Challenges Faced with Small Molecular Modulators of Potassium Current Channel Isoform Kv1.5

Figures

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  Figure 1. (A) Schematic representation of the hKv1.5 α-subunit with the sequence of the S6 region listed. (B) Homologous model of Kv1.5 (Q61672) with 67.2% similarity for the Kv1.5 sequence, obtained from the SWISS-MODEL database; some of the residues are slightly different from those published in previous research. (C) Basic Local Alignment Search Tool (BLAST) result of KCNA5_HUMAN (P22460), obtained from the NCBI BLAST+ database. (D) Sequence alignment ofKCNA1_HUMAN (Q09470), KCNA3_HUMAN (P22001), KCNA2_HUMAN (P16389), and KCNA5_HUMAN (P22460), acquired from the ESPript database.

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  Figure 2. (A) Pharmacophore model of vernakalant (cyan ball: hydrophobic center; yellow ball: aromatic center; green ball: hydrogen bond receptor; pink ball: hydrogen bond donor; red ball: ionizable positive center); (B) potential binding domain of vernakalant in Kv1.5 (H-bond is expressed as green dashed).

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  Figure 3. Biphenyl derivatives.

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  Figure 4. Anthranilic amides.

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  Figure 5. Phenoxyalkoxypsoralen analogues.

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  Figure 6. (2-phenethyl-2H-1,2,3-triazol-4-yl)(phenyl) methanones.

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  Figure 7. Tetrahydroindolone-derived carbamates.

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  Figure 8. Tetrahydroindolone-derived semicarbazones.

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  Figure 9. Diisopropyl amide derivatives.

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  Figure 10. Isoquinoline-3-nitriles.

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  Figure 11. Psoralen derivatives.

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  Figure 12. Thiazolidine derivatives.