抗体药物偶联物（Antibody-Drug Conjugates，简称ADC）是一种新型的靶向药物，将高效的小分子药物通过化学连接子与特异性抗体偶联在一起，实现靶向杀伤癌细胞。ADC技术结合了单克隆抗体的高靶向性和小分子药物的高杀伤力，能够在减少正常细胞损伤的同时，提高抗肿瘤治疗的效果。近年来，随着生物技术和化学合成技术的进步，...
参考文献: [1]Yamazaki, C.M., Yamaguchi, A., Anami, Y. et al. Antibody-drug conjugates with dual payloads for combating breast tumor heterogeneity and drug resistance. Nat Commun 12, 3528 (2021).https://doi.org/10.1038/s41467-021-23793-7 声明:研一的组会文献分享,原创解读。鉴于笔者知识...
[2] Chudasama V, Maruani A, Caddick S (2016) Recent advances in the construction of antibody–drug conjugates. Nat Chem 8(2):114–119 Nat Chem, 2016, 8, 114-119 [3] Chem Commun, 2012, 48, 7100–7102 [4] Bioconjug Chem, 2013, 24, 1650–1655 [5] Bioconjug Chem, 2015, 26, 223...
抗体偶联药物(Antibody–Drug Conjugates,ADC)是近年来各大药企合作和并购的焦点。ADC药物由单克隆抗体(mAb),具有细胞毒性的小分子药物(small molecule toxins),和连接二者的链接子(linker)构成。某种意义上来说,ADC药物可以说是化疗药物和抗体药物的结合。ADC分子可以利用抗体的高靶向性,选择性的富集到肿瘤细胞中,通过...
本次介绍的是一些双载荷ADC的相关文献,主要是为后边双载荷PDC药物的构建理清思路,铺垫基础。 双载荷ADC通过不同的构建方法对其药抗比(Drug-Antidiv Ratio, DAR)进行灵活调整,可以根据疾病类型及治疗目的微调ADC的理化特性、功效和毒性特征,充分利用ADC双药递送的优势,提高ADC活性;同时,在原子经济学的角度上可以减少...
Antibody–drug conjugates (ADCs) combine the specificity of monoclonal antibodies with the potency of highly cytotoxic agents, potentially reducing the severity of side effects by preferentially targeting their payload to the tumour site. ADCs are being increasingly used in combination with other agents,...
抗体药物以肿瘤细胞过度表达的抗原her2、EGFR、CD20, CD19, CD22, CD70等为靶点。 新靶点包括:SLC44A4(AGS-5), Mesothelin 等 多种治疗性单抗(曲妥单抗,西妥昔单抗,利妥昔单抗)。 靶向性强,但分子量大对于实体瘤治疗效果有限。 化学疗法: 烷化剂(氮芥等),抗体代谢剂(氨甲蝶呤等),抗肿瘤抗生素(阿霉素...
What are the components of antibody-drug conjugates? ADC drugs are composed of three parts: antibody, linker, and toxic payload. Antibody: The antibody is responsible for target engagement, it can be in form of Mab, Fab, Bispecific Ab or nanobody. Conjugate (Linker):Conjugates the payload to...
Antibody鈥揹rug conjugates (ADCs) are a relatively new class of anticancer agents designed to merge the selectivity of monoclonal antibodies with cell killing properties of chemotherapy. They are commonly described as the "Trojan Horses" of therapeutic armamentarium, because of their capability of ...
“Site-Specific Antibody−Drug Conjugates: The Nexus of Bioorthogonal Chemistry, Protein Engineering, and Drug Development” Agarwal, P.; Bertozzi, C. R.Bioconjugate Chem.2015,26, 176. DOI:10.1021/bc5004982(d) “Recent advances in the construction of antibody–drug conjugates” Chudasama, V.;...