PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 24023701-9 2013 Amiloride, a specific PLAU inhibitor, also suppressed these processes. Amiloride 0-9 plasminogen activator, urokinase Homo sapiens 22-26 25492830-4 2014 Amiloride, an ENaC inhibitor, inhibits urokinase-type plasminogen activator. Amiloride 0-9 plasminogen activator, urokinase Homo sapiens 39-75 25492830-5 2014 We hypothesized that amiloride (1) reduces blood pressure (BP); (2) attenuates plasminogen-to-plasmin activation; and (3) inhibits urine urokinase-type plasminogen activator in patients with resistant hypertension and type 2 diabetes mellitus (T2DM).In an open-label, non-randomized, 8-week intervention study, a cohort (n = 80) of patients with resistant hypertension and T2DM were included. Amiloride 21-30 plasminogen activator, urokinase Homo sapiens 137-173 33517269-6 2021 The growth-inhibitory effect of sorafenib was significantly enhanced by the uPA inhibitors UK122 and amiloride. Amiloride 101-110 plasminogen activator, urokinase Homo sapiens 76-79 29328476-2 2018 Amiloride, a synthetic inhibitor of urokinase plasminogen activator (uPA), is involved in these events. Amiloride 0-9 plasminogen activator, urokinase Homo sapiens 36-67 29328476-2 2018 Amiloride, a synthetic inhibitor of urokinase plasminogen activator (uPA), is involved in these events. Amiloride 0-9 plasminogen activator, urokinase Homo sapiens 69-72 29328476-5 2018 The results of RT-qPCR demonstrated that the mRNA expression of uPA and MMP-2 in HeLa cells was downregulated significantly in a dose-dependent manner when incubated with various concentrations of amiloride for 24 h. The migration distance of HeLa cells was significantly shorter at 6, 12 and 24 h following incubation with amiloride (P<0.01), and there was a positive correlation between cell migratory ability and cellular uPA protein expression level (r=0.955, P<0.01). Amiloride 197-206 plasminogen activator, urokinase Homo sapiens 64-67 29328476-5 2018 The results of RT-qPCR demonstrated that the mRNA expression of uPA and MMP-2 in HeLa cells was downregulated significantly in a dose-dependent manner when incubated with various concentrations of amiloride for 24 h. The migration distance of HeLa cells was significantly shorter at 6, 12 and 24 h following incubation with amiloride (P<0.01), and there was a positive correlation between cell migratory ability and cellular uPA protein expression level (r=0.955, P<0.01). Amiloride 197-206 plasminogen activator, urokinase Homo sapiens 428-431 29328476-5 2018 The results of RT-qPCR demonstrated that the mRNA expression of uPA and MMP-2 in HeLa cells was downregulated significantly in a dose-dependent manner when incubated with various concentrations of amiloride for 24 h. The migration distance of HeLa cells was significantly shorter at 6, 12 and 24 h following incubation with amiloride (P<0.01), and there was a positive correlation between cell migratory ability and cellular uPA protein expression level (r=0.955, P<0.01). Amiloride 324-333 plasminogen activator, urokinase Homo sapiens 64-67 29328476-6 2018 The number of HeLa cells that penetrated the Matrigel following incubation for 24 h with different concentrations of amiloride decreased significantly compared with the control group, indicating that cell invasiveness was positively correlated with the protein expression level of uPA in the cells (r=0.993, P<0.01). Amiloride 117-126 plasminogen activator, urokinase Homo sapiens 281-284 29328476-7 2018 The present study demonstrated that amiloride was able to specifically inhibit the mRNA expression levels of uPA in HeLa cells, and sequentially downregulate the mRNA expression of downstream MMP-2 in the uPA system, thereby suppressing the migratory and invasive ability of HeLa cells. Amiloride 36-45 plasminogen activator, urokinase Homo sapiens 109-112 29328476-7 2018 The present study demonstrated that amiloride was able to specifically inhibit the mRNA expression levels of uPA in HeLa cells, and sequentially downregulate the mRNA expression of downstream MMP-2 in the uPA system, thereby suppressing the migratory and invasive ability of HeLa cells. Amiloride 36-45 plasminogen activator, urokinase Homo sapiens 205-208 25972510-0 2015 Aberrant glomerular filtration of urokinase-type plasminogen activator in nephrotic syndrome leads to amiloride-sensitive plasminogen activation in urine. Amiloride 102-111 plasminogen activator, urokinase Homo sapiens 34-70 25972510-2 2015 The ENaC blocker amiloride is an off-target inhibitor of urokinase-type plasminogen activator (uPA) in vitro. Amiloride 17-26 plasminogen activator, urokinase Homo sapiens 57-93 25972510-2 2015 The ENaC blocker amiloride is an off-target inhibitor of urokinase-type plasminogen activator (uPA) in vitro. Amiloride 17-26 plasminogen activator, urokinase Homo sapiens 95-98 25972510-3 2015 It was hypothesized that uPA is abnormally filtered to preurine and is inhibited in urine by amiloride in nephrotic syndrome. Amiloride 93-102 plasminogen activator, urokinase Homo sapiens 25-28 25972510-11 2015 Amiloride inhibits urine uPA activity which attenuates plasminogen activation and urine protease activity in vivo. Amiloride 0-9 plasminogen activator, urokinase Homo sapiens 25-28 25972510-12 2015 Urine uPA is a relevant target for amiloride in vivo. Amiloride 35-44 plasminogen activator, urokinase Homo sapiens 6-9 24885350-14 2014 This role of uPA in cell invasion was confirmed using the uPA inhibitors, amiloride and UK122. Amiloride 74-83 plasminogen activator, urokinase Homo sapiens 13-16 23234499-0 2012 u-PA inhibitor amiloride suppresses peritoneal metastasis in gastric cancer. Amiloride 15-24 plasminogen activator, urokinase Homo sapiens 0-4 23234499-6 2012 In vitro, compared with controls, amiloride could not only significantly down-regulate the mRNA expression and protein level of u-PA from MKN45 cells with dose dependence but also inhibit the adhesion of HMrSV5 cells, migration and invasion of MKN45 cells. Amiloride 34-43 plasminogen activator, urokinase Homo sapiens 128-132 23234499-7 2012 CONCLUSIONS: The findings in our current report provide evidence that selective u-PA inhibitor amiloride has potent effects against peritoneal metastasis in gastric cancer, suggesting its possible therapeutic value for the treatment of gastric cancer. Amiloride 95-104 plasminogen activator, urokinase Homo sapiens 80-84 19436306-8 2009 u-PA and u-PAR function was inhibited with anti u-PA antibodies or the selective u-PA inhibitors amiloride or WXC-340, TLR-4 by TLR-4-blocking antibodies and NF-kappaB by the selective NF-kappaB inhibitor SN-50. Amiloride 97-106 plasminogen activator, urokinase Homo sapiens 0-4 22366654-1 2012 The relative non-toxicity of the diuretic amiloride, coupled with its selective inhibition of the protease urokinase plasminogen activator (uPA), makes this compound class attractive for structure-activity studies. Amiloride 42-51 plasminogen activator, urokinase Homo sapiens 107-138 22366654-1 2012 The relative non-toxicity of the diuretic amiloride, coupled with its selective inhibition of the protease urokinase plasminogen activator (uPA), makes this compound class attractive for structure-activity studies. Amiloride 42-51 plasminogen activator, urokinase Homo sapiens 140-143 21978672-0 2011 Synthesis and preliminary evaluation of amiloride analogs as inhibitors of the urokinase-type plasminogen activator (uPA). Amiloride 40-49 plasminogen activator, urokinase Homo sapiens 79-115 21978672-0 2011 Synthesis and preliminary evaluation of amiloride analogs as inhibitors of the urokinase-type plasminogen activator (uPA). Amiloride 40-49 plasminogen activator, urokinase Homo sapiens 117-120 21978672-1 2011 A known side-activity of the oral potassium-sparing diuretic drug amiloride is inhibition of the enzyme urokinase-type plasminogen activator (uPA, K(i)=7 muM), a promising anticancer target. Amiloride 66-75 plasminogen activator, urokinase Homo sapiens 104-140 21978672-1 2011 A known side-activity of the oral potassium-sparing diuretic drug amiloride is inhibition of the enzyme urokinase-type plasminogen activator (uPA, K(i)=7 muM), a promising anticancer target. Amiloride 66-75 plasminogen activator, urokinase Homo sapiens 142-145 21978672-2 2011 Several studies have demonstrated significant antitumor/metastasis properties for amiloride in animal cancer models and it would appear that these arise, at least in part, through inhibition of uPA. Amiloride 82-91 plasminogen activator, urokinase Homo sapiens 194-197 21978672-3 2011 Selective optimization of amiloride"s structure for more potent inhibition of uPA and loss of diuretic effects would thus appear as an attractive strategy towards novel anticancer agents. Amiloride 26-35 plasminogen activator, urokinase Homo sapiens 78-81 21978672-4 2011 The following report is a preliminary structure-activity exploration of amiloride analogs as inhibitors of uPA. Amiloride 72-81 plasminogen activator, urokinase Homo sapiens 107-110 21978672-5 2011 A key finding was that the well-studied 5-substituted analogs ethylisopropyl amiloride (EIPA) and hexamethylene amiloride (HMA) are approximately twofold more potent than amiloride as uPA inhibitors. Amiloride 77-86 plasminogen activator, urokinase Homo sapiens 184-187 21470685-5 2011 In contrast, the transmigration was significantly inhibited by Fab" fragment of anti-uPAR monoclonal antibody and proteolytically inactive urokinase (uPA), whereas inhibition of proteolytical activity of endogenous uPA (with amiloride or plasminogen activator inhibitor-1) did not affect the transmigration. Amiloride 225-234 plasminogen activator, urokinase Homo sapiens 85-88 21470685-5 2011 In contrast, the transmigration was significantly inhibited by Fab" fragment of anti-uPAR monoclonal antibody and proteolytically inactive urokinase (uPA), whereas inhibition of proteolytical activity of endogenous uPA (with amiloride or plasminogen activator inhibitor-1) did not affect the transmigration. Amiloride 225-234 plasminogen activator, urokinase Homo sapiens 150-153 20180817-9 2010 Blocking u-PA activity with the active site-directed protease inhibitor amiloride substantially decreased MCF-10CA1 cell motility. Amiloride 72-81 plasminogen activator, urokinase Homo sapiens 9-13 19436306-8 2009 u-PA and u-PAR function was inhibited with anti u-PA antibodies or the selective u-PA inhibitors amiloride or WXC-340, TLR-4 by TLR-4-blocking antibodies and NF-kappaB by the selective NF-kappaB inhibitor SN-50. Amiloride 97-106 plasminogen activator, urokinase Homo sapiens 9-13 19436306-8 2009 u-PA and u-PAR function was inhibited with anti u-PA antibodies or the selective u-PA inhibitors amiloride or WXC-340, TLR-4 by TLR-4-blocking antibodies and NF-kappaB by the selective NF-kappaB inhibitor SN-50. Amiloride 97-106 plasminogen activator, urokinase Homo sapiens 9-13 14973065-10 2004 Amiloride, an uPA inhibitor, not only inhibited the activity of uPA but was also able to suppress TNF-alpha-stimulated MMP-9 activity and prevented the TNF-alpha-stimulated remodeling of the basement membrane extracellular matrix, suggesting the contribution of uPA-mediated proteolytic cascade in this process. Amiloride 0-9 plasminogen activator, urokinase Homo sapiens 14-17 15543335-4 2004 This activation is prevented by amiloride, an inhibitor of u-PA, and epsilon-aminocaproic acid, epsilon-ACA, a lysine analogue that blocks plasminogen binding to PMNs. Amiloride 32-41 plasminogen activator, urokinase Homo sapiens 59-63 18366077-5 2008 This activity and PGN-induced aggregation were inhibited by the uPA inhibitor amiloride. Amiloride 78-87 plasminogen activator, urokinase Homo sapiens 64-67 17210677-7 2007 EMMPRIN-expressing cells also exhibited enhanced invasive potential in vitro, and the use of amiloride (uPA inhibitor) and marimastat (MMP inhibitor) showed that the two proteolytic systems reduced alone and in combination the invasive potential mediated through EMMPRIN. Amiloride 93-102 plasminogen activator, urokinase Homo sapiens 104-107 16611636-7 2006 Inhibition of uPA activity with natural (plasminogen activator inhibitor-1) or synthetic (amiloride) inhibitors diminished HT-hi/diss Matrigel invasion in vitro and intravasation and metastasis in vivo. Amiloride 90-99 plasminogen activator, urokinase Homo sapiens 14-17 16636720-13 2006 Inhibition of urokinase-type plasminogen activator and modulation of field strengths by amiloride seem to be responsible for this effect. Amiloride 88-97 plasminogen activator, urokinase Homo sapiens 14-50 15023541-4 2004 Using several different concentrations of amiloride, aminobenzamidine and PAI-1 and the urokinase-type plasminogen activator (uPA) function-blocking antibody (3689), we showed that uPA, acting as a protease, is responsible for production of alpha6p. Amiloride 42-51 plasminogen activator, urokinase Homo sapiens 181-184 14973065-10 2004 Amiloride, an uPA inhibitor, not only inhibited the activity of uPA but was also able to suppress TNF-alpha-stimulated MMP-9 activity and prevented the TNF-alpha-stimulated remodeling of the basement membrane extracellular matrix, suggesting the contribution of uPA-mediated proteolytic cascade in this process. Amiloride 0-9 plasminogen activator, urokinase Homo sapiens 64-67 14973065-10 2004 Amiloride, an uPA inhibitor, not only inhibited the activity of uPA but was also able to suppress TNF-alpha-stimulated MMP-9 activity and prevented the TNF-alpha-stimulated remodeling of the basement membrane extracellular matrix, suggesting the contribution of uPA-mediated proteolytic cascade in this process. Amiloride 0-9 plasminogen activator, urokinase Homo sapiens 64-67 14644129-7 2003 Thus, inhibitors of uPA and plasmin, such as amiloride and UTI, respectively, could be useful therapeutic tools with which to treat urothelial cancer. Amiloride 45-54 plasminogen activator, urokinase Homo sapiens 20-23 11758807-6 2001 The activity was inhibited by amiloride, a specific inhibitor of uPA. Amiloride 30-39 plasminogen activator, urokinase Homo sapiens 65-68 11991662-2 2002 Amiloride, a competitive inhibitor of uPA, can inhibit endothelial cell (EC) outgrowth during angiogenesis. Amiloride 0-9 plasminogen activator, urokinase Homo sapiens 38-41 11991662-3 2002 To address the question of whether amiloride blocked angiogenesis by inhibiting uPA, we undertook a study of uPA expression in sprouting EC in vitro and the effects of amiloride on both enzymatic and morphogenetic activity. Amiloride 35-44 plasminogen activator, urokinase Homo sapiens 80-83 11991662-4 2002 As expected, amiloride inhibited soluble uPA (suPA) with an IC(50) of 45-85 microm, however, receptor-bound uPA (rbuPA) from the sprouting EC was insensitive to amiloride. Amiloride 13-22 plasminogen activator, urokinase Homo sapiens 41-44 11991662-4 2002 As expected, amiloride inhibited soluble uPA (suPA) with an IC(50) of 45-85 microm, however, receptor-bound uPA (rbuPA) from the sprouting EC was insensitive to amiloride. Amiloride 13-22 plasminogen activator, urokinase Homo sapiens 47-50 11991662-5 2002 Removal of uPA from its receptors confers sensitivity to inhibition by amiloride suggesting that a reversible conformational change may mediate the insensitivity of rbuPA to amiloride and its analogs. Amiloride 71-80 plasminogen activator, urokinase Homo sapiens 11-14 11804183-4 2001 Antibodies to both uPA and uPA receptor (uPAR) were shown to significantly inhibit cell invasion, as did the uPA inhibitors (plasminogen activator inhibitor-1 [PAI-1], p-aminobenzamidine [PABN], aprotinin, and amiloride). Amiloride 210-219 plasminogen activator, urokinase Homo sapiens 19-22 11454671-8 2001 Matrigel invasion assay showed that prostate cancer cell line PC-3, containing amplification of the uPA gene, was more sensitive to the urokinase inhibitor, amiloride, than DU145 or LNCaP cell lines, which do not have the amplification. Amiloride 157-166 plasminogen activator, urokinase Homo sapiens 100-103 11835393-5 2002 Plasminogen-dependent [3H]-collagen IV degradation was inhibited by inhibitor of uPA (amiloride) and MMP (phenanthroline) and by antibodies against uPA or MMP-9 or alphavbeta6 integrin, indicating the involvement of alphavbeta6 integrin, uPA and MMP-9 in the process. Amiloride 86-95 plasminogen activator, urokinase Homo sapiens 81-84 11804183-4 2001 Antibodies to both uPA and uPA receptor (uPAR) were shown to significantly inhibit cell invasion, as did the uPA inhibitors (plasminogen activator inhibitor-1 [PAI-1], p-aminobenzamidine [PABN], aprotinin, and amiloride). Amiloride 210-219 plasminogen activator, urokinase Homo sapiens 27-30 11562773-11 2001 Amiloride is a specific inhibitor of uPA but does not inhibit tPA. Amiloride 0-9 plasminogen activator, urokinase Homo sapiens 37-40 10738907-0 1999 Molecular basis of specific inhibition of urokinase plasminogen activator by amiloride. Amiloride 77-86 plasminogen activator, urokinase Homo sapiens 42-73 10824746-0 2000 Suppression of the invasive capacity of human breast cancer cells by inhibition of urokinase plasminogen activator via amiloride and B428. Amiloride 119-128 plasminogen activator, urokinase Homo sapiens 83-114 10824746-3 2000 In this study using Matrigel invasion chambers and two separate uPA inhibitors, amiloride and B428, the invasive capacity of unaltered human breast cancer cells was significantly suppressed. Amiloride 80-89 plasminogen activator, urokinase Homo sapiens 64-67 10738907-6 1999 It has been found that amiloride competitively inhibits the catalytic activity of uPA but not tPA. Amiloride 23-32 plasminogen activator, urokinase Homo sapiens 82-85 10738907-8 1999 The X-ray structure of the uPA complex with amiloride is not known. Amiloride 44-53 plasminogen activator, urokinase Homo sapiens 27-30 10328652-9 1999 The activity was inhibited by amiloride, which is a specific inhibitor for uPA. Amiloride 30-39 plasminogen activator, urokinase Homo sapiens 75-78 8627323-6 1996 uPA activity was confirmed by incubating the extracts with amiloride, an inhibitor of uPA. Amiloride 59-68 plasminogen activator, urokinase Homo sapiens 0-3 9665481-7 1998 Cell motility is significantly reduced by inhibitors of u-PA proteolytic activity such as antibodies neutralizing u-PA activity, plasminogen activator inhibitor 1, and amiloride. Amiloride 168-177 plasminogen activator, urokinase Homo sapiens 56-60 8627323-6 1996 uPA activity was confirmed by incubating the extracts with amiloride, an inhibitor of uPA. Amiloride 59-68 plasminogen activator, urokinase Homo sapiens 86-89 3106085-0 1987 Amiloride selectively inhibits the urokinase-type plasminogen activator. Amiloride 0-9 plasminogen activator, urokinase Homo sapiens 35-71 7750207-3 1995 The effects of amiloride on the modulation of uPA mRNA and protein induced by phorbol ester (PMA) and cycloheximide (CHX) were studied in four colon cancer cell lines, HCT116, KM12SM, LIM1215 and LS123. Amiloride 15-24 plasminogen activator, urokinase Homo sapiens 46-49 7750207-7 1995 Amiloride profoundly inhibited uPA mRNA production at concentrations between 0.1-1 mM in the presence or absence of PMA or CHX. Amiloride 0-9 plasminogen activator, urokinase Homo sapiens 31-34 7750207-10 1995 The inhibitory effects of amiloride on uPA gene expression reported in this paper may offer the prospect of developing new therapeutic approaches to the prevention of invasion and metastasis by adenocarcinomas. Amiloride 26-35 plasminogen activator, urokinase Homo sapiens 39-42 8495419-7 1993 This level of inhibition represents 20- and 100-fold increases in potency, respectively, relative to the 6-7 microM potencies reported for amiloride and 4-chlorophenylguanidine, the two most potent selective synthetic uPA inhibitors previously described. Amiloride 139-148 plasminogen activator, urokinase Homo sapiens 218-221 1915841-6 1991 (4) Porcine urine PA activity is not affected by concentration of amiloride substantially suppressing human u-PA activity. Amiloride 66-75 plasminogen activator, urokinase Homo sapiens 108-112 33804289-5 2021 Together, these amilorides comprise a new toolkit of chemotype-matched, non-cytotoxic probes for dissecting the pharmacological effects of selective uPA and NHE1 inhibition versus dual-uPA/NHE1 inhibition. Amiloride 16-26 plasminogen activator, urokinase Homo sapiens 149-152 33804289-5 2021 Together, these amilorides comprise a new toolkit of chemotype-matched, non-cytotoxic probes for dissecting the pharmacological effects of selective uPA and NHE1 inhibition versus dual-uPA/NHE1 inhibition. Amiloride 16-26 plasminogen activator, urokinase Homo sapiens 185-188 3106085-1 1987 The diuretic drug amiloride, an inhibitor of Na+ uptake, competitively inhibits the catalytic activity of the urokinase-type plasminogen activator (u-PA), with a Ki of 7 X 10(-6) M. Generation of plasmin, cleavage of peptide substrates, and interaction of u-PA with a specific macromolecular proteinase inhibitor are all prevented in the presence of the drug. Amiloride 18-27 plasminogen activator, urokinase Homo sapiens 110-146 3106085-1 1987 The diuretic drug amiloride, an inhibitor of Na+ uptake, competitively inhibits the catalytic activity of the urokinase-type plasminogen activator (u-PA), with a Ki of 7 X 10(-6) M. Generation of plasmin, cleavage of peptide substrates, and interaction of u-PA with a specific macromolecular proteinase inhibitor are all prevented in the presence of the drug. Amiloride 18-27 plasminogen activator, urokinase Homo sapiens 148-152 3106085-1 1987 The diuretic drug amiloride, an inhibitor of Na+ uptake, competitively inhibits the catalytic activity of the urokinase-type plasminogen activator (u-PA), with a Ki of 7 X 10(-6) M. Generation of plasmin, cleavage of peptide substrates, and interaction of u-PA with a specific macromolecular proteinase inhibitor are all prevented in the presence of the drug. Amiloride 18-27 plasminogen activator, urokinase Homo sapiens 256-260 3106085-3 1987 The inhibition of u-PA by amiloride may be related to the previously reported inhibition of u-PA-type enzymes by Na+. Amiloride 26-35 plasminogen activator, urokinase Homo sapiens 18-22 3106085-3 1987 The inhibition of u-PA by amiloride may be related to the previously reported inhibition of u-PA-type enzymes by Na+. Amiloride 26-35 plasminogen activator, urokinase Homo sapiens 92-96 3106085-4 1987 Amiloride or related compounds could prove useful in selectively controlling u-PA-catalyzed extracellular proteolysis. Amiloride 0-9 plasminogen activator, urokinase Homo sapiens 77-81