PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 33940225-3 2021 Osteoblast maturation can be stimulated by genetic loss of the H3K27 methyltransferase Ezh2 which can also be mimicked pharmacologically using the classical Ezh2 inhibitor GSK126. GSK-2816126 172-178 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 87-91 33571671-7 2021 The Ezh2 inhibitor GSK126 could inhibit the differentiation of MEFs into white adipocytes but promoted their differentiation into brown/beige adipocytes. GSK-2816126 19-25 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 4-8 34015321-5 2021 Further, knockdown of EZH2 or its specific inhibitor GSK126 can decrease expression of Twist, while over expression of Twist can reverse si-EZH2-suppressed malignancy of GBM cells. GSK-2816126 53-59 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 22-26 34015321-5 2021 Further, knockdown of EZH2 or its specific inhibitor GSK126 can decrease expression of Twist, while over expression of Twist can reverse si-EZH2-suppressed malignancy of GBM cells. GSK-2816126 53-59 twist family bHLH transcription factor 1 Homo sapiens 87-92 33978549-6 2021 Screening a panel of methyltransferase inhibitors revealed that three inhibitors; GSK126, UNC1999 and EPZ-5687 are the most potent inhibitors that suppressed EZH2 activity selectively on lysine 27 which resulted in increased apoptosis and inhibition of AKT and ERK protein phosphorylation in THP-1 cells. GSK-2816126 82-88 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 158-162 33978549-6 2021 Screening a panel of methyltransferase inhibitors revealed that three inhibitors; GSK126, UNC1999 and EPZ-5687 are the most potent inhibitors that suppressed EZH2 activity selectively on lysine 27 which resulted in increased apoptosis and inhibition of AKT and ERK protein phosphorylation in THP-1 cells. GSK-2816126 82-88 AKT serine/threonine kinase 1 Homo sapiens 253-256 33978549-6 2021 Screening a panel of methyltransferase inhibitors revealed that three inhibitors; GSK126, UNC1999 and EPZ-5687 are the most potent inhibitors that suppressed EZH2 activity selectively on lysine 27 which resulted in increased apoptosis and inhibition of AKT and ERK protein phosphorylation in THP-1 cells. GSK-2816126 82-88 mitogen-activated protein kinase 1 Homo sapiens 261-264 33940225-3 2021 Osteoblast maturation can be stimulated by genetic loss of the H3K27 methyltransferase Ezh2 which can also be mimicked pharmacologically using the classical Ezh2 inhibitor GSK126. GSK-2816126 172-178 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 157-161 32772228-11 2021 Our results suggest that GSK-126 promotes seizure susceptibility due to its role as an EZH2 inhibitor. GSK-2816126 25-32 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 87-91 33370552-10 2021 A selective EZH2 inhibitor, GSK126 decreased H3K27me3 and elevated NaV1.5 in HL-1 cells. GSK-2816126 28-34 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 12-16 33370552-10 2021 A selective EZH2 inhibitor, GSK126 decreased H3K27me3 and elevated NaV1.5 in HL-1 cells. GSK-2816126 28-34 sodium channel, voltage-gated, type V, alpha Mus musculus 67-73 33370552-13 2021 GSK126 inhibited the enrichment of H3K27me3 in the Scn5a promoter and enhanced Scn5a transcriptional activity. GSK-2816126 0-6 sodium channel, voltage-gated, type V, alpha Mus musculus 51-56 33370552-13 2021 GSK126 inhibited the enrichment of H3K27me3 in the Scn5a promoter and enhanced Scn5a transcriptional activity. GSK-2816126 0-6 sodium channel, voltage-gated, type V, alpha Mus musculus 79-84 33792119-6 2021 In vitro growth assays showed that compared to an established EZH2-specific inhibitor GSK126, OR-S1 had a marked antitumor effect on MCL cell lines. GSK-2816126 86-92 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 62-66 33467134-6 2021 Our results show that UNC1999 and GSK126 increased CD56+ cell proliferation compared to the control condition. GSK-2816126 34-40 neural cell adhesion molecule 1 Homo sapiens 51-55 33103538-6 2021 Despite this success many questions remain; for instance, tazemetostat was briefly placed on clinical hold for safety concerns, while another EZH2 inhibitor (GSK126) demonstrated insufficient efficacy during a Phase I/II trial. GSK-2816126 158-164 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 142-146 32715799-2 2020 The EZH2-specific inhibitor GSK126 inhibits trimethylation of histone H3K27 and induces target gene expression. GSK-2816126 28-34 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 4-8 33384997-8 2020 Consistent with the flow data, by using small molecule Ezh2 inhibitor GSK126, we prove that Ezh2 is required for osteoclast differentiation. GSK-2816126 70-76 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 92-96 33303026-9 2020 GSK126 was used to inhibit Enhancer of Zeste 2 (EZH2). GSK-2816126 0-6 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 48-52 32799209-4 2021 Subsequently, the malignant CTCL cell lines were treated with GSK126 - an inhibitor of enhancer of zeste homolog 2 (EZH2) methyltransferase activity or assessed by bisulphite sequencing for TXNIP promoter methylation. GSK-2816126 62-68 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 87-114 32799209-4 2021 Subsequently, the malignant CTCL cell lines were treated with GSK126 - an inhibitor of enhancer of zeste homolog 2 (EZH2) methyltransferase activity or assessed by bisulphite sequencing for TXNIP promoter methylation. GSK-2816126 62-68 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 116-120 33262329-5 2020 We demonstrated that EZH2 depletion in dendritic cells (DCs) and pharmacological inhibition of EZH2 using GSK126 both significantly ameliorated liver injury and improved the survival rates of mice with P. acnes plus LPS-induced FHF, which could be attributed to the decreased infiltration and activation of CD4+ T cells in the liver, inhibition of T helper 1 cells and induction of regulatory T cells. GSK-2816126 106-112 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 95-99 32715799-6 2020 Only 1/4 EZH2 GOFmu B-NHL cell lines tested (PFEIFFER) were sensitive to GSK126 (400 nM) inducing growth arrest. GSK-2816126 73-79 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 9-13 33024029-3 2020 Herein, we report that the combination of metformin and EZH2 inhibitor GSK126 exerts synergistic inhibition on PCa cell growth, both in vitro and in vivo. GSK-2816126 71-77 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 56-60 33024029-7 2020 However, GSK126 can inhibit the methyltransferase-dependent interaction between AR and EZH2, thus restoring metformin"s efficacy in androgen-refractory PCa cells. GSK-2816126 9-15 androgen receptor Homo sapiens 80-82 33024029-7 2020 However, GSK126 can inhibit the methyltransferase-dependent interaction between AR and EZH2, thus restoring metformin"s efficacy in androgen-refractory PCa cells. GSK-2816126 9-15 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 87-91 33024029-8 2020 Collectively, our finding suggests that the combination of metformin and GSK126 would be an effective approach for future PCa therapy, and particularly effective for AR-positive CRPC. GSK-2816126 73-79 androgen receptor Homo sapiens 166-168 33207205-5 2020 Treatment of Baf155 CKO embryos with GSK126, an H3K27me2/3 methyltransferase EZH2 inhibitor, rescues myeloid lineage gene expression. GSK-2816126 37-43 SWI/SNF related, matrix associated, actin dependent regulator of chromatin subfamily c member 1 Homo sapiens 13-19 33207205-5 2020 Treatment of Baf155 CKO embryos with GSK126, an H3K27me2/3 methyltransferase EZH2 inhibitor, rescues myeloid lineage gene expression. GSK-2816126 37-43 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 77-81 32816909-8 2020 Co-administration of EZH2 inhibitor GSK126 and RAC1 inhibitor NSC23766 suppressed OCSC survival in vitro and inhibited tumor growth and increased platinum sensitivity in vivo. GSK-2816126 36-42 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 21-25 33011750-9 2020 In vivo, the inhibitor of EZH2, GSK126 could ameliorate the imiquimod-induced psoriasiform lesion. GSK-2816126 32-38 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 26-30 32906688-0 2020 Combination Treatment with GSK126 and Pomalidomide Induces B-Cell Differentiation in EZH2 Gain-of-Function Mutant Diffuse Large B-Cell Lymphoma. GSK-2816126 27-33 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 85-89 33085231-0 2020 [Effect of enhancer of zeste homolog 2 inhibitor GSK126 on the proliferation and apoptosis of tongue squamous cell carcinoma]. GSK-2816126 49-55 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 11-38 33085231-1 2020 OBJECTIVE: This study aims to study the effect of the enhancer of zeste homolog 2 (EZH2) inhibitor GSK126 on the proliferation and apoptosis of human tongue squamous cell carcinoma cells in vitro and explore its related mechanisms in order to obtain insights into the clinical treatment of tongue squamous cell carcinoma. GSK-2816126 99-105 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 54-81 33085231-1 2020 OBJECTIVE: This study aims to study the effect of the enhancer of zeste homolog 2 (EZH2) inhibitor GSK126 on the proliferation and apoptosis of human tongue squamous cell carcinoma cells in vitro and explore its related mechanisms in order to obtain insights into the clinical treatment of tongue squamous cell carcinoma. GSK-2816126 99-105 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 83-87 33085231-6 2020 GSK126 down-regulated the expression of p-ERK and Bcl-2 and increased the expression of Bax and Cleaved caspase-9 (P<0.05). GSK-2816126 0-6 mitogen-activated protein kinase 1 Homo sapiens 42-45 33085231-6 2020 GSK126 down-regulated the expression of p-ERK and Bcl-2 and increased the expression of Bax and Cleaved caspase-9 (P<0.05). GSK-2816126 0-6 BCL2 apoptosis regulator Homo sapiens 50-55 33085231-6 2020 GSK126 down-regulated the expression of p-ERK and Bcl-2 and increased the expression of Bax and Cleaved caspase-9 (P<0.05). GSK-2816126 0-6 BCL2 associated X, apoptosis regulator Homo sapiens 88-91 33085231-6 2020 GSK126 down-regulated the expression of p-ERK and Bcl-2 and increased the expression of Bax and Cleaved caspase-9 (P<0.05). GSK-2816126 0-6 caspase 9 Homo sapiens 104-113 33085231-7 2020 CONCLUSIONS: GSK126 can inhibit the proliferation of CAL-27 cells in tongue squamous cell carcinoma and promote its apoptosis, and the related mechanism may be associated with the inhibition of the MEK/ERK signaling pathway and activation of the Bax/Bcl-2 pathway. GSK-2816126 13-19 mitogen-activated protein kinase kinase 7 Homo sapiens 198-201 33085231-7 2020 CONCLUSIONS: GSK126 can inhibit the proliferation of CAL-27 cells in tongue squamous cell carcinoma and promote its apoptosis, and the related mechanism may be associated with the inhibition of the MEK/ERK signaling pathway and activation of the Bax/Bcl-2 pathway. GSK-2816126 13-19 mitogen-activated protein kinase 1 Homo sapiens 202-205 33085231-7 2020 CONCLUSIONS: GSK126 can inhibit the proliferation of CAL-27 cells in tongue squamous cell carcinoma and promote its apoptosis, and the related mechanism may be associated with the inhibition of the MEK/ERK signaling pathway and activation of the Bax/Bcl-2 pathway. GSK-2816126 13-19 BCL2 associated X, apoptosis regulator Homo sapiens 246-249 33085231-7 2020 CONCLUSIONS: GSK126 can inhibit the proliferation of CAL-27 cells in tongue squamous cell carcinoma and promote its apoptosis, and the related mechanism may be associated with the inhibition of the MEK/ERK signaling pathway and activation of the Bax/Bcl-2 pathway. GSK-2816126 13-19 BCL2 apoptosis regulator Homo sapiens 250-255 32805266-5 2020 The present study aimed to examine the effectiveness of combination using EZH2 inhibitor GSK126 with antiandrogen enzalutamide in the treatment of CRPC cells. GSK-2816126 89-95 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 74-78 32906688-3 2020 In the current study, a combination of pomalidomide and GSK126 synergistically inhibited the growth of EZH2 gain-of-function mutant Diffuse large B-cell lymphoma (DLBCL) cells. GSK-2816126 56-62 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 103-107 32606728-0 2020 Diosgenin and GSK126 Produce Synergistic Effects on Epithelial-Mesenchymal Transition in Gastric Cancer Cells by Mediating EZH2 via the Rho/ROCK Signaling Pathway. GSK-2816126 14-20 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 123-127 32298702-6 2020 In this study, our results showed that intracerebroventricular (i.c.v) injection of the EZH2 pharmacological inhibitor GSK 126 (10 nM) increased seizure severity and shortened seizure latency in a rat model of FS, and these effects were accompanied by reduced GABA content. GSK-2816126 119-126 enhancer of zeste 2 polycomb repressive complex 2 subunit Rattus norvegicus 88-92 32606728-14 2020 Conclusion: Collectively, combined treatment with diosgenin and GSK126 produced even more significant effects on GC cell inhibition by targeting EZH2 via Rho/ROCK signaling-mediated EMT, which might be a therapeutic strategy for improving the poor therapeutic outcomes obtained with GSK126 monotherapy. GSK-2816126 64-70 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 145-149 32582297-7 2020 We show that a combination treatment of BIX0194 and GSK126, significantly increased FXN gene expression levels and reduced the repressive histone marks. GSK-2816126 52-58 frataxin Homo sapiens 84-87 32332097-5 2020 Co-administration of BMP2 with the EZH2 inhibitor GSK126 enhanced differentiation of murine (MC3T3) osteoblasts, reflected by increased alkaline phosphatase activity, alizarin red staining, and expression of bone-related marker genes (e.g. Bglap and Phospho1). GSK-2816126 50-56 bone morphogenetic protein 2 Mus musculus 21-25 32332097-5 2020 Co-administration of BMP2 with the EZH2 inhibitor GSK126 enhanced differentiation of murine (MC3T3) osteoblasts, reflected by increased alkaline phosphatase activity, alizarin red staining, and expression of bone-related marker genes (e.g. Bglap and Phospho1). GSK-2816126 50-56 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 35-39 32332097-5 2020 Co-administration of BMP2 with the EZH2 inhibitor GSK126 enhanced differentiation of murine (MC3T3) osteoblasts, reflected by increased alkaline phosphatase activity, alizarin red staining, and expression of bone-related marker genes (e.g. Bglap and Phospho1). GSK-2816126 50-56 bone gamma carboxyglutamate protein Mus musculus 240-245 32332097-5 2020 Co-administration of BMP2 with the EZH2 inhibitor GSK126 enhanced differentiation of murine (MC3T3) osteoblasts, reflected by increased alkaline phosphatase activity, alizarin red staining, and expression of bone-related marker genes (e.g. Bglap and Phospho1). GSK-2816126 50-56 phosphatase, orphan 1 Mus musculus 250-258 32332097-7 2020 Similarly, the BMP2-GSK126 co-treatment stimulated osteogenic differentiation of human bone marrow-derived mesenchymal stem/stromal cells, reflected by induction of key osteogenic markers (e.g. Osterix/SP7 and IBSP). GSK-2816126 20-26 bone morphogenetic protein 2 Homo sapiens 15-19 32332097-7 2020 Similarly, the BMP2-GSK126 co-treatment stimulated osteogenic differentiation of human bone marrow-derived mesenchymal stem/stromal cells, reflected by induction of key osteogenic markers (e.g. Osterix/SP7 and IBSP). GSK-2816126 20-26 Sp7 transcription factor 7 Mus musculus 194-201 32332097-7 2020 Similarly, the BMP2-GSK126 co-treatment stimulated osteogenic differentiation of human bone marrow-derived mesenchymal stem/stromal cells, reflected by induction of key osteogenic markers (e.g. Osterix/SP7 and IBSP). GSK-2816126 20-26 Sp7 transcription factor 7 Mus musculus 202-205 32332097-7 2020 Similarly, the BMP2-GSK126 co-treatment stimulated osteogenic differentiation of human bone marrow-derived mesenchymal stem/stromal cells, reflected by induction of key osteogenic markers (e.g. Osterix/SP7 and IBSP). GSK-2816126 20-26 integrin binding sialoprotein Mus musculus 210-214 32300280-7 2020 Combination of Vincristine with TPA/GSK126, a drug combination shown to induce differentiation of RMS cell lines, is able to partially overcome MYOD1/NOG cells chemoresistance. GSK-2816126 36-42 myogenic differentiation 1 Homo sapiens 144-149 32453339-6 2020 Moreover, combined treatment with the USP7-specific inhibitor P5091 and EZH2 inhibitors, such as GSK126, EPZ6438, and DZNep, induced synergistic inhibitory effects on cell migration, invasion, and sphere-forming potential in prostate cancer cells. GSK-2816126 97-103 ubiquitin specific peptidase 7 Homo sapiens 38-42 32453339-6 2020 Moreover, combined treatment with the USP7-specific inhibitor P5091 and EZH2 inhibitors, such as GSK126, EPZ6438, and DZNep, induced synergistic inhibitory effects on cell migration, invasion, and sphere-forming potential in prostate cancer cells. GSK-2816126 97-103 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 72-76 32135158-7 2020 Finally, overexpression of TEM8 or treating by H3K27me3-specific inhibitor GSK126 attenuated the inhibitory effect of DON on cell migration. GSK-2816126 75-81 ANTXR cell adhesion molecule 1 Homo sapiens 27-31 32041748-7 2020 Enhancer of zeste 2 (EZH2) was blocked with GSK126 inhibitor. GSK-2816126 44-50 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 21-25 32127003-6 2020 Proliferation, apoptosis, cancer stem-like cells (CSCs) properties, migration and invasion were evaluated under circumstances of treatment with either EZH2 shRNA or EZH2 inhibitor GSK126. GSK-2816126 180-186 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 165-169 32127003-10 2020 Targeting EZH2 either by genetics or small molecule inhibitor GSK126 decreased CSCs and motility and abrogated the liver metastasis of UM. GSK-2816126 62-68 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 10-14 32300280-7 2020 Combination of Vincristine with TPA/GSK126, a drug combination shown to induce differentiation of RMS cell lines, is able to partially overcome MYOD1/NOG cells chemoresistance. GSK-2816126 36-42 noggin Homo sapiens 150-153 31471312-0 2019 Phase I Study of the Novel Enhancer of Zeste Homolog 2 (EZH2) Inhibitor GSK2816126 in Patients with Advanced Hematologic and Solid Tumors. GSK-2816126 72-82 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 27-54 31471312-0 2019 Phase I Study of the Novel Enhancer of Zeste Homolog 2 (EZH2) Inhibitor GSK2816126 in Patients with Advanced Hematologic and Solid Tumors. GSK-2816126 72-82 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 56-60 31408621-4 2019 Furthermore, either pharmacological GSK126 inhibition or molecular silencing of EZH2 can inhibit the differentiation of atrial fibroblasts and the ability to produce ECM induced by Ang-II. GSK-2816126 36-42 angiotensinogen Homo sapiens 181-187 31408621-7 2019 Finally, our in vivo experiments demonstrated that the EZH2 inhibitor GSK126 significantly inhibited Ang-II-induced atrial enlargement and fibrosis and reduced AF vulnerability. GSK-2816126 70-76 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 55-59 31408621-7 2019 Finally, our in vivo experiments demonstrated that the EZH2 inhibitor GSK126 significantly inhibited Ang-II-induced atrial enlargement and fibrosis and reduced AF vulnerability. GSK-2816126 70-76 angiotensinogen Homo sapiens 101-107 30690451-8 2019 Genome-wide expression analysis revealed that after NPD13668 treatment, about half of the upregulated genes overlapped with genes upregulated after treatment with GSK126, well-known EZH2 catalytic inhibitor, indicating that NPD13668 is a potential modulator of EZH2 methyltransferase activity. GSK-2816126 163-169 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 182-186 30979734-9 2019 RESULTS: Exposure to GSK126 and romidepsin demonstrated potent synergy in lymphoma cell lines with EZH2 dysregulation. GSK-2816126 21-27 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 99-103 31372511-5 2019 Epigenetic-modifying agents such as 5-azacitidine, GSK126 and mocetinostat further reveal cell state-dependent plasticity upon GRHL2 overexpression. GSK-2816126 51-57 grainyhead like transcription factor 2 Homo sapiens 127-132 31036541-6 2019 To explore whether EZH2 inhibition by GSK126 enhances sensitivity to platinum drugs in EZH2-overexpressing breast cancers we used a Brca1-deficient mouse model. GSK-2816126 38-44 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 19-23 31036541-9 2019 Combined treatment with the EZH2 inhibitor GSK126 and cisplatin decreased cell proliferation and improved survival in Brca1-deficient mice in comparison with single agents. GSK-2816126 43-49 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 28-32 31367252-9 2019 Accordingly, the EZH2 inhibitor GSK126 de-represses CDKN1C and decreases CDYL-induced chemoresistance in SCLC. GSK-2816126 32-38 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 17-21 31367252-9 2019 Accordingly, the EZH2 inhibitor GSK126 de-represses CDKN1C and decreases CDYL-induced chemoresistance in SCLC. GSK-2816126 32-38 cyclin dependent kinase inhibitor 1C Homo sapiens 52-58 31367252-9 2019 Accordingly, the EZH2 inhibitor GSK126 de-represses CDKN1C and decreases CDYL-induced chemoresistance in SCLC. GSK-2816126 32-38 chromodomain Y like Homo sapiens 73-77 30690451-8 2019 Genome-wide expression analysis revealed that after NPD13668 treatment, about half of the upregulated genes overlapped with genes upregulated after treatment with GSK126, well-known EZH2 catalytic inhibitor, indicating that NPD13668 is a potential modulator of EZH2 methyltransferase activity. GSK-2816126 163-169 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 261-265 31085587-7 2019 We show that combining the EZH2 inhibitor GSK126 with enzalutamide synergistically inhibits cell proliferation and colony formation and promotes apoptosis in enzalutamide-resistant PCa cells. GSK-2816126 42-48 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 27-31 30971429-4 2019 We found that the EZH2-selective inhibitor GSK126 induced lipid accumulation in human adipocytes, without altering adipocyte differentiation marker gene expression. GSK-2816126 43-49 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 18-22 31092221-7 2019 Finally, we checked WHSC1 expression after treatment with the selective inhibitor, GSK126. GSK-2816126 83-89 nuclear receptor binding SET domain protein 2 Homo sapiens 20-25 30971429-9 2019 Deletion of ApoE blocked the effects of GSK126 to promote lipoprotein-dependent lipid uptake in murine adipocytes. GSK-2816126 40-46 apolipoprotein E Mus musculus 12-16 30942459-5 2019 Mechanistically, targeting EZH2 with minimal toxic concentrations of a pharmacological inhibitor (GSK126) markedly weakened the accompanying increase in the histone trimethylation H3K27me3 and aggravated DNA damage response (DDR)-associated apoptosis in vitro. GSK-2816126 98-104 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 27-31 31190748-7 2019 The Ezh2 inhibitor, GSK126, significantly reversed the SPC-induced changes in expression of H3K27me3, Pten, pAkt, mTOR, LC3B-II, and Beclin1. GSK-2816126 20-26 enhancer of zeste 2 polycomb repressive complex 2 subunit Rattus norvegicus 4-8 31190748-7 2019 The Ezh2 inhibitor, GSK126, significantly reversed the SPC-induced changes in expression of H3K27me3, Pten, pAkt, mTOR, LC3B-II, and Beclin1. GSK-2816126 20-26 phosphatase and tensin homolog Rattus norvegicus 102-106 31190748-7 2019 The Ezh2 inhibitor, GSK126, significantly reversed the SPC-induced changes in expression of H3K27me3, Pten, pAkt, mTOR, LC3B-II, and Beclin1. GSK-2816126 20-26 mechanistic target of rapamycin kinase Rattus norvegicus 114-118 31190748-7 2019 The Ezh2 inhibitor, GSK126, significantly reversed the SPC-induced changes in expression of H3K27me3, Pten, pAkt, mTOR, LC3B-II, and Beclin1. GSK-2816126 20-26 beclin 1 Rattus norvegicus 133-140 30711627-9 2019 Mice with hepatomas were given injections of GSK126 (an inhibitor of histone H3 lysine 27 methyltransferase [EZH2]) and 5-AZA-dC (an inhibitor of DNA methyltransferases); tumor tissues were analyzed by immunofluorescence and immunohistochemistry for the presence of immune cells and cytokines. GSK-2816126 45-51 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 109-113 30711627-18 2019 Injection of mice with GSK126 and 5-AZA-dC induced expression of CXCL10 by tumor cells and caused plasma cell polarization, suppression of the anti-tumor T cell response, and hepatoma growth. GSK-2816126 23-29 chemokine (C-X-C motif) ligand 10 Mus musculus 65-71 30737232-0 2019 EZH2 Inhibitor GSK126 Suppresses Antitumor Immunity by Driving Production of Myeloid-Derived Suppressor Cells. GSK-2816126 15-21 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 0-4 30737232-3 2019 Here we report that suppressing EZH2 activity using EZH2 inhibitor GSK126 resulted in increased numbers of myeloid-derived suppressor cells (MDSC) and fewer CD4+ and IFNgamma+CD8+ T cells, which are involved in antitumor immunity. GSK-2816126 67-73 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 32-36 30737232-3 2019 Here we report that suppressing EZH2 activity using EZH2 inhibitor GSK126 resulted in increased numbers of myeloid-derived suppressor cells (MDSC) and fewer CD4+ and IFNgamma+CD8+ T cells, which are involved in antitumor immunity. GSK-2816126 67-73 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 52-56 30051352-7 2019 In support of a dynamic role of EZH2 in repressing marked synaptic genes, the specific EZH2 inhibitor GSK126 significantly upregulated, while the demethylase inhibitor GSKJ4 downregulated the expression of Egr3 and Grin2c. GSK-2816126 102-108 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 32-36 30737232-3 2019 Here we report that suppressing EZH2 activity using EZH2 inhibitor GSK126 resulted in increased numbers of myeloid-derived suppressor cells (MDSC) and fewer CD4+ and IFNgamma+CD8+ T cells, which are involved in antitumor immunity. GSK-2816126 67-73 CD4 molecule Homo sapiens 157-160 30737232-3 2019 Here we report that suppressing EZH2 activity using EZH2 inhibitor GSK126 resulted in increased numbers of myeloid-derived suppressor cells (MDSC) and fewer CD4+ and IFNgamma+CD8+ T cells, which are involved in antitumor immunity. GSK-2816126 67-73 CD8a molecule Homo sapiens 175-178 30737232-7 2019 SIGNIFICANCE: This study uncovers a potential mechanism behind disappointing results of a phase I clinical trial of EZH2 inhibitor GSK126 and identifies a translatable combinational strategy to overcome it. GSK-2816126 131-137 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 116-120 30051352-7 2019 In support of a dynamic role of EZH2 in repressing marked synaptic genes, the specific EZH2 inhibitor GSK126 significantly upregulated, while the demethylase inhibitor GSKJ4 downregulated the expression of Egr3 and Grin2c. GSK-2816126 102-108 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 87-91 30051352-8 2019 GSK126 also upregulated the expression of Bdnf in mutant primary neurons. GSK-2816126 0-6 brain derived neurotrophic factor Mus musculus 42-46 30003817-9 2018 Then, we observed the effect of GSK126 (Ezh2 inhibitor) on the induction within the same over 72 hours duration. GSK-2816126 32-38 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 40-44 30487290-4 2018 These tumors display sensitivity to EZH2 inhibition by GSK126 but also amplify an inflammatory program involving signaling through NF-kappaB and genes residing in PRC2-regulated chromatin. GSK-2816126 55-61 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 36-40 29904056-3 2018 Pyridone-containing inhibitors such as GSK126 compete with S-adenosylmethionine (SAM) for Ezh2 binding and effectively inhibit PRC2 activity. GSK-2816126 39-45 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 90-94 29473431-3 2018 Three EZH2 inhibitors: tazemetostat (EPZ-6438), GSK2816126 and CPI-1205 have moved into phase I/phase II clinical trials in patients with non-Hodgkin lymphoma and genetically defined solid tumors. GSK-2816126 48-58 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 6-10 29789597-5 2018 Furthermore, GSK126 (an inhibitor for EZH2 trimethylation function) was applied in liver failure mice in vivo, and lipopolysaccharide-stimulated mononuclear cells in vitro. GSK-2816126 13-19 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 38-42 29789597-7 2018 GSK126 ameliorated disease severity in liver failure mice, which maybe attribute to down-regulate circulating and hepatic proinflammatory cytokines, especially TNF via reducing H3K27me3. GSK-2816126 0-6 tumor necrosis factor Mus musculus 160-163 29789597-9 2018 Nuclear factor kappa B (NF-kappaB) and protein kinase B (Akt) signalling pathways were activated upon lipopolysaccharide stimulation, but attenuated by using GSK126, accompanied with decreased TNF in vitro. GSK-2816126 158-164 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 0-22 29789597-9 2018 Nuclear factor kappa B (NF-kappaB) and protein kinase B (Akt) signalling pathways were activated upon lipopolysaccharide stimulation, but attenuated by using GSK126, accompanied with decreased TNF in vitro. GSK-2816126 158-164 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 24-33 29789597-9 2018 Nuclear factor kappa B (NF-kappaB) and protein kinase B (Akt) signalling pathways were activated upon lipopolysaccharide stimulation, but attenuated by using GSK126, accompanied with decreased TNF in vitro. GSK-2816126 158-164 thymoma viral proto-oncogene 1 Mus musculus 57-60 29789597-9 2018 Nuclear factor kappa B (NF-kappaB) and protein kinase B (Akt) signalling pathways were activated upon lipopolysaccharide stimulation, but attenuated by using GSK126, accompanied with decreased TNF in vitro. GSK-2816126 158-164 tumor necrosis factor Mus musculus 193-196 28978137-3 2017 We designed an EZH2 inhibitor (EZH2i) as a simplified analog of EPZ005687 and GSK2816126, MC3629, and we tested its biological activity in SHH MB-SLCs. GSK-2816126 78-88 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 15-19 29654753-3 2018 Here, we investigated the effects of the Ezh2-specific inhibitor GSK126 in a mouse model of obesity induced by a high-fat diet (HFD). GSK-2816126 65-71 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 41-45 29572378-6 2018 The activation of the PI3K/AKT and MAPK pathways decreased TNFSF10 and BAD expression through a FOXO3-dependent mechanism, which was required for the antitumor effects of EZH2i GSK126. GSK-2816126 177-183 AKT serine/threonine kinase 1 Homo sapiens 27-30 29572378-6 2018 The activation of the PI3K/AKT and MAPK pathways decreased TNFSF10 and BAD expression through a FOXO3-dependent mechanism, which was required for the antitumor effects of EZH2i GSK126. GSK-2816126 177-183 TNF superfamily member 10 Homo sapiens 59-66 29572378-6 2018 The activation of the PI3K/AKT and MAPK pathways decreased TNFSF10 and BAD expression through a FOXO3-dependent mechanism, which was required for the antitumor effects of EZH2i GSK126. GSK-2816126 177-183 forkhead box O3 Homo sapiens 96-101 29572378-6 2018 The activation of the PI3K/AKT and MAPK pathways decreased TNFSF10 and BAD expression through a FOXO3-dependent mechanism, which was required for the antitumor effects of EZH2i GSK126. GSK-2816126 177-183 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 171-175 29572378-10 2018 Notably, EZH2 inhibitor GSK126- and EPZ-6438-resistant DLBCL cells remained sensitive to the EZH2 inhibitor UNC1999 and embryonic ectoderm development protein inhibitor EED226, which provides an opportunity to treat DLBCLs that are resistant to these drugs. GSK-2816126 24-30 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 9-13 29572378-10 2018 Notably, EZH2 inhibitor GSK126- and EPZ-6438-resistant DLBCL cells remained sensitive to the EZH2 inhibitor UNC1999 and embryonic ectoderm development protein inhibitor EED226, which provides an opportunity to treat DLBCLs that are resistant to these drugs. GSK-2816126 24-30 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 93-97 29896299-11 2018 Functionally, inhibition of H3K27me3 by EZH2 siRNA or GSK126 (a specific EZH2 inhibitor) reduced H3K27me3 levels and monocyte adhesion to endothelial cells. GSK-2816126 54-60 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 73-77 28722764-7 2018 The combination of TPA with GSK126, an inhibitor of the catalytic activity of EZH2, has a synergic effect on the induction of muscle differentiation in RD rhabdomyosarcoma cells, suggesting a new therapeutic combinatory approach for RMS treatment. GSK-2816126 28-34 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 78-82 29070525-0 2018 PTEN Is Fundamental for Elimination of Leukemia Stem Cells Mediated by GSK126 Targeting EZH2 in Chronic Myelogenous Leukemia. GSK-2816126 71-77 phosphatase and tensin homolog Mus musculus 0-4 29070525-0 2018 PTEN Is Fundamental for Elimination of Leukemia Stem Cells Mediated by GSK126 Targeting EZH2 in Chronic Myelogenous Leukemia. GSK-2816126 71-77 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 88-92 29070525-4 2018 Suppression of EZH2 by GSK126 or specific shRNA prolonged survival of CML mice and reduced the number of LSCs in mice. GSK-2816126 23-29 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 15-19 29070525-6 2018 The effect of EZH2 knockdown in the CML mice was at least partially reversed by PTEN knockdown.Conclusions: These findings improve the understanding of the epigenetic regulation of stemness in CML LSCs and warrant clinical trial of GSK126 in refractory patients with CML. GSK-2816126 232-238 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 14-18 29070525-6 2018 The effect of EZH2 knockdown in the CML mice was at least partially reversed by PTEN knockdown.Conclusions: These findings improve the understanding of the epigenetic regulation of stemness in CML LSCs and warrant clinical trial of GSK126 in refractory patients with CML. GSK-2816126 232-238 phosphatase and tensin homolog Mus musculus 80-84 28979810-8 2017 shRNA targeting enhancer of zeste homolog 2 (EZH2) or its inhibitor GSK126 significantly promoted chemotherapeutic drug-induced genotoxicity and increased HepG2 cell chemosensitivity. GSK-2816126 68-74 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 45-49 29545866-0 2018 GSK126 (EZH2 inhibitor) interferes with ultraviolet A radiation-induced photoaging of human skin fibroblast cells. GSK-2816126 0-6 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 8-12 29545866-5 2018 GSK126, a histone methylation enzyme inhibitor of EZH2, was used as an experimental factor. GSK-2816126 0-6 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 50-54 29545866-6 2018 Results suggested that GSK126 downregulated the mRNA expression levels of EZH2 and upregulated the mRNA expression levels of BMI-1. GSK-2816126 23-29 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 74-78 29545866-6 2018 Results suggested that GSK126 downregulated the mRNA expression levels of EZH2 and upregulated the mRNA expression levels of BMI-1. GSK-2816126 23-29 BMI1 proto-oncogene, polycomb ring finger Homo sapiens 125-130 27563817-8 2016 Furthermore, TGF-beta enhanced expression of ZEB2 in EZH2 siRNA- or GSK126-treated cells (P<0.01), suggesting that H3K27me3 plays a role in TGF-beta-stimulated ZEB2 induction. GSK-2816126 68-74 transforming growth factor beta 1 Homo sapiens 13-21 28826853-5 2017 The specific EZH2 inhibitor GSK126 directed hESC differentiation toward mesoderm and generated more MSCs by reducing H3K27me3. GSK-2816126 28-34 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 13-17 28246193-5 2017 Unexpectedly, administration of the Ezh2 inhibitor GSK126, which specifically decreases H3K27me3 without affecting Ezh2 protein, failed to prevent the disease. GSK-2816126 51-57 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 36-40 28214660-7 2017 Unexpectedly, treatment of 3 EZH2-high expressing neuroblastoma cell lines (IMR32, CHP134 and NMB), with EZH2-specific inhibitors (GSK126 and EPZ6438) resulted in only a slight G1 arrest, despite maximum histone methyltransferase activity inhibition. GSK-2816126 131-137 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 29-33 28214660-7 2017 Unexpectedly, treatment of 3 EZH2-high expressing neuroblastoma cell lines (IMR32, CHP134 and NMB), with EZH2-specific inhibitors (GSK126 and EPZ6438) resulted in only a slight G1 arrest, despite maximum histone methyltransferase activity inhibition. GSK-2816126 131-137 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 105-109 27253463-5 2017 The expression of XPA was significantly increased by EZH2 specific inhibitor GSK126 or lentiviral shEZH2 in nasopharyngeal carcinoma (NPC) CNE and 8F cell lines. GSK-2816126 77-83 XPA, DNA damage recognition and repair factor Homo sapiens 18-21 27253463-5 2017 The expression of XPA was significantly increased by EZH2 specific inhibitor GSK126 or lentiviral shEZH2 in nasopharyngeal carcinoma (NPC) CNE and 8F cell lines. GSK-2816126 77-83 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 53-57 28122578-7 2017 A differential synergistic effect was observed in combinations of gemcitabine with olaparib or GSK126 in KMBC cells and TSA or bAP15 in HuCCT1 cells, indicating BAP1 dependent target-specific synergism and sensitivity to gemcitabine. GSK-2816126 95-101 BRCA1 associated protein 1 Homo sapiens 161-165 27926488-0 2017 Blocking EZH2 methylation transferase activity by GSK126 decreases stem cell-like myeloma cells. GSK-2816126 50-56 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 9-13 27926488-6 2017 Progressive release of mitochondrial cytochrome c and AIF into the cytosol was detected in GSK126-treated MM cells. GSK-2816126 91-97 cytochrome c, somatic Homo sapiens 37-49 27926488-6 2017 Progressive release of mitochondrial cytochrome c and AIF into the cytosol was detected in GSK126-treated MM cells. GSK-2816126 91-97 apoptosis inducing factor mitochondria associated 1 Homo sapiens 54-57 27926488-7 2017 GSK126 treatment elicited caspase-3-dependent MCL-1 cleavage with accumulation of proapoptotic truncated MCL-1. GSK-2816126 0-6 caspase 3 Homo sapiens 26-35 27926488-7 2017 GSK126 treatment elicited caspase-3-dependent MCL-1 cleavage with accumulation of proapoptotic truncated MCL-1. GSK-2816126 0-6 MCL1 apoptosis regulator, BCL2 family member Homo sapiens 46-51 27926488-7 2017 GSK126 treatment elicited caspase-3-dependent MCL-1 cleavage with accumulation of proapoptotic truncated MCL-1. GSK-2816126 0-6 MCL1 apoptosis regulator, BCL2 family member Homo sapiens 105-110 27926488-10 2017 Using ALDH and side population (SP) assays to characterize CSCs, we found that GSK126 eliminated the stem-like myeloma cells by blocking the Wnt/beta-catenin pathway. GSK-2816126 79-85 catenin beta 1 Homo sapiens 145-157 27926488-12 2017 In conclusion, our findings suggest that EZH2 inactivation by GSK126 is effective in killing MM cells and CSCs as a single agent or in combination with bortezomib. GSK-2816126 62-68 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 41-45 28418882-7 2017 Consistent with these results, treatment with GSK126, a specific EZH2 inhibitor, suppressed endometrial cancer cell growth and decreased the number of cancer cell colonies. GSK-2816126 46-52 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 65-69 27563817-8 2016 Furthermore, TGF-beta enhanced expression of ZEB2 in EZH2 siRNA- or GSK126-treated cells (P<0.01), suggesting that H3K27me3 plays a role in TGF-beta-stimulated ZEB2 induction. GSK-2816126 68-74 zinc finger E-box binding homeobox 2 Homo sapiens 45-49 27563817-8 2016 Furthermore, TGF-beta enhanced expression of ZEB2 in EZH2 siRNA- or GSK126-treated cells (P<0.01), suggesting that H3K27me3 plays a role in TGF-beta-stimulated ZEB2 induction. GSK-2816126 68-74 transforming growth factor beta 1 Homo sapiens 143-151 27563817-8 2016 Furthermore, TGF-beta enhanced expression of ZEB2 in EZH2 siRNA- or GSK126-treated cells (P<0.01), suggesting that H3K27me3 plays a role in TGF-beta-stimulated ZEB2 induction. GSK-2816126 68-74 zinc finger E-box binding homeobox 2 Homo sapiens 163-167 26693692-3 2016 We show that the Ezh2 stem cell survival protein is enriched in MCS cells and that Ezh2 knockdown or treatment with small molecule Ezh2 inhibitors, GSK126 or EPZ-6438, reduces Ezh2 activity. GSK-2816126 148-154 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 17-21 26693692-3 2016 We show that the Ezh2 stem cell survival protein is enriched in MCS cells and that Ezh2 knockdown or treatment with small molecule Ezh2 inhibitors, GSK126 or EPZ-6438, reduces Ezh2 activity. GSK-2816126 148-154 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 83-87 26693692-3 2016 We show that the Ezh2 stem cell survival protein is enriched in MCS cells and that Ezh2 knockdown or treatment with small molecule Ezh2 inhibitors, GSK126 or EPZ-6438, reduces Ezh2 activity. GSK-2816126 148-154 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 83-87 26693692-3 2016 We show that the Ezh2 stem cell survival protein is enriched in MCS cells and that Ezh2 knockdown or treatment with small molecule Ezh2 inhibitors, GSK126 or EPZ-6438, reduces Ezh2 activity. GSK-2816126 148-154 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 83-87 26898301-0 2016 The novel EZH2 inhibitor, GSK126, suppresses cell migration and angiogenesis via down-regulating VEGF-A. GSK-2816126 26-32 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 10-14 27289323-4 2016 GSK126, a specific inhibitor of EZH2, is undergoing phase I trials for hypermethylation-related cancers. GSK-2816126 0-6 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 32-36 27634879-3 2016 To determine whether colorectal cancer cells respond to EZH2 inhibition and to explore which factors influence the degree of response, we treated a panel of 20 organoid lines derived from human colon tumors with different concentrations of the EZH2 inhibitor GSK126. GSK-2816126 259-265 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 244-248 27183582-5 2016 Inhibition of EZH2 by the small molecule GSK126, or decreasing its expression using antisense oligonucleotides, impeded osteoclast differentiation. GSK-2816126 41-47 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 14-18 27868408-0 2016 [Effect of a novel EZH2 inhibitor GSK126 on prostate cancer cells]. GSK-2816126 34-40 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 19-23 27868408-1 2016 Objective: To investigate the effect of a novel EZH2 inhibitor GSK126 on cell growth, apoptosis and migration of prostate cancer cells. GSK-2816126 63-69 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 48-52 27868408-10 2016 In addition, GSK126 up-regulated E-cadherin mRNA expression and down-regulated N-cadherin and Vimentin mRNA expression, whereas had no significant effect on Snail, Fibronectin and VEGF-A mRNA expression. GSK-2816126 13-19 cadherin 1 Homo sapiens 33-43 27868408-10 2016 In addition, GSK126 up-regulated E-cadherin mRNA expression and down-regulated N-cadherin and Vimentin mRNA expression, whereas had no significant effect on Snail, Fibronectin and VEGF-A mRNA expression. GSK-2816126 13-19 cadherin 2 Homo sapiens 79-89 27868408-10 2016 In addition, GSK126 up-regulated E-cadherin mRNA expression and down-regulated N-cadherin and Vimentin mRNA expression, whereas had no significant effect on Snail, Fibronectin and VEGF-A mRNA expression. GSK-2816126 13-19 vimentin Homo sapiens 94-102 26898301-0 2016 The novel EZH2 inhibitor, GSK126, suppresses cell migration and angiogenesis via down-regulating VEGF-A. GSK-2816126 26-32 vascular endothelial growth factor A Homo sapiens 97-103 26898301-10 2016 GSK126 reduced both the mRNA and protein expression of VEGF-A in a dose-dependent manner. GSK-2816126 0-6 vascular endothelial growth factor A Homo sapiens 55-61 26898301-12 2016 CONCLUSIONS: GSK126 inhibits cell migration and angiogenesis in solid tumor cell lines through down-regulation of VEGF-A expression. GSK-2816126 13-19 vascular endothelial growth factor A Homo sapiens 114-120 26572704-8 2016 Also administration of sorafenib, a multikinase inhibitor, can inhibit cancer proliferation with PIK3CA mutation and resistance to mTOR inhibitors and GSK126, a molecular-targeted drug can inhibit proliferation of ARID1A-mutated ovarian clear cell adenocarcinoma cells by targeting and inhibiting EZH2. GSK-2816126 151-157 AT-rich interaction domain 1A Homo sapiens 214-220 26936398-5 2016 Identified changes in target genes were validated by interrogation of microarray data from melanoma cells treated with the EZH2 inhibitor GSK126. GSK-2816126 138-144 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 123-127 26936398-8 2016 GSK126 treatment of melanoma lines containing EZH2 activation reversed such transcriptional repression in 98 candidate target genes. GSK-2816126 0-6 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 46-50 26657505-8 2016 We further showed that the EZH2 inhibitor GSK126 inhibits both Polycomb-dependent and -independent functions of EZH2 in PCa cells. GSK-2816126 42-48 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 27-31 26657505-8 2016 We further showed that the EZH2 inhibitor GSK126 inhibits both Polycomb-dependent and -independent functions of EZH2 in PCa cells. GSK-2816126 42-48 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 112-116 26572704-8 2016 Also administration of sorafenib, a multikinase inhibitor, can inhibit cancer proliferation with PIK3CA mutation and resistance to mTOR inhibitors and GSK126, a molecular-targeted drug can inhibit proliferation of ARID1A-mutated ovarian clear cell adenocarcinoma cells by targeting and inhibiting EZH2. GSK-2816126 151-157 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 297-301 25531315-6 2015 Furthermore, treatment with GSK126, an inhibitor of EZH2 methyltransferase activity, induced FOXA1 expression in BRCA1-deficient but not in BRCA1-reconstituted MMECs. GSK-2816126 28-34 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 52-56 26593398-8 2015 In vitro experiments revealed a significant (p <= 0.05) decrease of tumor cell proliferation using the EZH2 inhibitor GSK126. GSK-2816126 121-127 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 106-110 26304929-3 2015 In this study we have targeted EZH2 with a specific inhibitor (GSK126) or depleted EZH2 protein by stable shRNA knockdown. GSK-2816126 63-69 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 31-35 26515777-5 2016 Then GSK126 and GSK-J4, two small molecule inhibitors of H3K27me3 methylase (EZH2) and demethylases (UTX/JMJD3), were used to regulate the H3K27me3 level. GSK-2816126 5-11 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 77-81 26515777-5 2016 Then GSK126 and GSK-J4, two small molecule inhibitors of H3K27me3 methylase (EZH2) and demethylases (UTX/JMJD3), were used to regulate the H3K27me3 level. GSK-2816126 5-11 lysine demethylase 6A Homo sapiens 101-104 26515777-5 2016 Then GSK126 and GSK-J4, two small molecule inhibitors of H3K27me3 methylase (EZH2) and demethylases (UTX/JMJD3), were used to regulate the H3K27me3 level. GSK-2816126 5-11 lysine demethylase 6B Homo sapiens 105-110 26515777-6 2016 The results showed that H3K27me3 level was reduced in cloned embryos after treatment of PEF with 0.75 muM GSK126 for 48 h, incubation of one-cell reconstructed oocytes with 0.1 muM GSK126 and injection of antibody for EZH2 into oocyte. GSK-2816126 106-112 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 218-222 25868794-4 2015 All EZH2 inhibitors are transported by P-gp and BCRP, although in vitro the transporter affinity of GSK126 was obscured by very low membrane permeability. GSK-2816126 100-106 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 4-8 25868794-4 2015 All EZH2 inhibitors are transported by P-gp and BCRP, although in vitro the transporter affinity of GSK126 was obscured by very low membrane permeability. GSK-2816126 100-106 phosphoglycolate phosphatase Mus musculus 39-43 25868794-4 2015 All EZH2 inhibitors are transported by P-gp and BCRP, although in vitro the transporter affinity of GSK126 was obscured by very low membrane permeability. GSK-2816126 100-106 ATP binding cassette subfamily G member 2 (Junior blood group) Mus musculus 48-52 25868794-8 2015 Moreover, the oral bioavailability of GSK126 is only 0.2% in WT mice, which increases to 14.4% in Abcb1;Abcg2 knockout mice. GSK-2816126 38-44 ATP-binding cassette, sub-family B (MDR/TAP), member 1B Mus musculus 98-103 25868794-8 2015 Moreover, the oral bioavailability of GSK126 is only 0.2% in WT mice, which increases to 14.4% in Abcb1;Abcg2 knockout mice. GSK-2816126 38-44 ATP binding cassette subfamily G member 2 (Junior blood group) Mus musculus 104-109 25531315-6 2015 Furthermore, treatment with GSK126, an inhibitor of EZH2 methyltransferase activity, induced FOXA1 expression in BRCA1-deficient but not in BRCA1-reconstituted MMECs. GSK-2816126 28-34 forkhead box A1 Homo sapiens 93-98 25531315-6 2015 Furthermore, treatment with GSK126, an inhibitor of EZH2 methyltransferase activity, induced FOXA1 expression in BRCA1-deficient but not in BRCA1-reconstituted MMECs. GSK-2816126 28-34 BRCA1 DNA repair associated Homo sapiens 113-118 25175925-8 2014 Treatment with the EZH2 inhibitor (GSK126) significantly restored ARNTL expression in these cells (CP70 and MCP2). GSK-2816126 35-41 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 19-23 25633838-5 2015 The expression of VEGF-A and phosphorylated Ser(473)-AKT, cell proliferation, migration and metastasis were enhanced in EZH2-overexpressing A549 cells, but inhibited in parental H2087 cells with EZH2 silencing or GSK126 treatment. GSK-2816126 213-219 vascular endothelial growth factor A Homo sapiens 18-24 25633838-5 2015 The expression of VEGF-A and phosphorylated Ser(473)-AKT, cell proliferation, migration and metastasis were enhanced in EZH2-overexpressing A549 cells, but inhibited in parental H2087 cells with EZH2 silencing or GSK126 treatment. GSK-2816126 213-219 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 120-124 25477340-6 2015 Combined treatment with a DNA demethylating agent, 5-aza-2"-deoxycytidine (5-aza-dC) and an EZH2 inhibitor, GSK126, induced marked re-expression of genes with the dual modification, including known tumor-suppressor genes such as IGFBP7 and SFRP1, and showed an additive inhibitory effect on growth of cancer cells in vitro. GSK-2816126 108-114 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 92-96 25477340-6 2015 Combined treatment with a DNA demethylating agent, 5-aza-2"-deoxycytidine (5-aza-dC) and an EZH2 inhibitor, GSK126, induced marked re-expression of genes with the dual modification, including known tumor-suppressor genes such as IGFBP7 and SFRP1, and showed an additive inhibitory effect on growth of cancer cells in vitro. GSK-2816126 108-114 insulin like growth factor binding protein 7 Homo sapiens 229-235 25477340-6 2015 Combined treatment with a DNA demethylating agent, 5-aza-2"-deoxycytidine (5-aza-dC) and an EZH2 inhibitor, GSK126, induced marked re-expression of genes with the dual modification, including known tumor-suppressor genes such as IGFBP7 and SFRP1, and showed an additive inhibitory effect on growth of cancer cells in vitro. GSK-2816126 108-114 secreted frizzled related protein 1 Homo sapiens 240-245 25253781-8 2014 Treatment of A687V EZH2-mutant cells with GSK126, a selective EZH2 inhibitor, was associated with a global decrease in H3K27me3, robust gene activation, caspase activation, and decreased proliferation. GSK-2816126 42-48 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 19-23 25253781-8 2014 Treatment of A687V EZH2-mutant cells with GSK126, a selective EZH2 inhibitor, was associated with a global decrease in H3K27me3, robust gene activation, caspase activation, and decreased proliferation. GSK-2816126 42-48 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 62-66 25695204-8 2015 Following treatment of the Colo205 and HT-29 CRC cell lines, with the EZH2 inhibitor, GSK126, the level of histone H3 lysine 27 trimethylation (H3K27me3) was reduced and the mRNA and protein expression levels of CLDN23 were increased. GSK-2816126 86-92 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 70-74 25695204-8 2015 Following treatment of the Colo205 and HT-29 CRC cell lines, with the EZH2 inhibitor, GSK126, the level of histone H3 lysine 27 trimethylation (H3K27me3) was reduced and the mRNA and protein expression levels of CLDN23 were increased. GSK-2816126 86-92 claudin 23 Homo sapiens 212-218 25695204-9 2015 ChIP analysis confirmed that the level of H3K27m3 along the CLDN23 gene was decreased in the GSK126-treated cell lines. GSK-2816126 93-99 claudin 23 Homo sapiens 60-66 25605014-7 2015 Combination of the Top2 poison etoposide with the Ezh2 inhibitor GSK126 or DZNep significantly increased cell death in vitro in murine and human prostate cancer cell lines. GSK-2816126 65-71 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 50-54 25266721-6 2014 Treatment of malignant cells with the c-Rel inhibitor pentoxifylline not only reduced c-Rel nuclear translocation and Ezh2 expression, but also enhanced their sensitivity to the Ezh2-specific drug, GSK126 through increased growth inhibition and cell death. GSK-2816126 198-204 REL proto-oncogene, NF-kB subunit Homo sapiens 38-43 25266721-6 2014 Treatment of malignant cells with the c-Rel inhibitor pentoxifylline not only reduced c-Rel nuclear translocation and Ezh2 expression, but also enhanced their sensitivity to the Ezh2-specific drug, GSK126 through increased growth inhibition and cell death. GSK-2816126 198-204 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 178-182 25175925-8 2014 Treatment with the EZH2 inhibitor (GSK126) significantly restored ARNTL expression in these cells (CP70 and MCP2). GSK-2816126 35-41 aryl hydrocarbon receptor nuclear translocator like Homo sapiens 66-71 25175925-8 2014 Treatment with the EZH2 inhibitor (GSK126) significantly restored ARNTL expression in these cells (CP70 and MCP2). GSK-2816126 35-41 C-C motif chemokine ligand 8 Homo sapiens 108-112 23714854-6 2013 Treatment with EZH2 inhibitors, DZNep and GSK126, resulted in growth repression of SCLC cell lines. GSK-2816126 42-48 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 15-19 24304166-4 2014 Recent work has identified GSK126 as a potent, selective, SAM-competitive inhibitor of EZH2 capable of globally decreasing H3K27 trimethylation in cells. GSK-2816126 27-33 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 87-91 24304166-6 2014 Additionally, GSK126 is shown to have a significantly longer residence time of inhibition on the activated form of EZH2/PRC2 as compared to unactivated EZH2/PRC2. GSK-2816126 14-20 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 115-119 24304166-8 2014 The data suggest that activation of EZH2 allows the enzyme to adopt a conformation that possesses greater affinity for GSK126. GSK-2816126 119-125 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 36-40 34820775-7 2021 The expression and function of EZH2 in trophoblasts were knocked down either by the use of siRNA or GSK126 as an inhibitor. GSK-2816126 100-106 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 31-35 23051747-8 2012 Here we demonstrate that GSK126, a potent, highly selective, S-adenosyl-methionine-competitive, small-molecule inhibitor of EZH2 methyltransferase activity, decreases global H3K27me3 levels and reactivates silenced PRC2 target genes. GSK-2816126 25-31 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 124-128 23051747-9 2012 GSK126 effectively inhibits the proliferation of EZH2 mutant DLBCL cell lines and markedly inhibits the growth of EZH2 mutant DLBCL xenografts in mice. GSK-2816126 0-6 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 49-53 23051747-9 2012 GSK126 effectively inhibits the proliferation of EZH2 mutant DLBCL cell lines and markedly inhibits the growth of EZH2 mutant DLBCL xenografts in mice. GSK-2816126 0-6 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 114-118 33234056-6 2021 Results Pre-treatment of BMSCs with BMP2 and BMP2/GSK126 co-stimulated expression of osteoblast-related genes (e.g., IBSP, SP7, RUNX2 and DLX5), as well as protein accumulation (e.g., collagen Type 1/COL1A1 and osteocalcin/BGLAP) based on immunofluorescence staining. GSK-2816126 50-56 bone morphogenetic protein 2 Mus musculus 45-49 33234056-6 2021 Results Pre-treatment of BMSCs with BMP2 and BMP2/GSK126 co-stimulated expression of osteoblast-related genes (e.g., IBSP, SP7, RUNX2 and DLX5), as well as protein accumulation (e.g., collagen Type 1/COL1A1 and osteocalcin/BGLAP) based on immunofluorescence staining. GSK-2816126 50-56 integrin binding sialoprotein Homo sapiens 117-121 33234056-6 2021 Results Pre-treatment of BMSCs with BMP2 and BMP2/GSK126 co-stimulated expression of osteoblast-related genes (e.g., IBSP, SP7, RUNX2 and DLX5), as well as protein accumulation (e.g., collagen Type 1/COL1A1 and osteocalcin/BGLAP) based on immunofluorescence staining. GSK-2816126 50-56 Sp7 transcription factor Homo sapiens 123-126 33234056-6 2021 Results Pre-treatment of BMSCs with BMP2 and BMP2/GSK126 co-stimulated expression of osteoblast-related genes (e.g., IBSP, SP7, RUNX2 and DLX5), as well as protein accumulation (e.g., collagen Type 1/COL1A1 and osteocalcin/BGLAP) based on immunofluorescence staining. GSK-2816126 50-56 RUNX family transcription factor 2 Homo sapiens 128-133 33234056-6 2021 Results Pre-treatment of BMSCs with BMP2 and BMP2/GSK126 co-stimulated expression of osteoblast-related genes (e.g., IBSP, SP7, RUNX2 and DLX5), as well as protein accumulation (e.g., collagen Type 1/COL1A1 and osteocalcin/BGLAP) based on immunofluorescence staining. GSK-2816126 50-56 distal-less homeobox 5 Homo sapiens 138-142 33234056-6 2021 Results Pre-treatment of BMSCs with BMP2 and BMP2/GSK126 co-stimulated expression of osteoblast-related genes (e.g., IBSP, SP7, RUNX2 and DLX5), as well as protein accumulation (e.g., collagen Type 1/COL1A1 and osteocalcin/BGLAP) based on immunofluorescence staining. GSK-2816126 50-56 collagen type I alpha 1 chain Homo sapiens 200-206 33234056-6 2021 Results Pre-treatment of BMSCs with BMP2 and BMP2/GSK126 co-stimulated expression of osteoblast-related genes (e.g., IBSP, SP7, RUNX2 and DLX5), as well as protein accumulation (e.g., collagen Type 1/COL1A1 and osteocalcin/BGLAP) based on immunofluorescence staining. GSK-2816126 50-56 bone gamma-carboxyglutamate protein Homo sapiens 211-222 33234056-6 2021 Results Pre-treatment of BMSCs with BMP2 and BMP2/GSK126 co-stimulated expression of osteoblast-related genes (e.g., IBSP, SP7, RUNX2 and DLX5), as well as protein accumulation (e.g., collagen Type 1/COL1A1 and osteocalcin/BGLAP) based on immunofluorescence staining. GSK-2816126 50-56 bone gamma-carboxyglutamate protein Homo sapiens 223-228 34175897-7 2021 We show that combined treatment with GSK126 and 5-Aza-2d treatment wit synergistically inhibited methyltransferase activity of EZH2 and DNMT3B, resulting in a profound block of EC cell proliferation as well as EC tumor progression in cell line-derived xenograft (CDX) and patient-derived xenograft (PDX) mouse models. GSK-2816126 37-43 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 127-131 34175897-7 2021 We show that combined treatment with GSK126 and 5-Aza-2d treatment wit synergistically inhibited methyltransferase activity of EZH2 and DNMT3B, resulting in a profound block of EC cell proliferation as well as EC tumor progression in cell line-derived xenograft (CDX) and patient-derived xenograft (PDX) mouse models. GSK-2816126 37-43 DNA methyltransferase 3 beta Homo sapiens 136-142 34876150-12 2021 GDSC and drug-resistance assays suggested that low SNF5 expression renders T24 and 5637 cells high sensitivity to EGFR inhibitor gefitinib, and combination of EZH2 inhibitor GSK126 and cisplatin. GSK-2816126 174-180 SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily b, member 1 Homo sapiens 51-55 34876150-12 2021 GDSC and drug-resistance assays suggested that low SNF5 expression renders T24 and 5637 cells high sensitivity to EGFR inhibitor gefitinib, and combination of EZH2 inhibitor GSK126 and cisplatin. GSK-2816126 174-180 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 159-163 34638497-4 2021 Viability of PanNEN cell lines treated with EZH2 inhibitor (GSK126) was determined in vitro. GSK-2816126 60-66 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 44-48 34815475-6 2021 The EZH2 inhibitor GSK126 also repressed proliferation of CNDT2.5 cells. GSK-2816126 19-25 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 4-8 34789399-9 2021 Notably, studies on esophagogastroduodenal anastomosis (EGDA) rat models showed the attenuation of Claudin-1 level and barrier function could be rescued by an Ezh2 inhibitor GSK126. GSK-2816126 174-180 claudin 1 Rattus norvegicus 99-108 34789399-9 2021 Notably, studies on esophagogastroduodenal anastomosis (EGDA) rat models showed the attenuation of Claudin-1 level and barrier function could be rescued by an Ezh2 inhibitor GSK126. GSK-2816126 174-180 enhancer of zeste 2 polycomb repressive complex 2 subunit Rattus norvegicus 159-163 35432300-9 2022 In vivo, we found that the percentage of CD206+ macrophages of the TME was decreased under the treatment of EPZ6438, but it increased upon GSK126 treatment. GSK-2816126 139-145 mannose receptor C-type 1 Homo sapiens 41-46 34149887-0 2021 Pharmacological inhibition of EZH2 by GSK126 decreases atherosclerosis by modulating foam cell formation and monocyte adhesion in apolipoprotein E-deficient mice. GSK-2816126 38-44 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 30-34 34149887-4 2021 The present study aimed to determine the effects of the EZH2 inhibitor, GSK126, on the suppression and regression of atherosclerosis in apolipoprotein E-deficient mouse models. GSK-2816126 72-78 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 56-60 34149887-5 2021 In vitro, it was found that pharmacological inhibition of EZH2 by GSK126 markedly reduced lipid transportation and monocyte adhesion during atherogenesis, predominantly through increasing the expression levels of ATP-binding cassette transporter A1 and suppressing vascular cell adhesion molecule 1 in human THP-1 cells. GSK-2816126 66-72 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 58-62 34149887-5 2021 In vitro, it was found that pharmacological inhibition of EZH2 by GSK126 markedly reduced lipid transportation and monocyte adhesion during atherogenesis, predominantly through increasing the expression levels of ATP-binding cassette transporter A1 and suppressing vascular cell adhesion molecule 1 in human THP-1 cells. GSK-2816126 66-72 ATP binding cassette subfamily A member 1 Homo sapiens 213-248 34149887-5 2021 In vitro, it was found that pharmacological inhibition of EZH2 by GSK126 markedly reduced lipid transportation and monocyte adhesion during atherogenesis, predominantly through increasing the expression levels of ATP-binding cassette transporter A1 and suppressing vascular cell adhesion molecule 1 in human THP-1 cells. GSK-2816126 66-72 vascular cell adhesion molecule 1 Homo sapiens 265-298 34335707-4 2021 In vitro, PC cell lines PANC-1 and AsPC-1 were cultured, and MTT and flow cytometry were performed to observe the effects of pan-PPAR agonist bezafibrate and EZH2 selective inhibitor GSK126 on cell viability and apoptosis. GSK-2816126 183-189 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 158-162 34335707-8 2021 It also significantly enhanced the effects of GSK126 on upregulating the expression level of p-beta-catenin and that of cleaved caspase 3 in vitro and in vivo. GSK-2816126 46-52 catenin beta 1 Homo sapiens 95-107 34335707-10 2021 These results suggest that the combination of bezafibrate and GSK126 has synergistic effects on PC, and the molecular mechanism may be related to the enhanced inhibition of the Wnt/beta-catenin signaling pathway. GSK-2816126 62-68 catenin beta 1 Homo sapiens 181-193 35617639-7 2022 Furthermore, when the methyltransferase activity of EZH2 was inhibited by its specific inhibitor GSK126, the level of miR-101 was increased in OGD/R-exposed SH-SY5Y cells. GSK-2816126 97-103 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 52-56 34336705-6 2021 In this study we evaluated the ability of GSK126, a blood-brain barrier (BBB) permeable small molecule inhibitor of EZH2, to reverse GBM immune evasion by epigenetic suppression of T cell chemotaxis. GSK-2816126 42-48 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 116-120 34336705-12 2021 Closer examination of the mechanism of action of GSK126 revealed its ability to promote the expression of IFN-gamma driven chemokines CXCL9 and CXCL10 from the tumor cells, that work to traffic T cells without directly affecting T maturation and/or proliferation. GSK-2816126 49-55 interferon gamma Mus musculus 106-115 34336705-12 2021 Closer examination of the mechanism of action of GSK126 revealed its ability to promote the expression of IFN-gamma driven chemokines CXCL9 and CXCL10 from the tumor cells, that work to traffic T cells without directly affecting T maturation and/or proliferation. GSK-2816126 49-55 chemokine (C-X-C motif) ligand 9 Mus musculus 134-139 34336705-12 2021 Closer examination of the mechanism of action of GSK126 revealed its ability to promote the expression of IFN-gamma driven chemokines CXCL9 and CXCL10 from the tumor cells, that work to traffic T cells without directly affecting T maturation and/or proliferation. GSK-2816126 49-55 chemokine (C-X-C motif) ligand 10 Mus musculus 144-150 35623249-2 2022 However, current EZH2 inhibitors, including Tazemetostat and GSK126, affect the methyl catalytic capacity of EZH2 and have little effect on the tumorigenic activity of EZH2 itself, resulting in poor efficacy against most solid tumors. GSK-2816126 61-67 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 17-21 35623249-2 2022 However, current EZH2 inhibitors, including Tazemetostat and GSK126, affect the methyl catalytic capacity of EZH2 and have little effect on the tumorigenic activity of EZH2 itself, resulting in poor efficacy against most solid tumors. GSK-2816126 61-67 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 109-113 35449124-5 2022 The combination of FXR agonist OCA plus EZH2 inhibitor GSK126 acted in a synergistic manner across four colon cancer cells, efficiently inhibiting clonogenic growth and invasion in vitro, retarding tumor growth in vivo, preventing the G0/G1 to S phase transition, and inducing caspase-dependent apoptosis. GSK-2816126 55-61 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 40-44 35091962-7 2022 Collectively, we demonstrated the potential of H3K27me3 as a novel stroke therapeutic target, and GSK-126 exerted a neuroprotective function in ischemic brain injury, which might be associated with activation of the MAPK/ERK pathway. GSK-2816126 98-105 Eph receptor B1 Rattus norvegicus 221-224 35351858-6 2022 Based on the above, therapeutics targeting the role of MEIS1 in oxaliplatin resistance were developed and our results suggested that the combination of oxaliplatin with either ELFN1-AS1 ASO or EZH2 inhibitor GSK126 could largely suppress tumor growth and reverse oxaliplatin resistance. GSK-2816126 208-214 Meis homeobox 1 Mus musculus 55-60 35351858-6 2022 Based on the above, therapeutics targeting the role of MEIS1 in oxaliplatin resistance were developed and our results suggested that the combination of oxaliplatin with either ELFN1-AS1 ASO or EZH2 inhibitor GSK126 could largely suppress tumor growth and reverse oxaliplatin resistance. GSK-2816126 208-214 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 193-197 35158113-4 2022 In this study, we utilized the multiple cancer cell lines, which are less sensitive to the EZH2 inhibitor GSK126, combining animal model and clinical data to investigate the underlying mechanism. GSK-2816126 106-112 enhancer of zeste 2 polycomb repressive complex 2 subunit Mus musculus 91-95 35158113-14 2022 SCD1 knockdown increased cellular sensitivity to GSK126. GSK-2816126 49-55 stearoyl-Coenzyme A desaturase 1 Mus musculus 0-4 35158113-15 2022 Based on the findings above, the application of the combination with SCD1 inhibitor significantly attenuated the proliferation of cancer and increased the sensitivity to GSK126 by suppressing desaturation of fatty acids. GSK-2816126 170-176 stearoyl-Coenzyme A desaturase 1 Mus musculus 69-73 35228654-7 2022 TNFalpha induced the nuclear translocation of enhancer of zeste homolog-2 (EZH2), and its chemical inhibitor GSK126 blocked TNFalpha-induced endothelial barrier disruption and subsequent TNBC transendothelial migration. GSK-2816126 109-115 tumor necrosis factor Homo sapiens 0-8 35228654-7 2022 TNFalpha induced the nuclear translocation of enhancer of zeste homolog-2 (EZH2), and its chemical inhibitor GSK126 blocked TNFalpha-induced endothelial barrier disruption and subsequent TNBC transendothelial migration. GSK-2816126 109-115 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 46-73 35228654-7 2022 TNFalpha induced the nuclear translocation of enhancer of zeste homolog-2 (EZH2), and its chemical inhibitor GSK126 blocked TNFalpha-induced endothelial barrier disruption and subsequent TNBC transendothelial migration. GSK-2816126 109-115 enhancer of zeste 2 polycomb repressive complex 2 subunit Homo sapiens 75-79 35228654-7 2022 TNFalpha induced the nuclear translocation of enhancer of zeste homolog-2 (EZH2), and its chemical inhibitor GSK126 blocked TNFalpha-induced endothelial barrier disruption and subsequent TNBC transendothelial migration. GSK-2816126 109-115 tumor necrosis factor Homo sapiens 124-132