Aptamer-based modulation of blood coagulation

Summary

Nucleic acid based aptamers are singlestranded oligonucleotide ligands isolated from random libraries by an in-vitro selection procedure. Through the formation of unique three-dimensional structures, aptamers are able to selectively interact with a variety of target molecules and are therefore also promising candidates for the development of anticoagulant drugs. While thrombin represents the most prominent enzymatic target in this field, also aptamers directed against other coagulation proteins and proteases have been identified with some currently being tested in clinical trials.

In this review, we summarize recent developments in the design and evaluation of aptamers for anticoagulant therapy and research.

Zusammenfassung

Auf Nukleinsäuren basierende Aptamere sind einzelsträngige Oligonukleotide, die durch einen In-vitro-Selektionsprozess aus randomisierten Nukleinsäurebibliotheken isoliert werden. Aufgrund ihrer dreidimensionalen Struktur können Aptamere selektiv mit diversen Zielmolekülen interagieren und repräsentieren somit eine viel versprechende Substanzklasse für die Entwicklung von Antikoagulanzien. Neben Thrombin, dem bisher am häufigsten verwendeten Zielmolekül in diesem Anwendungsgebiet, wurden Aptamere auch für andere Proteine und Proteasen aus der Blutgerinnungskaskade selektiert. Einige dieser Moleküle durchlaufen bereits klinische Studien.

In diesem Übersichtsartikel fassen wir die neuesten Entwicklungen hinsichtlich des Designs und der Evaluierung von Aptameren in den Gebieten der antikoagulatorischen Therapie und der Forschung zusammen.

Keywords

Aptamer - SELEX - coagulation - photo-control

Schlüsselwörter

Aptamere - SELEX - Blutgerinnung - Licht-kontrolle

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