FIGURE 4.

CT‐001 binding affinities to sEPCR and flTF are not altered but are lowered toward sTF versus WT FVIIa. sEPCR, flTF, and sTF sEPCR were immobilized on sensor chips, and FVIIa variants of varying concentrations were injected over the surface of flow cells. The substitution of amino acids (P10Q, K32E, T106 N, V253 N) in CT‐001(Sial) led to lower K_Ds toward sEPCR, flTF, and sTF relative to WT FVIIa. The desialylation of CT‐001(Sial) to become CT‐001appears to restore some of the lowered affinity of the molecule towards sEPCR, flTF, and sTF. This increase in affinity by desialyation was also observed in dWT FVIIa in comparison to WT FVIIa. dWT, desialylated wild‐type; flTF, full‐length tissue factor; FVIIa, activated factor VII; sEPCR, soluble endothelial protein C receptor; sTF, soluble tissue factor; WT, wild‐type