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首页> 外文期刊>Anti-cancer agents in medicinal chemistry >Overcoming Cancer Cell Drug Resistance by a Folic Acid Targeted Polymeric Conjugate of Buthionine Sulfoximine
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Overcoming Cancer Cell Drug Resistance by a Folic Acid Targeted Polymeric Conjugate of Buthionine Sulfoximine

机译：克服甲磺酸亚磺酰胺的叶酸靶向聚合物缀合物克服癌细胞耐药性

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Background: Glutathione (GSH), which is the predominant low molecular weight intracellular thiol in mammals, has multiple functions, such as those of protecting against oxidative stress and detoxifying endogenous and exogenous electrophiles. High GSH levels, which have been observed in various types of tumors, have been thought to contribute to the resistance of neoplastic cells to apoptotic stimuli triggered by pro-oxidant therapy. Although L-(S,R)-Buthionine Sulfoximine (BSO), a selective irreversible inhibitor of glutamate cysteine ligase, depletes GSH in vitro and in in vivo and sensitizes tumor cells to radiation and some cancer chemotherapeutics, its toxicity and short in vivo half-life have limited its application to combination anticancer therapies.
机译：背景：乳腺肠道（GSH），其是哺乳动物中主要的低分子量细胞内硫醇，具有多种功能，例如保护氧化应激和解毒内源和外源和外源性电子手术的那些。 已在各种类型的肿瘤中观察到的高GSH水平，已被认为有助于肿瘤细胞对通过氧化剂治疗引发的凋亡刺激的抗性。 虽然L-（S，R）-buthionine磺酰昔亚胺（BSO），谷氨酸半胱氨酸酶的选择性不可逆抑制剂，在体外和体内均匀，并敏感肿瘤细胞与辐射和一些癌症化学治疗剂，其毒性和体内含有短暂的一半 -Life将其应用于组合抗癌疗法。

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