PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 20597485-0 2010 Structural basis for inhibition of Eg5 by dihydropyrimidines: stereoselectivity of antimitotic inhibitors enastron, dimethylenastron and fluorastrol. dimethylenastron 116-132 kinesin family member 11 Homo sapiens 35-38 20597485-2 2010 Here, we report the crystal structures of the Eg5 motor domain complexed with enastron, dimethylenastron, and fluorastrol. dimethylenastron 88-104 kinesin family member 11 Homo sapiens 46-49 20597485-4 2010 We also noticed preferential binding of the S-enantiomer of enastron and dimethylenastron to Eg5, while the R-enantiomer of fluorastrol binds preferentially to Eg5. dimethylenastron 73-89 kinesin family member 11 Homo sapiens 93-96 19270519-4 2009 Here, we show that targeting the mitotic kinesin Eg5 (also known as kinesin spindle protein, KSP) by a small interfering RNA (siRNA) or by the pharmacological inhibitor dimethylenastron (DIMEN) kills tetraploid tumor cells more efficiently than their diploid precursors. dimethylenastron 169-185 kinesin family member 11 Homo sapiens 49-52 34972948-1 2022 This paper describes an easy method to enrich the harvest of adherent mammalian cells at each stage of mitosis (from prometaphase to cytokinesis) by combining Eg5 inhibition using dimethylenastron (DMA) with mitotic shake-off, followed by timed release from the drug. dimethylenastron 180-196 kinesin family member 11 Homo sapiens 159-162 34972948-1 2022 This paper describes an easy method to enrich the harvest of adherent mammalian cells at each stage of mitosis (from prometaphase to cytokinesis) by combining Eg5 inhibition using dimethylenastron (DMA) with mitotic shake-off, followed by timed release from the drug. dimethylenastron 198-201 kinesin family member 11 Homo sapiens 159-162 21986572-0 2011 Dimethylenastron suppresses human pancreatic cancer cell migration and invasion in vitro via allosteric inhibition of mitotic kinesin Eg5. dimethylenastron 0-16 kinesin family member 11 Homo sapiens 134-137 29736710-4 2018 This screen is based on the analysis of monopolar mitotic spindle structures, which form upon inhibition of the mitotic kinesin Eg5/KSP by the small-molecule inhibitor dimethylenastron (DME) or similar compounds. dimethylenastron 168-184 kinesin family member 11 Homo sapiens 128-131 29736710-4 2018 This screen is based on the analysis of monopolar mitotic spindle structures, which form upon inhibition of the mitotic kinesin Eg5/KSP by the small-molecule inhibitor dimethylenastron (DME) or similar compounds. dimethylenastron 186-189 kinesin family member 11 Homo sapiens 128-131 24732354-0 2014 Significant decrease of ADP release rate underlies the potent activity of dimethylenastron to inhibit mitotic kinesin Eg5 and cancer cell proliferation. dimethylenastron 74-90 kinesin family member 11 Homo sapiens 118-121 24732354-2 2014 Dimethylenastron is potent specific small molecule inhibitor of Eg5. dimethylenastron 0-16 kinesin family member 11 Homo sapiens 64-67 24732354-3 2014 The mechanism by which dimethylenastron inhibits Eg5 function remains unclear. dimethylenastron 23-39 kinesin family member 11 Homo sapiens 49-52 24732354-5 2014 We analyze their interactions with ADP-bound Eg5 crystal structure, and find that dimethylenastron binds Eg5 motor domain with higher affinity. dimethylenastron 82-98 kinesin family member 11 Homo sapiens 45-48 24732354-5 2014 We analyze their interactions with ADP-bound Eg5 crystal structure, and find that dimethylenastron binds Eg5 motor domain with higher affinity. dimethylenastron 82-98 kinesin family member 11 Homo sapiens 105-108 21986572-2 2011 This study was undertaken to investigate the effect of dimethylenastron, a specific inhibitor of Eg5, on the migration and invasion of pancreatic cancer cells. dimethylenastron 55-71 kinesin family member 11 Homo sapiens 97-100 21986572-7 2011 The binding of dimethylenastron to Eg5 was analyzed with a molecular modeling study, and the ADP release rate was examined with the MANT-ADP reagent. dimethylenastron 15-31 kinesin family member 11 Homo sapiens 35-38 21986572-11 2011 However, treatment of PANC1 cells with dimethylenastron (3 and 10 mumol/L) for 24 h had no detectable effect on their proliferation, which was inhibited when the cancer cells were treated with the drug for 72 h. Molecular modeling study showed that dimethylenastron could allosterically inhibit the motor domain ATPase of Eg5 by decreasing the rate of ADP release. dimethylenastron 39-55 kinesin family member 11 Homo sapiens 322-325 21986572-11 2011 However, treatment of PANC1 cells with dimethylenastron (3 and 10 mumol/L) for 24 h had no detectable effect on their proliferation, which was inhibited when the cancer cells were treated with the drug for 72 h. Molecular modeling study showed that dimethylenastron could allosterically inhibit the motor domain ATPase of Eg5 by decreasing the rate of ADP release. dimethylenastron 249-265 kinesin family member 11 Homo sapiens 322-325 21613548-4 2011 When satisfaction of the MC was prevented with 500 nM nocodazole or 2.5 muM dimethylenastron (an Eg5 inhibitor), 92-100% of RPE-1 cells slipped from mitosis in the presence of pan-caspase inhibitors or after simultaneously depleting caspase-3 and -9, and they did so with the same kinetics (~21-22 h) as after treatment with nocodazole or Eg5 inhibitors alone. dimethylenastron 76-92 kinesin family member 11 Homo sapiens 97-100 21613548-4 2011 When satisfaction of the MC was prevented with 500 nM nocodazole or 2.5 muM dimethylenastron (an Eg5 inhibitor), 92-100% of RPE-1 cells slipped from mitosis in the presence of pan-caspase inhibitors or after simultaneously depleting caspase-3 and -9, and they did so with the same kinetics (~21-22 h) as after treatment with nocodazole or Eg5 inhibitors alone. dimethylenastron 76-92 kinesin family member 11 Homo sapiens 339-342