Plasminogen activators are proteins involved in the breakdown of blood clots. And an elevated level of plasminogen activator inhibitor-1 (PAI-1) is associated with an increased risk for cardiovascular disease and clotting.
No PAI-1 inhibitors are currently available for clinical use, but a novel therapeutic approach using a targeted RNA aptamer drug that has been shown to block PAI-1 activity and prevent PAI-1-associated vascular events is described in Nucleic Acid Therapeutics, a peer-reviewed journal from Nucleic Acid Therapeutics. The article is available free on the Nucleic Acid Therapeutics website.
Jared Damare, Stephanie Brandal, and Yolanda Fortenberry, Johns Hopkins University School of Medicine, Baltimore, MD, designed a library of small RNA molecules that target different regions of PAI-1. They then screened the library and enriched for the aptamers that were the most selective for binding to and inhibiting the function of PAI-1. The authors demonstrate the ability of these RNA aptamers to prevent PAI-1 from interacting with plasminogen activators in the article "Inhibition of PAI-1 Antiproteolytic Activity Against tPA by RNA Aptamers."
Nucleic Acid Therapeutics is under the editorial leadership of Co-Editors-in-Chief Bruce A. Sullenger, PhD, Duke Translational Research Institute, Duke University Medical Center, Durham, NC, and C.A. Stein, MD, PhD, City of Hope National Medical Center, Duarte, CA; and Executive Editor Graham C. Parker, PhD.