《生命科学》 2019, 31(3): 241-247

基于力达霉素的靶向药物与肿瘤治疗

徐　珊1，2，王艳林1*

(1 三峡大学医学院，肿瘤微环境与免疫治疗湖北省重点实验室，宜昌 443002；2 宜昌市疾病预防控制中心，宜昌 443000)

摘　要：摘　要：作为一种抗肿瘤抗生素，力达霉素(lidamycin， LDM) 对人类癌细胞显示出很强的细胞毒性。LDM由一个载体蛋白(LDP) 和一个具有肿瘤杀伤活性的烯二炔发色团(AE) 以非共价键方式组合而成，这一特征使得LDM 成为构建肿瘤靶向药物的良好材料。通过基因重组技术将具有肿瘤靶向能力的蛋白质和( 或) 多肽与LDP 偶联，由此获得具有肿瘤靶向能力的融合蛋白，在此基础上，再将AE 整合到融合蛋白的LDP 中，最终得到既具有肿瘤靶向能力，又具有LDM 杀伤活性的肿瘤靶向药物。随着研究的逐步深入，可望有一批基于LDM 的靶向药物能用于肿瘤的临床治疗。

Lidamycin-based targeting drugs and tumor therapy

XU Shan1，2， WANG Yan-Lin1*

(1 Hubei Key Laboratory of Tumor Microenvironment and Immunotherapy， Medical College of China Three Gorges University， Yichang 443002， China; 2 Yichang Center for Disease Control and Prevention， Yichang 443000， China)

Abstract: Abstract: As an anti-tumor antibiotic， lidamycin (LDM) has strong cytotoxicity to human cancer cells. LDM is composed of a carrier protein (LDP) and an active enediyne chromophore (AE) which has tumor-killing activity. LDP combines AE in a non-covalent manner， which makes LDM a good material for constructing tumor-targeting drugs. The tumor targeting fusion proteins could be obtained by coupling the proteins and/or peptide that have tumor targeting ability with LDP through gene recombination technology. And then， AE was integrated into the LDP of the fusion protein， which would finally produce the tumor targeting drugs with both tumor targeting ability and killing activity. With the deepening of research， it is expected that a number of LDM-based targeting drugs can be used in the clinical treatment of cancers.