Issue 57, 2023

Regulation of thrombin activity by ligand-induced topological alteration in a thrombin-binding aptamer

Abstract

Thrombin-binding aptamer (TBA), which forms a G-quadruplex (G4) structure with anti-parallel topology, interacts with thrombin to inhibit its enzymatic activity. Here we show that the G4-topology-altering ligand L2H2-2M2EA-6LCO (6LCO) changes the anti-parallel topology of TBA G4 to the parallel topology, thereby abrogating the thrombin-inhibitory activity of TBA. This finding suggests that G4 ligands that alter topology may be promising drug candidates for diseases involving G4-binding proteins.

Graphical abstract: Regulation of thrombin activity by ligand-induced topological alteration in a thrombin-binding aptamer

Supplementary files

Article information

Article type
Communication
Submitted
12 May 2023
Accepted
17 Jun 2023
First published
21 Jun 2023

Chem. Commun., 2023,59, 8862-8865

Author version available

Regulation of thrombin activity by ligand-induced topological alteration in a thrombin-binding aptamer

S. Sasaki, Y. Ma, T. Hirokawa, K. Ikebukuro, M. Tera and K. Nagasawa, Chem. Commun., 2023, 59, 8862 DOI: 10.1039/D3CC02308G

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