TY - JOUR
T1 - Plasminogen activator inhibitor-1 inhibitors
T2 - A patent review (2006-present)
AU - Fortenberry, Yolanda M.
N1 - Funding Information:
This study was financially supported by a grant from the National Heart, Lung, and Blood Institute (NHLBI; HL096407). The authors state no conflict of interest and have received no payment in preparation of this manuscript.
PY - 2013/7
Y1 - 2013/7
N2 - Introduction: Plasminogen activator inhibitor-1 (PAI-1), the serine protease inhibitor (serpin), binds to and inhibits the plasminogen activators-tissue-type plasminogen activator (tPA) and the urokinase-type plasminogen activator (uPA). This results in both a decrease in plasmin production and a decrease in the dissolution of fibrin clots. Elevated levels of PAI-1 are correlated with an increased risk for cardiovascular disease and have been linked to obesity and metabolic syndrome. Consequently, the pharmacological suppression of PAI-1 might prevent or treat vascular disease. Areas covered: This article provides an overview of the patenting activity on PAI-1 inhibitors. Patents filed by pharmaceutical companies or individual research groups are described, and the biological and biochemical evaluation of the inhibitors, including in vitro and in vivo studies, is discussed. An overview of patents pertaining to using these inhibitors for treating various diseases is also included. Expert opinion: Although there is still no PAI-1 inhibitor being evaluated in a clinical setting or approved for human therapy, research in this field has progressed, and promising new compounds have been designed. Most research has focused on improving the pharmacological profile of these compounds, which will hopefully allow them to proceed to clinical studies. Despite the need for further testing and research, the potential use of PAI-1 inhibitors for treating cardiovascular disease appears quite promising.
AB - Introduction: Plasminogen activator inhibitor-1 (PAI-1), the serine protease inhibitor (serpin), binds to and inhibits the plasminogen activators-tissue-type plasminogen activator (tPA) and the urokinase-type plasminogen activator (uPA). This results in both a decrease in plasmin production and a decrease in the dissolution of fibrin clots. Elevated levels of PAI-1 are correlated with an increased risk for cardiovascular disease and have been linked to obesity and metabolic syndrome. Consequently, the pharmacological suppression of PAI-1 might prevent or treat vascular disease. Areas covered: This article provides an overview of the patenting activity on PAI-1 inhibitors. Patents filed by pharmaceutical companies or individual research groups are described, and the biological and biochemical evaluation of the inhibitors, including in vitro and in vivo studies, is discussed. An overview of patents pertaining to using these inhibitors for treating various diseases is also included. Expert opinion: Although there is still no PAI-1 inhibitor being evaluated in a clinical setting or approved for human therapy, research in this field has progressed, and promising new compounds have been designed. Most research has focused on improving the pharmacological profile of these compounds, which will hopefully allow them to proceed to clinical studies. Despite the need for further testing and research, the potential use of PAI-1 inhibitors for treating cardiovascular disease appears quite promising.
KW - Antagonist
KW - Inhibitors
KW - PAI-1
KW - Plasminogen
KW - Serpin
UR - http://www.scopus.com/inward/record.url?scp=84879333770&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84879333770&partnerID=8YFLogxK
U2 - 10.1517/13543776.2013.782393
DO - 10.1517/13543776.2013.782393
M3 - Review article
C2 - 23521527
AN - SCOPUS:84879333770
SN - 1354-3776
VL - 23
SP - 801
EP - 815
JO - Expert Opinion on Therapeutic Patents
JF - Expert Opinion on Therapeutic Patents
IS - 7
ER -