School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, China.
Department of Urology, Peking University Cancer Hospital, Beijing Institute for Cancer Research, Beijing, China.
Leuk Lymphoma. 2020 Jul;61(7):1660-1668. doi: 10.1080/10428194.2020.1728746. Epub 2020 Feb 24.
AKR1C3 overexpression has been reported in various types of cancers, including T-ALL. AST-006 (TH-3424), an AKR1C3-specific prodrug, was reported recently to have potent cytotoxicity against liver cancer cells overexpressing AKR1C3 and T-ALL. In this study, AST-006 demonstrated potent anti-tumor activity against different T-ALL cell lines and , including patient-derived xenograft (PDX) model. AST-006 also exhibited minimal cytotoxicity against primary human T-cells and lymphocytes in cynomolgus monkeys , indicating that AST-006 is a promising therapeutic for T-ALL.
AKR1C3 的过表达已在多种类型的癌症中被报道，包括 T-ALL。AST-006（TH-3424）是一种 AKR1C3 特异性前药，最近有报道称其对过表达 AKR1C3 的肝癌细胞和 T-ALL 具有很强的细胞毒性。在这项研究中，AST-006 对不同的 T-ALL 细胞系和 ，包括患者来源的异种移植（PDX）模型，表现出很强的抗肿瘤活性。AST-006 对原代人 T 细胞和食蟹猴的淋巴细胞的细胞毒性也很小 ，表明 AST-006 是一种有前途的 T-ALL 治疗药物。
