Procopio Antonio, Alcaro Stefano, Cundari Sante, De Nino Antonio, Ortuso Francesco, Sacchetta Paolo, Pennelli Alfonso, Sindona Giovanni
Dipartimento di Scienze Farmaco-Biologiche, Università della Magna Graecia, Complesso Ninì Barbieri, 88021 Roccelletta di Borgia (Cz), Italy.
J Med Chem. 2005 Sep 22;48(19):6084-9. doi: 10.1021/jm0504609.
Changes in the GSH/GST system have been found to correlate with resistance to anticancer alkylating agents, presumably through accelerated detoxification of these drugs since some GSTs have been shown to catalyze the conjugation of GSH to specific antineoplastic agents. GSH-alkyl derivatives were designed by molecular modeling, synthesized, and tested as inhibitors of human GST-Pi.
已发现谷胱甘肽/谷胱甘肽S-转移酶（GSH/GST）系统的变化与对抗癌烷化剂的耐药性相关，这可能是由于这些药物的解毒作用加速，因为一些GST已被证明可催化谷胱甘肽与特定抗肿瘤药物的结合。通过分子模拟设计、合成了谷胱甘肽-烷基衍生物，并将其作为人GST-Pi的抑制剂进行了测试。
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