A Novel Inhibitor of Plasminogen Activator Inhibitor-1 Provides Antithrombotic Benefits Devoid of Bleeding Effect in Nonhuman Primates

Inhibition of plasminogen activator inhibitor (PAI)-1 is useful to treat several disorders including thrombosis. An inhibitor of PAI-1 (TM5275) was newly identified by an extensive study of structure-activity relationship based on a lead compound (TM5007) which was obtained through virtual screening...

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Veröffentlicht in:	Journal of cerebral blood flow and metabolism 2010-05, Vol.30 (5), p.904-912
Hauptverfasser:	Izuhara, Yuko, Yamaoka, Nagahisa, Kodama, Hidehiko, Dan, Takashi, Takizawa, Shunya, Hirayama, Noriaki, Meguro, Kanji, van Ypersele de Strihou, Charles, Miyata, Toshio
Format:	Artikel
Sprache:	eng
Schlagworte:	4-Aminobenzoic Acid - chemical synthesis 4-Aminobenzoic Acid - chemistry 4-Aminobenzoic Acid - pharmacology 4-Aminobenzoic Acid - therapeutic use Animals Biological and medical sciences Blood. Blood coagulation. Reticuloendothelial system Cynomolgus Disease Models, Animal Drug Design Female Fibrinolytic Agents - chemical synthesis Fibrinolytic Agents - chemistry Fibrinolytic Agents - pharmacology Fibrinolytic Agents - therapeutic use Hemorrhage - drug therapy Humans Macaca fascicularis Male Medical sciences Mice Models, Molecular Molecular Structure Neurology Original para-Aminobenzoates Pharmacology. Drug treatments Piperazines - chemical synthesis Piperazines - chemistry Piperazines - pharmacology Piperazines - therapeutic use Plasminogen Activator Inhibitor 1 - chemistry Plasminogen Activator Inhibitor 1 - metabolism Primates Protein Conformation Rats Rats, Sprague-Dawley Rats, Wistar Serine Proteinase Inhibitors - chemistry Serine Proteinase Inhibitors - metabolism Structure-Activity Relationship Thrombosis - drug therapy Ticlopidine - pharmacology Ticlopidine - therapeutic use Tissue Plasminogen Activator - therapeutic use Vascular diseases and vascular malformations of the nervous system
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