Figure 5.

Derivative analysis for the inhibition capacity to HBV infection and to NTCP-mediated bile acid uptake. (A) Chemical structures of NPD8716 analogs having significant anti-HBV activities. (B) HBV infection to primary human hepatocytes were examined essentially as described in Fig. 2A in the presence or absence of the indicated compounds (100 nM preS1 peptide, 270 μM NPD8716 and its analogs). HBV infection was monitored by detecting HBs antigen in the culture supernatant at 12 days postinfection. (C) NTCP-dependent bile acid uptake was evaluated as described in Fig. 4 with or without the indicated compounds (100 nM preS1 peptide, 270 μM NPD8716 and its analogs). (D) Kinetics for interaction of NPD8716 analogs to NTCP-His measured by SPR analysis as in Fig. 1D. Various concentrations (1.1, 3.3, 10, or 30 μM for purple, green, red, and blue) of NPD8716 analogs were injected over a sensor chip immobilized with NTCP-His protein.