Ontology highlight
ABSTRACT:
SUBMITTER: Li SH
PROVIDER: S-EPMC3870673 | biostudies-literature | 2013 Dec
REPOSITORIES: biostudies-literature
Li Shih-Hon SH Reinke Ashley A AA Sanders Karen L KL Emal Cory D CD Whisstock James C JC Stuckey Jeanne A JA Lawrence Daniel A DA
Proceedings of the National Academy of Sciences of the United States of America 20131202 51
Plasminogen activator inhibitor type-1 (PAI-1) is a member of the serine protease inhibitor (serpin) family. Excessive PAI-1 activity is associated with human disease, making it an attractive pharmaceutical target. However, like other serpins, PAI-1 has a labile structure, making it a difficult target for the development of small molecule inhibitors, and to date, there are no US Food and Drug Administration-approved small molecule inactivators of any serpins. Here we describe the mechanistic and ...[more]