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Tfpi inhibitors and methods of use
专利权人:
Baxter Healthcare S.A.
发明人:
Hartmann Rudolf,Polakowski Thomas,Osterkamp Frank,Scheiflinger Friedrich,Fries Markus,Ehrlich Hartmut,Reineke Ulrich,Dockal Michael
申请号:
NZ71043411
公开号:
NZ710434A
申请日:
2011.02.11
申请国别(地区):
NZ
年份:
2017
代理人:
摘要:
Disclosed is a method for identifying a TFPI-binding compound, the method comprising (a) contacting a peptide comprising TFPI Kunitz domain 1 (KD1) with a TFPI-binding peptide and a test compound under conditions that allow formation of KD1-TFPI-binding peptide complexes, wherein the TFPI-binding peptide comprising the structure as herein defined (b) measuring KD1-TFPI-binding peptide complexes formed in step (a) and (c) comparing the number of KD1-TFPI-binding peptide complexes formed in the presence of the test compound with the number of KD1-TFPI-binding peptide complexes formed in the absence of the test compound, wherein a reduction in the number of KD1-TFPI-binding peptide complexes formed in the presence of the test compound compared to the number of KD1-TFPI-binding peptide complexes formed in the absence of the test compound indicates that the test compound is a TFPI-binding compound. Further disclosed is a method for identifying a TFPI-binding compound, the method comprising (a) contacting a peptide comprising TFPI Kunitz domain 1 (KD1) with a test compound, and (b) detecting binding of the test compound to a TFPI binding site defined by KD1 amino acid residues corresponding to human TFPI residues Phe28, Lys29, Ala30, Asp32, Ile46, Phe47, and Ile55.
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