PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 24451252-10 2014 Furthermore, the EGF receptor inhibitor GW2974 significantly suppressed THP- and EGF-enhanced PMN phagocytosis and p38 and ERK1/2 phosphorylation in differentiated HL-60 cells. GW2974 40-46 epidermal growth factor receptor Homo sapiens 17-29 28586051-6 2017 GW2974, an EGFR inhibitor, suppressed the protein expression of EGFR, inhibited cell proliferation, increased LDH activity, induced apoptosis and promoted caspase-3/-8 activities and Bax/Bcl-2 protein expression, downregulated PI3K, p-Akt and p-mTOR protein expression in the transfected HCC cells overexpressing miRNA-133b. GW2974 0-6 epidermal growth factor receptor Homo sapiens 11-15 28586051-6 2017 GW2974, an EGFR inhibitor, suppressed the protein expression of EGFR, inhibited cell proliferation, increased LDH activity, induced apoptosis and promoted caspase-3/-8 activities and Bax/Bcl-2 protein expression, downregulated PI3K, p-Akt and p-mTOR protein expression in the transfected HCC cells overexpressing miRNA-133b. GW2974 0-6 epidermal growth factor receptor Homo sapiens 64-68 28586051-6 2017 GW2974, an EGFR inhibitor, suppressed the protein expression of EGFR, inhibited cell proliferation, increased LDH activity, induced apoptosis and promoted caspase-3/-8 activities and Bax/Bcl-2 protein expression, downregulated PI3K, p-Akt and p-mTOR protein expression in the transfected HCC cells overexpressing miRNA-133b. GW2974 0-6 caspase 3 Homo sapiens 155-167 28586051-6 2017 GW2974, an EGFR inhibitor, suppressed the protein expression of EGFR, inhibited cell proliferation, increased LDH activity, induced apoptosis and promoted caspase-3/-8 activities and Bax/Bcl-2 protein expression, downregulated PI3K, p-Akt and p-mTOR protein expression in the transfected HCC cells overexpressing miRNA-133b. GW2974 0-6 BCL2 associated X, apoptosis regulator Homo sapiens 183-186 28586051-6 2017 GW2974, an EGFR inhibitor, suppressed the protein expression of EGFR, inhibited cell proliferation, increased LDH activity, induced apoptosis and promoted caspase-3/-8 activities and Bax/Bcl-2 protein expression, downregulated PI3K, p-Akt and p-mTOR protein expression in the transfected HCC cells overexpressing miRNA-133b. GW2974 0-6 BCL2 apoptosis regulator Homo sapiens 187-192 28586051-6 2017 GW2974, an EGFR inhibitor, suppressed the protein expression of EGFR, inhibited cell proliferation, increased LDH activity, induced apoptosis and promoted caspase-3/-8 activities and Bax/Bcl-2 protein expression, downregulated PI3K, p-Akt and p-mTOR protein expression in the transfected HCC cells overexpressing miRNA-133b. GW2974 0-6 AKT serine/threonine kinase 1 Homo sapiens 235-238 28586051-6 2017 GW2974, an EGFR inhibitor, suppressed the protein expression of EGFR, inhibited cell proliferation, increased LDH activity, induced apoptosis and promoted caspase-3/-8 activities and Bax/Bcl-2 protein expression, downregulated PI3K, p-Akt and p-mTOR protein expression in the transfected HCC cells overexpressing miRNA-133b. GW2974 0-6 mechanistic target of rapamycin kinase Homo sapiens 245-249 28586051-6 2017 GW2974, an EGFR inhibitor, suppressed the protein expression of EGFR, inhibited cell proliferation, increased LDH activity, induced apoptosis and promoted caspase-3/-8 activities and Bax/Bcl-2 protein expression, downregulated PI3K, p-Akt and p-mTOR protein expression in the transfected HCC cells overexpressing miRNA-133b. GW2974 0-6 microRNA 133b Homo sapiens 313-323 30592329-12 2019 GW2974 (EGFR inhibitor) increased SLC34A2 knockdown-inhibited cell proliferation, migration/invasion, as well as enhanced SLC34A2 knockdown-increased the TMZ sensitivity of glioma cells. GW2974 0-6 epidermal growth factor receptor Homo sapiens 8-12 30592329-12 2019 GW2974 (EGFR inhibitor) increased SLC34A2 knockdown-inhibited cell proliferation, migration/invasion, as well as enhanced SLC34A2 knockdown-increased the TMZ sensitivity of glioma cells. GW2974 0-6 solute carrier family 34 member 2 Homo sapiens 34-41 24451252-10 2014 Furthermore, the EGF receptor inhibitor GW2974 significantly suppressed THP- and EGF-enhanced PMN phagocytosis and p38 and ERK1/2 phosphorylation in differentiated HL-60 cells. GW2974 40-46 epidermal growth factor Homo sapiens 17-20 24451252-10 2014 Furthermore, the EGF receptor inhibitor GW2974 significantly suppressed THP- and EGF-enhanced PMN phagocytosis and p38 and ERK1/2 phosphorylation in differentiated HL-60 cells. GW2974 40-46 mitogen-activated protein kinase 1 Homo sapiens 115-118 24451252-10 2014 Furthermore, the EGF receptor inhibitor GW2974 significantly suppressed THP- and EGF-enhanced PMN phagocytosis and p38 and ERK1/2 phosphorylation in differentiated HL-60 cells. GW2974 40-46 mitogen-activated protein kinase 3 Homo sapiens 123-129 22414725-0 2012 GW583340 and GW2974, human EGFR and HER-2 inhibitors, reverse ABCG2- and ABCB1-mediated drug resistance. GW2974 13-19 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 62-67 23115024-0 2013 Differential effects of low- and high-dose GW2974, a dual epidermal growth factor receptor and HER2 kinase inhibitor, on glioblastoma multiforme invasion. GW2974 43-49 epidermal growth factor receptor Homo sapiens 58-90 23115024-0 2013 Differential effects of low- and high-dose GW2974, a dual epidermal growth factor receptor and HER2 kinase inhibitor, on glioblastoma multiforme invasion. GW2974 43-49 erb-b2 receptor tyrosine kinase 2 Homo sapiens 95-99 23115024-2 2013 In the present study, a dual EGFR and HER2 inhibitor (GW2974) was evaluated for its effects in GBM in vitro and in vivo. GW2974 54-60 erb-b2 receptor tyrosine kinase 2 Homo sapiens 38-42 23115024-5 2013 By protein microarray and Western blot analyses, the p38 mitogen-activated protein kinase (MAPK) pathway was found to be activated in GBM cells under high-concentration GW2974. GW2974 169-175 mitogen-activated protein kinase 14 Homo sapiens 53-89 22414725-8 2012 In addition, a docking model predicted the binding conformation of GW583340 and GW2974 to be within the transmembrane region of homology modeled human ABCB1 and ABCG2. GW2974 80-86 ATP binding cassette subfamily B member 1 Homo sapiens 151-156 22414725-0 2012 GW583340 and GW2974, human EGFR and HER-2 inhibitors, reverse ABCG2- and ABCB1-mediated drug resistance. GW2974 13-19 ATP binding cassette subfamily B member 1 Homo sapiens 73-78 22414725-8 2012 In addition, a docking model predicted the binding conformation of GW583340 and GW2974 to be within the transmembrane region of homology modeled human ABCB1 and ABCG2. GW2974 80-86 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 161-166 22414725-9 2012 We conclude that GW583340 and GW2974, at clinically achievable plasma concentrations, reverse ABCB1- and ABCG2-mediated MDR by blocking the drug efflux function of these transporters. GW2974 30-36 ATP binding cassette subfamily B member 1 Homo sapiens 94-99 22414725-9 2012 We conclude that GW583340 and GW2974, at clinically achievable plasma concentrations, reverse ABCB1- and ABCG2-mediated MDR by blocking the drug efflux function of these transporters. GW2974 30-36 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 105-110 22414725-3 2012 In the present study, we conducted in vitro experiments to evaluate if GW583340 and GW2974, structural analogues of lapatinib, could reverse ABCB1- and ABCG2-mediated MDR. GW2974 84-90 ATP binding cassette subfamily B member 1 Homo sapiens 141-146 22414725-3 2012 In the present study, we conducted in vitro experiments to evaluate if GW583340 and GW2974, structural analogues of lapatinib, could reverse ABCB1- and ABCG2-mediated MDR. GW2974 84-90 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 152-157 22414725-4 2012 Our results showed that GW583340 and GW2974 significantly sensitized ABCB1 and ABCG2 overexpressing MDR cells to their anticancer substrates. GW2974 37-43 ATP binding cassette subfamily B member 1 Homo sapiens 69-74 22414725-4 2012 Our results showed that GW583340 and GW2974 significantly sensitized ABCB1 and ABCG2 overexpressing MDR cells to their anticancer substrates. GW2974 37-43 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 79-84 22414725-5 2012 GW583340 and GW2974 significantly increased the intracellular accumulation of [(3)H]-paclitaxel in ABCB1 overexpressing cells and [(3)H]-mitoxantrone in ABCG2 overexpressing cells respectively. GW2974 13-19 ATP binding cassette subfamily B member 1 Homo sapiens 99-104 22414725-6 2012 In addition, GW583340 and GW2974 significantly inhibited ABCG2-mediated transport of methotrexate in ABCG2 overexpressing membrane vesicles. GW2974 26-32 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 57-62 22414725-6 2012 In addition, GW583340 and GW2974 significantly inhibited ABCG2-mediated transport of methotrexate in ABCG2 overexpressing membrane vesicles. GW2974 26-32 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 101-106 17556544-2 2007 Here, we show that GW2974 (HER2/EGF receptor tyrosine kinase inhibitor), but not trastuzumab, activates AMP-activated protein kinase (AMPK), initiating a metabolic stress response in human cardiomyocytes that protects against TNFalpha-induced cell death. GW2974 19-25 erb-b2 receptor tyrosine kinase 2 Homo sapiens 27-31 20962673-6 2010 On the basis of the MTT assay results, GW2974, a dual inhibitor of epidermal growth factor receptor and HER-2/neu, exhibited only a weak cytotoxic response in SS-ES-1 cells. GW2974 39-45 epidermal growth factor receptor Homo sapiens 67-99 20962673-6 2010 On the basis of the MTT assay results, GW2974, a dual inhibitor of epidermal growth factor receptor and HER-2/neu, exhibited only a weak cytotoxic response in SS-ES-1 cells. GW2974 39-45 erb-b2 receptor tyrosine kinase 2 Homo sapiens 104-113 21673090-4 2011 Here, we show that expression of a 95-kDa tyrosine phosphorylated form of ErbB2, herein referred to as p95L (lapatinib-induced p95) was increased in ErbB2(+) breast cancer cells treated with potent ErbB2 TKIs (lapatinib, GW2974). GW2974 221-227 erb-b2 receptor tyrosine kinase 2 Homo sapiens 74-79 21673090-4 2011 Here, we show that expression of a 95-kDa tyrosine phosphorylated form of ErbB2, herein referred to as p95L (lapatinib-induced p95) was increased in ErbB2(+) breast cancer cells treated with potent ErbB2 TKIs (lapatinib, GW2974). GW2974 221-227 nibrin Homo sapiens 103-106 21673090-4 2011 Here, we show that expression of a 95-kDa tyrosine phosphorylated form of ErbB2, herein referred to as p95L (lapatinib-induced p95) was increased in ErbB2(+) breast cancer cells treated with potent ErbB2 TKIs (lapatinib, GW2974). GW2974 221-227 erb-b2 receptor tyrosine kinase 2 Homo sapiens 149-154 21673090-4 2011 Here, we show that expression of a 95-kDa tyrosine phosphorylated form of ErbB2, herein referred to as p95L (lapatinib-induced p95) was increased in ErbB2(+) breast cancer cells treated with potent ErbB2 TKIs (lapatinib, GW2974). GW2974 221-227 erb-b2 receptor tyrosine kinase 2 Homo sapiens 149-154 20682802-5 2010 GW2974 effectively inhibited skin tumor promotion by 12-O-tetradecanoylphorbol-13-acetate in wild-type and BK5.erbB2 mice, although a more marked effect was seen in BK5.erbB2 mice. GW2974 0-6 erb-b2 receptor tyrosine kinase 2 Mus musculus 111-116 20682802-5 2010 GW2974 effectively inhibited skin tumor promotion by 12-O-tetradecanoylphorbol-13-acetate in wild-type and BK5.erbB2 mice, although a more marked effect was seen in BK5.erbB2 mice. GW2974 0-6 erb-b2 receptor tyrosine kinase 2 Mus musculus 169-174 20682802-7 2010 GW2974 inhibited 12-O-tetradecanoylphorbol-13-acetate-induced epidermal hyperproliferation, which correlated with reduced activation of both the EGFR and erbB2. GW2974 0-6 epidermal growth factor receptor Mus musculus 145-149 20682802-7 2010 GW2974 inhibited 12-O-tetradecanoylphorbol-13-acetate-induced epidermal hyperproliferation, which correlated with reduced activation of both the EGFR and erbB2. GW2974 0-6 erb-b2 receptor tyrosine kinase 2 Mus musculus 154-159 20682802-9 2010 Furthermore, the marked sensitivity of BK5.erbB2 mice to the inhibitory effects of GW2974 during tumor promotion suggest greater efficacy for this compound when erbB2 is overexpressed or amplified as an early event in the carcinogenic process. GW2974 83-89 erb-b2 receptor tyrosine kinase 2 Mus musculus 43-48 20682802-9 2010 Furthermore, the marked sensitivity of BK5.erbB2 mice to the inhibitory effects of GW2974 during tumor promotion suggest greater efficacy for this compound when erbB2 is overexpressed or amplified as an early event in the carcinogenic process. GW2974 83-89 erb-b2 receptor tyrosine kinase 2 Mus musculus 161-166 19352663-8 2009 Additionally, animals exercised prior to DOX/GW2974 injections had significantly lower levels of myocardial lipid peroxidation and caspase-3 and -8 activities compared to their sedentary counterparts. GW2974 45-51 caspase 3 Rattus norvegicus 131-147 17936675-3 2008 The goal of this study was to evaluate the chemopreventive effects of a dual inhibitor of EGFR and ErbB2 tyrosine kinases, GW2974, in the 7,12-dimethylbenz[a]anthracene (DMBA)-induced hamster cheek pouch model. GW2974 123-129 epidermal growth factor receptor Homo sapiens 90-94 17936675-3 2008 The goal of this study was to evaluate the chemopreventive effects of a dual inhibitor of EGFR and ErbB2 tyrosine kinases, GW2974, in the 7,12-dimethylbenz[a]anthracene (DMBA)-induced hamster cheek pouch model. GW2974 123-129 erb-b2 receptor tyrosine kinase 2 Homo sapiens 99-104 17936675-8 2008 In summary, our study indicated that dual inhibition of EGFR and ErbB2 tyrosine kinases by GW2974 was effective in preventing oral carcinogenesis in DMBA-induced hamster cheek pouch model. GW2974 91-97 epidermal growth factor receptor Homo sapiens 56-60 17936675-8 2008 In summary, our study indicated that dual inhibition of EGFR and ErbB2 tyrosine kinases by GW2974 was effective in preventing oral carcinogenesis in DMBA-induced hamster cheek pouch model. GW2974 91-97 erb-b2 receptor tyrosine kinase 2 Homo sapiens 65-70 18594201-7 2008 Our results show that treatments directed to ErbB1/2 receptors using GW-2974 (a generic ErbB1/2 inhibitor) activated AMPK, a key regulator in mitochondrial energy production pathways in human cardiac cells and cancer cells. GW2974 69-76 epidermal growth factor receptor Homo sapiens 45-52 18594201-7 2008 Our results show that treatments directed to ErbB1/2 receptors using GW-2974 (a generic ErbB1/2 inhibitor) activated AMPK, a key regulator in mitochondrial energy production pathways in human cardiac cells and cancer cells. GW2974 69-76 epidermal growth factor receptor Homo sapiens 88-95 18594201-9 2008 When treated in combination with TNFalpha, a known cytokine associated with cardiac toxicity, GW-2974 protected cardiac cells from cell death whereas Herceptin contributed to TNFalpha-induced cellular killing. GW2974 94-101 tumor necrosis factor Homo sapiens 33-41 18171992-9 2007 Activation of the epidermal growth factor receptor (EGFR) seemed to underlie the ability of TPA to activate Akt as both PD153035, an inhibitor of EGFR, and GW2974, a dual-specific inhibitor of both EGFR and erbB2, were able to effectively reduce TPA-induced Akt phosphorylation as well as TPA-stimulated EGFR and erbB2 tyrosine phosphorylation in a dose-dependent manner. GW2974 156-162 epidermal growth factor receptor Mus musculus 18-50 18171992-9 2007 Activation of the epidermal growth factor receptor (EGFR) seemed to underlie the ability of TPA to activate Akt as both PD153035, an inhibitor of EGFR, and GW2974, a dual-specific inhibitor of both EGFR and erbB2, were able to effectively reduce TPA-induced Akt phosphorylation as well as TPA-stimulated EGFR and erbB2 tyrosine phosphorylation in a dose-dependent manner. GW2974 156-162 epidermal growth factor receptor Mus musculus 52-56 17556544-2 2007 Here, we show that GW2974 (HER2/EGF receptor tyrosine kinase inhibitor), but not trastuzumab, activates AMP-activated protein kinase (AMPK), initiating a metabolic stress response in human cardiomyocytes that protects against TNFalpha-induced cell death. GW2974 19-25 epidermal growth factor Homo sapiens 32-35 17556544-2 2007 Here, we show that GW2974 (HER2/EGF receptor tyrosine kinase inhibitor), but not trastuzumab, activates AMP-activated protein kinase (AMPK), initiating a metabolic stress response in human cardiomyocytes that protects against TNFalpha-induced cell death. GW2974 19-25 ret proto-oncogene Homo sapiens 36-60 17556544-2 2007 Here, we show that GW2974 (HER2/EGF receptor tyrosine kinase inhibitor), but not trastuzumab, activates AMP-activated protein kinase (AMPK), initiating a metabolic stress response in human cardiomyocytes that protects against TNFalpha-induced cell death. GW2974 19-25 tumor necrosis factor Homo sapiens 226-234 16934227-4 2006 We have shown that the RTK inhibitor GW282974A (an analogue of GW2016; lapatinib) is effective in chemosensitisation of drug resistant EGFR over-expressing cells giving rise to a synergistic effect when used in combination with either cisplatin or paclitaxel in chemosensitivity assays. GW2974 37-46 ret proto-oncogene Homo sapiens 23-26 17203189-8 2007 EGFR/HER-2/neu tyrosine kinase inhibitors (lapatinib and GW2974) were combined with Bcl-2 inhibitors (HA14-1 or GX15-070) and the anti-proliferative effects were determined by the MTT tetrazolium dye assay. GW2974 57-63 epidermal growth factor receptor Homo sapiens 0-4 17203189-10 2007 A synergistic inhibitory effect was observed with the combination of inhibitors of EGFR-HER-2/neu (lapatinib or GW2974) and Bcl-2 (GX15-070 or HA14-1) on the growth of the MCF-7, MCF/18, and MTR-3 human breast cancer cell lines. GW2974 112-118 epidermal growth factor receptor Homo sapiens 83-87 17203189-10 2007 A synergistic inhibitory effect was observed with the combination of inhibitors of EGFR-HER-2/neu (lapatinib or GW2974) and Bcl-2 (GX15-070 or HA14-1) on the growth of the MCF-7, MCF/18, and MTR-3 human breast cancer cell lines. GW2974 112-118 erb-b2 receptor tyrosine kinase 2 Homo sapiens 88-93 17203189-10 2007 A synergistic inhibitory effect was observed with the combination of inhibitors of EGFR-HER-2/neu (lapatinib or GW2974) and Bcl-2 (GX15-070 or HA14-1) on the growth of the MCF-7, MCF/18, and MTR-3 human breast cancer cell lines. GW2974 112-118 erb-b2 receptor tyrosine kinase 2 Mus musculus 94-97 16934227-4 2006 We have shown that the RTK inhibitor GW282974A (an analogue of GW2016; lapatinib) is effective in chemosensitisation of drug resistant EGFR over-expressing cells giving rise to a synergistic effect when used in combination with either cisplatin or paclitaxel in chemosensitivity assays. GW2974 37-46 epidermal growth factor receptor Homo sapiens 135-139 16934227-6 2006 A reduction in the downstream signalling effector phosphorylated ERK was seen in both resistant cell lines when GW282974A was used in combination with either cisplatin or paclitaxel. GW2974 112-121 EPH receptor B2 Homo sapiens 65-68 16934227-9 2006 However, the paclitaxel resistant cell line appeared more sensitive to the chemosensitising effects of GW282974A, in line with its increased EGFR expression. GW2974 103-112 epidermal growth factor receptor Homo sapiens 141-145 16061875-7 2005 In addition, we examined the effect of another quinazoline derivative, GW2974, which is able to block the activation of both the EGFR and erbB2, in this model. GW2974 71-77 epidermal growth factor receptor Mus musculus 129-133 16061875-7 2005 In addition, we examined the effect of another quinazoline derivative, GW2974, which is able to block the activation of both the EGFR and erbB2, in this model. GW2974 71-77 erb-b2 receptor tyrosine kinase 2 Mus musculus 138-143