B-ring substituted 5,7-dihydroxyflavonols with high-affinity binding to P-glycoprotein responsible for cell multidrug resistance.

Boumendjel A; Bois F; Beney C; Mariotte AM; Conseil G; Di-Pietro A

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B-ring substituted 5,7-dihydroxyflavonols with high-affinity binding to P-glycoprotein responsible for cell multidrug resistance.

机译：B环取代了与P-糖蛋白具有高亲和力的5,7-二羟基黄酮醇，负责细胞的多药耐药性。

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Starting from the interaction of galangin (3,5,7-trihydroxyflavone) with a cytosolic nucleotide-binding domain of P-glycoprotein, a series of flavonol derivatives was synthesized and tested for their binding affinity towards the same target. The 5,7-dihydroxy-4'-iodoflavonol and 5,7-dihydroxy-4'-n-octylflavonol derivatives displayed much higher binding affinities, with respective increases of 6- and 93-fold as compared to galangin.

机译：从高良姜精（3,5,7-三羟基黄酮）与P-糖蛋白的胞质核苷酸结合结构域的相互作用开始，合成了一系列黄酮醇衍生物并测试了它们对同一靶标的结合亲和力。与高良姜精相比，5,7-二羟基-4'-碘黄酮醇和5,7-二羟基-4'-正辛基黄酮醇衍生物显示出更高的结合亲和力，分别增加了6倍和93倍。

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《Bioorganic and Medicinal Chemistry Letters》 |2001年第1期|共3页
作者
Boumendjel A; Bois F; Beney C; Mariotte AM; Conseil G; Di-Pietro A;
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正文语种 eng
中图分类药学;生物化学;
关键词
Drug Resistance; Multiple; Flavones; P-Glycoprotein; Quercetin; Recombinant Proteins; 抗药性; 多药; 黄酮类; P-糖蛋白; 槲皮素;

机译：Drug Resistance;Multiple;Flavones;P-Glycoprotein;Quercetin;Recombinant Proteins;抗药性;多药;黄酮类;P-糖蛋白;槲皮素;

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1. B-ring substituted 5,7-dihydroxyflavonols with high-affinity binding to P-glycoprotein responsible for cell multidrug resistance. [J] . Boumendjel A, Bois F, Beney C, Bioorganic and Medicinal Chemistry Letters . 2001,第1期

机译：B环取代了与P-糖蛋白具有高亲和力的5,7-二羟基黄酮醇，负责细胞的多药耐药性。
2. Recent advances in the discovery of flavonoids and analogs with high-affinity binding to P-glycoprotein responsible for cancer cell multidrug resistance. [J] . Boumendjel A, Di Pietro A, Dumontet C, Medicinal research reviews . 2002,第5期

机译：黄酮类化合物和与P-糖蛋白具有高亲和力结合的类似物的最新进展，这些黄酮类化合物和P-糖蛋白对癌细胞具有多重耐药性。
3. Halogenated chalcones with high-affinity binding to P-glycoprotein: potential modulators of multidrug resistance. [J] . Bois F, Beney C, Boumendjel A, Journal of Medicinal Chemistry . 1998,第21期

机译：与P-糖蛋白具有高亲和力的卤代查耳酮：潜在的多药耐药调节剂。
4. THE E3 UBIQUITIN LIGASE CBL-B REVERSES MULTIDRUG RESISTANCE OF MCF-7/ADR CELLS THROUGH SUPPRESSION OF PI3K/AKT SIGNALING PATHWAY AND DOWN-REGULATION OF P-GLYCOPROTEIN [C] . Ye Zhang, Xiujuan Qu, Xuejun Hu, 2011 Asia-Pacific Conference of tumor biology and medicine . 2011

机译：E3泛素连接酶CBL-B通过抑制PI3K / AKT信号通路和P-糖蛋白下调逆转MCF-7 / ADR细胞的多药耐药性
5. Characterization of novel semi-synthetic taxanes capable of modulating P-glycoprotein multidrug resistance. [D] . Vredenburg, Michael Ryan. 2005

机译：能够调节P-糖蛋白多药耐药性的新型半合成紫杉烷类化合物的表征。
6. Amino acid substitutions in the sixth transmembrane domain of P-glycoprotein alter multidrug resistance. [O] . S E Devine, V Ling, P W Melera 1992

机译：P-糖蛋白第六个跨膜结构域中的氨基酸取代改变了多药耐药性。
7. Amino acid substitutions in the sixth transmembrane domain of P-glycoprotein alter multidrug resistance. [O] . Devine, S E, Ling, V, Melera, P W 1992

机译：P-糖蛋白第六个跨膜结构域中的氨基酸取代改变了多药耐药性。
8. Role of ABCB5 P-Glycoprotein in Breast Cancer Multidrug Resistance. [R] . Frank, M. H. 2005

机译：aBCB5 p-糖蛋白在乳腺癌多药耐药中的作用。

B-ring substituted 5,7-dihydroxyflavonols with high-affinity binding to P-glycoprotein responsible for cell multidrug resistance.

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