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靶向凋亡抑制蛋白(IAPs)用于癌症治疗。

Targeting inhibitor of apoptosis proteins (IAPs) for cancer therapy.

作者信息

Fulda Simone

机构信息

University Children's Hospital, Eythstr. 24, 89075 Ulm, Germany.

出版信息

Anticancer Agents Med Chem. 2008 Jun;8(5):533-9. doi: 10.2174/187152008784533107.

DOI:10.2174/187152008784533107
PMID:18537535
Abstract

Since cell death by apoptosis plays a key role in the regulation of tissue homeostasis, dysregulation of the cell's intrinsic death program may foster tumor formation and progression. "Inhibitor of apoptosis proteins" (IAPs) block apoptosis at the core of the apoptotic machinery by inhibiting effector caspases. Aberrant expression and/or function of IAPs are found in many human cancers and have been implied in resistance to current treatment approaches. Recent insights into the role of IAPs have provided the basis for various exciting discoveries that aim at modulating expression or function of IAPs. Thus, targeting IAPs, e.g. by antisense approaches or small molecule inhibitors, presents a promising novel approach for future drug development and may proof to be a successful strategy to overcome apoptosis resistance of human cancers.

摘要

由于细胞凋亡在组织稳态调节中起关键作用,细胞内在死亡程序的失调可能促进肿瘤的形成和进展。“凋亡抑制蛋白”(IAPs)通过抑制效应半胱天冬酶在凋亡机制的核心部位阻断细胞凋亡。IAPs的异常表达和/或功能在许多人类癌症中都有发现,并与对当前治疗方法的耐药性有关。最近对IAPs作用的深入了解为旨在调节IAPs表达或功能的各种令人兴奋的发现提供了基础。因此,通过反义方法或小分子抑制剂靶向IAPs,为未来药物开发提供了一种有前景的新方法,并且可能被证明是克服人类癌症凋亡抗性的成功策略。

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