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industry
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furin may be applied in mass production of a potent antimicrobial peptide histonin as a natural form, whereby overcoming its inherent toxicity and the low yield of production
pharmacology
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development of an immunoproapoptotic molecule with antitumor activity: Her2-antigen e23sFv-TD-tBID with a 10-amino acid residue furin cleavage sequence. e23sFv-TD-tBID shows therapeutic value to humans by its cytotoxic effects on primary patient-derived breast tumor cells but not on endothelial cells. It also shows in vivo antitumor activity in female BALB/c athymic mice, overview
analysis
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bioluminogenic probes can specifically image furin activity in xenografted breast cancer tumors in mice
analysis
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sensitive and specific assay for furin activity using an antibody capture step to immobilise furin from whole cell lysates. The assay has a minimum detection limit of 0.006 nM and is sensitive enough to determine the furin activity of many of the cell lines tested
drug development
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extensive clinical use, high bioavailability and relatively low toxicity of dicoumarols suggests that the dicoumarol structure will be a good starting point for development of drug-like inhibitors of furin and other proprotein convertases that can act both intracellularly and at the cell surface
drug development
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good prospect of using quantitative structure-activity relationship models for the rational design of novel therapeutic furin inhibitors toward anthrax and furin-dependent diseases
drug development
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furin is considered a major target for intervention of cancer, tumorgenesis, viral and bacterial pathogenesis
drug development
furin inhibitors are promising therapeutics for the treatment of cancer and numerous infections caused by bacteria and viruses, including the highly lethal Bacillus anthracis or the pandemic influenza virus
drug development
the activation of viral glycoproteins by the host protease furin is an essential step in the replipation of numerous pathogenic viruses. Thus, effective inhibitors of furin can serve as broad-spectrum antiviral drugs, rational design of various types of cyclic inhibitors
drug development
the deglycosylated active recombinant enzyme can be used for structure-guided drug discovery
medicine
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potential therapeutic value of furin inhibitors, alpha1-PDX is able to block in vivo maturation of pro-gB, the cytomegalovirus envelope glycoprotein
medicine
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copper and zinc complexes of terpyridine derivatives are stable under various conditions and are not expected to pose delivery problems, qualities vital for the development of a wide-scope anti-bioterror agent for civil and military uses
medicine
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cell-to-cell spread of Borna disease virus requires neither the expression of cellular receptors involved in virus primary infection, nor the furin-mediated processing of Borna disease virus glycoprotein
medicine
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furin is predominantely expressed in tumors from patients surviving less than five years. Furin may constitute a marker for ovarian tumor progression and may contribute to predict the outcome of the disease
medicine
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furin-like protease activity may be involved in mediating host-parasite interactions. Inhibition of infection is due to an effect on the parasite-derived furin activity rather than the host cell furin
medicine
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inhibiting furin-like proprotein convertases protects the host from the distinct furin-dependent infections and lay a foundation for novel, host cell-focused therapies against acute diseases
medicine
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inhibiting furin-like proprotein convertases protects the host from the distinct furin-dependent infections and lay a foundation for novel, host cell-focused therapies against acute diseases
medicine
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interleukin 12 induction of furin plays a role in interferon gamma protein regulation and control of T helper 1 cell differentiation
medicine
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interleukin 12 induction of furin plays a role in interferon gamma protein regulation and control of T helper 1 cell differentiation
medicine
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introduction of a prototypic furin recognition motif at R667 of the SARS coronavirus spike glycoprotein allows for efficient cleavage of the mutant glycoprotein and increases cell-cell fusion activity but shows no effect on virion infectivity
medicine
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massive vaccination of host poultry results in an influenza variant Fujian-like H5N1 strain with two mutations at the furin-processing site of hemagglutinin, which is resistant to immunization
medicine
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pivotal role for furin, MT1-MMP, and MMP2 in tumor necrosis factor alpha-induced sphingolipid signaling. This system may be a possible target to inhibit smooth muscle cell proliferation in vascular diseases
medicine
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some mutations of H5N1 H5 cleavage sequence fit less well into furin and hence may reduce the high pathogenicity of the H5N1 virus
medicine
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specific and opposing roles of furin and PACE4 in the regulation of MMP-9/TIMP-1 mediated cell motility and invasion. Furin prosegment inhibits cell migration and invasion as well as MMP-9 activity without affecting TIMP-1. It prevents adequate repair of scratch wounds
medicine
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furin expression is detected in all rhabdomyosarcoma cell lines tested at high levels, while myoblasts and fibroblasts show low levels of furin transcripts. Peptide CMGTINTRTKKC has strong affinity for rhabdomyosarcoma cells in vitro and in vivo, by binding to furin
medicine
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hypoxia triggers relocalization of furin from the trans-Golgi network to endosomomal compartments and the cell surface in cancer cells. Exposing these cells back to normoxic conditions reverses furin redistribution, suggesting that the tumor microenvironment modulates furin trafficking in a highly regulated manner. Both Rab4GTPase-dependent recycling and interaction of furin with the cytoskeletal anchoring protein, filamin-A, are essential for the cell surface relocalization of furin. Interference with the association of furin with filamin A, prevents cell surface relocalization of furin and abolishes the ability of cancer cells to migrate in response to hypoxia
medicine
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increased replication of heaptitis C virus RNA in hepatitis C-infected cells is significantly reduced in the presence of transforming growth factor TGF-beta1 siRNA, thrombospondin-1 siRNA or furin siRNA
medicine
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peptide CMGTINTRTKKC has strong affinity for rhabdomyosarcoma cells in vitro and in vivo, by binding to furin. Treatment of rhabdomyosarcoma cells in mice with doxorubicin coupled to the targeting peptide results in a two-fold increase in therapeutic efficacy compared to doxorubicin treatment alone. Surface-furin binding may be used as novel mechanism for therapeutic cell penetration
medicine
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inhibiting furin-like proprotein convertases protects the host from the distinct furin-dependent infections and lay a foundation for novel, host cell-focused therapies against acute diseases
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additional information
furin A activates endothelin 1 signaling
additional information
furin A activates endothelin 1 signaling
additional information
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furin A activates endothelin 1 signaling
additional information
furin B activates endothelin 1 signaling
additional information
furin B activates endothelin 1 signaling
additional information
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furin B activates endothelin 1 signaling
additional information
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Sox-9 regulates furin during chondrogenesis
additional information
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Sox-9 regulates furin during chondrogenesis
additional information
compartment-specific biosensors can be used to gain insight into the regulation of proprotein convertase trafficking and to map the tropism of PC-specific inhibitors