ALPHA-1-ANTITRYPSIN AND ANTITHROMBINE-III VARIANTS

摘要

Serine protease inhibitors (serpins) are provided which: (a) are substantially incapable of inhibiting activated protein C; (b) do not require activation by heparin; and (c) comprise a target sequence capable of interacting with the proteolytic active site of thrombin thereby to inhibit the proteolytic activity of thrombin. Preferred serpins are muteins or variants of alpha 1-antitrypsin, modified by inclusion of a thrombin-specific target sequence derived from antithrombin-III (AT-III). Such serpins have the specificity and irreversibility of action of AT-III, but do not have to be co-administered with heparin.