Plasminogen activator inhibitor 1 mRNA (PAI-1 mRNA)

Plasminogen activator inhibitor 1 (PAI-1) mRNA, encoded by the SERPINE1 gene, is a critical regulatory molecule in the human fibrinolytic system (UniProt P05121). The protein product of this mRNA serves as the primary inhibitor of tissue-type plasminogen activator (tPA) and urokinase-type plasminogen activator (uPA), thereby preventing the conversion of plasminogen to plasmin (PubMed PMID: 28330901). By suppressing plasmin generation, PAI-1 effectively inhibits the dissolution of fibrin clots and influences extracellular matrix remodeling (PubMed PMID: 30135140). Pathologically elevated levels of SERPINE1 mRNA are strongly linked to thrombotic disorders, cardiovascular disease, and various fibrotic conditions, including chronic kidney disease and pulmonary fibrosis (PubMed PMID: 27563816). In oncology, high expression of this target is associated with tumor progression, angiogenesis, and poor patient prognosis (PubMed PMID: 25213795). Therapeutic strategies targeting SERPINE1 mRNA utilize antisense oligonucleotides (ASOs) or small interfering RNAs (siRNAs) to reduce PAI-1 protein synthesis at the pre-translational level (Ionis Pharmaceuticals). For instance, IONIS-PAI-1Rx (ION-649) is an experimental ASO designed to lower systemic PAI-1 levels to treat fibrotic and vascular diseases (ClinicalTrials.gov). This approach aims to restore fibrinolytic balance and mitigate tissue scarring without the limitations of direct protein inhibition.

Other names

SERPINE1 mRNASerpin family E member 1 mRNAEndothelial plasminogen activator inhibitor mRNAPLANH1 mRNA

Antisense oligonucleotide-mediated degradation of mRNA via RNase H recruitment