发明名称 Tfpi inhibitors and methods of use
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.
申请公布号 NZ710434(A) 申请公布日期 2017.01.27
申请号 NZ20110710434 申请日期 2011.02.11
申请人 Baxter Healthcare S.A.;Baxter International Inc. 发明人 Hartmann Rudolf;Polakowski Thomas;Osterkamp Frank;Scheiflinger Friedrich;Fries Markus;Ehrlich Hartmut;Reineke Ulrich;Dockal Michael
分类号 A61K38/18;A61K38/16;C40B40/10 主分类号 A61K38/18
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