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. 2019 Mar 6;7:113. doi: 10.3389/fchem.2019.00113

Figure 4.

Figure 4

Oxime and CuAAC ligations for modular synthesis of bispecific ISErs. (A) An aldehyde-bearing EphA2-binding peptide was generated from the corresponding N-terminal serine-bearing precursor by oxidation using NaIO4. This binder peptide was ligated to the effector-PEG27 scaffold using oxime ligation and then an azide-bearing integrin α3β1 binding peptide was ligated using CuAAC ligation. MS and analytical HPLC of the bivalent bispecific ISEr product. MWcalc: 6819.9 Da, MWobs: 6818.5 Da. (B) Aldehyde-bearing EphA2 binders were ligated to the effector-PEG27 scaffold using oxime ligation followed by azide-bearing integrin α3β1 binding peptides using CuAAC ligation. MS and analytical HPLC of the tetravalent bispecific ISEr product. MWcalc: 10335.8 Da, MWobs: 10338.5 Da.