PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 32645997-6 2020 We validated this association in vitro using four mutated and four wild-type SCLC cell lines and two PLK1 inhibitors (Volasertib and BI2536), confirming that the effect of PLK1 inhibitors depended on the mutational status of CREBBP. BI 2536 133-139 polo like kinase 1 Homo sapiens 172-176 33638254-2 2021 By taking BI-2536 (PLK1 and BRD4 inhibitor) as the lead compound, sixteen novel BRD4 inhibitors with the 4,4-difluoro-1-methyl-N,6-diphenyl-5,6-dihydro-4H-pyrimido[4,5-b] [1,2,4] triazolo[4,3-d] [1,4] diazepine-8-amine structure were designed and synthetized. BI 2536 10-17 polo like kinase 1 Homo sapiens 19-23 33638254-2 2021 By taking BI-2536 (PLK1 and BRD4 inhibitor) as the lead compound, sixteen novel BRD4 inhibitors with the 4,4-difluoro-1-methyl-N,6-diphenyl-5,6-dihydro-4H-pyrimido[4,5-b] [1,2,4] triazolo[4,3-d] [1,4] diazepine-8-amine structure were designed and synthetized. BI 2536 10-17 bromodomain containing 4 Homo sapiens 80-84 32962858-7 2020 Compared to monotherapy, combined treatment of glioma cells with PLK1 and STAT3 inhibitors, BI2536 and Stattic, respectively, showed lower expression of MYC, synergistic induction of cell invasion and apoptosis in vitro, and tumor inhibition in xenografts. BI 2536 92-98 polo like kinase 1 Homo sapiens 65-69 32962858-7 2020 Compared to monotherapy, combined treatment of glioma cells with PLK1 and STAT3 inhibitors, BI2536 and Stattic, respectively, showed lower expression of MYC, synergistic induction of cell invasion and apoptosis in vitro, and tumor inhibition in xenografts. BI 2536 92-98 signal transducer and activator of transcription 3 Homo sapiens 74-79 32962858-7 2020 Compared to monotherapy, combined treatment of glioma cells with PLK1 and STAT3 inhibitors, BI2536 and Stattic, respectively, showed lower expression of MYC, synergistic induction of cell invasion and apoptosis in vitro, and tumor inhibition in xenografts. BI 2536 92-98 MYC proto-oncogene, bHLH transcription factor Homo sapiens 153-156 33222770-4 2020 Here, we show that if the Plk1 inhibitor BI 2536 is co-encapsulated in a liposome with a pair of anions, its release rate is dependent on both the identity and stoichiometry of the anions. BI 2536 41-48 polo like kinase 1 Mus musculus 26-30 32896567-7 2020 Furthermore, Saracatinib (Src inhibition) and BI2536 (PLK1 inhibition) diminished GSC self-renewal in vitro, and combining the two inhibitors increased survival of orthotopic tumor-bearing mice. BI 2536 46-52 polo like kinase 1 Mus musculus 54-58 32970049-1 2020 Using a probe consisting of a fluorescein-labeled variant of the potent polo-like kinase 1 (Plk1) inhibitor BI2536 [FITC-PEG-Lys(BI2536) 4], we were able to determine half maximal inhibitory concentration (IC50) of ATP-competitive Type 1 inhibitors of Plk1 by means of a fluorescence recovery assay. BI 2536 108-114 polo like kinase 1 Homo sapiens 72-90 32970049-1 2020 Using a probe consisting of a fluorescein-labeled variant of the potent polo-like kinase 1 (Plk1) inhibitor BI2536 [FITC-PEG-Lys(BI2536) 4], we were able to determine half maximal inhibitory concentration (IC50) of ATP-competitive Type 1 inhibitors of Plk1 by means of a fluorescence recovery assay. BI 2536 108-114 polo like kinase 1 Homo sapiens 92-96 32970049-1 2020 Using a probe consisting of a fluorescein-labeled variant of the potent polo-like kinase 1 (Plk1) inhibitor BI2536 [FITC-PEG-Lys(BI2536) 4], we were able to determine half maximal inhibitory concentration (IC50) of ATP-competitive Type 1 inhibitors of Plk1 by means of a fluorescence recovery assay. BI 2536 108-114 polo like kinase 1 Homo sapiens 252-256 33067313-4 2021 Among the top consensus candidates, we selected a PLK1 inhibitor (BI-2536) for further experimental validation. BI 2536 66-73 polo like kinase 1 Mus musculus 50-54 33067313-8 2021 In vitro, either BI-2536 treatment or knockdown of PLK1 dampened the NF-kappaB and Smad3 signal transduction and transcriptional activation. BI 2536 17-24 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 69-78 33067313-8 2021 In vitro, either BI-2536 treatment or knockdown of PLK1 dampened the NF-kappaB and Smad3 signal transduction and transcriptional activation. BI 2536 17-24 SMAD family member 3 Mus musculus 83-88 33067313-9 2021 Together, these results suggest that the PLK1 inhibitor BI-2536 should be further investigated as a novel therapy for DKD. BI 2536 56-63 polo like kinase 1 Mus musculus 41-45 33584305-5 2020 To improve the cytotoxicity, we screened the chemicals that improve the effects of gatastatin and found that BI 2536, a Plk1 inhibitor, greatly increases the cytotoxicity of gatastatin. BI 2536 109-116 polo like kinase 1 Homo sapiens 120-124 33315519-9 2021 Both AAV8-mediated Plk1 knockdown and PLK1 inhibitor BI-2536 could mitigate the gefitinib-induced hepatotoxicity in vivo by abrogating the autophagic degradation of the COX6A1 protein. BI 2536 53-60 polo like kinase 1 Mus musculus 38-42 33315519-9 2021 Both AAV8-mediated Plk1 knockdown and PLK1 inhibitor BI-2536 could mitigate the gefitinib-induced hepatotoxicity in vivo by abrogating the autophagic degradation of the COX6A1 protein. BI 2536 53-60 cytochrome c oxidase subunit 6A1 Mus musculus 169-175 32645997-6 2020 We validated this association in vitro using four mutated and four wild-type SCLC cell lines and two PLK1 inhibitors (Volasertib and BI2536), confirming that the effect of PLK1 inhibitors depended on the mutational status of CREBBP. BI 2536 133-139 CREB binding protein Homo sapiens 225-231 32496211-2 2020 Moreover, we have shown that BI-2536, a small molecule PLK1 inhibitor, was very efficient at inhibiting HBV DNA neosynthesis, notably by affecting nucleocapsid assembly as a result of the modulation of HBc phosphorylation. BI 2536 29-36 polo like kinase 1 Homo sapiens 55-59 32231733-0 2020 The dual role of BI 2536, a small-molecule inhibitor that targets PLK1, in induction of apoptosis and attenuation of autophagy in neuroblastoma cells. BI 2536 17-24 polo like kinase 1 Homo sapiens 66-70 32231733-4 2020 BI2536, a small molecule inhibitor against PLK1, significantly reduced cell viability in a panel of NB cell lines, with IC50 less than 100 nM. BI 2536 0-6 polo like kinase 1 Homo sapiens 43-47 32231733-5 2020 PLK1 inhibition by BI 2536 treatment induced cell cycle arrest at G2/M phase and cell apoptosis in NB cells. BI 2536 19-26 polo like kinase 1 Homo sapiens 0-4 32496211-2 2020 Moreover, we have shown that BI-2536, a small molecule PLK1 inhibitor, was very efficient at inhibiting HBV DNA neosynthesis, notably by affecting nucleocapsid assembly as a result of the modulation of HBc phosphorylation. BI 2536 29-36 keratin 88, pseudogene Homo sapiens 202-205 32088495-3 2020 In this study, a series of 4,5-dihydro-[1,2,4]triazolo [4,3-f]pteridine derivatives were designed and synthesized based on the structure of PLK1 inhibitor BI-2536. BI 2536 155-162 polo like kinase 1 Mus musculus 140-144 30876762-12 2019 Our study also reveals that the PLK1 inhibitor BI2536 may be an attractive candidate for ESCC targeted therapy, especially when combined with DDP for treating the GSDME overexpression subtype. BI 2536 47-53 polo like kinase 1 Homo sapiens 32-36 30488440-11 2019 PLK1 inhibition, including si-PLK1 and BI2536 treatment, could restore the chemosensitivity of drug-resistant SGC-7901/DDP cells and enhance the efficacy of DDP, revealing the potential value of PLK1 inhibition in GC chemotherapy. BI 2536 39-45 polo like kinase 1 Homo sapiens 0-4 30800581-7 2019 Interestingly, the docking results of these three drugs were better than the known PLK1 inhibitors (BI-2536 and rigosertib). BI 2536 100-107 polo like kinase 1 Homo sapiens 83-87 30996295-3 2019 Knockdown of PLK1 as well as a small compound inhibitor for PLK1, BI-2536, induced G2/M arrest and created polyploid cell population, shown by increased DNA content and nuclear size. BI 2536 66-73 polo like kinase 1 Homo sapiens 13-17 30996295-3 2019 Knockdown of PLK1 as well as a small compound inhibitor for PLK1, BI-2536, induced G2/M arrest and created polyploid cell population, shown by increased DNA content and nuclear size. BI 2536 66-73 polo like kinase 1 Homo sapiens 60-64 30996295-7 2019 Although future in vivo studies are warranted, targeting PLK1 by a selective inhibitor such as BI-2536 can be an attractive molecular-targeted therapy for TNBC. BI 2536 95-102 polo like kinase 1 Homo sapiens 57-61 31227645-8 2019 shRNA knockdown or pharmacologic inhibition of PLK1 using BI2536 or BI6727 (volasertib) in B-ALL cell lines and patient samples led to p53 stabilization and cell death. BI 2536 58-64 polo like kinase 1 Homo sapiens 47-51 31118282-8 2019 Plk1 phosphorylated p31comet on S102, as suggested by the prevention of the phosphorylation of this residue in checkpoint extracts by the selective Plk1 inhibitor BI-2536 and by the phosphorylation of S102 with purified Plk1. BI 2536 163-170 polo like kinase 1 Homo sapiens 0-4 31118282-8 2019 Plk1 phosphorylated p31comet on S102, as suggested by the prevention of the phosphorylation of this residue in checkpoint extracts by the selective Plk1 inhibitor BI-2536 and by the phosphorylation of S102 with purified Plk1. BI 2536 163-170 ATPase H+ transporting V1 subunit E1 Homo sapiens 20-23 30481982-5 2019 In an initial series of experiments in this study, BI2536, a Plk1 inhibitor, was treated to in vivo-fertilized embryos and the embryos failed to develop beyond the 2-cell stage. BI 2536 51-57 polo like kinase 1 Mus musculus 61-65 30217950-8 2018 Furthermore, rational combination of midostaurin with the potent PLK1 inhibitor BI2536 elicited strong synergy. BI 2536 80-86 polo like kinase 1 Homo sapiens 65-69 30836927-0 2019 Inhibition of Polo-Like Kinase 1 by BI2536 Reverses the Multidrug Resistance of Human Hepatoma Cells In Vitro and In Vivo. BI 2536 36-42 polo like kinase 1 Homo sapiens 14-32 30836927-2 2019 Polo-Like Kinase 1 (PLK1) is a serine/threonine kinase associated with tumor growth and clinical prognosis in HCC and BI2536 is its potent inhibitor with IC50 of 0.83nM. BI 2536 118-124 polo like kinase 1 Homo sapiens 0-18 30836927-2 2019 Polo-Like Kinase 1 (PLK1) is a serine/threonine kinase associated with tumor growth and clinical prognosis in HCC and BI2536 is its potent inhibitor with IC50 of 0.83nM. BI 2536 118-124 polo like kinase 1 Homo sapiens 20-24 30836927-3 2019 AIMS: To test whether the down-regulation of PLK1 by its inhibitor BI2536 would have beneficial effects on the reversal of MDR in HCC cells. BI 2536 67-73 polo like kinase 1 Homo sapiens 45-49 30836927-4 2019 METHODS: The CCK-8 assay was used to determine the viability of HepG2/ADM and SMMC7721/ADM cells and their parental cells treated with BI2536. BI 2536 135-141 adrenomedullin Homo sapiens 70-73 30836927-9 2019 RESULTS: BI2536 down-regulated the expression of PLK1 protein and mRNA specifically. BI 2536 9-15 polo like kinase 1 Homo sapiens 49-53 30836927-10 2019 BI2536 can significantly reduce IC50 for ADM and other drugs in ADM-resistant HCC cells. BI 2536 0-6 adrenomedullin Homo sapiens 41-44 30836927-10 2019 BI2536 can significantly reduce IC50 for ADM and other drugs in ADM-resistant HCC cells. BI 2536 0-6 adrenomedullin Homo sapiens 64-67 30836927-12 2019 CONCLUSION: Our results suggest that PLK1 inhibitor BI2536 can re-sensitize HCC cancer cell with MDR through induction of apoptosis. BI 2536 52-58 polo like kinase 1 Homo sapiens 37-41 30836927-13 2019 Thus, PLK1 inhibitor BI2536 may act as an effective chemotherapeutic drug in the clinical treatment of HCC patients with MDR. BI 2536 21-27 polo like kinase 1 Homo sapiens 6-10 29437878-5 2018 Real-time monitoring of cell proliferation also showed that TAMR-MCF-7 cells were more sensitive to inhibition of cell proliferation by the ATP-competitive Plk1 inhibitor BI2536 than were the parent MCF-7 cells. BI 2536 171-177 polo like kinase 1 Homo sapiens 156-160 30102854-3 2018 The clinical activities of PLK inhibitor BI-2536 and JAK2-FLT3 inhibitor TG101348 have been attributed to this unexpected polypharmacology, indicating that dual-kinase/bromodomain activity may be advantageous in a therapeutic context. BI 2536 41-48 polo like kinase 1 Homo sapiens 27-30 29959473-6 2018 More importantly, the mTOR inhibitor rapamycin synergized with PLK1 inhibitor BI 2536 to inhibit ESCC cell proliferation in culture and in mice. BI 2536 78-85 polo like kinase 1 Mus musculus 63-67 29959473-7 2018 Notably, combined treatment with BI 2536 and rapamycin produced more potent inhibitory effects on the activation of S6 and AKT than either alone. BI 2536 33-40 AKT serine/threonine kinase 1 Homo sapiens 123-126 29959473-10 2018 These results provide evidence that the mTOR inhibitor rapamycin synergistically enhances the antitumor effect of PLK1 inhibitor BI 2536 in ESCC cells. BI 2536 129-136 mechanistic target of rapamycin kinase Mus musculus 40-44 29959473-10 2018 These results provide evidence that the mTOR inhibitor rapamycin synergistically enhances the antitumor effect of PLK1 inhibitor BI 2536 in ESCC cells. BI 2536 129-136 polo like kinase 1 Mus musculus 114-118 29525435-2 2018 Along this line, starting from PLK1-BRD4 dual inhibitor BI-2536, we discovered a new series of dihydroquinoxalin-2(1H)-one with aniline and indoline WPF binders as selective BRD4 inhibitors. BI 2536 56-63 bromodomain containing 4 Homo sapiens 36-40 29525435-2 2018 Along this line, starting from PLK1-BRD4 dual inhibitor BI-2536, we discovered a new series of dihydroquinoxalin-2(1H)-one with aniline and indoline WPF binders as selective BRD4 inhibitors. BI 2536 56-63 bromodomain containing 4 Homo sapiens 174-178 29525435-2 2018 Along this line, starting from PLK1-BRD4 dual inhibitor BI-2536, we discovered a new series of dihydroquinoxalin-2(1H)-one with aniline and indoline WPF binders as selective BRD4 inhibitors. BI 2536 56-63 polo like kinase 1 Homo sapiens 31-35 27582537-5 2016 The PI3-kinase blocker BEZ235, the pan-BCL-2 inhibitor obatoclax, the Hsp90-targeting drug 17AAG, and the Polo-like kinase-1 inhibitor BI2536, were found to exert major growth-inhibitory effects in all 5 MM cell lines tested. BI 2536 135-141 polo like kinase 1 Homo sapiens 106-124 29476067-0 2018 BI-2536 and BI-6727, dual Polo-like kinase/bromodomain inhibitors, effectively reactivate latent HIV-1. BI 2536 0-7 polo like kinase 1 Homo sapiens 26-42 30299205-7 2018 HTS revealed no cytotoxic efficacy of SHH pathway inhibitors while sensitivity was observed to the mTOR inhibitor temsirolimus, the ALK inhibitor ceritinib, and the PLK1 inhibitor BI2536. BI 2536 180-186 polo like kinase 1 Homo sapiens 165-169 29541386-6 2018 Upon BI-2536 treatment, Plk1 cleavage occurred only in the cytosolic fraction and cleaved Plk1 accumulated in this subcellular compartment. BI 2536 5-12 polo like kinase 1 Homo sapiens 24-28 29541386-6 2018 Upon BI-2536 treatment, Plk1 cleavage occurred only in the cytosolic fraction and cleaved Plk1 accumulated in this subcellular compartment. BI 2536 5-12 polo like kinase 1 Homo sapiens 90-94 28531794-0 2017 Binding of the anticancer drug BI-2536 to human serum albumin. BI 2536 31-38 albumin Homo sapiens 48-61 28531794-3 2017 The binding affinity of BI-2536 for human serum albumin (HSA) protein may define its pharmacokinetic and pharmacodynamic profile. BI 2536 24-31 albumin Homo sapiens 42-55 28212994-0 2017 An open-label, phase II study of the polo-like kinase-1 (Plk-1) inhibitor, BI 2536, in patients with relapsed small cell lung cancer (SCLC). BI 2536 75-82 polo like kinase 1 Homo sapiens 37-55 28212994-0 2017 An open-label, phase II study of the polo-like kinase-1 (Plk-1) inhibitor, BI 2536, in patients with relapsed small cell lung cancer (SCLC). BI 2536 75-82 polo like kinase 1 Homo sapiens 57-62 28212994-1 2017 OBJECTIVES: This phase II, open-label study was designed to evaluate the response rate to the polo-like kinase 1 (Plk-1) inhibitor BI 2536 in patients with sensitive-relapsed small cell lung cancer (SCLC). BI 2536 131-138 polo like kinase 1 Homo sapiens 94-112 28212994-1 2017 OBJECTIVES: This phase II, open-label study was designed to evaluate the response rate to the polo-like kinase 1 (Plk-1) inhibitor BI 2536 in patients with sensitive-relapsed small cell lung cancer (SCLC). BI 2536 131-138 polo like kinase 1 Homo sapiens 114-119 27671301-10 2017 PLK1-targeting nanoparticles inhibited cell proliferation through inducing G2/M phase arrest with a higher efficacy than a selective and potent PLK1 inhibitor BI 2536. BI 2536 159-166 polo like kinase 1 Homo sapiens 0-4 27671301-10 2017 PLK1-targeting nanoparticles inhibited cell proliferation through inducing G2/M phase arrest with a higher efficacy than a selective and potent PLK1 inhibitor BI 2536. BI 2536 159-166 polo like kinase 1 Homo sapiens 144-148 29393385-0 2018 BI2536, a potent and selective inhibitor of polo-like kinase 1, in combination with cisplatin exerts synergistic effects on gastric cancer cells. BI 2536 0-6 polo like kinase 1 Homo sapiens 44-62 29393385-1 2018 BI2536 is a highly selective and potent inhibitor of polo-like kinase 1 (PLK1). BI 2536 0-6 polo like kinase 1 Homo sapiens 53-71 29393385-1 2018 BI2536 is a highly selective and potent inhibitor of polo-like kinase 1 (PLK1). BI 2536 0-6 polo like kinase 1 Homo sapiens 73-77 28445592-8 2017 PLK1 inhibition by BI-2536 or siRNA-mediated knockdown suppressed HBV DNA biosynthesis, whereas overexpression of PLK1CA increased it, suggesting that the PLK1 effects on viral biosynthesis are specific and that PLK1 is a proviral cellular factor. BI 2536 19-26 polo like kinase 1 Homo sapiens 0-4 28445592-9 2017 Significantly, BI-2536 administration to HBV-infected humanized liver FRG mice strongly inhibited HBV infection, validating PLK1 as an antiviral target in vivo. BI 2536 15-22 polo like kinase 1 Homo sapiens 124-128 27463838-8 2017 The combined regimen of BI-2536 (a Plk1 inhibitor) and fasudil (a ROCK inhibitor) promoted a significant inhibition of patient-derived lung cancer xenografts and prolonged the survival of LSL-KRASG12D mice. BI 2536 24-31 polo like kinase 1 Homo sapiens 35-39 28586718-2 2017 Interestingly, some kinase inhibitors have been demonstrated to be potent bromodomain inhibitors, especially the PLK1 inhibitor BI-2536 and the JAK2 inhibitor TG101209, which can bind to BRD4 with IC50 values of 0.025 muM and 0.13 muM, respectively. BI 2536 128-135 polo like kinase 1 Homo sapiens 113-117 28586718-2 2017 Interestingly, some kinase inhibitors have been demonstrated to be potent bromodomain inhibitors, especially the PLK1 inhibitor BI-2536 and the JAK2 inhibitor TG101209, which can bind to BRD4 with IC50 values of 0.025 muM and 0.13 muM, respectively. BI 2536 128-135 bromodomain containing 4 Homo sapiens 187-191 28184925-11 2017 The phosphorylation of mTOR was reduced significantly in NB4 cells treated with RO3280 and BI2536, and was also reduced significantly when PLK1 expression was downregulated in the NB4, K562 and HL-60 cells. BI 2536 91-97 mechanistic target of rapamycin kinase Homo sapiens 23-27 28184925-11 2017 The phosphorylation of mTOR was reduced significantly in NB4 cells treated with RO3280 and BI2536, and was also reduced significantly when PLK1 expression was downregulated in the NB4, K562 and HL-60 cells. BI 2536 91-97 polo like kinase 1 Homo sapiens 139-143 28178660-6 2017 Checkpoint adaptation was accompanied by PLK1 activation and IDH1 mutant astrocytes were more sensitive to treatment with BI2536 and TMZ in combination (<20% clonogenic survival) than either TMZ (~60%) or BI2536 (~75%) as single agents. BI 2536 122-128 polo like kinase 1 Mus musculus 41-45 28178660-6 2017 Checkpoint adaptation was accompanied by PLK1 activation and IDH1 mutant astrocytes were more sensitive to treatment with BI2536 and TMZ in combination (<20% clonogenic survival) than either TMZ (~60%) or BI2536 (~75%) as single agents. BI 2536 122-128 isocitrate dehydrogenase 1 (NADP+), soluble Mus musculus 61-65 28628916-0 2017 Comprehensive Biomarker Analyses in Patients with Advanced or Metastatic Non-Small Cell Lung Cancer Prospectively Treated with the Polo-Like Kinase 1 Inhibitor BI2536. BI 2536 160-166 polo like kinase 1 Homo sapiens 131-149 28628916-4 2017 To this end, we conducted a post-hoc biomarker analysis of tumor samples from non-small cell lung cancer (NSCLC) patients treated with the PLK1 inhibitor BI2536 in a phase II study. BI 2536 154-160 polo like kinase 1 Homo sapiens 139-143 27713178-6 2016 We show that both visceral and subcutaneous ASCs display monopolar spindles, reduced viability and strong apoptosis induction upon treatment with BI 2536 and BI 6727, the Plk1 kinase domain inhibitors, and with Poloxin, the regulatory Polo-box domain inhibitor. BI 2536 146-153 polo like kinase 1 Homo sapiens 171-175 26713885-9 2016 The PLK1 inhibitor, BI2536, demonstrated marked inhibition of cell proliferation with IC50 in the low nM range (from 10.07-12.39 nM). BI 2536 20-26 polo like kinase 1 Homo sapiens 4-8 27193833-6 2016 Co-administration of BI-2536 and fasudil either in the LSL-KRAS(G12D) mouse model or in a patient tumour explant mouse model of KRAS-mutant lung cancer suppresses tumour growth and significantly prolongs mouse survival, suggesting a strong synergy in vivo and a potential avenue for therapeutic treatment of KRAS-mutant cancers. BI 2536 21-28 Kirsten rat sarcoma viral oncogene homolog Mus musculus 59-63 27193833-6 2016 Co-administration of BI-2536 and fasudil either in the LSL-KRAS(G12D) mouse model or in a patient tumour explant mouse model of KRAS-mutant lung cancer suppresses tumour growth and significantly prolongs mouse survival, suggesting a strong synergy in vivo and a potential avenue for therapeutic treatment of KRAS-mutant cancers. BI 2536 21-28 Kirsten rat sarcoma viral oncogene homolog Mus musculus 128-132 27193833-6 2016 Co-administration of BI-2536 and fasudil either in the LSL-KRAS(G12D) mouse model or in a patient tumour explant mouse model of KRAS-mutant lung cancer suppresses tumour growth and significantly prolongs mouse survival, suggesting a strong synergy in vivo and a potential avenue for therapeutic treatment of KRAS-mutant cancers. BI 2536 21-28 Kirsten rat sarcoma viral oncogene homolog Mus musculus 128-132 26634982-3 2016 Here we report the development of Plk1 inhibitors that incorporate both an ATP-competitive ligand of the enzymatic domain, derived from BI 2536, and a functional inhibitor of the PBD, based either on the small molecule poloxin-2 or on a PBD-binding peptide. BI 2536 136-143 polo like kinase 1 Homo sapiens 34-38 26754547-8 2016 RESULTS: Knocking down expression of PLK-1 with siRNA or inhibition of PLK-1 by a small molecule inhibitor, BI-2536, resulted in a loss of viability of up to 70 % in the ACC cell lines H295R and SW-13. BI 2536 108-115 polo like kinase 1 Homo sapiens 71-76 26754547-10 2016 BI-2536 treatment resulted in a decrease in mutant p53 protein in SW-13 cells but had no effect on wild-type p53 protein levels in H295R cells. BI 2536 0-7 tumor protein p53 Homo sapiens 51-54 25975351-7 2015 Furthermore, treatment with BI 2536 or GSK461364 resulted in activation of the BubR1 spindle checkpoint kinase, suggesting that treatment with ATP-binding domain inhibitors induces metaphase arrest. BI 2536 28-35 BUB1 mitotic checkpoint serine/threonine kinase B Homo sapiens 79-84 26900800-4 2016 Herein, SIRT1 inhibitor Tenovin-1 and polo-like kinase 1 (Plk1) inhibitor BI2536 were used to stabilize p53. BI 2536 74-80 polo like kinase 1 Homo sapiens 38-56 26900800-4 2016 Herein, SIRT1 inhibitor Tenovin-1 and polo-like kinase 1 (Plk1) inhibitor BI2536 were used to stabilize p53. BI 2536 74-80 polo like kinase 1 Homo sapiens 58-62 26900800-4 2016 Herein, SIRT1 inhibitor Tenovin-1 and polo-like kinase 1 (Plk1) inhibitor BI2536 were used to stabilize p53. BI 2536 74-80 tumor protein p53 Homo sapiens 104-107 26046302-2 2016 Here, we identify a synergistic induction of apoptosis by the PLK1 inhibitor BI 2536 and vinca alkaloids in NB cells. BI 2536 77-84 polo like kinase 1 Homo sapiens 62-66 26468278-5 2015 Treatment of cells with the PLK1 kinase inhibitor BI2536 suppressed binding of the Forkhead box protein K1 (FOXK1) transcriptional repressor to JLP. BI 2536 50-56 polo like kinase 1 Homo sapiens 28-32 26468278-5 2015 Treatment of cells with the PLK1 kinase inhibitor BI2536 suppressed binding of the Forkhead box protein K1 (FOXK1) transcriptional repressor to JLP. BI 2536 50-56 forkhead box K1 Homo sapiens 83-106 26468278-5 2015 Treatment of cells with the PLK1 kinase inhibitor BI2536 suppressed binding of the Forkhead box protein K1 (FOXK1) transcriptional repressor to JLP. BI 2536 50-56 forkhead box K1 Homo sapiens 108-113 26468278-5 2015 Treatment of cells with the PLK1 kinase inhibitor BI2536 suppressed binding of the Forkhead box protein K1 (FOXK1) transcriptional repressor to JLP. BI 2536 50-56 sperm associated antigen 9 Homo sapiens 144-147 25917079-3 2015 Eribulin and the PLK1 inhibitor BI 2536 at subtoxic concentrations synergize to induce apoptosis in RMS cells as confirmed by calculation of combination index (CI). BI 2536 32-39 polo like kinase 1 Homo sapiens 17-21 26438599-7 2015 Furthermore, inhibition of Wnt/beta-catenin signaling significantly potentiates the antineoplastic activity of the Plk1 inhibitor BI2536 in both cultured prostate cancer cells and CRPC xenograft tumors. BI 2536 130-136 catenin beta 1 Homo sapiens 31-43 26438599-7 2015 Furthermore, inhibition of Wnt/beta-catenin signaling significantly potentiates the antineoplastic activity of the Plk1 inhibitor BI2536 in both cultured prostate cancer cells and CRPC xenograft tumors. BI 2536 130-136 polo like kinase 1 Homo sapiens 115-119 26349973-0 2015 BI2536--A PLK inhibitor augments paclitaxel efficacy in suppressing tamoxifen induced senescence and resistance in breast cancer cells. BI 2536 0-6 polo like kinase 1 Homo sapiens 10-13 26349973-5 2015 Further to mitigate the undesirable complications of paclitaxel (PAC), we employed this drug in combination along with BI2536 (BI), a PLK inhibitor for this study to sensitize the tamoxifen resistant cells to apoptosis. BI 2536 119-125 polo like kinase 1 Homo sapiens 134-137 25891802-1 2015 PLK (Polo-like kinase) inhibitors, such as BI-2536, have been reported to suppress IFNB (encoding IFNbeta, interferon beta) gene transcription induced by ligands that activate TLR3 (Toll-like receptor 3) and TLR4. BI 2536 43-50 interferon beta 1 Homo sapiens 83-87 25891802-1 2015 PLK (Polo-like kinase) inhibitors, such as BI-2536, have been reported to suppress IFNB (encoding IFNbeta, interferon beta) gene transcription induced by ligands that activate TLR3 (Toll-like receptor 3) and TLR4. BI 2536 43-50 interferon beta 1 Homo sapiens 98-122 25891802-1 2015 PLK (Polo-like kinase) inhibitors, such as BI-2536, have been reported to suppress IFNB (encoding IFNbeta, interferon beta) gene transcription induced by ligands that activate TLR3 (Toll-like receptor 3) and TLR4. BI 2536 43-50 toll like receptor 3 Homo sapiens 176-180 25891802-1 2015 PLK (Polo-like kinase) inhibitors, such as BI-2536, have been reported to suppress IFNB (encoding IFNbeta, interferon beta) gene transcription induced by ligands that activate TLR3 (Toll-like receptor 3) and TLR4. BI 2536 43-50 toll like receptor 3 Homo sapiens 182-202 25891802-1 2015 PLK (Polo-like kinase) inhibitors, such as BI-2536, have been reported to suppress IFNB (encoding IFNbeta, interferon beta) gene transcription induced by ligands that activate TLR3 (Toll-like receptor 3) and TLR4. BI 2536 43-50 toll like receptor 4 Homo sapiens 208-212 25891802-3 2015 Although BI-2536 inhibits few other kinases tested, it interacts with BET (bromodomain and extra-terminal) family members and displaces them from acetylated lysine residues on histones. BI 2536 9-16 delta/notch like EGF repeat containing Homo sapiens 70-73 25891802-3 2015 Although BI-2536 inhibits few other kinases tested, it interacts with BET (bromodomain and extra-terminal) family members and displaces them from acetylated lysine residues on histones. BI 2536 9-16 delta/notch like EGF repeat containing Homo sapiens 75-105 25891802-4 2015 We found that BET inhibitors that do not inhibit PLKs phenocopied the effect of BI-2536 on IFNB gene transcription. BI 2536 80-87 delta/notch like EGF repeat containing Homo sapiens 14-17 25891802-4 2015 We found that BET inhibitors that do not inhibit PLKs phenocopied the effect of BI-2536 on IFNB gene transcription. BI 2536 80-87 interferon beta 1 Homo sapiens 91-95 26059434-6 2015 Although BI2536 significantly augmented the anti-neoplastic effect of EGFR inhibitors in the Ink4a/Arf(-/-) EGFRvIII model, durable response was not achieved until TMZ was added. BI 2536 9-15 epidermal growth factor receptor Homo sapiens 70-74 25992548-8 2015 For Sm-PLK-1 the same effects were seen with the specific inhibitor, BI2536, which also affected viable egg production in adult worms. BI 2536 69-75 polo like kinase 1 Homo sapiens 7-12 26059434-6 2015 Although BI2536 significantly augmented the anti-neoplastic effect of EGFR inhibitors in the Ink4a/Arf(-/-) EGFRvIII model, durable response was not achieved until TMZ was added. BI 2536 9-15 cyclin dependent kinase inhibitor 2A Homo sapiens 93-98 26191363-4 2015 Meanwhile, substitution of the pyrimidine NH with an oxygen atom reversed the PLK1/BRD4 selectivity to convert BI-2536 into a BRD4-selective inhibitor, likely owing to the loss of a critical hydrogen bond in PLK1. BI 2536 111-118 polo like kinase 1 Homo sapiens 78-82 26191363-4 2015 Meanwhile, substitution of the pyrimidine NH with an oxygen atom reversed the PLK1/BRD4 selectivity to convert BI-2536 into a BRD4-selective inhibitor, likely owing to the loss of a critical hydrogen bond in PLK1. BI 2536 111-118 bromodomain containing 4 Homo sapiens 83-87 26191363-4 2015 Meanwhile, substitution of the pyrimidine NH with an oxygen atom reversed the PLK1/BRD4 selectivity to convert BI-2536 into a BRD4-selective inhibitor, likely owing to the loss of a critical hydrogen bond in PLK1. BI 2536 111-118 bromodomain containing 4 Homo sapiens 126-130 26191363-4 2015 Meanwhile, substitution of the pyrimidine NH with an oxygen atom reversed the PLK1/BRD4 selectivity to convert BI-2536 into a BRD4-selective inhibitor, likely owing to the loss of a critical hydrogen bond in PLK1. BI 2536 111-118 polo like kinase 1 Homo sapiens 208-212 26191363-0 2015 BRD4 Structure-Activity Relationships of Dual PLK1 Kinase/BRD4 Bromodomain Inhibitor BI-2536. BI 2536 85-92 bromodomain containing 4 Homo sapiens 0-4 25697066-2 2015 Small molecule inhibitors targeting PLK1, such as BI2536 or BI6727 (Volasertib) are a promising therapeutic approach in such malignancies. BI 2536 50-56 polo like kinase 1 Homo sapiens 36-40 26191363-0 2015 BRD4 Structure-Activity Relationships of Dual PLK1 Kinase/BRD4 Bromodomain Inhibitor BI-2536. BI 2536 85-92 bromodomain containing 4 Homo sapiens 58-62 26191363-1 2015 A focused library of analogues of the dual PLK1 kinase/BRD4 bromodomain inhibitor BI-2536 was prepared and then analyzed for BRD4 and PLK1 inhibitory activities. BI 2536 82-89 polo like kinase 1 Homo sapiens 43-47 26191363-1 2015 A focused library of analogues of the dual PLK1 kinase/BRD4 bromodomain inhibitor BI-2536 was prepared and then analyzed for BRD4 and PLK1 inhibitory activities. BI 2536 82-89 bromodomain containing 4 Homo sapiens 55-59 25826089-3 2015 We investigated the role of PLK1 in the cell response to CPTs in squamous cell carcinoma (SCC) and pediatric sarcoma cell lines and explored the therapeutic potential of the combination of CPT11 and the PLK1 inhibitor BI2536 in CPT-sensitive and -resistant tumor models. BI 2536 218-224 polo like kinase 1 Mus musculus 203-207 25697066-3 2015 Here, we show a loss of specifically localized PLK1 in AML blasts in vivo, accompanied by mitotic arrest with transition into apoptosis, in bone marrow biopsies of AML patients after treatment with BI2536. BI 2536 198-204 polo like kinase 1 Homo sapiens 47-51 24519995-5 2014 Moreover, the effects of a specific PLK1 inhibitor, BI 2536, was tested against a panel of nine ALL cell lines at nanomolar concentrations (10, 50, 100 nM). BI 2536 52-59 polo like kinase 1 Homo sapiens 36-40 25187116-8 2015 However, treatment with BI-2536, an inhibitor of polo-like kinase 1 (Plk1), dramatically decreased the expression level of IP3 R1 in pig oocytes in a dose-dependent manner. BI 2536 24-31 polo like kinase 1 Sus scrofa 49-67 25187116-8 2015 However, treatment with BI-2536, an inhibitor of polo-like kinase 1 (Plk1), dramatically decreased the expression level of IP3 R1 in pig oocytes in a dose-dependent manner. BI 2536 24-31 polo like kinase 1 Sus scrofa 69-73 25187116-8 2015 However, treatment with BI-2536, an inhibitor of polo-like kinase 1 (Plk1), dramatically decreased the expression level of IP3 R1 in pig oocytes in a dose-dependent manner. BI 2536 24-31 inositol 1,4,5-trisphosphate receptor 1 Mus musculus 123-129 25505174-2 2015 In this study, we show that BI2536, a specific Plk1 inhibitor, acted synergistically with metformin in inhibiting PCa cell proliferation. BI 2536 28-34 polo like kinase 1 Homo sapiens 47-51 25505174-4 2015 Mechanistically, we found that co-treatment with BI2536 and metformin induced p53-dependent apoptosis and further activated the p53/Redd-1 pathway. BI 2536 49-55 tumor protein p53 Homo sapiens 78-81 25505174-4 2015 Mechanistically, we found that co-treatment with BI2536 and metformin induced p53-dependent apoptosis and further activated the p53/Redd-1 pathway. BI 2536 49-55 tumor protein p53 Homo sapiens 128-131 25505174-4 2015 Mechanistically, we found that co-treatment with BI2536 and metformin induced p53-dependent apoptosis and further activated the p53/Redd-1 pathway. BI 2536 49-55 DNA damage inducible transcript 4 Homo sapiens 132-138 25927139-7 2015 Furthermore, Plk1 inhibitor BI2536 down-regulated SREBP-dependent expression of enzymes involved in androgen biosynthesis. BI 2536 28-34 polo like kinase 1 Homo sapiens 13-17 25927139-10 2015 Overall, our data support the concept that Plk1 inhibitor such as BI2536 prevents AR signaling pathway and might have therapeutic potential for CRPC patients. BI 2536 66-72 polo like kinase 1 Homo sapiens 43-47 25927139-10 2015 Overall, our data support the concept that Plk1 inhibitor such as BI2536 prevents AR signaling pathway and might have therapeutic potential for CRPC patients. BI 2536 66-72 androgen receptor Homo sapiens 82-84 26654596-6 2015 The specific Plk1 inhibitor, BI2536, repressed pPlk1(Ser137) accumulation at MTOCs and between chromosome arms, consequently disturbed gamma-tubulin and pericentrin recruiting to MTOCs, destroyed meiotic spindle formation, and delayed REC8 cleavage, therefore arresting oocytes at metaphase I (MI) with chromosome misalignment. BI 2536 29-35 pericentrin (kendrin) Mus musculus 153-164 26654596-6 2015 The specific Plk1 inhibitor, BI2536, repressed pPlk1(Ser137) accumulation at MTOCs and between chromosome arms, consequently disturbed gamma-tubulin and pericentrin recruiting to MTOCs, destroyed meiotic spindle formation, and delayed REC8 cleavage, therefore arresting oocytes at metaphase I (MI) with chromosome misalignment. BI 2536 29-35 REC8 meiotic recombination protein Mus musculus 235-239 26654596-7 2015 BI2536 completely reversed the premature degradation of REC8 and precocious segregation of chromosomes induced with okadaic acid (OA), an inhibitor to protein phosphatase 2A. BI 2536 0-6 REC8 meiotic recombination protein Mus musculus 56-60 25925375-6 2015 Further, DNA-PKcs-deficient cells are highly sensitive to Plk1 inhibitor BI2536, suggesting that the coordination between DNA-PKcs and Plk1 is not only crucial to ensure normal cell cycle progression through G2/M phases but also required for cellular resistance to mitotic stress. BI 2536 73-79 protein kinase, DNA-activated, catalytic subunit Homo sapiens 9-17 25925375-6 2015 Further, DNA-PKcs-deficient cells are highly sensitive to Plk1 inhibitor BI2536, suggesting that the coordination between DNA-PKcs and Plk1 is not only crucial to ensure normal cell cycle progression through G2/M phases but also required for cellular resistance to mitotic stress. BI 2536 73-79 polo like kinase 1 Homo sapiens 58-62 25925375-6 2015 Further, DNA-PKcs-deficient cells are highly sensitive to Plk1 inhibitor BI2536, suggesting that the coordination between DNA-PKcs and Plk1 is not only crucial to ensure normal cell cycle progression through G2/M phases but also required for cellular resistance to mitotic stress. BI 2536 73-79 protein kinase, DNA-activated, catalytic subunit Homo sapiens 122-130 25925375-6 2015 Further, DNA-PKcs-deficient cells are highly sensitive to Plk1 inhibitor BI2536, suggesting that the coordination between DNA-PKcs and Plk1 is not only crucial to ensure normal cell cycle progression through G2/M phases but also required for cellular resistance to mitotic stress. BI 2536 73-79 polo like kinase 1 Homo sapiens 135-139 25524551-0 2015 Polo-like kinase 1 inhibitor BI2536 causes mitotic catastrophe following activation of the spindle assembly checkpoint in non-small cell lung cancer cells. BI 2536 29-35 polo like kinase 1 Homo sapiens 0-18 25524551-2 2015 One of these compounds, the PLK1-specific inhibitor BI2536, has been investigated as a cytotoxic drug in several cancers, including lung cancer; however, the detailed mechanism by which BI2536 induces defects in cell proliferation of non-small cell lung cancer (NSCLC) has not yet been determined. BI 2536 52-58 polo like kinase 1 Homo sapiens 28-32 25565629-0 2015 Pharmacological inhibition of Polo-like kinase 1 (PLK1) by BI-2536 decreases the viability and survival of hamartin and tuberin deficient cells via induction of apoptosis and attenuation of autophagy. BI 2536 59-66 polo like kinase 1 Homo sapiens 30-48 25565629-0 2015 Pharmacological inhibition of Polo-like kinase 1 (PLK1) by BI-2536 decreases the viability and survival of hamartin and tuberin deficient cells via induction of apoptosis and attenuation of autophagy. BI 2536 59-66 polo like kinase 1 Homo sapiens 50-54 25565629-0 2015 Pharmacological inhibition of Polo-like kinase 1 (PLK1) by BI-2536 decreases the viability and survival of hamartin and tuberin deficient cells via induction of apoptosis and attenuation of autophagy. BI 2536 59-66 TSC complex subunit 1 Homo sapiens 107-115 25565629-0 2015 Pharmacological inhibition of Polo-like kinase 1 (PLK1) by BI-2536 decreases the viability and survival of hamartin and tuberin deficient cells via induction of apoptosis and attenuation of autophagy. BI 2536 59-66 TSC complex subunit 2 Homo sapiens 120-127 25565629-6 2015 Pharmacological inhibition of PLK1 by the small-molecule inhibitor BI-2536 significantly decreased the viability and clonogenic survival of hamartin and tuberin deficient cells, which was associated with increased apoptosis. BI 2536 67-74 polo like kinase 1 Homo sapiens 30-34 25565629-6 2015 Pharmacological inhibition of PLK1 by the small-molecule inhibitor BI-2536 significantly decreased the viability and clonogenic survival of hamartin and tuberin deficient cells, which was associated with increased apoptosis. BI 2536 67-74 TSC complex subunit 1 Homo sapiens 140-148 25565629-6 2015 Pharmacological inhibition of PLK1 by the small-molecule inhibitor BI-2536 significantly decreased the viability and clonogenic survival of hamartin and tuberin deficient cells, which was associated with increased apoptosis. BI 2536 67-74 TSC complex subunit 2 Homo sapiens 153-160 25565629-7 2015 BI-2536 increased p62, LC3B-I and GFP-LC3 punctae, and inhibited HBSS-induced degradation of p62, suggesting that PLK1 inhibition attenuates autophagy. BI 2536 0-7 nucleoporin 62 Homo sapiens 18-21 25565629-7 2015 BI-2536 increased p62, LC3B-I and GFP-LC3 punctae, and inhibited HBSS-induced degradation of p62, suggesting that PLK1 inhibition attenuates autophagy. BI 2536 0-7 nucleoporin 62 Homo sapiens 93-96 25565629-7 2015 BI-2536 increased p62, LC3B-I and GFP-LC3 punctae, and inhibited HBSS-induced degradation of p62, suggesting that PLK1 inhibition attenuates autophagy. BI 2536 0-7 polo like kinase 1 Homo sapiens 114-118 24519995-11 2014 CONCLUSIONS: PLK1 mRNA expression level is not associated with prognosis in childhood ALL; however, considering the great variability observed in the sample and the in vitro experiments presented herein, BI 2536 treatment might serve as a promising therapeutic to enhance the efficacy of conventional treatment modalities in some childhood ALL cases. BI 2536 204-211 polo like kinase 1 Homo sapiens 13-17 24771642-3 2014 Our finding was validated using shRNA or PLK1-specific inhibitor BI 2536. BI 2536 65-72 polo like kinase 1 Homo sapiens 41-45 24568369-3 2014 Among these, the PLK1 inhibitor BI2536 and the JAK2 inhibitor TG101209 displayed strongest inhibitory potential against BRD4 (IC50=25 nM and 130 nM, respectively) and high selectivity for BET bromodomains. BI 2536 32-38 polo like kinase 1 Homo sapiens 17-21 24568369-3 2014 Among these, the PLK1 inhibitor BI2536 and the JAK2 inhibitor TG101209 displayed strongest inhibitory potential against BRD4 (IC50=25 nM and 130 nM, respectively) and high selectivity for BET bromodomains. BI 2536 32-38 bromodomain containing 4 Homo sapiens 120-124 24568369-3 2014 Among these, the PLK1 inhibitor BI2536 and the JAK2 inhibitor TG101209 displayed strongest inhibitory potential against BRD4 (IC50=25 nM and 130 nM, respectively) and high selectivity for BET bromodomains. BI 2536 32-38 delta/notch like EGF repeat containing Homo sapiens 188-191 24484936-8 2014 Thus, the clinical Plk1 inhibitor BI 2536 decreases the threshold of different cancer cell types toward Fas-induced cell death. BI 2536 34-41 polo like kinase 1 Homo sapiens 19-23 24019381-8 2013 In patient-derived primary medulloblastoma isolates, the PLK1 small-molecule inhibitor BI2536 suppressed the self-renewal of cells with high PLK1 but not low PLK1 expression. BI 2536 87-93 polo like kinase 1 Homo sapiens 57-61 24502970-4 2014 MATERIALS AND METHODS: Human osteosarcoma U2OS and colorectal cancer HT29 and SW620 cells were treated with the PLK1-inhibitor BI2536 before or after X-ray irradiation (0-6 Gy). BI 2536 127-133 polo like kinase 1 Homo sapiens 112-116 24802643-0 2014 Inhibition of Polo kinase by BI2536 affects centriole separation during Drosophila male meiosis. BI 2536 29-35 polo Drosophila melanogaster 14-25 24019381-8 2013 In patient-derived primary medulloblastoma isolates, the PLK1 small-molecule inhibitor BI2536 suppressed the self-renewal of cells with high PLK1 but not low PLK1 expression. BI 2536 87-93 polo like kinase 1 Homo sapiens 141-145 24019381-8 2013 In patient-derived primary medulloblastoma isolates, the PLK1 small-molecule inhibitor BI2536 suppressed the self-renewal of cells with high PLK1 but not low PLK1 expression. BI 2536 87-93 polo like kinase 1 Homo sapiens 141-145 23949254-5 2013 Monotherapy with BI 2536, the first human study of PLK1 inhibitors, has been terminated now, but its combinational study is still available in several solid tumors. BI 2536 17-24 polo like kinase 1 Homo sapiens 51-55 23962445-2 2013 BI 2536 is the first selective inhibitor of Plk1 that inhibits cancer cell proliferation by promoting G2/M cell cycle arrest at nanomolar concentrations. BI 2536 0-7 polo like kinase 1 Homo sapiens 44-48 23962445-6 2013 Moreover, BI 2536 stimulates the ATPase activity of both ABCB1 and ABCG2 in a concentration-dependent manner, and inhibits the drug substrate transport mediated by these transporters. BI 2536 10-17 ATP binding cassette subfamily B member 1 Homo sapiens 57-62 23962445-6 2013 Moreover, BI 2536 stimulates the ATPase activity of both ABCB1 and ABCG2 in a concentration-dependent manner, and inhibits the drug substrate transport mediated by these transporters. BI 2536 10-17 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 67-72 23962445-8 2013 Taken together, our findings indicate that in order to circumvent ABCB1 or ABCG2-mediated acquired resistance to BI 2536, a combined regimen of BI 2536 and inhibitors or clinically active drugs that potently inhibit the function of ABC drug transporters, should be considered as a potential treatment strategy in the clinic. BI 2536 113-120 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 75-80 23962445-8 2013 Taken together, our findings indicate that in order to circumvent ABCB1 or ABCG2-mediated acquired resistance to BI 2536, a combined regimen of BI 2536 and inhibitors or clinically active drugs that potently inhibit the function of ABC drug transporters, should be considered as a potential treatment strategy in the clinic. BI 2536 144-151 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 75-80 23770244-6 2013 Performing large-scale phosphoproteomics of estradiol-treated MCF7 cells in the presence or absence of the specific PLK1 inhibitor BI2536, we identified several PLK1 end targets involved in transcription, including the histone H3K4 trimethylase MLL2, the function of which on ER target genes was impaired by PLK1 inhibition. BI 2536 131-137 polo like kinase 1 Homo sapiens 116-120 23861345-7 2013 The reduction of BCL-2 expression in endocrine-resistant cells lowered their apoptotic threshold to antimitotic agents: nocodazole, paclitaxel, and the PLK1 inhibitor BI2536. BI 2536 167-173 BCL2 apoptosis regulator Homo sapiens 17-22 23861345-7 2013 The reduction of BCL-2 expression in endocrine-resistant cells lowered their apoptotic threshold to antimitotic agents: nocodazole, paclitaxel, and the PLK1 inhibitor BI2536. BI 2536 167-173 polo like kinase 1 Homo sapiens 152-156 24033250-2 2013 BI 2536, a novel Plk inhibitor, induces mitotic arrest and apoptosis. BI 2536 0-7 polo like kinase 1 Homo sapiens 17-20 23713868-3 2013 Here, we aimed at testing the radiosensitizing effects of the PLK1 inhibitor BI 2536 on eight GBM cell lines. BI 2536 77-84 polo like kinase 1 Homo sapiens 62-66 23770244-6 2013 Performing large-scale phosphoproteomics of estradiol-treated MCF7 cells in the presence or absence of the specific PLK1 inhibitor BI2536, we identified several PLK1 end targets involved in transcription, including the histone H3K4 trimethylase MLL2, the function of which on ER target genes was impaired by PLK1 inhibition. BI 2536 131-137 polo like kinase 1 Homo sapiens 161-165 23770244-6 2013 Performing large-scale phosphoproteomics of estradiol-treated MCF7 cells in the presence or absence of the specific PLK1 inhibitor BI2536, we identified several PLK1 end targets involved in transcription, including the histone H3K4 trimethylase MLL2, the function of which on ER target genes was impaired by PLK1 inhibition. BI 2536 131-137 polo like kinase 1 Homo sapiens 161-165 22807983-0 2012 Effects of the Polo-like-kinase-1-inhibitor BI2536 in squamous cell carcinoma cell lines of the head and neck. BI 2536 44-50 polo like kinase 1 Homo sapiens 15-33 22978685-0 2013 The Plk1 inhibitor BI 2536 in patients with refractory or relapsed non-Hodgkin lymphoma: a phase I, open-label, single dose-escalation study. BI 2536 19-26 polo like kinase 1 Homo sapiens 4-8 22978685-2 2013 This phase I study determined the maximum tolerated dose (MTD) of BI 2536, a Plk1 inhibitor, as a 1 h infusion once every 3 weeks in post-transplant relapsed (n = 17) and transplant-naive (n = 24) patients with relapsed/refractory NHL. BI 2536 66-73 polo like kinase 1 Homo sapiens 77-81 22978685-8 2013 The activity and safety of BI 2536 in this pretreated patient population support Plk inhibitors as a therapeutic strategy in oncology. BI 2536 27-34 polo like kinase 1 Homo sapiens 81-84 23146687-8 2013 In a xenograft mouse model with p53-deficient cells, low dose BI2536 significantly inhibited tumor growth. BI 2536 62-68 transformation related protein 53, pseudogene Mus musculus 32-35 24649162-0 2013 Antitumoral effect of PLK-1-inhibitor BI2536 in combination with cisplatin and docetaxel in squamous cell carcinoma cell lines of the head and neck. BI 2536 38-44 polo like kinase 1 Homo sapiens 22-27 24649162-2 2013 In this systemic in vitro study, the antitumor effect of BI2536, a small molecule inhibitor of PLK-1, in combination with cisplatin and docetaxel was examined in nine squamous cell carcinoma cell lines, most of which had a head and neck origin (SCCHN). BI 2536 57-63 polo like kinase 1 Homo sapiens 95-100 24649162-6 2013 The findings of this study showed that the addition of PLK-1-inhibitor BI2536 to conventional chemotherapeutic drugs led to a statistically higher antiproliferative and apoptotic effect in SCCHN cell lines compared with cisplatin or docetaxel alone. BI 2536 71-77 polo like kinase 1 Homo sapiens 55-60 23204129-5 2013 RESULTS: Cotreatment with BI2536 and vorinostat synergistically induced cell death in parental or imatinib mesylate-resistant BCR/ABL(+) cells and primary CD34(+) bone marrow cells but was minimally toxic to normal cells. BI 2536 26-32 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 126-133 23204129-5 2013 RESULTS: Cotreatment with BI2536 and vorinostat synergistically induced cell death in parental or imatinib mesylate-resistant BCR/ABL(+) cells and primary CD34(+) bone marrow cells but was minimally toxic to normal cells. BI 2536 26-32 CD34 molecule Homo sapiens 155-159 23226805-0 2012 Fighting cancer from different signalling pathways: Effects of the proteasome inhibitor Bortezomib in combination with the polo-like-kinase-1-inhibitor BI2536 in SCCHN. BI 2536 152-158 polo like kinase 1 Homo sapiens 123-141 23226805-6 2012 A combination treatment regime consisting of the proteasome inhibitor, Bortezomib, and the inhibitor of PLK-1, BI2536, leads to an enhanced anti-proliferative and apoptotic effect in SCCHN cell lines, compared to single agent treatment with Bortezomib alone. BI 2536 111-117 polo like kinase 1 Homo sapiens 104-109 23593196-13 2013 Inhibition of ABCB1 with XR9576 and cyclosporin A enhanced the cytotoxicity of BI 2536 to ABCB1-overexpressing cancer cells, HCT-15-Pgp, and decreased the IC50 value of BI 2536 by several orders of magnitude. BI 2536 79-86 ATP binding cassette subfamily B member 1 Homo sapiens 14-19 23593196-13 2013 Inhibition of ABCB1 with XR9576 and cyclosporin A enhanced the cytotoxicity of BI 2536 to ABCB1-overexpressing cancer cells, HCT-15-Pgp, and decreased the IC50 value of BI 2536 by several orders of magnitude. BI 2536 79-86 ATP binding cassette subfamily B member 1 Homo sapiens 90-95 23593196-13 2013 Inhibition of ABCB1 with XR9576 and cyclosporin A enhanced the cytotoxicity of BI 2536 to ABCB1-overexpressing cancer cells, HCT-15-Pgp, and decreased the IC50 value of BI 2536 by several orders of magnitude. BI 2536 79-86 phosphoglycolate phosphatase Homo sapiens 132-135 22080235-0 2013 Antiproliferative in vitro effects of BI 2536-mediated PLK1 inhibition on cervical adenocarcinoma cells. BI 2536 38-45 polo like kinase 1 Homo sapiens 55-59 22080235-3 2013 BI 2536, an unambiguous inhibitor of Polo-like kinase 1 (PLK1), has shown anticancer activity in a variety of tumor cell types. BI 2536 0-7 polo like kinase 1 Homo sapiens 37-55 22080235-3 2013 BI 2536, an unambiguous inhibitor of Polo-like kinase 1 (PLK1), has shown anticancer activity in a variety of tumor cell types. BI 2536 0-7 polo like kinase 1 Homo sapiens 57-61 23144294-5 2013 In triple-negative cell lines, RNAi-mediated PLK1 depletion or inhibition of PLK1 activity with a small molecule (BI-2536) induced an increase in phosphorylated H2AX, G(2)-M arrest, and apoptosis. BI 2536 114-121 polo like kinase 1 Homo sapiens 77-81 23144294-5 2013 In triple-negative cell lines, RNAi-mediated PLK1 depletion or inhibition of PLK1 activity with a small molecule (BI-2536) induced an increase in phosphorylated H2AX, G(2)-M arrest, and apoptosis. BI 2536 114-121 H2A.X variant histone Homo sapiens 161-165 22658814-1 2013 INTRODUCTION: BI 2536 is a potent, highly selective inhibitor of polo-like kinase (Plk) 1. BI 2536 14-21 polo like kinase 1 Homo sapiens 65-81 22658814-1 2013 INTRODUCTION: BI 2536 is a potent, highly selective inhibitor of polo-like kinase (Plk) 1. BI 2536 14-21 polo like kinase 1 Homo sapiens 83-89 22854038-8 2012 However, treatment of pachytene spermatocytes with the PLK inhibitor BI 2536 prevented the okadaic-acid-induced meiotic prophase exit and inhibited phosphorylation of the central element proteins as well as their removal from the SC. BI 2536 69-76 polo like kinase 1 Mus musculus 55-58 22807983-2 2012 In this in vitro study, we examined the antitumor effect of BI2536, a small molecule inhibitor of PLK1, in squamous cell carcinoma of the head and neck (SCCHN) cell lines. BI 2536 60-66 polo like kinase 1 Homo sapiens 98-102 22415968-6 2012 Moreover, BTICs rely on PLK1 for survival because the PLK1 inhibitor BI2536 inhibited their growth in tumorsphere cultures. BI 2536 69-75 polo like kinase 1 Homo sapiens 24-28 22422077-7 2012 Structural modeling demonstrates that this mutation not only enables Plk1(as) to function in vivo but also occludes BI-2536 from the ATP-binding pocket. BI 2536 116-123 polo like kinase 1 Homo sapiens 69-73 22415968-6 2012 Moreover, BTICs rely on PLK1 for survival because the PLK1 inhibitor BI2536 inhibited their growth in tumorsphere cultures. BI 2536 69-75 polo like kinase 1 Homo sapiens 54-58 22309939-14 2012 The PLK1 inhibitor BI 2536 showed similar effects on growth, mammosphere formation, and apoptosis as did PLK1 siRNAs. BI 2536 19-26 polo like kinase 1 Homo sapiens 4-8 22745587-0 2012 Reduced efficacy of the Plk1 inhibitor BI 2536 on the progression of hepatocellular carcinoma due to low intratumoral drug levels. BI 2536 39-46 polo like kinase 1 Mus musculus 24-28 22745587-4 2012 Inhibition of Plk1 by an adenovirus encoding for a short hairpin RNA against Plk1 or by the small-molecule inhibitor BI 2536 reduced the viability of HCC cell lines and inhibited HCC xenograft progression in nude mice. BI 2536 117-124 polo like kinase 1 Mus musculus 14-18 22745587-4 2012 Inhibition of Plk1 by an adenovirus encoding for a short hairpin RNA against Plk1 or by the small-molecule inhibitor BI 2536 reduced the viability of HCC cell lines and inhibited HCC xenograft progression in nude mice. BI 2536 117-124 HCC Homo sapiens 150-153 22745587-4 2012 Inhibition of Plk1 by an adenovirus encoding for a short hairpin RNA against Plk1 or by the small-molecule inhibitor BI 2536 reduced the viability of HCC cell lines and inhibited HCC xenograft progression in nude mice. BI 2536 117-124 HCC Homo sapiens 179-182 22745587-8 2012 In conclusion, low intratumoral levels are a novel mechanism of resistance to the Plk1 inhibitor BI 2536. BI 2536 97-104 polo like kinase 1 Mus musculus 82-86 22527426-3 2012 In the present study we tested the in vitro antitumor activities of BI 2536, a selective inhibitor of PLK1, against two melanoma cell lines. BI 2536 68-75 polo like kinase 1 Homo sapiens 102-106 21822121-0 2011 BI 2536-mediated PLK1 inhibition suppresses HOS and MG-63 osteosarcoma cell line growth and clonogenicity. BI 2536 0-7 polo like kinase 1 Homo sapiens 17-21 22328845-0 2012 Phase i study of the Plk1 inhibitor BI 2536 administered intravenously on three consecutive days in advanced solid tumours. BI 2536 36-43 polo like kinase 1 Homo sapiens 21-25 22328845-1 2012 BACKGROUND: This open-label phase i study with an accelerated titration design was performed to determine the maximum tolerated dose of BI 2536, a potent, highly selective small-molecule polo-like kinase 1 (Plk1) inhibitor. BI 2536 136-143 polo like kinase 1 Homo sapiens 187-205 22328845-1 2012 BACKGROUND: This open-label phase i study with an accelerated titration design was performed to determine the maximum tolerated dose of BI 2536, a potent, highly selective small-molecule polo-like kinase 1 (Plk1) inhibitor. BI 2536 136-143 polo like kinase 1 Homo sapiens 207-211 21816470-2 2011 The present study explored the expression and prognostic significance of the centrosome-associated protein PLK1 in myeloma and the effect of BI 2536, a potent and selective inhibitor of PLK1, on myeloma cells. BI 2536 141-148 polo like kinase 1 Homo sapiens 186-190 21822121-4 2011 BI 2536, an innovative selective inhibitor of Polo-like kinase 1, has shown anticancer potential promoting mitotic arrest and apoptosis in a variety of tumor cells, including osteosarcoma. BI 2536 0-7 polo like kinase 1 Homo sapiens 46-64 21965739-4 2011 BI 2536, the first compound of the chemical class of dihydropteridinones, is a highly selective and potent inhibitor of PLK1. BI 2536 0-7 polo like kinase 1 Homo sapiens 120-124 21399492-6 2011 Here, we describe the in-vitro and in-vivo effects of BI 2536, a small-molecule inhibitor of PLK1, which through inhibiting PLK1 enzymatic activity, causes mitotic arrest and eventually induces cancer cell apoptosis. BI 2536 54-61 polo like kinase 1 Mus musculus 93-97 21642374-8 2011 BI 2536 inhibited the proliferation of ccRCC cell lines at concentrations required to inhibit PLK1 kinase activity, and sustained inhibition of PLK1 by BI 2536 led to dramatic regression of ccRCC xenograft tumors in vivo. BI 2536 0-7 polo like kinase 1 Homo sapiens 94-98 21642374-8 2011 BI 2536 inhibited the proliferation of ccRCC cell lines at concentrations required to inhibit PLK1 kinase activity, and sustained inhibition of PLK1 by BI 2536 led to dramatic regression of ccRCC xenograft tumors in vivo. BI 2536 152-159 polo like kinase 1 Homo sapiens 144-148 21670883-9 2011 The anti-cancer drug BI 2536 (the most potent and selective Plk1 inhibitor) inhibits specifically the catalytic activity of SmPlk1 and induced profound alterations in schistosome gonads, indicating a role of SmPlk1 in parasite gametogenesis and its potential as a novel chemotherapeutic target against schistosomiasis. BI 2536 21-28 polo like kinase 1 Mus musculus 60-64 21399492-6 2011 Here, we describe the in-vitro and in-vivo effects of BI 2536, a small-molecule inhibitor of PLK1, which through inhibiting PLK1 enzymatic activity, causes mitotic arrest and eventually induces cancer cell apoptosis. BI 2536 54-61 polo like kinase 1 Mus musculus 124-128 21399492-7 2011 In this study, we show that the PLK1 inhibitor, BI 2536, inhibits proliferation and induces apoptosis in two-dimensional and three-dimensional cultures of osteosarcoma cell lines, KHOS and U-2OS. BI 2536 48-55 polo like kinase 1 Mus musculus 32-36 21399492-10 2011 Immunofluorescence and western blotting analysis confirmed that the administration of BI 2536 led to significant decrease of PLK1 and Mcl-1 protein expression levels in dose-dependent and time-dependent manners. BI 2536 86-93 polo like kinase 1 Mus musculus 125-129 21399492-10 2011 Immunofluorescence and western blotting analysis confirmed that the administration of BI 2536 led to significant decrease of PLK1 and Mcl-1 protein expression levels in dose-dependent and time-dependent manners. BI 2536 86-93 myeloid cell leukemia sequence 1 Mus musculus 134-139 21415595-0 2011 Polo-like kinase 1 inhibitors SBE13 and BI 2536 induce different responses in primary cells. BI 2536 40-47 polo like kinase 1 Homo sapiens 0-18 21242189-8 2011 BI 2536, a drug targeting Polo-like kinase-1, was found to inhibit proliferation in HMC-1 cells in a dose-dependent manner. BI 2536 0-7 polo like kinase 1 Homo sapiens 26-44 21184800-2 2011 We have investigated whether this kinase plays a role in multiple myeloma (MM) using the Plk1 inhibitor BI 2536. BI 2536 104-111 polo like kinase 1 Homo sapiens 89-93 21252232-5 2011 Precocious segregation induced by MYPT1 depletion requires PLK1 activity because a PLK1 inhibitor, BI-2536, blocked precocious segregation. BI 2536 99-106 protein phosphatase 1 regulatory subunit 12A Homo sapiens 34-39 21252232-5 2011 Precocious segregation induced by MYPT1 depletion requires PLK1 activity because a PLK1 inhibitor, BI-2536, blocked precocious segregation. BI 2536 99-106 polo like kinase 1 Homo sapiens 59-63 21252232-5 2011 Precocious segregation induced by MYPT1 depletion requires PLK1 activity because a PLK1 inhibitor, BI-2536, blocked precocious segregation. BI 2536 99-106 polo like kinase 1 Homo sapiens 83-87 28927329-0 2011 Polo-like kinase 1 inhibitors SBE13 and BI 2536 induce different responses in primary cells. BI 2536 40-47 polo like kinase 1 Homo sapiens 0-18 21079244-6 2010 Endogenous Cep55 behaves similarly after Plk1 inhibition by the drugs BI2536 or GW842862. BI 2536 70-76 centrosomal protein 55 Homo sapiens 11-16 21169242-2 2011 The Polo-like kinase 1 (PLK1) is highly expressed in many human cancers and is a target of the novel small-molecule inhibitor BI 2536, which has shown promising anticancer activity in adult malignancies. BI 2536 126-133 polo like kinase 1 Homo sapiens 4-22 21169242-2 2011 The Polo-like kinase 1 (PLK1) is highly expressed in many human cancers and is a target of the novel small-molecule inhibitor BI 2536, which has shown promising anticancer activity in adult malignancies. BI 2536 126-133 polo like kinase 1 Homo sapiens 24-28 21750699-3 2011 We studied the PLK 1, 2, 3 inhibitor BI 2536 and observed potent (IC50<40 nM) and rapid (commitment to cell death <24 hrs) in vitro activity against MM cells in isolation, as well as in vivo activity against a traditional subcutaneous xenograft mouse model. BI 2536 37-44 polo like kinase 1 Mus musculus 15-20 20682708-1 2010 PURPOSE: This phase I, open-label, dose-escalation study investigated the maximum tolerated dose (MTD) of BI 2536, a small-molecule polo-like kinase (Plk)-1 inhibitor, in two treatment schedules in patients with advanced solid tumors. BI 2536 106-113 polo like kinase 1 Homo sapiens 132-156 20927084-0 2010 Prediction of neutropenia-related effects of a new combination therapy with the anticancer drugs BI 2536 (a Plk1 inhibitor) and pemetrexed. BI 2536 97-104 polo like kinase 1 Homo sapiens 108-112 20927084-1 2010 This study investigated the feasibility of predicting the neutropenia-related effects of a therapy that combines the investigational drug BI 2536 (inhibitor of Polo-like kinase 1) and pemetrexed, an approved anticancer drug. BI 2536 138-145 polo like kinase 1 Homo sapiens 160-178 20886032-0 2010 The Plk1 inhibitor BI 2536 temporarily arrests primary cardiac fibroblasts in mitosis and generates aneuploidy in vitro. BI 2536 19-26 polo like kinase 1 Homo sapiens 4-8 20886032-1 2010 BI 2536 is a new anti-mitotic drug that targets polo-like kinase 1 (Plk1) and is currently under clinical development for cancer therapy. BI 2536 0-7 polo like kinase 1 Homo sapiens 48-66 20886032-1 2010 BI 2536 is a new anti-mitotic drug that targets polo-like kinase 1 (Plk1) and is currently under clinical development for cancer therapy. BI 2536 0-7 polo like kinase 1 Homo sapiens 68-72 20682708-14 2010 CONCLUSIONS: BI 2536 administered in either treatment schedule has adequate safety in patients with advanced solid tumors, warranting further clinical investigation of polo-like kinase-1 inhibitors. BI 2536 13-20 polo like kinase 1 Homo sapiens 168-186 20526206-0 2010 The efficacy and safety of BI 2536, a novel Plk-1 inhibitor, in patients with stage IIIB/IV non-small cell lung cancer who had relapsed after, or failed, chemotherapy: results from an open-label, randomized phase II clinical trial. BI 2536 27-34 polo like kinase 1 Homo sapiens 44-49 20062994-0 2010 Semi-mechanistic population pharmacokinetic/pharmacodynamic model for neutropenia following therapy with the Plk-1 inhibitor BI 2536 and its application in clinical development. BI 2536 125-132 polo like kinase 1 Homo sapiens 109-114 20553902-7 2010 Treatment of embryos with the Plk1 inhibitor, BI 2536, caused a block in mitosis, which was more severe when used to treat plk1 morphants. BI 2536 46-53 polo-like kinase 1 (Drosophila) Danio rerio 30-34 20553902-7 2010 Treatment of embryos with the Plk1 inhibitor, BI 2536, caused a block in mitosis, which was more severe when used to treat plk1 morphants. BI 2536 46-53 polo-like kinase 1 (Drosophila) Danio rerio 123-127 20526206-1 2010 OBJECTIVE: To investigate the efficacy, safety, and pharmacokinetics of two dosing schedules of BI 2536, a novel polo-like kinase-1 inhibitor, in patients with relapsed stage IIIB/IV non-small cell lung cancer. BI 2536 96-103 polo like kinase 1 Homo sapiens 113-131 18005335-3 2007 BI 2536 (Boehringer Ingelheim, Ingelheim, Germany), a Polo-like kinase 1 inhibitor currently in clinical trials, exhibits nanomolar potency against Polo-like kinase isoforms and high selectivity against other kinases. BI 2536 0-7 polo like kinase 1 Homo sapiens 54-72 19482353-4 2009 In this study, the recently discovered specific Polo-like kinase (Plk) inhibitor BI2536 was used to investigate the role of Plk1 in this process. BI 2536 81-87 polo like kinase 1 Homo sapiens 48-64 19482353-4 2009 In this study, the recently discovered specific Polo-like kinase (Plk) inhibitor BI2536 was used to investigate the role of Plk1 in this process. BI 2536 81-87 polo like kinase 1 Homo sapiens 66-69 19482353-4 2009 In this study, the recently discovered specific Polo-like kinase (Plk) inhibitor BI2536 was used to investigate the role of Plk1 in this process. BI 2536 81-87 polo like kinase 1 Homo sapiens 124-128 19482353-5 2009 BI2536 inactivates Plk1 in oocytes at the early stages of maturation and significantly decreases IP(3)R1 phosphorylation at an MPM-2 epitope at this stage. BI 2536 0-6 polo like kinase 1 Homo sapiens 19-23 19482353-5 2009 BI2536 inactivates Plk1 in oocytes at the early stages of maturation and significantly decreases IP(3)R1 phosphorylation at an MPM-2 epitope at this stage. BI 2536 0-6 inositol 1,4,5-trisphosphate receptor type 1 Homo sapiens 97-104 18955456-1 2008 PURPOSE: BI 2536 is a novel, potent, and highly specific inhibitor of polo-like kinase 1 (Plk1), which has an essential role in the regulation of mitotic progression. BI 2536 9-16 polo like kinase 1 Homo sapiens 90-94 20145140-0 2010 Polo-like kinase 1 (Plk1) as a novel drug target in chronic myeloid leukemia: overriding imatinib resistance with the Plk1 inhibitor BI 2536. BI 2536 133-140 polo like kinase 1 Homo sapiens 0-18 20145140-0 2010 Polo-like kinase 1 (Plk1) as a novel drug target in chronic myeloid leukemia: overriding imatinib resistance with the Plk1 inhibitor BI 2536. BI 2536 133-140 polo like kinase 1 Homo sapiens 20-24 20145140-0 2010 Polo-like kinase 1 (Plk1) as a novel drug target in chronic myeloid leukemia: overriding imatinib resistance with the Plk1 inhibitor BI 2536. BI 2536 133-140 polo like kinase 1 Homo sapiens 118-122 20072841-0 2010 BI_2536--targeting the mitotic kinase Polo-like kinase 1 (Plk1). BI 2536 0-7 polo like kinase 1 Homo sapiens 38-56 20072841-0 2010 BI_2536--targeting the mitotic kinase Polo-like kinase 1 (Plk1). BI 2536 0-7 polo like kinase 1 Homo sapiens 58-62 20072841-3 2010 The Plk1 inhibitor BI_2536 was well tolerated and showed antitumor activity in the first clinical trials enrolling patients with advanced solid tumors and refractory or relapsed acute myeloid leukemia. BI 2536 19-26 polo like kinase 1 Homo sapiens 4-8 19243593-4 2009 However, both p53-positive and -negative cells arrest in mitosis if treated with low doses of siRNA against NEDD1 combined with low doses of the inhibitor BI2536 against the mitotic kinase Plk1. BI 2536 155-161 tumor protein p53 Homo sapiens 14-17 19243593-4 2009 However, both p53-positive and -negative cells arrest in mitosis if treated with low doses of siRNA against NEDD1 combined with low doses of the inhibitor BI2536 against the mitotic kinase Plk1. BI 2536 155-161 polo like kinase 1 Homo sapiens 189-193 34700228-11 2021 Targeting the mevalonate pathway contributes to re-sensitizing BI2536-resistant cells in vitro and in vivo, raising as a new strategy for the clinical management of PLK1 inhibitors. BI 2536 63-69 polo like kinase 1 Homo sapiens 165-169 17488623-3 2007 Here we have used BI 2536, an inhibitor of the mitotic kinase Plk1, to analyze the functions of this enzyme during late mitosis in human cells. BI 2536 18-25 polo like kinase 1 Homo sapiens 62-66 17437704-2 2007 Analysis of the cytological and anti-tumor activities of BI 2536, a novel, selective pharmacological inhibitor of Plk1, has connected chemistry and biology to the bedside. BI 2536 57-64 polo like kinase 1 Homo sapiens 114-118 17291761-0 2007 The small-molecule inhibitor BI 2536 reveals novel insights into mitotic roles of polo-like kinase 1. BI 2536 29-36 polo like kinase 1 Homo sapiens 82-100 17291761-3 2007 RESULTS: We describe the cellular effects of a novel compound, BI 2536, a potent and selective inhibitor of Plk1. BI 2536 63-70 polo like kinase 1 Homo sapiens 108-112 17291761-5 2007 Cells treated with BI 2536 are delayed in prophase but eventually import Cdk1-cyclin B into the nucleus, enter prometaphase, and degrade cyclin A, although BI 2536 prevents degradation of the APC/C inhibitor Emi1. BI 2536 19-26 cyclin dependent kinase 1 Homo sapiens 73-77 17291761-5 2007 Cells treated with BI 2536 are delayed in prophase but eventually import Cdk1-cyclin B into the nucleus, enter prometaphase, and degrade cyclin A, although BI 2536 prevents degradation of the APC/C inhibitor Emi1. BI 2536 19-26 cyclin A2 Homo sapiens 137-145 17291761-5 2007 Cells treated with BI 2536 are delayed in prophase but eventually import Cdk1-cyclin B into the nucleus, enter prometaphase, and degrade cyclin A, although BI 2536 prevents degradation of the APC/C inhibitor Emi1. BI 2536 19-26 F-box protein 5 Homo sapiens 208-212 17291761-8 2007 BI 2536 prevents Plk1"s enrichment at kinetochores and centrosomes, and when added to metaphase cells, it induces detachment of microtubules from kinetochores and leads to spindle collapse. BI 2536 0-7 polo like kinase 1 Homo sapiens 17-21 35211471-7 2022 Combined drug sensitivity analysis (CTRP/PRISM/CMap/GDSC) revealed that BI-2536 might serve as a new therapeutic compound for patients in C1. BI 2536 72-79 cystatin F Homo sapiens 47-51 34376582-6 2021 In addition, ISQ-1 treatment showed remarkable synergistic depletion of oncogenic c-Myc protein level in vitro and induced strong tumor remission in vivo when administered together with BI2536, a polo-like kinase-1 (Plk1) inhibitor. BI 2536 186-192 MYC proto-oncogene, bHLH transcription factor Homo sapiens 82-87 34376582-6 2021 In addition, ISQ-1 treatment showed remarkable synergistic depletion of oncogenic c-Myc protein level in vitro and induced strong tumor remission in vivo when administered together with BI2536, a polo-like kinase-1 (Plk1) inhibitor. BI 2536 186-192 polo like kinase 1 Homo sapiens 196-214 34376582-6 2021 In addition, ISQ-1 treatment showed remarkable synergistic depletion of oncogenic c-Myc protein level in vitro and induced strong tumor remission in vivo when administered together with BI2536, a polo-like kinase-1 (Plk1) inhibitor. BI 2536 186-192 polo like kinase 1 Homo sapiens 216-220 34493069-8 2021 In addition, L1 overcomes cellular drug resistance mediated by betaIII tubulin overexpression and has a strong synergistic effect when combined with the Plk1 inhibitor BI2536. BI 2536 168-174 polo like kinase 1 Homo sapiens 153-157 35436627-7 2022 PLK1 inhibition with BI2536 did not affect cell viability in any group over 24 h but deterred fusion more significantly in PAD myoblasts. BI 2536 21-27 polo like kinase 1 Homo sapiens 0-4