| 摘要 |
<P>PROBLEM TO BE SOLVED: To provide a plasmin inhibitor that is as potent as a bovine pancreatic trypsin inhibitor (BPTI), and almost identical to a human protein domain, thereby posing less potential for antigenicity. <P>SOLUTION: Human tissue factor pathway inhibitor-2 (TFPI-2), contains three Kunitz-type (similar to BPTI) domains in tandem with a short acidic amino terminus and very basic C-terminal tail. A polypeptide including the Kunitz-type domains is provided with one or more of the following substitutions: leucine is changed to arginine or lysine at position 17 (BPTI numbering); tyrosine is changed to glutamic acid at position 46; tyrosine is changed to threonine at position 11; aspartic acid is changed to tyrosine or glutamic acid at position 10; alanine is changed to methionine at position 16; alanine is changed to glycine at position 16; alanine is changed to serine at position 16. <P>COPYRIGHT: (C)2013,JPO&INPIT |
