microtubule-targeted

Maytansine (NSC-153858) 是从变叶美登木中分离的一种高效微管靶向天然产物，可诱导有丝分裂阻滞并在亚纳摩尔浓度杀死肿瘤细胞。

Mal-PEG2-VCP-Eribulin is a chemotherapeutic compound comprising an antibody-drug conjugate (ADC) linker (Mal-PEG2-VCP) and the microtubule inhibitor Eribulin[1]. This compound uniquely targets microtubules, offering a novel approach to cancer treatment. Eribulin is specifically utilized in creating targeted Eribulin-based drugs for antibody conjugates[1].

Tubulin Polymerization-IN-1 prodrug (Compound 2b) 是一种通过Pd-介导的微管蛋白聚合抑制剂前药。它基于秋水仙碱结合位点抑制剂 (CBSIs) 设计，通过降低毒性和提升靶向释放性能。相较于母体化合物，Tubulin Polymerization-IN-1 prodrug 的细胞毒性减少了68.3倍，但在存在Pd树脂时，可原位恢复其细胞毒性。机制研究显示，其抗肿瘤活性与CBSIs一致。在体内实验中，经Pd树脂激活后，Tubulin Polymerization-IN-1 prodrug 能明显抑制肿瘤生长（抑制率63.2%）。该化合物在抗癌研究中展现出潜在应用前景。

Trastuzumab emtansine (Ado-Trastuzumab emtansine) is an antibody-drug conjugate (ADC) that combines the HER2-targeted antitumor properties of trastuzumab with the cytotoxic activity of DM1, a microtubule-inhibitory derivative of maytansine. This compound is utilized in the investigation of advanced breast cancer[1][2].

Epofolate is folate receptor-targeting antimitotic agent with potential antineoplastic activity. Folate receptor-targeted epothilone BMS753493 contains an epothilone moiety linked to a single folate molecule. Mediated through the folate moiety, this agent delivers the antimitotic epothilone component into cells expressing folic acid receptors, frequently upregulated in many types of tumor cells. After ligand-receptor internalization, the epothilone moiety induces microtubule polymerization and stabilizes microtubules against depolymerization, resulting in the inhibition of mitosis and cellular proliferation. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Zilovertamab vedotin (VLS-101) 是一种抗体-活性分子偶联物 (ADC), 主要由人源化单克隆抗体 zilovertamab 和单甲基 vedotin 组成的抗微管细胞毒素。该药物通过与肿瘤细胞表面的ROR1结合, 触发快速内化及向溶酶体的转运, 进而裂解释放单甲基 vedotin, 诱导细胞凋亡。适用于癌症的研究领域。

Naratuximab emtansine (IMGN529) 作为一种针对CD37的ADC，由人源化IgG1 mAb和微管破坏剂DM1耦合而成。该药物对CD37具有高度的亲和性与特异性，能有效地促进DM1的内化、处理及在细胞内的释放。DM1的作用机制在于干扰微管结构的组装，进而诱导细胞周期停滞及细胞死亡（apoptosis）。