Fig. 1: SPR-based fragment screening.
From: Regulation of cadherin dimerization by chemical fragments as a trigger to inhibit cell adhesion
a Illustration of the stepwise dimerization of P-cadherin to mediate cell adhesion and a schematic of the protein (EC12). b Schematic of fragment screening. The numbers in the parentheses show decreases in the number of fragment candidates. c Representative sensorgram from ABA assay. EC12, in monomer-S–S dimer equilibrium, was immobilized on Sensor Chip CM5. The decrease of response upon injection of solution B shows that the compound disrupted the dimer formed on the sensor chip. d Dose–response analysis of binding of Hit 1 to REC12 immobilized on Sensor Chip SA. The putative KD was calculated by the Scatchard method using the SPR responses in equilibrium. Note that the KD value is not reliable, since the binding response was not saturated even at the highest concentration of Hit 1. N = 3. e Chemical structure of Hit 1.
