PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 33116269-0 2020 Dinaciclib, a cyclin-dependent kinase inhibitor, suppresses cholangiocarcinoma growth by targeting CDK2/5/9. dinaciclib 0-10 cyclin dependent kinase 2 Homo sapiens 99-107 34688130-3 2021 The 7-(4-Bromo-phenyl)-3-(3-chloro/2-chloro-phenylazo)-pyrazolo(1,5-a)pyrimidin-2-ylamines 5 h and 5i revealed the best CDK2 inhibitory activity with comparable potency (IC50 = 22 and 24 nM, respectively) to that of dinaciclib (IC50 = 18 nM). dinaciclib 216-226 cyclin dependent kinase 2 Homo sapiens 120-124 34688130-10 2021 The molecular docking simulations indicated, as expected, that the dinaciclib analogues can well-accommodate the CDK2 binding site, forming a variety of interactions. dinaciclib 67-77 cyclin dependent kinase 2 Homo sapiens 113-117 35053380-10 2022 As well-known CDK inhibitors, dinaciclib and kenpaullone stabilize PXR and result in elevated expression and activity of PXR-targeted DMETs, including carboxylesterases, CYP3A4 and P-gp. dinaciclib 30-40 cyclin dependent kinase 2 Homo sapiens 14-17 32395375-12 2020 The use of dinaciclib, a selective CDK inhibitor, significantly inhibited tumor growth in the PDX model. dinaciclib 11-21 cyclin dependent kinase 2 Homo sapiens 35-38 32433863-3 2020 Here, we detail the positive cooperativity between ANS and orthosteric Cdk2 inhibitors dinaciclib and roscovitine, which increase the affinity of ANS toward Cdk2 5-fold to 10-fold, and the relatively noncooperative effects of ATP. dinaciclib 87-97 cyclin dependent kinase 2 Homo sapiens 71-75 32433863-3 2020 Here, we detail the positive cooperativity between ANS and orthosteric Cdk2 inhibitors dinaciclib and roscovitine, which increase the affinity of ANS toward Cdk2 5-fold to 10-fold, and the relatively noncooperative effects of ATP. dinaciclib 87-97 cyclin dependent kinase 2 Homo sapiens 157-161 33050377-10 2020 Interestingly, HAA2020 and dinaciclib showed a synergistic apoptotic and G1 cell cycle effect in MCF7 cells, which was supported by their synergistic CDK2, cyclin D1, and PCNA inhibition activities. dinaciclib 27-37 cyclin dependent kinase 2 Homo sapiens 150-154 32368395-1 2020 The cyclin-dependent kinase 2 (CDK2) inhibitor dinaciclib, a potential anti-cancer drug, has been tested in clinical trials and reported to suppress tumor initiating cells. dinaciclib 47-57 cyclin dependent kinase 2 Homo sapiens 4-29 32368395-1 2020 The cyclin-dependent kinase 2 (CDK2) inhibitor dinaciclib, a potential anti-cancer drug, has been tested in clinical trials and reported to suppress tumor initiating cells. dinaciclib 47-57 cyclin dependent kinase 2 Homo sapiens 31-35 31529315-9 2020 Moreover, it sensitized cells to the chemotherapeutic agents such as cisplatin, pemetrexed, and etoposide (VP-16), and this effect by dinaciclib may induce cell cycle arrest via abrogating CDK2 activity. dinaciclib 134-144 cyclin dependent kinase 2 Homo sapiens 189-193 29507054-7 2018 Notably, we found that MITF expression correlates with CDK2 upregulation in patients; thus, dinaciclib would warrant consideration for treatment of patients unresponsive to BRAF-MEK and/or Hsp90 inhibitors and/or harboring MITF amplification/overexpression. dinaciclib 92-102 cyclin dependent kinase 2 Homo sapiens 55-59 31439587-6 2019 Importantly, olaparib (OLA) or talazoparib (TALA) suppressed these activities, and the combination of OLA and dinaciclib (DINA), an inhibitor of CDK2 and CDK5, which also inhibits Rb1 phosphorylation, suppressed NED, and significantly improved therapeutic efficiency in neuroendocrine prostate cancer (NEPC) cells in vitro and in NEPC tumors in vivo. dinaciclib 110-120 cyclin dependent kinase 2 Homo sapiens 145-149 29507054-6 2018 The CDK2 inhibitor, dinaciclib, attenuated resistance to both classes of inhibitors and combinations thereof. dinaciclib 20-30 cyclin dependent kinase 2 Homo sapiens 4-8 28107181-4 2017 Because IBC cell lines were highly sensitive to the CDK2 inhibitors dinaciclib and meriolin 5, we developed a high-throughput survival assay (HTSA) to design novel sequential combination strategies based on the presence of cyclin E and CDK2. dinaciclib 68-78 cyclin dependent kinase 2 Homo sapiens 52-56 28947566-7 2017 LMW-E expression overcame cell-cycle inhibition by AIs in a CDK2/Rb-dependent manner, and inhibition of CDK2 by dinaciclib reversed LMW-E-mediated resistance, whereas treatment with palbociclib, a CDK4/6 inhibitor, did not.Conclusions: Collectively, these findings suggest that cell-cycle deregulation by LMW-E mediates resistance to AIs and a combination of CDK2 inhibitors and AIs may be an effective treatment in patients with HR-positive tumors that express LMW-E. Clin Cancer Res; 23(23); 7288-300. dinaciclib 112-122 cyclin dependent kinase 2 Homo sapiens 104-108 28947566-7 2017 LMW-E expression overcame cell-cycle inhibition by AIs in a CDK2/Rb-dependent manner, and inhibition of CDK2 by dinaciclib reversed LMW-E-mediated resistance, whereas treatment with palbociclib, a CDK4/6 inhibitor, did not.Conclusions: Collectively, these findings suggest that cell-cycle deregulation by LMW-E mediates resistance to AIs and a combination of CDK2 inhibitors and AIs may be an effective treatment in patients with HR-positive tumors that express LMW-E. Clin Cancer Res; 23(23); 7288-300. dinaciclib 112-122 cyclin dependent kinase 2 Homo sapiens 104-108 28249908-8 2017 Treatment with GSK2334470 or the CDK2 inhibitor dinaciclib was sufficient to reverse these events and to restore the sensitivity of ribociclib-resistant cells to CDK4/6 inhibitors. dinaciclib 48-58 cyclin dependent kinase 2 Homo sapiens 33-37 29137354-3 2017 Using a newly developed anti-pS294 monoclonal antibody, a combination of CDK specific siRNA knockdown studies and a broad panel of CDK selective inhibitors against ligand (E2)-stimulated MCF7 cells, we first identified CDK2 as the primary mediator of pS294 formation and showed that CDK2-selective inhibitors like Dinaciclib, but not CDK4/6 inhibitors like Palbociclib, can selectively prevent pS294 formation and repress ER-dependent gene expression. dinaciclib 314-324 cyclin dependent kinase 2 Homo sapiens 219-223 27550941-8 2016 Overexpression of CP110, which is a mediator of CDK2 inhibitor-induced anaphase catastrophe (and a CDK1 and 2 phosphorylation substrate), antagonized anaphase catastrophe and apoptosis following dinaciclib treatment. dinaciclib 195-205 cyclin dependent kinase 2 Homo sapiens 48-52 27378523-0 2016 Multiple CDK inhibitor dinaciclib suppresses neuroblastoma growth via inhibiting CDK2 and CDK9 activity. dinaciclib 23-33 cyclin dependent kinase 2 Homo sapiens 81-85 27378523-4 2016 Here we show that a novel multiple-CDK inhibitor, dinaciclib (SCH727965, MK-7965), exhibits potent anti-proliferative effects on a panel of NB cell lines by blocking the activity of CDK2 and CDK9. dinaciclib 50-60 cyclin dependent kinase 2 Homo sapiens 182-186 27378523-4 2016 Here we show that a novel multiple-CDK inhibitor, dinaciclib (SCH727965, MK-7965), exhibits potent anti-proliferative effects on a panel of NB cell lines by blocking the activity of CDK2 and CDK9. dinaciclib 62-71 cyclin dependent kinase 2 Homo sapiens 182-186 27378523-4 2016 Here we show that a novel multiple-CDK inhibitor, dinaciclib (SCH727965, MK-7965), exhibits potent anti-proliferative effects on a panel of NB cell lines by blocking the activity of CDK2 and CDK9. dinaciclib 73-80 cyclin dependent kinase 2 Homo sapiens 182-186 24007471-2 2013 Dinaciclib is a potent inhibitor of cyclin-dependent kinases (CDKs), which recently advanced to Phase III clinical trials for the treatment of leukemia. dinaciclib 0-10 cyclin dependent kinase 2 Homo sapiens 62-66 25947565-2 2015 CDK1/CDK2 inhibitors, such as dinaciclib, combined with anthracyclines, were synergistic in decreasing viability of TNBC cell lines. dinaciclib 30-40 cyclin dependent kinase 2 Homo sapiens 5-9 25962959-2 2015 Dinaciclib, a novel small molecule inhibitor of CDK1, CDK2, CDK5 and CDK9, is assessed in clinical trials for the treatment of several types of cancers. dinaciclib 0-10 cyclin dependent kinase 2 Homo sapiens 54-58 25395429-2 2015 Dinaciclib is a novel potent small molecule inhibitor of cyclin-dependent kinases (CDK)1, CDK2, CDK5, and CDK9. dinaciclib 0-10 cyclin dependent kinase 2 Homo sapiens 90-94 25217392-1 2014 PURPOSE: Dinaciclib is a novel selective inhibitor of cyclin-dependent kinase (CDK)1, CDK2, CDK5, and CDK9. dinaciclib 9-19 cyclin dependent kinase 2 Homo sapiens 86-90 24007471-3 2013 We determined the crystal structure of dinaciclib in complex with CDK2 at 1.7 A resolution, revealing an elaborate network of binding interactions in the ATP site, which explains the extraordinary potency and selectivity of this inhibitor. dinaciclib 39-49 cyclin dependent kinase 2 Homo sapiens 66-70 23053255-1 2012 PURPOSE: Dinaciclib, a selective inhibitor of cyclin-dependent kinase (CDK) 1, CDK2, CDK5, and CDK9, is metabolized via CYP3A4. dinaciclib 9-19 cyclin dependent kinase 2 Homo sapiens 79-83