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. 2022 Jul 12;65(14):9858–9872. doi: 10.1021/acs.jmedchem.2c00505

Figure 2.

Figure 2

Chemical structures of representative CD137 and Nectin-4 Bicycles and linkers used in the synthesis of Bicycle TICAs. (A) Structure of CD137-binding bicycle (left). One of the three positions highlighted was modified to incorporate nucleophilic amine containing amino acids (Lys3, dLys4, C-terminal Dap). Nectin-4-binding Bicycle (right) with N-terminal amine or dAsp3 → dLys3 substitution used for conjugation highlighted. (B) Structure of four linkers used to assess the impact of linker length on the potency of Bicycle TICAs. Dashed bonds represent the attachment point to Nectin-4- or CD137-binding Bicycle via an amide bond.