The ubiquitin-proteasome pathway plays a central role in the targeted destruction of cellular proteins, including cell cycle regulatory proteins. Because these pathways are critical for the proliferation and survival of all cells, and in particular cancerous cells, proteasome inhibition is a potentially attractive anticancer therapy. Based on encouraging cytotoxic activity, bortezomib was the first proteasome inhibitor to be evaluated in clinical trials. Efficacy and safety results from a phase 2 clinical trial contributed to approval of bortezomib for use in patients with relapsed and refractory multiple myeloma who have received at least 2 prior therapies and have demonstrated disease progression on their last therapy.

中文翻译：

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蛋白酶体抑制剂作为抗癌药的发展。

泛素-蛋白酶体途径在靶向破坏细胞蛋白（包括细胞周期调节蛋白）中起着核心作用。由于这些途径对于所有细胞，特别是癌细胞的增殖和存活至关重要，因此蛋白酶体抑制是一种潜在的有吸引力的抗癌疗法。基于令人鼓舞的细胞毒性活性，硼替佐米是首个在临床试验中评估的蛋白酶体抑制剂。一项2期临床试验的疗效和安全性结果促使硼替佐米被批准用于复发性和难治性多发性骨髓瘤患者，这些患者已接受过至少2种先前的治疗，并在最近的治疗中证明其疾病进展。