School of Pharmacy, Sungkyunkwan University, Suwon 16419, South Korea.
AbTis Co., Ltd., A-815, Suwon Venture Valley II, 142-10, Saneop-ro 156beon-gil, Gwonseon-gu, Suwon 16648, South Korea.
Org Lett. 2020 Nov 6;22(21):8419-8423. doi: 10.1021/acs.orglett.0c03049. Epub 2020 Oct 19.
Antibody-drug conjugates (ADCs) in current clinical usage have been constructed via the nonspecific conjugation of drugs to antibodies, rendering the manufacturing processes difficult. In this study, a high-affinity IgG Fc-binding peptide equipped with a photoreactive amino acid was developed and successfully conjugated to Glu-382 of trastuzumab in a site-specific manner. The resulting conjugate was employed to generate a DAR 2 ADC product using click chemistry.
抗体偶联药物（ADCs）在当前临床应用中是通过将药物非特异性地连接到抗体上来构建的，这使得制造过程变得困难。在这项研究中，开发了一种具有高亲和力 IgG Fc 结合肽，并在其侧链上装备了一个光反应性氨基酸，成功地以位点特异性方式与曲妥珠单抗的 Glu-382 结合。所得到的偶联物被用于使用点击化学来生成一个 DAR2 ADC 产物。
