究表明GST与头颈部肿瘤MDR有关,尤其是鳞癌。有报道GST-π已成为头颈部鳞癌原发及继发病灶早期诊断的血清学诊断依据[2]。 多药耐药相关蛋白(multidrug resistance-associated protein,MRP) 是一种膜糖蛋白。MRP与P-gp同属于三磷酸腺苷依赖性跨膜转运蛋白类,它们在分子
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