Fig. 2: Inhibitor development.
From: Development of supramolecular anticoagulants with on-demand reversibility
a, Schematic representation of cooperative dynamic drug assembly. The inhibitors disclosed in this study are composed of two fragments: the active site-directed fragments, which are numbered A1 to A8, and the exosite II-directed fragments, which are numbered E1 to E23. Combination of the two fragments yields a potent inhibitor named as the combination of the two assembled fragments (for example, A1–E1 is the combination of active site fragment A1 and exosite II fragment E1). b, Thrombin inhibition data for the combined inhibitor versus the two fragments alone. c, Selectivity data for A1–E1 against a panel of common proteases. d, Effect of PNA length on inhibition. e, Structure–activity relationship data of the exosite II binder by different charge. f, Structure–activity relationship data of the exosite II binder by different hydrophobic amino acids instead of isoleucine. For all data, n = 3 replicates, with individual data points presented as mean values ± s.d., with the exception of the data in c where n = 2.
