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. 2021 Dec 24;12(5):2417–2428. doi: 10.1016/j.apsb.2021.12.013

Figure 5.

Figure 5

Synthesis of glycosite-specific ADCs using LacNAc-based substrates. (A) General procedure of one-step or two-step synthesis of gsADCs. (B) Small molecules used in gsADCs assembly. (C–E), LC‒MS profiles of Az-LacNAc-Tras 6a (C), gsADC-1 (D) and gsADC-2 (E). (F) SDS-PAGE of one-step synthesis of gsADC-2. Lane 0: protein marker; Lane 1: deglycosylated Tras (1a); Lane 2: gsADC-2. (G) Conjugation-site analysis of gsADC-2 via PNGase F digestion. (H) Antibody molecular weight of gsADC-2 after digestion with PNGase F. (I) HRMS profile of glycan–drug complex released from gsADC-2.