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Compound class:
Endogenous peptide in human, mouse or rat
Comment: TFPI is a serine protease inhibitor that regulates the tissue factor (TF)-dependent blood coagulation pathway (extrinsic pathway). It inhibits activated factor X (Xa) and VIIa-TF proteases in an autoregulatory loop. Some isoforms are tethered to the cell membrane by expression of a glycosylphosphatidylinositol (GPI) anchor, others isoforms are secreted [1-2]. Inhibition of the TFPI restores hemostasis, which is a mechanism being exploited for therapeutic benefit in inherited bleeding disorders.
Species: Human
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| References |
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1. Hansen L, Petersen LC, Lauritzen B, Clausen JT, Grell SN, Agersø H, Sørensen BB, Hilden I, Almholt K. (2014)
Target-mediated clearance and bio-distribution of a monoclonal antibody against the Kunitz-type protease inhibitor 2 domain of Tissue Factor Pathway Inhibitor. Thromb Res, 133 (3): 464-71. [PMID:24393663] |
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2. Hilden I, Lauritzen B, Sørensen BB, Clausen JT, Jespersgaard C, Krogh BO, Bowler AN, Breinholt J, Gruhler A, Svensson LA et al.. (2012)
Hemostatic effect of a monoclonal antibody mAb 2021 blocking the interaction between FXa and TFPI in a rabbit hemophilia model. Blood, 119 (24): 5871-8. [PMID:22563084] |
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3. Parng C, Singh P, Pittman DD, Wright K, Leary B, Patel-Hett S, Rakhe S, Stejskal J, Peraza M, Dufield D et al.. (2018)
Translational Pharmacokinetic/Pharmacodynamic Characterization and Target-Mediated Drug Disposition Modeling of an Anti-Tissue Factor Pathway Inhibitor Antibody, PF-06741086. J Pharm Sci, 107 (7): 1995-2004. [PMID:29571739] |
