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

Thrombin / chemistry Ligands Aptamers, Nucleotide / chemistry G-Quadruplexes

Journal

Chemical communications (Cambridge, England)
ISSN: 1364-548X
Titre abrégé: Chem Commun (Camb)
Pays: England
ID NLM: 9610838

Informations de publication

Date de publication:
13 Jul 2023
Historique:
medline: 17 7 2023
pubmed: 28 6 2023
entrez: 28 6 2023
Statut: epublish

Résumé

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.

Identifiants

DOI: 10.1039/d3cc02308g PMID: 37377065
pubmed: 37377065
doi: 10.1039/d3cc02308g
doi:

Substances chimiques

thrombin aptamer 145563-68-4
Thrombin EC 3.4.21.5
Ligands 0
Aptamers, Nucleotide 0

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

8862-8865

Auteurs

Shogo Sasaki (S)

Department of Biotechnology and Life Science, Tokyo University of Agriculture and Technology, 2-24-16 Naka-cho, Koganei, Tokyo 184-8588, Japan. knaga@go.tuat.ac.jp.

Yue Ma (Y)

Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, 2-3-10 Kanda-Surugadai, Chiyoda-ku, Tokyo 101-0062, Japan.
Research Core Center, Tokyo Medical and Dental University, 1-5-45 Yushima, Bunkyo-ku, Tokyo 113-8510, Japan.

Takatsugu Hirokawa (T)

Transborder Medical Research Center, University of Tsukuba, Tsukuba, 1-1-1 Tennodai, Tsukuba, Ibaraki 305-8575, Japan.
Division of Biomedical Science, Faculty of Medicine, University of Tsukuba, Tsukuba, 1-1-1 Tennodai, Tsukuba, Ibaraki 305-8575, Japan.

Kazunori Ikebukuro (K)

Department of Biotechnology and Life Science, Tokyo University of Agriculture and Technology, 2-24-16 Naka-cho, Koganei, Tokyo 184-8588, Japan. knaga@go.tuat.ac.jp.

Masayuki Tera (M)

Department of Biotechnology and Life Science, Tokyo University of Agriculture and Technology, 2-24-16 Naka-cho, Koganei, Tokyo 184-8588, Japan. knaga@go.tuat.ac.jp.
ORCID: 0000-0003-4430-579X

Kazuo Nagasawa (K)

Department of Biotechnology and Life Science, Tokyo University of Agriculture and Technology, 2-24-16 Naka-cho, Koganei, Tokyo 184-8588, Japan. knaga@go.tuat.ac.jp.
ORCID: 0000-0002-0437-948X

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Classifications MeSH

questionsmedicales.fr › Facteurs biologiques › Facteurs de la coagulation sanguine › Thrombine › Regulation of thrombin activity by...
questionsmedicales.fr › Actions chimiques et utilisations › Utilisations spécialisées de produits chimiques › Produits chimiques de laboratoire › Ligands › Regulation of thrombin activity by...
questionsmedicales.fr › Acides nucléiques, nucléotides et nucléosides › Nucléotides › Polynucléotides › Oligonucléotides › Aptamères nucléotidiques › Regulation of thrombin activity by...
questionsmedicales.fr › Phénomènes génétiques › Structures génétiques › Conformation d'acide nucléique › G-quadruplexes › Regulation of thrombin activity by...