PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 31509830-5 2020 This effect was reduced by the use of a Cdk5 inhibitor (Roscovitine). Roscovitine 56-67 cyclin dependent kinase 5 Homo sapiens 40-44 32660255-4 2021 Inhibition of Cdk5 with roscovitine or dominant negative Cdk5 led to the attenuation of podocyte injury, by upregulating synaptopodin and nephrin. Roscovitine 24-35 cyclin dependent kinase 5 Homo sapiens 14-18 32692785-8 2020 Additionally, a cyclin-dependent kinase 5 inhibitor (Roscovitine) and a calcium chelator (EGTA) showed contrasting results between the two neuronal cultures. Roscovitine 53-64 cyclin dependent kinase 5 Homo sapiens 16-41 32666227-8 2020 Treatment with hypothermia, or a selective CDK4 inhibitor, or roscovitine (CDK5 inhibitor) prevented MPP+-induced mitochondrial fission, upregulation of mitochondrial fission protein dynamin-related protein 1 (Drp1), and neuron death. Roscovitine 62-73 cyclin dependent kinase 5 Homo sapiens 75-79 32883957-6 2020 Both the pharmacological inhibition of Cdk5 by roscovitine and the inhibition of Drp1 by mdivi-1 inhibited mitochondrial fission and the production of ROS associated with radiation-induced neuronal loss. Roscovitine 47-58 cyclin dependent kinase 5 Homo sapiens 39-43 32974274-3 2020 Since the successful discovery and development of Roscovitine, several ATP-competitive inhibitors of CDK5 and peptide inhibitors of CDK5/p25 interface have been developed. Roscovitine 50-61 cyclin dependent kinase 5 Homo sapiens 101-105 32974274-3 2020 Since the successful discovery and development of Roscovitine, several ATP-competitive inhibitors of CDK5 and peptide inhibitors of CDK5/p25 interface have been developed. Roscovitine 50-61 cyclin dependent kinase 5 Homo sapiens 132-136 32190166-7 2020 Moreover, our study revealed that the expression of VGLUT2 protein in the DRG and spinal cord was remarkably increased between days 1 and 3 following CFA injection and was significantly reduced by roscovitine, a selective antagonist of Cdk5. Roscovitine 197-208 cyclin dependent kinase 5 Homo sapiens 236-240 32190166-8 2020 Additionally, p25 but not p35, an activator of Cdk5, protein was significantly increased by CFA and reduced by roscovitine. Roscovitine 111-122 cyclin dependent kinase 5 Homo sapiens 47-51 31163256-11 2019 Inhibition of CDK5 with myricetin or roscovitine, a CDK5 inhibitor attenuates thapsigargin induced p66Shc serine 36 phosphorylation and also reduced mitochondrial dysfunction by decreasing mitochondrial ROS and caspase-3 activation. Roscovitine 37-48 cyclin dependent kinase 5 Homo sapiens 52-56 29944965-7 2019 Consequently, MK-2206 and roscovitine, which are selective AKT and CDK5 inhibitors, respectively, protected young and aging WM function only when applied before OGD. Roscovitine 26-37 cyclin dependent kinase 5 Homo sapiens 67-71 31395805-7 2019 The blocking of CDK5 activity by its small interfering RNAs (siRNA) or Roscovitine, a pan-CDK inhibitor, reduces the cellular AR protein level and triggers the death of prostate cancer cells. Roscovitine 71-82 cyclin dependent kinase 5 Homo sapiens 16-20 31354714-4 2019 In addition, the anti-cancer drug roscovitine, that is currently being tested in clinical trials, was recently described to regulate inflammatory processes by inhibiting different Cdks such as cyclin-dependent kinase 5 (Cdk5). Roscovitine 34-45 cyclin dependent kinase 5 Homo sapiens 180-184 31354714-4 2019 In addition, the anti-cancer drug roscovitine, that is currently being tested in clinical trials, was recently described to regulate inflammatory processes by inhibiting different Cdks such as cyclin-dependent kinase 5 (Cdk5). Roscovitine 34-45 cyclin dependent kinase 5 Homo sapiens 193-218 31354714-4 2019 In addition, the anti-cancer drug roscovitine, that is currently being tested in clinical trials, was recently described to regulate inflammatory processes by inhibiting different Cdks such as cyclin-dependent kinase 5 (Cdk5). Roscovitine 34-45 cyclin dependent kinase 5 Homo sapiens 220-224 31073393-5 2019 Structure-based pharmacophore investigated the essential complementary chemical features of ATP-binding site of Cdk5 in complex with roscovitine. Roscovitine 133-144 cyclin dependent kinase 5 Homo sapiens 112-116 30911317-8 2019 Analysis of the mechanism underlying these changes using Cdk5 inhibitor, roscovitine, indicated that expressions of Cdk5 and Sox6 corresponded to metformin treatment. Roscovitine 73-84 cyclin dependent kinase 5 Homo sapiens 116-120 29308980-5 2018 Additionally, the presence of active Cdk5 was associated with increased TRPA1 phosphorylation in transfected HEK293 cells that was roscovitine-sensitive and absent in the mouse mutant S449A full-length channel. Roscovitine 131-142 cyclin dependent kinase 5 Homo sapiens 37-41 30079618-7 2018 Roscovitine, an ATP-competitive CDK5 inhibitor, disrupted localization of the expressed MBP peptide. Roscovitine 0-11 cyclin dependent kinase 5 Homo sapiens 32-36 29314417-7 2018 Inhibition of Cdk5 using RNAi or a chemical inhibitor (roscovitine) induces mitochondrial elongation and promotes mitochondrial respiration, indicating that Cdk5-dependent Drp1 phosphorylation participates in mitochondrial metabolism and NSPC stemness regulation. Roscovitine 55-66 cyclin dependent kinase 5 Homo sapiens 14-18 29314417-7 2018 Inhibition of Cdk5 using RNAi or a chemical inhibitor (roscovitine) induces mitochondrial elongation and promotes mitochondrial respiration, indicating that Cdk5-dependent Drp1 phosphorylation participates in mitochondrial metabolism and NSPC stemness regulation. Roscovitine 55-66 cyclin dependent kinase 5 Homo sapiens 157-161 29996940-11 2018 Accordingly, 3D cultures of E-cadherin-expressing EOC cells are sensitive to the CDK5 inhibitor roscovitine combined with cisplatin. Roscovitine 96-107 cyclin dependent kinase 5 Homo sapiens 81-85 29227343-10 2018 Meanwhile, pharmacological inhibition of Cdk5 activity by 8 microM roscovitine alleviated isoflurane-induced Golgi fragmentation and neurotoxicity. Roscovitine 67-78 cyclin dependent kinase 5 Homo sapiens 41-45 29467671-8 2018 This effect was significantly blocked by VAS2870 (NADPH oxidase inhibitor) or by roscovitine (Cdk5 activity inhibitor). Roscovitine 81-92 cyclin dependent kinase 5 Homo sapiens 94-98 29111393-6 2018 This event was attenuated by negative regulation of endogenous Cdk5 activity by the pharmacological Cdk5 inhibitor, roscovitine, or by lentiviral knockdown of Cdk5. Roscovitine 116-127 cyclin dependent kinase 5 Homo sapiens 63-67 27053712-5 2016 Also, a knock down of Cdk5 in jck cells using small interfering RNA results in significant shortening of ciliary length, similar to what we observed with R-roscovitine. Roscovitine 154-167 cyclin dependent kinase 5 Homo sapiens 22-26 28842255-6 2017 Selective inhibition of CDK5 expression by roscovitine or siRNA significantly decreased VM formation in A549 cells both in vitro and in vivo and retarded tumor growth. Roscovitine 43-54 cyclin dependent kinase 5 Homo sapiens 24-28 30023695-0 2017 A Simple Isomerization of the Purine Scaffold of a Kinase Inhibitor, Roscovitine, Affords a Four- to Seven-Fold Enhancement of Its Affinity for Four CDKs. Roscovitine 69-80 cyclin dependent kinase 5 Homo sapiens 149-153 30023695-2 2017 Roscovitine is an antitumor purine inhibitor of cyclin-dependent kinase CDK5, for which it displays submicromolar affinity. Roscovitine 0-11 cyclin dependent kinase 5 Homo sapiens 72-76 27402274-7 2016 Importantly, inhibition of Cdk5 kinase activity by roscovitine protected neurons from death under hypoxic stress. Roscovitine 51-62 cyclin dependent kinase 5 Homo sapiens 27-31 27371933-0 2016 Binding mechanism of CDK5 with roscovitine derivatives based on molecular dynamics simulations and MM/PBSA methods. Roscovitine 31-42 cyclin dependent kinase 5 Homo sapiens 21-25 27371933-1 2016 Roscovitine derivatives are potent inhibitors of cyclin-dependent kinase 5 (CDK5), but they exhibit different activities, which has not been understood clearly up to now. Roscovitine 0-11 cyclin dependent kinase 5 Homo sapiens 49-74 27371933-1 2016 Roscovitine derivatives are potent inhibitors of cyclin-dependent kinase 5 (CDK5), but they exhibit different activities, which has not been understood clearly up to now. Roscovitine 0-11 cyclin dependent kinase 5 Homo sapiens 76-80 27371933-3 2016 In this context, the methods of molecular docking, molecular dynamics (MD) simulation, and binding free energy analysis are applied to investigate and reveal the detailed binding mechanism of four roscovitine derivatives with CDK5. Roscovitine 197-208 cyclin dependent kinase 5 Homo sapiens 226-230 26806339-10 2016 Inhibition of Cdk5 with Roscovitine reduced activation of NF-kappaB and expression of inflammation-related genes, demonstrating the critical role of Cdk5 in regulation of gene transcription during SIR. Roscovitine 24-35 cyclin dependent kinase 5 Homo sapiens 149-153 26966064-5 2016 Interestingly, pretreatment with roscovitine, an inhibitor of Cdk5, or transfection with small interfering (si) RNAs specific to Cdk5 and p35 significantly attenuated the TGF-beta1-induced p27KIP1 expression and cell cycle arrest. Roscovitine 33-44 cyclin dependent kinase 5 Homo sapiens 62-66 26806339-10 2016 Inhibition of Cdk5 with Roscovitine reduced activation of NF-kappaB and expression of inflammation-related genes, demonstrating the critical role of Cdk5 in regulation of gene transcription during SIR. Roscovitine 24-35 cyclin dependent kinase 5 Homo sapiens 14-18 26018459-5 2015 Inhibition of CDK5 by roscovitine and small interfering (si)RNA was used to investigate the mechanism of CDK5 in the process of A549 lung cancer cell proliferation, migration and invasion. Roscovitine 22-33 cyclin dependent kinase 5 Homo sapiens 14-18 26160434-7 2015 In C6 cells and primary astrocytes, CDK5 RNAi prevented the cell death generated by glutamate-induced gliotoxicity, and this finding was corroborated by pharmacological inhibition with roscovitine. Roscovitine 185-196 cyclin dependent kinase 5 Homo sapiens 36-40 26018459-6 2015 The results demonstrated that functional inhibition of CDK5 using roscovitine and siRNA markedly suppressed the proliferation of A549 cells and resulted in a reduced tumor mass in vivo. Roscovitine 66-77 cyclin dependent kinase 5 Homo sapiens 55-59 25829494-4 2015 Inhibition of CDK5 activity with roscovitine-sensitized cells to heat induced apoptosis indicating a protective role for CDK5 in inhibiting heat-induced apoptosis. Roscovitine 33-44 cyclin dependent kinase 5 Homo sapiens 14-18 26002103-7 2015 In addition, pharmacological inhibition of CDK5 by Roscovitine inhibits DRP1 phosphorylation and mitochondrial fission associated with NMDA-induced neuronal loss. Roscovitine 51-62 cyclin dependent kinase 5 Homo sapiens 43-47 25829494-4 2015 Inhibition of CDK5 activity with roscovitine-sensitized cells to heat induced apoptosis indicating a protective role for CDK5 in inhibiting heat-induced apoptosis. Roscovitine 33-44 cyclin dependent kinase 5 Homo sapiens 121-125 25117211-4 2014 Inhibitors of CDK5, such as roscovitine, have neuroprotective effects; however, CNS penetration is low. Roscovitine 28-39 cyclin dependent kinase 5 Homo sapiens 14-18 25346443-9 2015 Cdk5 inhibitors (roscovitine, AT7519) reduced EPX release when cells were stimulated by PMA or secretory IgA. Roscovitine 17-28 cyclin dependent kinase 5 Homo sapiens 0-4 24058495-8 2013 To understand the molecular basis of higher potency and selectivity of these inhibitors, here, we present molecular dynamics simulation results of CDK5/p25 and CDK2/CyclinE complexed with a series of cyclobutyl-substituted imidazole inhibitors and roscovitine. Roscovitine 248-259 cyclin dependent kinase 5 Homo sapiens 147-151 24498195-9 2014 Cdk5 inhibitor roscovitine intrathecal administration also suppressed CFA-induced heat hyperalgesia and Cdk5 phosphorylation, but did not attenuate ERK activation. Roscovitine 15-26 cyclin dependent kinase 5 Homo sapiens 0-4 24498195-9 2014 Cdk5 inhibitor roscovitine intrathecal administration also suppressed CFA-induced heat hyperalgesia and Cdk5 phosphorylation, but did not attenuate ERK activation. Roscovitine 15-26 cyclin dependent kinase 5 Homo sapiens 104-108 24091658-7 2013 The lack of the phosphorylation on Ser732 as well as the inhibition of CDK5 activity by roscovitine impaired mitotic spindle assembly and correct chromosome alignment during mitosis. Roscovitine 88-99 cyclin dependent kinase 5 Homo sapiens 71-75 24098701-3 2013 Cdk5 inhibition (roscovitine) resulted in actin-cytoskeleton disorganisation, prevention of protein co-localization and inhibition of movement. Roscovitine 17-28 cyclin dependent kinase 5 Homo sapiens 0-4 22696682-6 2012 When the kinase activity was inhibited by the Cdk5 inhibitor roscovitine or dominant-negative (dn) Cdk5, the migration of lung cancer cells was reduced. Roscovitine 61-72 cyclin dependent kinase 5 Homo sapiens 46-50 22820052-9 2012 We also found that apomorphine-induced locomotor activity was further increased following intra-accumbens infusions of roscovitine, a cdk-5 blocker, in a dose-dependent manner. Roscovitine 119-130 cyclin dependent kinase 5 Homo sapiens 134-139 23042366-5 2013 Moreover, Roscovitine, an inhibitor of Cdks, blunted overexpression of Cdk2 and Cdk5 and Cdk2 activity induced by the YY1-dependent signal secreted by SaOS cells. Roscovitine 10-21 cyclin dependent kinase 5 Homo sapiens 80-84 23185265-2 2012 Roscovitine is an inhibitor of cyclin-dependent kinases that promote cell cycling (CDK1, 2), neuronal development (CDK5) and control transcription (CDK7,9). Roscovitine 0-11 cyclin dependent kinase 5 Homo sapiens 115-119 21465480-8 2012 Decreased GTP-induced vimentin Ser56 phosphorylation and secretion resulted from inhibition of Cdk5 activity by roscovitine or olomoucine or by depletion of Cdk5 by siRNA, suggesting that GTP-induced Cdk5-mediated vimentin Ser56 phosphorylation may be related to GTP-induced Cdk5-mediated secretion by neutrophils. Roscovitine 112-123 cyclin dependent kinase 5 Homo sapiens 95-99 22496693-5 2012 Moreover, we report that roscovitine, a potent inhibitor of cyclin-dependent kinases, including Cdk5, decreases p27(Kip) protein levels and restores actin stress fibers formation in CKIgamma2 overexpressing cells, suggesting the existence of a CKIgamma2-Cdk5-p27(Kip)-RhoA pathway in regulating actin remodeling. Roscovitine 25-36 cyclin dependent kinase 5 Homo sapiens 96-100 22496693-5 2012 Moreover, we report that roscovitine, a potent inhibitor of cyclin-dependent kinases, including Cdk5, decreases p27(Kip) protein levels and restores actin stress fibers formation in CKIgamma2 overexpressing cells, suggesting the existence of a CKIgamma2-Cdk5-p27(Kip)-RhoA pathway in regulating actin remodeling. Roscovitine 25-36 cyclin dependent kinase 5 Homo sapiens 254-258 22276149-4 2012 Recently, the broad range cyclin-dependent kinase (CDK) inhibitor R-roscovitine was shown to increase neutrophil apoptosis, implicating CDKs in the regulation of neutrophil lifespan. Roscovitine 66-79 cyclin dependent kinase 5 Homo sapiens 136-140 21825040-6 2011 Inhibition of CDK5 kinase activity using a CDK5 dominant-negative mutant or the drug roscovitine significantly decreased the migration and invasion of pancreatic cancer cells in vitro. Roscovitine 85-96 cyclin dependent kinase 5 Homo sapiens 14-18 21641213-3 2011 These results are substantiated using computer docking methods (DarwinDock/GenDock), which predict that Roscovitine and the triazole 7 bind to the ATP-binding site of CDK5/p25 with comparable binding energies, whereas the corresponding pentafluorophenylmethyl-triazole, 9, has dramatically reduced binding energy (in accordance with its lack of neuroprotection). Roscovitine 104-115 cyclin dependent kinase 5 Homo sapiens 167-171 21391976-0 2011 Roscovitine blocks leukocyte extravasation by inhibition of cyclin-dependent kinases 5 and 9. Roscovitine 0-11 cyclin dependent kinase 5 Homo sapiens 60-92 21391976-11 2011 Experiments using kinase inhibitors and siRNA showed that the decreased endothelial activation was due solely to blockade of CDK5 and CDK9 by roscovitine. Roscovitine 142-153 cyclin dependent kinase 5 Homo sapiens 125-129 21391976-12 2011 CONCLUSIONS AND IMPLICATIONS: Our study highlights a novel mode of action for roscovitine, preventing endothelial activation and leukocyte-endothelial cell interaction by inhibition of CDK5 and 9. Roscovitine 78-89 cyclin dependent kinase 5 Homo sapiens 185-189 21671254-12 2011 On the other hand, the CDK5 involvement in tau phosphorylation was confirmed by both the increase in its enzymatic activity and the absence of MT-2 neurite retraction in the presence of roscovitine or CDK5 siRNA transfection. Roscovitine 186-197 cyclin dependent kinase 5 Homo sapiens 23-27 20977891-6 2011 Importantly, we demonstrate that Cdk5-mediated signaling is involved in Hif-1alpha stabilisation since inhibition of Cdk5 by roscovitine abrogates Hif-1alpha accumulation and induces cell death. Roscovitine 125-136 cyclin dependent kinase 5 Homo sapiens 33-37 21435449-0 2011 Increased CDK5 expression in HIV encephalitis contributes to neurodegeneration via tau phosphorylation and is reversed with Roscovitine. Roscovitine 124-135 cyclin dependent kinase 5 Homo sapiens 10-14 20977891-6 2011 Importantly, we demonstrate that Cdk5-mediated signaling is involved in Hif-1alpha stabilisation since inhibition of Cdk5 by roscovitine abrogates Hif-1alpha accumulation and induces cell death. Roscovitine 125-136 cyclin dependent kinase 5 Homo sapiens 117-121 21209116-5 2011 This screening identified roscovitine, a selective inhibitor of cyclin-dependent kinase 1 (CDK1), CDK2, CDK5, and CDK7. Roscovitine 26-37 cyclin dependent kinase 5 Homo sapiens 104-108 21144757-6 2011 Beginning with the structure of Roscovitine, a moderately selective CDK5 inhibitor, we sought to conduct structural modifications to increase inhibitory potency of CDK5 and increase selectivity over a similar enzyme, cyclin dependent kinase 2 (CDK2). Roscovitine 32-43 cyclin dependent kinase 5 Homo sapiens 68-72 21144757-6 2011 Beginning with the structure of Roscovitine, a moderately selective CDK5 inhibitor, we sought to conduct structural modifications to increase inhibitory potency of CDK5 and increase selectivity over a similar enzyme, cyclin dependent kinase 2 (CDK2). Roscovitine 32-43 cyclin dependent kinase 5 Homo sapiens 164-168 20711428-10 2010 Our results show therefore that roscovitine protects in vivo neurons possibly through CDK5 dependent mechanisms. Roscovitine 32-43 cyclin dependent kinase 5 Homo sapiens 86-90 21677377-4 2011 In addition, in cells expressing 3PO-tau, both the percentage of cells with aggregates, as well as the size of aggregates, was increased following overexpression of cdk5 or GSK3beta, decreased following treatment with pharmacological agents (roscovitine and lithium) active against these kinases, and increased following treatment with the phosphatase inhibitor okadaic acid. Roscovitine 242-253 cyclin dependent kinase 5 Homo sapiens 165-169 21912693-7 2011 Tat rapidly inhibited Cdk5 kinase activity and mRNA production, and roscovitine, a well-known Cdk5 inhibitor, induced a very similar pattern of DRG hyperexcitability. Roscovitine 68-79 cyclin dependent kinase 5 Homo sapiens 94-98 20839922-2 2010 One roscovitine-sensitive cdk that functions in neurons is cdk5, which is activated in part by its binding partner, p35. Roscovitine 4-15 cyclin dependent kinase 5 Homo sapiens 59-63 19156541-8 2009 When Cdk5 activity was inhibited, either by roscovitine or overexpression of dominant negative Cdk5, there was a reduction of pSTAT3 activation. Roscovitine 44-55 cyclin dependent kinase 5 Homo sapiens 5-9 27713242-6 2010 On the contrary, inhibition of JNK and Cdk5 with D-JNKI1 and Roscovitine respectively did not prevent NMDA-induced P-APP increase. Roscovitine 61-72 cyclin dependent kinase 5 Homo sapiens 39-43 19628755-9 2009 To explore the involvement of Cdk5 in roscovitine-induced down-regulation of DAT activity, Cdk5 protein was knocked down via Cdk5-small interfering RNA by as much as 86% in porcine aortic endothelial cells stably expressing human (h)DATs. Roscovitine 38-49 cyclin dependent kinase 5 Homo sapiens 91-95 19628755-9 2009 To explore the involvement of Cdk5 in roscovitine-induced down-regulation of DAT activity, Cdk5 protein was knocked down via Cdk5-small interfering RNA by as much as 86% in porcine aortic endothelial cells stably expressing human (h)DATs. Roscovitine 38-49 cyclin dependent kinase 5 Homo sapiens 91-95 20022952-6 2010 Roscovitine and PP2, inhibitors for Cdk5 and Src family kinases, respectively, suppressed the locomotion mode of migration. Roscovitine 0-11 cyclin dependent kinase 5 Homo sapiens 36-40 18829967-7 2008 Moreover, supporting a detrimental role of Cdk5 in striatal cell death, neuronal loss can be widely prevented by roscovitine, a potent Cdk5 inhibitor. Roscovitine 113-124 cyclin dependent kinase 5 Homo sapiens 43-47 19534817-6 2009 Phosphorylation of NMHC-B was evident only in cells that were double transfected with Cdk5/p25 and was dose-dependently inhibited by Roscovitine and other Cdk5 inhibitors. Roscovitine 133-144 cyclin dependent kinase 5 Homo sapiens 86-90 19255425-4 2009 Phosphorylated E-Syt1 associates with GLUT4, an event inhibited by the Cdks inhibitor roscovitine. Roscovitine 86-97 cyclin dependent kinase 5 Homo sapiens 71-75 19326393-0 2009 The Cdk5 inhibitor roscovitine strongly inhibits glucose uptake in 3T3-L1 adipocytes without altering GLUT4 translocation from internal pools to the cell surface. Roscovitine 19-30 cyclin dependent kinase 5 Homo sapiens 4-8 19326393-2 2009 Treatment of 3T3-L1 adipocytes with the Cdk5 inhibitor roscovitine strongly inhibits insulin-stimulated/GLUT4-mediated glucose transport. Roscovitine 55-66 cyclin dependent kinase 5 Homo sapiens 40-44 19071093-10 2009 Conversely, inhibition of cyclin-dependent kinase-5 (CDK5) by roscovitine decreased phosphorylated tau but failed to alter tau protein levels. Roscovitine 62-73 cyclin dependent kinase 5 Homo sapiens 26-51 19071093-10 2009 Conversely, inhibition of cyclin-dependent kinase-5 (CDK5) by roscovitine decreased phosphorylated tau but failed to alter tau protein levels. Roscovitine 62-73 cyclin dependent kinase 5 Homo sapiens 53-57 19158430-8 2009 To determine the role of cdk5 in tau phosphorylation at Ser396/404 in lipid rafts, we pre-incubated cells with cdk5 inhibitor roscovitine, and observed that the Abeta-induced tau phosphorylation at Ser 396/404 in rafts was abolished as well as cdk5/p35 association with rafts. Roscovitine 126-137 cyclin dependent kinase 5 Homo sapiens 111-115 19158430-8 2009 To determine the role of cdk5 in tau phosphorylation at Ser396/404 in lipid rafts, we pre-incubated cells with cdk5 inhibitor roscovitine, and observed that the Abeta-induced tau phosphorylation at Ser 396/404 in rafts was abolished as well as cdk5/p35 association with rafts. Roscovitine 126-137 cyclin dependent kinase 5 Homo sapiens 111-115 18722528-6 2008 Roscovitine, a cdk5 inhibitor, protected neurons from ammonia-induced cell death. Roscovitine 0-11 cyclin dependent kinase 5 Homo sapiens 15-19 18722528-7 2008 However, roscovitine also impaired axonal growth, probably through inhibition of the remaining cdk5/p35 activity, which is involved in neurite outgrowth. Roscovitine 9-20 cyclin dependent kinase 5 Homo sapiens 95-99 18829967-7 2008 Moreover, supporting a detrimental role of Cdk5 in striatal cell death, neuronal loss can be widely prevented by roscovitine, a potent Cdk5 inhibitor. Roscovitine 113-124 cyclin dependent kinase 5 Homo sapiens 135-139 18512759-8 2008 This effect of NAC was blocked by the Cdk5 inhibitors roscovitine and butyrolactone. Roscovitine 54-65 cyclin dependent kinase 5 Homo sapiens 38-42 18042622-3 2007 Here, we show that cyclin-dependent kinase (Cdk) 5 is activated following the induction of differentiation, and that the Cdk5 inhibitor roscovitine inhibits OL differentiation. Roscovitine 136-147 cyclin dependent kinase 5 Homo sapiens 121-125 18701695-5 2008 PDGF stimulates Cdk5 activity in a time-dependent manner, whereas suppression of Cdk5 by the specific inhibitor roscovitine or by the retrovirus encoding short-hairpin RNA for Cdk5 impairs PDGF-dependent OPC migration. Roscovitine 112-123 cyclin dependent kinase 5 Homo sapiens 81-85 18701695-5 2008 PDGF stimulates Cdk5 activity in a time-dependent manner, whereas suppression of Cdk5 by the specific inhibitor roscovitine or by the retrovirus encoding short-hairpin RNA for Cdk5 impairs PDGF-dependent OPC migration. Roscovitine 112-123 cyclin dependent kinase 5 Homo sapiens 81-85 17713901-2 2007 In the present paper, eight Molecular Dynamics (MD) simulations are carried out to examine the importance of structure and dynamics of water in the active site of both CDK2 and CDK5 complexes with roscovitine and indirubin analogues. Roscovitine 197-208 cyclin dependent kinase 5 Homo sapiens 177-181 17713901-5 2007 Different binding patterns of roscovitine in CDK2 and CDK5 are detected during the simulations because of the different binding conformations of the group on the C2 side chain, which might offer a clue toward finding highly selective inhibitors with regards to CDK2 and CDK5. Roscovitine 30-41 cyclin dependent kinase 5 Homo sapiens 54-58 17713901-5 2007 Different binding patterns of roscovitine in CDK2 and CDK5 are detected during the simulations because of the different binding conformations of the group on the C2 side chain, which might offer a clue toward finding highly selective inhibitors with regards to CDK2 and CDK5. Roscovitine 30-41 cyclin dependent kinase 5 Homo sapiens 270-274 16887799-7 2006 To test this hypothesis, the pancreatic cell line INS-1 was selected as a known in vitro model of glucotoxicity, and roscovitine (10 mum) was used as a CDK5 inhibitor. Roscovitine 117-128 cyclin dependent kinase 5 Homo sapiens 152-156 17295212-9 2007 Pretreatment of the scratched astrocytes with a Cdk5 inhibitor, roscovitine, could delay wound healing by inhibiting the reorganization of tubulin, GFAP, and the extension of hypertrophic processes. Roscovitine 64-75 cyclin dependent kinase 5 Homo sapiens 48-52 17113760-8 2007 As a potential underlying mechanism, we were able to determine that transient ischemia induced tau hyperphosphorylation and NFT-like conformations are associated with aberrant activation of cyclin dependent kinase 5 (Cdk5) and can be rescued by delivery of a potent, but non-specific cyclin dependent kinase inhibitor, roscovitine to the brain. Roscovitine 319-330 cyclin dependent kinase 5 Homo sapiens 190-215 17113760-8 2007 As a potential underlying mechanism, we were able to determine that transient ischemia induced tau hyperphosphorylation and NFT-like conformations are associated with aberrant activation of cyclin dependent kinase 5 (Cdk5) and can be rescued by delivery of a potent, but non-specific cyclin dependent kinase inhibitor, roscovitine to the brain. Roscovitine 319-330 cyclin dependent kinase 5 Homo sapiens 217-221 17125805-9 2007 Biochemical and cellular effects of roscovitine, a potent and selective inhibitor of the cyclin-dependent kinases cdc2, cdk2 and cdk5. Roscovitine 36-47 cyclin dependent kinase 5 Homo sapiens 129-133 17081516-0 2007 Roscovitine regulates invasive breast cancer cell (MDA-MB231) proliferation and survival through cell cycle regulatory protein cdk5. Roscovitine 0-11 cyclin dependent kinase 5 Homo sapiens 127-131 17081516-4 2007 In the present study, cyclic-dependent kinase 5 (cdk5) proved to be a molecular target for roscovitine-triggered apoptosis for highly invasive breast cancer cell death. Roscovitine 91-102 cyclin dependent kinase 5 Homo sapiens 22-47 17081516-4 2007 In the present study, cyclic-dependent kinase 5 (cdk5) proved to be a molecular target for roscovitine-triggered apoptosis for highly invasive breast cancer cell death. Roscovitine 91-102 cyclin dependent kinase 5 Homo sapiens 49-53 17081516-12 2007 Roscovitine specifically inhibits cdk5 expression/activity in a dose-dependent manner with concomitant inhibition of MDA-MB231 cell proliferation and induction of apoptosis. Roscovitine 0-11 cyclin dependent kinase 5 Homo sapiens 34-38 17081516-13 2007 By contrast, the roscovitine analog olomoucine, a specific inhibitor of cdk4, failed to affect MDA-MB231 cell proliferation and apoptosis which implies the specific involvement of cdk5 in roscovitine-triggered cell death/proliferation. Roscovitine 188-199 cyclin dependent kinase 5 Homo sapiens 180-184 17081516-16 2007 These results suggest that Cdk5 is a novel player in roscovitine-triggered breast cancer cell apoptosis and inhibition of proliferation, therefore, may be a potential therapeutic target. Roscovitine 53-64 cyclin dependent kinase 5 Homo sapiens 27-31 16770643-1 2007 Molecular dynamics simulations were performed to elucidate the interactions of CDK2 and CDK5 complexes with three inhibitors: R-roscovitine, S-roscovitine, and indirubin-3"-oxime. Roscovitine 126-139 cyclin dependent kinase 5 Homo sapiens 88-92 16770643-1 2007 Molecular dynamics simulations were performed to elucidate the interactions of CDK2 and CDK5 complexes with three inhibitors: R-roscovitine, S-roscovitine, and indirubin-3"-oxime. Roscovitine 141-154 cyclin dependent kinase 5 Homo sapiens 88-92 16770643-4 2007 The simulations also showed two amino acid mutations in the active site of CDK5/R-roscovitine that favor binding-enhanced electrostatic contributions, making the inhibitor more effective for CDK5 than for CDK2. Roscovitine 82-93 cyclin dependent kinase 5 Homo sapiens 75-79 16770643-4 2007 The simulations also showed two amino acid mutations in the active site of CDK5/R-roscovitine that favor binding-enhanced electrostatic contributions, making the inhibitor more effective for CDK5 than for CDK2. Roscovitine 82-93 cyclin dependent kinase 5 Homo sapiens 191-195 16879821-5 2006 Blocking CDK5 activity by pharmacologic inhibitor, roscovitine or overexpression of dominant negative CDK5 augmented activation of cell death markers and diminished mu-opioid receptor agonist protection. Roscovitine 51-62 cyclin dependent kinase 5 Homo sapiens 9-13 17160145-10 2006 Drugs like roscovitine, flavopiridol, calpain inhibitors, kenpaullone and induribins, which inhibit cdk5/p25 formation, constitute potential drugs for the treatment of neurological disorders. Roscovitine 11-22 cyclin dependent kinase 5 Homo sapiens 100-104 16802322-6 2006 To simulate the downregulation of postsynaptic Cdk5 in invitro experiments, we used the Cdk5 inhibitor roscovitine. Roscovitine 103-114 cyclin dependent kinase 5 Homo sapiens 47-51 16802322-6 2006 To simulate the downregulation of postsynaptic Cdk5 in invitro experiments, we used the Cdk5 inhibitor roscovitine. Roscovitine 103-114 cyclin dependent kinase 5 Homo sapiens 88-92 16802322-7 2006 The inhibition of Cdk5 activity by roscovitine enhanced CaMKII autophosphorylation and activation in cultured neurons, and in an isolated postsynaptic-density-enriched fraction. Roscovitine 35-46 cyclin dependent kinase 5 Homo sapiens 18-22 15741232-7 2005 Indeed, this phosphorylation was observed 6 hours after p25 induction and was abolished in the presence of a Cdk5 inhibitor, roscovitine, which does not inhibit the usual Rb cyclin-D kinases Cdk4 and Cdk6. Roscovitine 125-136 cyclin dependent kinase 5 Homo sapiens 109-113 16678793-8 2006 However, application of the Cdk5 inhibitor Roscovitine did not result in inhibition of tau phosphorylation possibly due to activation of extracellular regulated kinase 1/2 (Erk1/2), which also is capable of phosphorylating tau. Roscovitine 43-54 cyclin dependent kinase 5 Homo sapiens 28-32 17054019-4 2006 In this paper, we present simulation results of CDK2 and CDK5 with roscovitine using models with and without their activators (cyclinA and p25). Roscovitine 67-78 cyclin dependent kinase 5 Homo sapiens 57-61 17054019-7 2006 Comparisons between P/CDK2/cyclinA/roscovitine and CDK5/p25/roscovitine complexes reveal differences in the conformations of the glutamine around the active sites, which may be exploited to find highly selective inhibitors with respect to CDK2 and CDK5. Roscovitine 35-46 cyclin dependent kinase 5 Homo sapiens 248-252 17054019-7 2006 Comparisons between P/CDK2/cyclinA/roscovitine and CDK5/p25/roscovitine complexes reveal differences in the conformations of the glutamine around the active sites, which may be exploited to find highly selective inhibitors with respect to CDK2 and CDK5. Roscovitine 60-71 cyclin dependent kinase 5 Homo sapiens 51-55 17054019-7 2006 Comparisons between P/CDK2/cyclinA/roscovitine and CDK5/p25/roscovitine complexes reveal differences in the conformations of the glutamine around the active sites, which may be exploited to find highly selective inhibitors with respect to CDK2 and CDK5. Roscovitine 60-71 cyclin dependent kinase 5 Homo sapiens 248-252 16885348-3 2006 Blocking of CDK5 activity with a dominant-negative CDK5 construct, small interfering RNA, or roscovitine resulted in changes in the microtubule cytoskeleton, loss of cellular polarity, and loss of motility. Roscovitine 93-104 cyclin dependent kinase 5 Homo sapiens 12-16 16407256-1 2006 A detailed analysis is presented of the dynamics of human CDK5 in complexes with the protein activator p25 and the purine-like inhibitor roscovitine. Roscovitine 137-148 cyclin dependent kinase 5 Homo sapiens 58-62 16029324-8 2005 Roscovitine, an inhibitor of CDK5, enhanced Ca2+-dependent (cadherin-dependent) aggregation of HaCaT cells whereas it inhibited adhesion of HaCaT cells to fibronectin associated with reduced active states of beta1 integrin. Roscovitine 0-11 cyclin dependent kinase 5 Homo sapiens 29-33 15485494-4 2004 Inhibition of Cdk5 activity either by an inhibitor, roscovitine, or by transfection with a dominant negative form of Cdk5 caused a dramatic decrease in RA-induced differentiation, suggesting the requirement of Cdk5 kinase activity for the RA-induced neurite outgrowth. Roscovitine 52-63 cyclin dependent kinase 5 Homo sapiens 14-18 15689152-5 2005 The crystals were used to solve the structure of CDK5/p25 with (R)-roscovitine and aloisine at a resolution of 2.2 and 2.3 A, respectively. Roscovitine 63-78 cyclin dependent kinase 5 Homo sapiens 49-53 15689152-6 2005 The structure of CDK5/p25/roscovitine provides a rationale for the preference of CDK5 for the R over the S stereoisomer. Roscovitine 26-37 cyclin dependent kinase 5 Homo sapiens 17-21 15689152-6 2005 The structure of CDK5/p25/roscovitine provides a rationale for the preference of CDK5 for the R over the S stereoisomer. Roscovitine 26-37 cyclin dependent kinase 5 Homo sapiens 81-85 15331630-1 2004 Hormone secretion by pituitary cells is decreased by roscovitine, an inhibitor of cyclin-dependent kinase 5 (Cdk5). Roscovitine 53-64 cyclin dependent kinase 5 Homo sapiens 82-107 15331630-1 2004 Hormone secretion by pituitary cells is decreased by roscovitine, an inhibitor of cyclin-dependent kinase 5 (Cdk5). Roscovitine 53-64 cyclin dependent kinase 5 Homo sapiens 109-113 15331630-4 2004 Roscovitine inhibits the ability of Trio to activate Rac, and peptides corresponding to the Cdk5 consensus sites in Trio are phosphorylated by Cdk5. Roscovitine 0-11 cyclin dependent kinase 5 Homo sapiens 92-96 15331630-4 2004 Roscovitine inhibits the ability of Trio to activate Rac, and peptides corresponding to the Cdk5 consensus sites in Trio are phosphorylated by Cdk5. Roscovitine 0-11 cyclin dependent kinase 5 Homo sapiens 143-147 14990704-2 2004 Roscovitine (Rosco) is a purine derivative that inhibits cyclin-dependent kinase 1 (cdk1), cdk2, cdk5, cdk7, and cdk9, which are key regulators of the cell cycle and transcription. Roscovitine 0-5 cyclin dependent kinase 5 Homo sapiens 97-101 15308730-4 2004 In contrast, roscovitine and other purine PCIs inhibit with high potency only CDK1, CDK2, CDK5, and CDK7, and they specifically inhibit the expression of viral but not cellular genes. Roscovitine 13-24 cyclin dependent kinase 5 Homo sapiens 90-94 15160391-6 2004 These effects were prevented by treatment with the cdk5 inhibitor roscovitine or transfection with a construct expressing the endogenous cdk5 inhibitor peptide. Roscovitine 66-77 cyclin dependent kinase 5 Homo sapiens 51-55 15160391-6 2004 These effects were prevented by treatment with the cdk5 inhibitor roscovitine or transfection with a construct expressing the endogenous cdk5 inhibitor peptide. Roscovitine 66-77 cyclin dependent kinase 5 Homo sapiens 137-141 14990704-2 2004 Roscovitine (Rosco) is a purine derivative that inhibits cyclin-dependent kinase 1 (cdk1), cdk2, cdk5, cdk7, and cdk9, which are key regulators of the cell cycle and transcription. Roscovitine 0-11 cyclin dependent kinase 5 Homo sapiens 97-101 14602088-3 2004 Roscovitine (10 microM), an antitumoral drug that inhibits cyclin-dependent kinase 1 (cdk1), cdk2 and cdk5, showed a significant neuroprotective effect on CGNs deprived of S/K. Roscovitine 0-11 cyclin dependent kinase 5 Homo sapiens 102-106 15123618-6 2004 Butyrolactone-I and roscovitine, two Cdk5 kinase inhibitors, were also found to prevent digoxin-triggered LNCaP cell death. Roscovitine 20-31 cyclin dependent kinase 5 Homo sapiens 37-41 14976144-10 2004 Functional studies show that p35 stimulates the activity of the insulin promoter and that the stimulation requires CDK5 because stimulation is blocked by roscovitine, an inhibitor of CDK5 activity, a dominant negative form of CDK5, and small interfering RNAs against p35. Roscovitine 154-165 cyclin dependent kinase 5 Homo sapiens 115-119 14976144-10 2004 Functional studies show that p35 stimulates the activity of the insulin promoter and that the stimulation requires CDK5 because stimulation is blocked by roscovitine, an inhibitor of CDK5 activity, a dominant negative form of CDK5, and small interfering RNAs against p35. Roscovitine 154-165 cyclin dependent kinase 5 Homo sapiens 183-187 14976144-10 2004 Functional studies show that p35 stimulates the activity of the insulin promoter and that the stimulation requires CDK5 because stimulation is blocked by roscovitine, an inhibitor of CDK5 activity, a dominant negative form of CDK5, and small interfering RNAs against p35. Roscovitine 154-165 cyclin dependent kinase 5 Homo sapiens 183-187 15033170-6 2004 Administration of Cdk5 inhibitors, roscovitine and olomoucine, into the crushed nerves resulted in decreases in Cdk5 kinase activity in nerves and retardation of nerve fiber regrowth. Roscovitine 35-46 cyclin dependent kinase 5 Homo sapiens 18-22 15033170-6 2004 Administration of Cdk5 inhibitors, roscovitine and olomoucine, into the crushed nerves resulted in decreases in Cdk5 kinase activity in nerves and retardation of nerve fiber regrowth. Roscovitine 35-46 cyclin dependent kinase 5 Homo sapiens 112-116 12743103-4 2003 Similarly, application of roscovitine, an inhibitor of the NFH side arm kinase Cdk5/p35, accelerates neurofilament transport. Roscovitine 26-37 cyclin dependent kinase 5 Homo sapiens 79-83 12941380-7 2003 Accordingly, a cdk5 inhibitor such as roscovitine, but not a cdk4 inhibitor such as 3-ATA, was also able to protect neurons from apoptosis as well as prevent accumulation of cdk5 and Par-4 in response to colchicine. Roscovitine 38-49 cyclin dependent kinase 5 Homo sapiens 15-19 12941380-7 2003 Accordingly, a cdk5 inhibitor such as roscovitine, but not a cdk4 inhibitor such as 3-ATA, was also able to protect neurons from apoptosis as well as prevent accumulation of cdk5 and Par-4 in response to colchicine. Roscovitine 38-49 cyclin dependent kinase 5 Homo sapiens 174-178 14704484-10 2003 The aim of this study was to compare the anti-proliferative effect of roscovitine (ROSC), a potent CDKs inhibitor, with that of cisplatin (CP) on human breast cancer MCF-7 cells. Roscovitine 70-81 cyclin dependent kinase 5 Homo sapiens 99-103 11443123-7 2001 Inhibition of Cdk5 with roscovitine reduced insulin secretion with approximately 35% compared with control after glucose stimulation and with approximately 65% after depolarization with glucose and KCl. Roscovitine 24-35 cyclin dependent kinase 5 Homo sapiens 14-18 12740122-5 2003 Decreasing Cdk5 kinase activity with the inhibitor roscovitine increased the amount of beta-catenin that was co-immunoprecipitated with cadherin. Roscovitine 51-62 cyclin dependent kinase 5 Homo sapiens 11-15 12372407-0 2002 Molecular model of cyclin-dependent kinase 5 complexed with roscovitine. Roscovitine 60-71 cyclin dependent kinase 5 Homo sapiens 19-44 12372407-1 2002 Here is described a structural model for the binary complex CDK5-roscovitine. Roscovitine 65-76 cyclin dependent kinase 5 Homo sapiens 60-64 12372407-2 2002 Roscovitine has been shown to potently inhibit cyclin-dependent kinases 1, 2 and 5 (CDK1, 2, and 5), and the structure of CDK2 complexed with roscovitine has been reported; however, no structural data are available for complexes of CDK5 with inhibitors. Roscovitine 0-11 cyclin dependent kinase 5 Homo sapiens 232-236 12372407-3 2002 The structural model indicates that roscovitine strongly binds to the ATP-binding pocket of CDK5 and structural comparison of the CDK2-roscovitine complex correlates the structural differences with differences in inhibition of these CDKs by this inhibitor. Roscovitine 36-47 cyclin dependent kinase 5 Homo sapiens 92-96 12372407-3 2002 The structural model indicates that roscovitine strongly binds to the ATP-binding pocket of CDK5 and structural comparison of the CDK2-roscovitine complex correlates the structural differences with differences in inhibition of these CDKs by this inhibitor. Roscovitine 135-146 cyclin dependent kinase 5 Homo sapiens 92-96 11168528-10 2001 Inhibition of p35/cdk5 with roscovitine did not alter the steady state levels of either beta-catenin or presenilin-1 but reduced the amount of presenilin-1 bound to beta-catenin. Roscovitine 28-39 cyclin dependent kinase 5 Homo sapiens 18-22 11483735-6 2001 (iii) The processing of ICP0 forms E and F was blocked in HEL fibroblasts infected with R325 or with wild-type virus and treated with roscovitine, a specific inhibitor of cell cycle-dependent kinases cdc2, cdk2, and cdk5. Roscovitine 134-145 cyclin dependent kinase 5 Homo sapiens 216-220 9727024-9 1998 Inhibition of Cdk5 activity by a specific Cdk inhibitor, roscovitine, or by overexpression of a dominant negative mutant of Cdk5 increases the stability of p35 by 2- to 3-fold. Roscovitine 57-68 cyclin dependent kinase 5 Homo sapiens 14-18 9030781-0 1997 Biochemical and cellular effects of roscovitine, a potent and selective inhibitor of the cyclin-dependent kinases cdc2, cdk2 and cdk5. Roscovitine 36-47 cyclin dependent kinase 5 Homo sapiens 129-133 9030781-16 1997 Through its unique selectivity for some cyclin-dependent kinases, roscovitine provides a useful antimitotic reagent for cell cycle studies and may prove interesting to control cells with deregulated cdc2, cdk2 or cdk5 kinase activities. Roscovitine 66-77 cyclin dependent kinase 5 Homo sapiens 213-217 35570516-11 2022 Docking studies of all the synthesized compounds were carried out using "structural mechanism for the inhibition of CDK5-p25 by roscovitine, aloisine and indirubin" (PDB ID: 1UNG), which showed favourable results with compound (Vb3), showing a MolDock Score of -85.9788 that was comparable to that of the active ligand (ALH_1288 (B)) with MolDock Score of - 87.7609. Roscovitine 128-139 cyclin dependent kinase 5 Homo sapiens 116-120 35023537-6 2022 Herein, a self-amplifying nanodrug (RCH NPs) was designed by co-assembling hemin (ferric porphyrin), celecoxib (anti-inflammatory drug) and roscovitine (cyclin-dependent kinase 5 inhibitor) with the assistance of human serum albumin for reprograming the Janus-faced nature of ferroptosis. Roscovitine 140-151 cyclin dependent kinase 5 Homo sapiens 153-178 34391837-4 2021 Herein, a platelet-engineered nanoplatform (PMF@DR NPs) capable of harmonizing janus-faced nature of IFN-gamma was designed via uniquely co-assembling doxorubicin (Dox) and cyclin-dependent kinase 5 inhibitor roscovitine (Rosco) with platelet membrane fragment (PMF) as the particulate stabilizer. Roscovitine 209-220 cyclin dependent kinase 5 Homo sapiens 173-198 34391837-4 2021 Herein, a platelet-engineered nanoplatform (PMF@DR NPs) capable of harmonizing janus-faced nature of IFN-gamma was designed via uniquely co-assembling doxorubicin (Dox) and cyclin-dependent kinase 5 inhibitor roscovitine (Rosco) with platelet membrane fragment (PMF) as the particulate stabilizer. Roscovitine 222-227 cyclin dependent kinase 5 Homo sapiens 173-198