Evidence map›Paper›PMID 24891448›Full record

ArticleNeuro-oncology2014

Impact of meriolins, a new class of cyclin-dependent kinase inhibitors, on malignant glioma proliferation and neo-angiogenesis.

Marie Jarry, Céline Lecointre, Céline Malleval, Laurence Desrues, Marie-Thérèse Schouft, Vadim Lejoncour, François Liger, Gildas Lyvinec, Benoît Joseph, Nadège Loaëc and 4 more

Open access · bronzeAbstract read
In one paragraph

Article in Neuro-oncology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers, 1 of them a synthesis that pooled it.

0numbers the graph read from it
0cells of the map it votes in
15citing papers in PubMed, 1 pooled it
0.9field-weighted citation impact, top 24% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

15 citing papers in PubMed, 1 synthesis or guideline pooled it, 30 citations in OpenAlex.

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4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

14 authors at 1 institution in 1 country.

Marie JarryInserm U982, Laboratory of Neuronal and Neuroendocrine Communication and Differentiation, Astrocyte and Vascular Niche, Biomedical Research Institute (IRIB), PRES Normandy, TC2N network, University of Rouen, Mont-Saint-Aignan, France (M.J., C.L., L.D., M.-T.S., V.L., P.G., H.C.); Neuro-oncology department, Hospices Civils de Lyon, Hôpital Neurologique, Bron, France (C.M., J.H.); Lyon Neuroscience Research Center INSERM U1028/CNRS UMR 5292, Lyon, France (C.M., J.H.); University of Claude Bernard - Lyon 1, Villeurbanne, France (C.M., J.H.); Institut de Chimie et Biochimie Moléculaires et Supramoléculaires UMR 5246, University of Claude Bernard - Lyon 1, Villeurbanne, France (F.L., G.L., B.J., N.L.); Protein Phosphorylation & Human Disease Group & USR3151, Station Biologique, Roscoff, France (N.L., L.M.); ManRos Therapeutics, Roscoff, France (L.M.).
Céline LecointreInserm U982, Laboratory of Neuronal and Neuroendocrine Communication and Differentiation, Astrocyte and Vascular Niche, Biomedical Research Institute (IRIB), PRES Normandy, TC2N network, University of Rouen, Mont-Saint-Aignan, France (M.J., C.L., L.D., M.-T.S., V.L., P.G., H.C.); Neuro-oncology department, Hospices Civils de Lyon, Hôpital Neurologique, Bron, France (C.M., J.H.); Lyon Neuroscience Research Center INSERM U1028/CNRS UMR 5292, Lyon, France (C.M., J.H.); University of Claude Bernard - Lyon 1, Villeurbanne, France (C.M., J.H.); Institut de Chimie et Biochimie Moléculaires et Supramoléculaires UMR 5246, University of Claude Bernard - Lyon 1, Villeurbanne, France (F.L., G.L., B.J., N.L.); Protein Phosphorylation & Human Disease Group & USR3151, Station Biologique, Roscoff, France (N.L., L.M.); ManRos Therapeutics, Roscoff, France (L.M.).
Céline MallevalInserm U982, Laboratory of Neuronal and Neuroendocrine Communication and Differentiation, Astrocyte and Vascular Niche, Biomedical Research Institute (IRIB), PRES Normandy, TC2N network, University of Rouen, Mont-Saint-Aignan, France (M.J., C.L., L.D., M.-T.S., V.L., P.G., H.C.); Neuro-oncology department, Hospices Civils de Lyon, Hôpital Neurologique, Bron, France (C.M., J.H.); Lyon Neuroscience Research Center INSERM U1028/CNRS UMR 5292, Lyon, France (C.M., J.H.); University of Claude Bernard - Lyon 1, Villeurbanne, France (C.M., J.H.); Institut de Chimie et Biochimie Moléculaires et Supramoléculaires UMR 5246, University of Claude Bernard - Lyon 1, Villeurbanne, France (F.L., G.L., B.J., N.L.); Protein Phosphorylation & Human Disease Group & USR3151, Station Biologique, Roscoff, France (N.L., L.M.); ManRos Therapeutics, Roscoff, France (L.M.).
Laurence DesruesInserm U982, Laboratory of Neuronal and Neuroendocrine Communication and Differentiation, Astrocyte and Vascular Niche, Biomedical Research Institute (IRIB), PRES Normandy, TC2N network, University of Rouen, Mont-Saint-Aignan, France (M.J., C.L., L.D., M.-T.S., V.L., P.G., H.C.); Neuro-oncology department, Hospices Civils de Lyon, Hôpital Neurologique, Bron, France (C.M., J.H.); Lyon Neuroscience Research Center INSERM U1028/CNRS UMR 5292, Lyon, France (C.M., J.H.); University of Claude Bernard - Lyon 1, Villeurbanne, France (C.M., J.H.); Institut de Chimie et Biochimie Moléculaires et Supramoléculaires UMR 5246, University of Claude Bernard - Lyon 1, Villeurbanne, France (F.L., G.L., B.J., N.L.); Protein Phosphorylation & Human Disease Group & USR3151, Station Biologique, Roscoff, France (N.L., L.M.); ManRos Therapeutics, Roscoff, France (L.M.).
Marie-Thérèse SchouftInserm U982, Laboratory of Neuronal and Neuroendocrine Communication and Differentiation, Astrocyte and Vascular Niche, Biomedical Research Institute (IRIB), PRES Normandy, TC2N network, University of Rouen, Mont-Saint-Aignan, France (M.J., C.L., L.D., M.-T.S., V.L., P.G., H.C.); Neuro-oncology department, Hospices Civils de Lyon, Hôpital Neurologique, Bron, France (C.M., J.H.); Lyon Neuroscience Research Center INSERM U1028/CNRS UMR 5292, Lyon, France (C.M., J.H.); University of Claude Bernard - Lyon 1, Villeurbanne, France (C.M., J.H.); Institut de Chimie et Biochimie Moléculaires et Supramoléculaires UMR 5246, University of Claude Bernard - Lyon 1, Villeurbanne, France (F.L., G.L., B.J., N.L.); Protein Phosphorylation & Human Disease Group & USR3151, Station Biologique, Roscoff, France (N.L., L.M.); ManRos Therapeutics, Roscoff, France (L.M.).
Vadim LejoncourInserm U982, Laboratory of Neuronal and Neuroendocrine Communication and Differentiation, Astrocyte and Vascular Niche, Biomedical Research Institute (IRIB), PRES Normandy, TC2N network, University of Rouen, Mont-Saint-Aignan, France (M.J., C.L., L.D., M.-T.S., V.L., P.G., H.C.); Neuro-oncology department, Hospices Civils de Lyon, Hôpital Neurologique, Bron, France (C.M., J.H.); Lyon Neuroscience Research Center INSERM U1028/CNRS UMR 5292, Lyon, France (C.M., J.H.); University of Claude Bernard - Lyon 1, Villeurbanne, France (C.M., J.H.); Institut de Chimie et Biochimie Moléculaires et Supramoléculaires UMR 5246, University of Claude Bernard - Lyon 1, Villeurbanne, France (F.L., G.L., B.J., N.L.); Protein Phosphorylation & Human Disease Group & USR3151, Station Biologique, Roscoff, France (N.L., L.M.); ManRos Therapeutics, Roscoff, France (L.M.).
François LigerInserm U982, Laboratory of Neuronal and Neuroendocrine Communication and Differentiation, Astrocyte and Vascular Niche, Biomedical Research Institute (IRIB), PRES Normandy, TC2N network, University of Rouen, Mont-Saint-Aignan, France (M.J., C.L., L.D., M.-T.S., V.L., P.G., H.C.); Neuro-oncology department, Hospices Civils de Lyon, Hôpital Neurologique, Bron, France (C.M., J.H.); Lyon Neuroscience Research Center INSERM U1028/CNRS UMR 5292, Lyon, France (C.M., J.H.); University of Claude Bernard - Lyon 1, Villeurbanne, France (C.M., J.H.); Institut de Chimie et Biochimie Moléculaires et Supramoléculaires UMR 5246, University of Claude Bernard - Lyon 1, Villeurbanne, France (F.L., G.L., B.J., N.L.); Protein Phosphorylation & Human Disease Group & USR3151, Station Biologique, Roscoff, France (N.L., L.M.); ManRos Therapeutics, Roscoff, France (L.M.).
Gildas LyvinecInserm U982, Laboratory of Neuronal and Neuroendocrine Communication and Differentiation, Astrocyte and Vascular Niche, Biomedical Research Institute (IRIB), PRES Normandy, TC2N network, University of Rouen, Mont-Saint-Aignan, France (M.J., C.L., L.D., M.-T.S., V.L., P.G., H.C.); Neuro-oncology department, Hospices Civils de Lyon, Hôpital Neurologique, Bron, France (C.M., J.H.); Lyon Neuroscience Research Center INSERM U1028/CNRS UMR 5292, Lyon, France (C.M., J.H.); University of Claude Bernard - Lyon 1, Villeurbanne, France (C.M., J.H.); Institut de Chimie et Biochimie Moléculaires et Supramoléculaires UMR 5246, University of Claude Bernard - Lyon 1, Villeurbanne, France (F.L., G.L., B.J., N.L.); Protein Phosphorylation & Human Disease Group & USR3151, Station Biologique, Roscoff, France (N.L., L.M.); ManRos Therapeutics, Roscoff, France (L.M.).
Benoît JosephInserm U982, Laboratory of Neuronal and Neuroendocrine Communication and Differentiation, Astrocyte and Vascular Niche, Biomedical Research Institute (IRIB), PRES Normandy, TC2N network, University of Rouen, Mont-Saint-Aignan, France (M.J., C.L., L.D., M.-T.S., V.L., P.G., H.C.); Neuro-oncology department, Hospices Civils de Lyon, Hôpital Neurologique, Bron, France (C.M., J.H.); Lyon Neuroscience Research Center INSERM U1028/CNRS UMR 5292, Lyon, France (C.M., J.H.); University of Claude Bernard - Lyon 1, Villeurbanne, France (C.M., J.H.); Institut de Chimie et Biochimie Moléculaires et Supramoléculaires UMR 5246, University of Claude Bernard - Lyon 1, Villeurbanne, France (F.L., G.L., B.J., N.L.); Protein Phosphorylation & Human Disease Group & USR3151, Station Biologique, Roscoff, France (N.L., L.M.); ManRos Therapeutics, Roscoff, France (L.M.).
Nadège LoaëcInserm U982, Laboratory of Neuronal and Neuroendocrine Communication and Differentiation, Astrocyte and Vascular Niche, Biomedical Research Institute (IRIB), PRES Normandy, TC2N network, University of Rouen, Mont-Saint-Aignan, France (M.J., C.L., L.D., M.-T.S., V.L., P.G., H.C.); Neuro-oncology department, Hospices Civils de Lyon, Hôpital Neurologique, Bron, France (C.M., J.H.); Lyon Neuroscience Research Center INSERM U1028/CNRS UMR 5292, Lyon, France (C.M., J.H.); University of Claude Bernard - Lyon 1, Villeurbanne, France (C.M., J.H.); Institut de Chimie et Biochimie Moléculaires et Supramoléculaires UMR 5246, University of Claude Bernard - Lyon 1, Villeurbanne, France (F.L., G.L., B.J., N.L.); Protein Phosphorylation & Human Disease Group & USR3151, Station Biologique, Roscoff, France (N.L., L.M.); ManRos Therapeutics, Roscoff, France (L.M.).
Laurent MeijerInserm U982, Laboratory of Neuronal and Neuroendocrine Communication and Differentiation, Astrocyte and Vascular Niche, Biomedical Research Institute (IRIB), PRES Normandy, TC2N network, University of Rouen, Mont-Saint-Aignan, France (M.J., C.L., L.D., M.-T.S., V.L., P.G., H.C.); Neuro-oncology department, Hospices Civils de Lyon, Hôpital Neurologique, Bron, France (C.M., J.H.); Lyon Neuroscience Research Center INSERM U1028/CNRS UMR 5292, Lyon, France (C.M., J.H.); University of Claude Bernard - Lyon 1, Villeurbanne, France (C.M., J.H.); Institut de Chimie et Biochimie Moléculaires et Supramoléculaires UMR 5246, University of Claude Bernard - Lyon 1, Villeurbanne, France (F.L., G.L., B.J., N.L.); Protein Phosphorylation & Human Disease Group & USR3151, Station Biologique, Roscoff, France (N.L., L.M.); ManRos Therapeutics, Roscoff, France (L.M.).
Jérôme HonnoratInserm U982, Laboratory of Neuronal and Neuroendocrine Communication and Differentiation, Astrocyte and Vascular Niche, Biomedical Research Institute (IRIB), PRES Normandy, TC2N network, University of Rouen, Mont-Saint-Aignan, France (M.J., C.L., L.D., M.-T.S., V.L., P.G., H.C.); Neuro-oncology department, Hospices Civils de Lyon, Hôpital Neurologique, Bron, France (C.M., J.H.); Lyon Neuroscience Research Center INSERM U1028/CNRS UMR 5292, Lyon, France (C.M., J.H.); University of Claude Bernard - Lyon 1, Villeurbanne, France (C.M., J.H.); Institut de Chimie et Biochimie Moléculaires et Supramoléculaires UMR 5246, University of Claude Bernard - Lyon 1, Villeurbanne, France (F.L., G.L., B.J., N.L.); Protein Phosphorylation & Human Disease Group & USR3151, Station Biologique, Roscoff, France (N.L., L.M.); ManRos Therapeutics, Roscoff, France (L.M.).
Pierrick GandolfoInserm U982, Laboratory of Neuronal and Neuroendocrine Communication and Differentiation, Astrocyte and Vascular Niche, Biomedical Research Institute (IRIB), PRES Normandy, TC2N network, University of Rouen, Mont-Saint-Aignan, France (M.J., C.L., L.D., M.-T.S., V.L., P.G., H.C.); Neuro-oncology department, Hospices Civils de Lyon, Hôpital Neurologique, Bron, France (C.M., J.H.); Lyon Neuroscience Research Center INSERM U1028/CNRS UMR 5292, Lyon, France (C.M., J.H.); University of Claude Bernard - Lyon 1, Villeurbanne, France (C.M., J.H.); Institut de Chimie et Biochimie Moléculaires et Supramoléculaires UMR 5246, University of Claude Bernard - Lyon 1, Villeurbanne, France (F.L., G.L., B.J., N.L.); Protein Phosphorylation & Human Disease Group & USR3151, Station Biologique, Roscoff, France (N.L., L.M.); ManRos Therapeutics, Roscoff, France (L.M.).
Hélène CastelInserm U982, Laboratory of Neuronal and Neuroendocrine Communication and Differentiation, Astrocyte and Vascular Niche, Biomedical Research Institute (IRIB), PRES Normandy, TC2N network, University of Rouen, Mont-Saint-Aignan, France (M.J., C.L., L.D., M.-T.S., V.L., P.G., H.C.); Neuro-oncology department, Hospices Civils de Lyon, Hôpital Neurologique, Bron, France (C.M., J.H.); Lyon Neuroscience Research Center INSERM U1028/CNRS UMR 5292, Lyon, France (C.M., J.H.); University of Claude Bernard - Lyon 1, Villeurbanne, France (C.M., J.H.); Institut de Chimie et Biochimie Moléculaires et Supramoléculaires UMR 5246, University of Claude Bernard - Lyon 1, Villeurbanne, France (F.L., G.L., B.J., N.L.); Protein Phosphorylation & Human Disease Group & USR3151, Station Biologique, Roscoff, France (N.L., L.M.); ManRos Therapeutics, Roscoff, France (L.M.).
Université Claude Bernard Lyon 1 · FR

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

backgroundGlioblastomas are the most frequent and most aggressive primary brain tumors in adults. The median overall survival is limited to a few months despite surgery, radiotherapy, and chemotherapy. It is now clearly established that hyperactivity of cyclin-dependent kinases (CDKs) is one of the processes underlying hyperproliferation and tumoral growth. The marine natural products meridianins and variolins, characterized as CDK inhibitors, display a kinase-inhibitory activity associated with cytotoxic effects. In order to improve selectivity and efficiency of these CDK inhibitors, a series of hybrid compounds called meriolins have been synthesized.

methodsThe potential antitumoral activity of meriolins was investigated in vitro on glioma cell lines (SW1088 and U87), native neural cells, and a human endothelial cell line (HUV-EC-C). The impact of intraperitoneal or intratumoral administrations of meriolin 15 was evaluated in vivo on 2 different nude mice-xenografted glioma models.

resultsMeriolins 3, 5, and 15 exhibited antiproliferative properties with nanomolar IC50 and induced cell-cycle arrest and CDK inhibition associated with apoptotic events in human glioma cell lines. These meriolins blocked the proliferation rate of HUV-EC-C through cell cycle arrest and apoptosis. In vivo, meriolin 15 provoked a robust reduction in tumor volume in spite of toxicity for highest doses, associated with inhibition of cell division, activation of caspase 3, reduction of CD133 cells, and modifications of the vascular architecture.

conclusionMeriolins, and meriolin 15 in particular, exhibit antiproliferative and proapoptotic activities on both glioma and intratumoral endothelial cells, constituting key promising therapeutic lead compounds for the treatment of glioblastoma.

Indexed as

AnimalsApoptosisBlotting, WesternBridged Bicyclo Compounds, HeterocyclicCell CycleCell ProliferationCells, CulturedCyclin-Dependent KinasesGliomaHumansHuman Umbilical Vein Endothelial CellsImmunoenzyme TechniquesMaleMiceMice, NudeNeovascularization, PathologicBridged Bicyclo Compounds, HeterocyclicCyclin-Dependent Kinasesmeriolin 3Pyrimidinescyclin-dependent kinasegliomameriolinnude micetumor growth

Identifiers

PMID24891448
PMCPMC4201071
OpenAlexW2140502982

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