A wide variety of drugs, drug delivery systems (DDS) that carry them, technologies, and treatment methodologies have been developed to treat cancer, and none of them have achieved full efficacy owing to several known and unknown factors. Glioblastoma multiforme (GBM), as grade IV brain tumors, have become an eminent threat in recent clinical practice. Inhibitors of apoptosis proteins (IAP) have been identified as an effective target to activate the apoptosis of cancer cells and overcome chemotherapy resistance. Now scientists/engineers are dealing with the hurdles to treating gliomas and how to overcome them with the development of target-specific DDS with active ligands. Further, this review discusses the importance of second mitochondria derived activator of caspase mimetics, interacting with siRNA, as IAP inhibitors that induce apoptosis of cancer cells, including gliomas. The combination of IAP antagonists with anticancer drugs has decreased the resistance to chemotherapeutic remedies. Moreover, biomaterial-based DDS have improved the activity of IAP antagonists by ameliorating their docking capacity and bioavailability in GBM. The development of DDS with active ligands carrying IAP antagonists and chemotherapeutic drugs becomes an essential issue for IAP in GBM targeting to enhance apoptosis, and that this can be an effective approach to GBM treatment.

已经开发出用于治疗癌症的各种各样的药物，载有它们的药物递送系统（DDS），技术和治疗方法，并且由于几种已知和未知因素，它们均未达到完全的功效。多形性胶质母细胞瘤（GBM），作为IV级脑肿瘤，已成为近期临床实践中的重大威胁。凋亡蛋白抑制剂（IAP）已被确定为激活癌细胞凋亡和克服化疗耐药性的有效靶标。现在，科学家/工程师正在研究治疗神经胶质瘤的障碍，以及如何通过开发具有活性配体的靶标特异性DDS来克服它们。此外，本文还讨论了第二个线粒体衍生的半胱天冬酶模拟物激活剂与siRNA相互作用的重要性，作为IAP抑制剂，可诱导包括神经胶质瘤在内的癌细胞凋亡。IAP拮抗剂与抗癌药的结合降低了对化学疗法的抵抗力。此外，基于生物材料的DDS通过改善IAP拮抗剂在GBM中的对接能力和生物利用度，提高了其活性。具有携带IAP拮抗剂和化学治疗药物的活性配体的DDS的开发成为GBP靶向IAP增强细胞凋亡的重要问题，这可能是GBM治疗的有效方法。