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本文引用的文献

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Targeting PP2A for cancer therapeutic modulation.针对癌症治疗调节的 PP2A 靶向治疗。
Cancer Biol Med. 2022 Nov 1;19(10):1428-39. doi: 10.20892/j.issn.2095-3941.2022.0330.
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Protein phosphatase 2A inactivation induces microsatellite instability, neoantigen production and immune response.蛋白磷酸酶 2A 的失活会导致微卫星不稳定、新抗原产生和免疫反应。
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Pharmacological Inhibition of PP2A Overcomes Nab-Paclitaxel Resistance by Downregulating MCL1 in Esophageal Squamous Cell Carcinoma (ESCC).PP2A的药理学抑制通过下调食管鳞状细胞癌(ESCC)中的MCL1克服纳武单抗-紫杉醇耐药性。
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Protein Phosphatase 2A as a Therapeutic Target in Small Cell Lung Cancer.蛋白磷酸酶 2A 作为小细胞肺癌的治疗靶点。
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Inhibition of protein phosphatase-2A with LB-100 enhances antitumor immunity against glioblastoma.蛋白磷酸酶-2A 的抑制作用与 LB-100 增强了胶质母细胞瘤的抗肿瘤免疫。
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Inhibition of PP2A with LB-100 Enhances Efficacy of CAR-T Cell Therapy Against Glioblastoma.用LB-100抑制蛋白磷酸酶2A可增强嵌合抗原受体T细胞疗法治疗胶质母细胞瘤的疗效。
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Targeting phosphatases in cancer: suppression of many versus the ablation of one.癌症中靶向磷酸酶:抑制多种磷酸酶与去除一种磷酸酶的比较
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一种同时测定人血浆中 LB-100 及其活性代谢物草甘膦的 LC-MS/MS 方法。

An LC-MS/MS method for simultaneous determination of LB-100 and its active metabolite, endothall, in human plasma.

机构信息

Department of Medical Oncology & Therapeutics Research, City of Hope, 1500 East Duarte Rd, Duarte, CA 91010, USA.

LIXTE Biotechnology, Inc. 680 E Colorado Blvd, Suite 180, Pasadena, CA 91101, USA.

出版信息

Bioanalysis. 2023 Sep;15(17):1095-1107. doi: 10.4155/bio-2023-0078. Epub 2023 Aug 16.

DOI:10.4155/bio-2023-0078
PMID:37584370
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10505989/
Abstract

We have developed and validated a novel LC-MS/MS method for the simultaneous quantification of LB-100 and its active metabolite, endothall, in human plasma following solid-phase extraction. LB-105 and endothall-D6 were used as internal standards. Chromatographic separation was achieved on a Hypercarb™ column using 5 mM (NH)CO and 30:70 (v/v) 100 mM (NH)CO:acetonitrile as mobile phases. Detection was performed via positive electrospray ionization mode with multiple reaction monitoring. The assay exhibited linearity in the concentration range of 2.5-500 ng/ml for both analytes. Intra- and inter-assay precision and accuracy were within ±11%. LB-100 and endothall recoveries were 78.7 and 86.7%, respectively. The validated LC-MS/MS method enabled the accurate measurement of LB-100 and endothall in patient samples from an ongoing clinical trial (NCT04560972).

摘要

我们开发并验证了一种新的 LC-MS/MS 方法,可用于固相萃取后同时定量人血浆中的 LB-100 及其活性代谢物草甘膦。LB-105 和草甘膦-D6 用作内标。采用 Hypercarb™柱,以 5 mM(NH)CO 和 30:70(v/v)100 mM(NH)CO:乙腈作为流动相进行色谱分离。采用正电喷雾电离模式,以多反应监测进行检测。该分析方法对两种分析物的浓度范围为 2.5-500 ng/ml 时呈线性。日内和日间精密度和准确度均在±11%范围内。LB-100 和草甘膦的回收率分别为 78.7%和 86.7%。验证后的 LC-MS/MS 方法可用于准确测量正在进行的临床试验(NCT04560972)中患者样本中的 LB-100 和草甘膦。