创新链/学科链/研发链/产业链

新药研发前沿动态 / 医药领域趋势进展

李明莹, 汪琳, 马宁宁. 定点偶联技术在抗体药物偶联物中的应用[J]. 药学进展, 2021, 45(3): 180-187.
引用本文: 李明莹, 汪琳, 马宁宁. 定点偶联技术在抗体药物偶联物中的应用[J]. 药学进展, 2021, 45(3): 180-187.
LI Mingying, WANG Lin, MA Ningning. Application of Site-specific Conjugation Techniques in Antibody-drug Conjugates[J]. Progress in Pharmaceutical Sciences, 2021, 45(3): 180-187.
Citation: LI Mingying, WANG Lin, MA Ningning. Application of Site-specific Conjugation Techniques in Antibody-drug Conjugates[J]. Progress in Pharmaceutical Sciences, 2021, 45(3): 180-187.

定点偶联技术在抗体药物偶联物中的应用

Application of Site-specific Conjugation Techniques in Antibody-drug Conjugates

  • 摘要: 化疗是肿瘤前期治疗的主要手段,化学药物在杀死肿瘤细胞的同时,也会对正常细胞造成杀伤作用。为使化学药物准确作用于病灶部位,抗体药物偶联物应运而生。传统的抗体药物偶联物是利用抗体的赖氨酸残基或还原抗体二硫键获得的巯基进行偶联,其偶联产物存在均一性差、稳定性低的弊端。利用定点偶联技术可获得高度均一性的抗体药物偶联物,保证生产过程批次间的重现性。对应用于抗体药物偶联物的几种定点偶联技术进行综述。

     

    Abstract: Chemotherapy is the main method of pre-tumor treatment, yet chemical drugs also kill normal cells while killing tumor cells. Antibody-drug conjugates (ADCs) were produced in order to ensure the precise action of chemical drugs on the lesion site. Traditional ADCs, which are conjugated using lysine residues of antibodies or sulfhydryl groups obtained by reducing the disulfide bond of antibodies, have the disadvantages of poor homogeneity and low stability. Highly homogeneous ADCs can be obtained using site-specific conjugation techniques to ensure reproducibility between batches in the manufacturing process. This paper reviews several site-specific conjugation techniques for ADCs.

     

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