title: Plasminogen Activator Inhibitor-1 in Cancer: Rationale and Insight for Future Therapeutic Testing.
abstract: Despite its function as an inhibitor of urokinase and tissue-type plasminogen activator (PA), PA inhibitor-1 (PAI-1) has a paradoxical protumorigenic role in cancer, promoting angiogenesis and tumor cell survival. In this review, we summarize preclinical evidence in support of the protumorigenic function of PAI-1 that has led to the testing of small-molecule PAI-1 inhibitors, initially developed as antithrombotic agents, in animal models of cancer. The review discusses the challenges and the opportunities that lay ahead to the development of efficacious and nontoxic PAI-1 inhibitors as anticancer agents.
authors.affiliation: Division of Hematology, Oncology and Blood and Bone Marrow Transplantation, Department of Pediatrics, University of Southern California, Los Angeles, California. The Saban Research Institute of Children's Hospital Los Angeles, Los Angeles, California.
authors.forename: Veronica R
authors.initials: VR
authors.lastname: Placencio
authors.affiliation: Division of Hematology, Oncology and Blood and Bone Marrow Transplantation, Department of Pediatrics, University of Southern California, Los Angeles, California. The Saban Research Institute of Children's Hospital Los Angeles, Los Angeles, California. Department of Biochemistry and Molecular Biology, University of Southern California, Los Angeles, California. declerck@usc.edu.
authors.forename: Yves A
authors.initials: YA
authors.lastname: DeClerck
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D017209:Apoptosis / Q000502:physiology; D004195:Disease Models, Animal; D006801:Humans; D051379:Mice; D058990:Molecular Targeted Therapy / Q000379:methods*; D009369:Neoplasms / Q000188:drug therapy / Q000473:pathology; D009389:Neovascularization, Pathologic / Q000188:drug therapy; D017395:Plasminogen Activator Inhibitor 1 / Q000378:metabolism* / Q000502:physiology
chemical_list: D000970:Antineoplastic Agents; D017395:Plasminogen Activator Inhibitor 1; C051321:SERPINE1 protein, human