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蛋白酶体抑制剂(proteasom e inh ib itor)通过抑制26S蛋白酶体活性,激活胱冬肽酶(caspase)-3诱导凋亡,抑制核因子(NF)-κB依赖性基因转录,影响细胞内多种信号级联,破坏维持机体正常内稳态的机制导致肿瘤细胞生长延迟或死亡。V e lcade(化学名Bortezom ib,前用名PS-341)是美国FDA批准的第一个已供临床应用的蛋白酶体抑制剂。临床用于治疗初治或复发性、难治性多发性骨髓瘤,其次为造血组织恶性肿瘤及进展性实体瘤等显示具有良好的抗瘤活性,安全性好,不良反应少。其临床应用研究正在迅速扩展中。
Proteasome e inh ib itor activates caspase-3-induced apoptosis by inhibiting 26S proteasome activity, inhibits nuclear factor (NF) -κB-dependent gene transcription and affects multiple intracellular Signaling cascades, disrupting the mechanisms that maintain normal homeostasis in the body, lead to the delay or death of tumor cells. Vedecade (chemical name Bortezom ib, formerly known as PS-341) is the first FDA-approved proteasome inhibitor approved by the U.S. FDA. Clinical for the treatment of naive or recurrent, refractory multiple myeloma, followed by hematopoietic tissue malignancies and solid tumors showed good anti-tumor activity, good safety, fewer adverse reactions. Its clinical application research is rapidly expanding.