PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 27183917-4 2016 When combining Nutlin-3a with the Wip1 inhibitor GSK2830371 in the treatment of p53-proficient but not p53-deficient cells, we observed enhanced phosphorylation (Ser 15) and acetylation (Lys 382) of p53, increased expression of p53 target gene products, and synergistic inhibition of cell proliferation. GSK2830371 49-59 tumor protein p53 Homo sapiens 80-83 27991505-0 2016 Wip1 inhibitor GSK2830371 inhibits neuroblastoma growth by inducing Chk2/p53-mediated apoptosis. GSK2830371 15-25 tumor protein p53 Homo sapiens 73-76 27991505-3 2016 Wip1 is a negative regulator of p53 and hindrance of Wip1 activity by novel inhibitor GSK2830371 is a potential strategy to activate p53"s tumor suppressing function in NB. GSK2830371 86-96 tumor protein p53 Homo sapiens 133-136 27991505-5 2016 Here we report that novel Wip1 inhibitor GSK2830371 induced Chk2/p53-mediated apoptosis in NB cells in a p53-dependent manner. GSK2830371 41-51 tumor protein p53 Homo sapiens 65-68 27991505-5 2016 Here we report that novel Wip1 inhibitor GSK2830371 induced Chk2/p53-mediated apoptosis in NB cells in a p53-dependent manner. GSK2830371 41-51 tumor protein p53 Homo sapiens 105-108 27991505-6 2016 In addition, GSK2830371 suppressed the colony-formation potential of p53 wild-type NB cell lines. GSK2830371 13-23 tumor protein p53 Homo sapiens 69-72 27991505-9 2016 Taken together, this study suggests that GSK2830371 induces Chk2/p53-mediated apoptosis both in vitro and in vivo in a p53 dependent manner. GSK2830371 41-51 tumor protein p53 Homo sapiens 65-68 27991505-9 2016 Taken together, this study suggests that GSK2830371 induces Chk2/p53-mediated apoptosis both in vitro and in vivo in a p53 dependent manner. GSK2830371 41-51 tumor protein p53 Homo sapiens 119-122 27626308-6 2016 GSK2830371 inhibited the cell growth, being prominent in p53 wild-type cells. GSK2830371 0-10 tumor protein p53 Homo sapiens 57-60 27626308-9 2016 GSK2830371 increased the levels of total and Ser15-phosphorylated p53, and p53 targets p21 and PUMA. GSK2830371 0-10 tumor protein p53 Homo sapiens 66-69 27626308-9 2016 GSK2830371 increased the levels of total and Ser15-phosphorylated p53, and p53 targets p21 and PUMA. GSK2830371 0-10 tumor protein p53 Homo sapiens 75-78 27626308-10 2016 GSK2830371 and the MDM2 inhibitor Nutlin-3a acted synergistically in p53 wild-type cells. GSK2830371 0-10 tumor protein p53 Homo sapiens 69-72 27626308-11 2016 Interestingly, GSK2830371 sensitized MCL cells to bortezomib and doxorubicin in p53 wild-type and mutant cells; p38 signaling appeared to be involved in the GSK2830371/bortezomib lethality. GSK2830371 15-25 tumor protein p53 Homo sapiens 80-83 30045945-6 2018 The combination of ATSP-7041 with P5091, GSK2830371, and chemotherapeutic agents showed synergistic action on the p53 pathway. GSK2830371 41-51 tumor protein p53 Homo sapiens 114-117 29235570-6 2018 RESULTS: GSK2830371, at doses (<=10 muM) that alone had no growth-inhibitory or cytotoxic effects on the cells, nevertheless significantly potentiated the growth-inhibitory and clonogenic cell killing effects of MDM2 inhibitors in p53WT but not p53MUT melanoma cells, indicating the potentiation worked in a p53-dependent manner. GSK2830371 9-19 tumor protein p53 Homo sapiens 234-237 29235570-8 2018 GSK2830371 increased p53 stabilisation through Ser15 phosphorylation and consequent Lys382 acetylation, and decreased ubiquitination and proteasome-dependent degradation when it was combined with MDM2 inhibitors. GSK2830371 0-10 tumor protein p53 Homo sapiens 21-24 29235570-10 2018 GSK2830371 enhanced the induction of p53 transcriptional target genes, cell cycle arrest and apoptosis. GSK2830371 0-10 tumor protein p53 Homo sapiens 37-40 29235570-11 2018 CONCLUSIONS: GSK2830371, a WIP1 inhibitor, at doses with no growth-inhibitory activity alone, potentiated the growth-inhibitory and cytotoxic activity of MDM2 inhibitors by increasing phosphorylation, acetylation and stabilisation of p53 in cutaneous melanoma cells in a functional p53-dependent manner. GSK2830371 13-23 tumor protein p53 Homo sapiens 234-237 29235570-11 2018 CONCLUSIONS: GSK2830371, a WIP1 inhibitor, at doses with no growth-inhibitory activity alone, potentiated the growth-inhibitory and cytotoxic activity of MDM2 inhibitors by increasing phosphorylation, acetylation and stabilisation of p53 in cutaneous melanoma cells in a functional p53-dependent manner. GSK2830371 13-23 tumor protein p53 Homo sapiens 282-285 26832796-0 2016 Chemical Inhibition of Wild-Type p53-Induced Phosphatase 1 (WIP1/PPM1D) by GSK2830371 Potentiates the Sensitivity to MDM2 Inhibitors in a p53-Dependent Manner. GSK2830371 75-85 tumor protein p53 Homo sapiens 33-36 26883108-7 2016 In addition, combined treatment with GSK2830371 and doxorubicin or nutlin-3 potentiated cell death through a strong induction of p53 pathway and activation of caspase 9. GSK2830371 37-47 tumor protein p53 Homo sapiens 129-132 26883108-8 2016 We conclude that efficient inhibition of WIP1 by GSK2830371 sensitizes breast cancer cells with amplified PPM1D and wild type p53 to chemotherapy. GSK2830371 49-59 tumor protein p53 Homo sapiens 126-129 26832796-7 2016 However, a non-growth-inhibitory dose of GSK2830371 markedly potentiated the response to MDM2 inhibitors in TP53 wild-type cell lines, most notably in those harboring PPM1D-activating mutations or copy number gain (up to 5.8-fold decrease in GI50). GSK2830371 41-51 tumor protein p53 Homo sapiens 108-112 34359777-0 2021 WIP1 Inhibition by GSK2830371 Potentiates HDM201 through Enhanced p53 Phosphorylation and Activation in Liver Adenocarcinoma Cells. GSK2830371 19-29 tumor protein p53 Homo sapiens 66-69 25658463-5 2015 We therefore sought to determine whether inhibiting WIP1 with a selective antagonist, GSK2830371, can attenuate neuroblastoma cell growth through reactivation of p53 mediated tumor suppression. GSK2830371 86-96 tumor protein p53 Homo sapiens 162-165 25658463-6 2015 Neuroblastoma cell lines with wild-type TP53 alleles were highly sensitive to GSK2830371 treatment, while cell lines with mutant TP53 were resistant to GSK2830371. GSK2830371 78-88 tumor protein p53 Homo sapiens 40-44 25658463-9 2015 Treatment of wild-type TP53 neuroblastoma cell lines with both GSK2830371 and either doxorubicin or carboplatin resulted in enhanced cell death, mediated through caspase 3/7 induction, as compared to either agent alone. GSK2830371 63-73 tumor protein p53 Homo sapiens 23-27 34359777-8 2021 Combination with GSK2830371 increased p53 phosphorylation, resulting in an increase in both p53 accumulation and p53-dependent trans-activation. GSK2830371 17-27 tumor protein p53 Homo sapiens 92-95 34359777-8 2021 Combination with GSK2830371 increased p53 phosphorylation, resulting in an increase in both p53 accumulation and p53-dependent trans-activation. GSK2830371 17-27 tumor protein p53 Homo sapiens 38-41 34359777-8 2021 Combination with GSK2830371 increased p53 phosphorylation, resulting in an increase in both p53 accumulation and p53-dependent trans-activation. GSK2830371 17-27 tumor protein p53 Homo sapiens 113-116 34359777-12 2021 CONCLUSION: The current study demonstrated that GSK2830371 enhanced the p53-dependent antiproliferative and cytotoxic effect of HDM201 on RBE and SK-Hep-1 cells, providing a novel strategy for potentiating the efficacy of targeting the p53 pathway in iCCA. GSK2830371 48-58 tumor protein p53 Homo sapiens 72-75 34359777-12 2021 CONCLUSION: The current study demonstrated that GSK2830371 enhanced the p53-dependent antiproliferative and cytotoxic effect of HDM201 on RBE and SK-Hep-1 cells, providing a novel strategy for potentiating the efficacy of targeting the p53 pathway in iCCA. GSK2830371 48-58 tumor protein p53 Homo sapiens 236-239