Novel potent pharmacological cyclin-dependent kinase inhibitors (Q37855812)

24 August 2017

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title

Novel potent pharmacological cyclin-dependent kinase inhibitors (English)

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24 August 2017

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3

Vladimír Kryštof

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24 August 2017

Józefa Wesierska-Gadek

series ordinal

1

object named as

Józefa Węsierska-Gądek

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24 August 2017

Ivo Chamrád

2

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24 August 2017

publication date

1 December 2009

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Future Medicinal Chemistry

24 August 2017

published in

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24 August 2017

volume

1

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24 August 2017

issue

9

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24 August 2017

page(s)

1561-1581

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Animal cell cycles and their control

24 August 2017

cites work

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Cyclin-dependent kinases: engines, clocks, and microprocessors

21 January 2018

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CDK inhibitors: cell cycle regulators and beyond

21 January 2018

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Mammalian cyclin-dependent kinases

21 January 2018

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Ubiquitin ligases: cell-cycle control and cancer

21 January 2018

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Secrets of a double agent: CDK7 in cell-cycle control and transcription

21 January 2018

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Mechanism of CDK activation revealed by the structure of a cyclinA-CDK2 complex

21 January 2018

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Structural basis of cyclin-dependent kinase activation by phosphorylation

21 January 2018

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Principles of CDK regulation

21 January 2018

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Cdk2 knockout mice are viable

21 January 2018

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Mammalian cells cycle without the D-type cyclin-dependent kinases Cdk4 and Cdk6

21 January 2018

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Cyclin-dependent kinase 2 is essential for meiosis but not for mitotic cell division in mice

21 January 2018

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Cdk1 is sufficient to drive the mammalian cell cycle

21 January 2018

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Loss of Cdk4 expression causes insulin-deficient diabetes and Cdk4 activation results in beta-islet cell hyperplasia

21 January 2018

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Phosphorylation of p27Kip1 regulates assembly and activation of cyclin D1-Cdk4

21 January 2018

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Investigating RNA polymerase II carboxyl-terminal domain (CTD) phosphorylation.

21 January 2018

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Expression and activity of p40MO15, the catalytic subunit of cdk-activating kinase, during Xenopus oogenesis and embryogenesis

21 January 2018

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Activation of cyclin-dependent kinase 4 (cdk4) by mouse MO15-associated kinase

21 January 2018

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T-loop phosphorylation stabilizes the CDK7-cyclin H-MAT1 complex in vivo and regulates its CTD kinase activity

21 January 2018

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Requirements for Cdk7 in the assembly of Cdk1/cyclin B and activation of Cdk2 revealed by chemical genetics in human cells.

21 January 2018

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Inability to enter S phase and defective RNA polymerase II CTD phosphorylation in mice lacking Mat1

21 January 2018

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The cyclin H/cdk7/Mat1 kinase activity is regulated by CK2 phosphorylation of cyclin H.

21 January 2018

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PITALRE, a nuclear CDC2-related protein kinase that phosphorylates the retinoblastoma protein in vitro

21 January 2018

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Mechanisms controlling CDK9 activity

21 January 2018

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Transcription regulation through promoter-proximal pausing of RNA polymerase II.

21 January 2018

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The multi-tasking P-TEFb complex

21 January 2018

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Cyclin-dependent kinase 9: a key transcriptional regulator and potential drug target in oncology, virology and cardiology.

21 January 2018

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CDK inhibitors: positive and negative regulators of G1-phase progression

21 January 2018

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Small-molecule cyclin-dependent kinase modulators

21 January 2018

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Post-translational regulation of the tumor suppressor p27(KIP1).

21 January 2018

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The Cdk inhibitor p27 in human cancer: prognostic potential and relevance to anticancer therapy

21 January 2018

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Cell cycle, CDKs and cancer: a changing paradigm

21 January 2018

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21 January 2018

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The cdk5/p35 kinase is essential for neurite outgrowth during neuronal differentiation

21 January 2018

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An unusual member of the Cdk family: Cdk5.

21 January 2018

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Regulation of NMDA receptors by cyclin-dependent kinase-5

21 January 2018

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Molecular diversity of glutamate receptors and implications for brain function

21 January 2018

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Role of cyclin-dependent kinase 5 in the neurodegenerative process triggered by amyloid-Beta and prion peptides: implications for Alzheimer's disease and prion-related encephalopathies.

21 January 2018

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Role of cell cycle proteins in CNS injury

21 January 2018

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Roscovitine reduces neuronal loss, glial activation, and neurologic deficits after brain trauma

21 January 2018

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Cyclin-dependent kinase pathways as targets for cancer treatment

21 January 2018

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Combined depletion of cell cycle and transcriptional cyclin-dependent kinase activities induces apoptosis in cancer cells

21 January 2018

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Transient treatment with CDK inhibitors eliminates proliferative potential even when their abilities to evoke apoptosis and DNA damage are blocked

21 January 2018

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Phase I trial of continuous infusion flavopiridol, a novel cyclin-dependent kinase inhibitor, in patients with refractory neoplasms.

21 January 2018

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Potent inhibition of CDC2 kinase activity by the flavonoid L86-8275.

21 January 2018

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Alteration of the phosphorylation state of p34cdc2 kinase by the flavone L86-8275 in breast carcinoma cells. Correlation with decreased H1 kinase activity

21 January 2018

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Flavopiridol inhibits P-TEFb and blocks HIV-1 replication

21 January 2018

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Flavopiridol inactivates P-TEFb and blocks most RNA polymerase II transcription in vivo

21 January 2018

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Mechanism of H-8 inhibition of cyclin-dependent kinase 9: study using inhibitor-immobilized matrices

21 January 2018

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The structure of P-TEFb (CDK9/cyclin T1), its complex with flavopiridol and regulation by phosphorylation

21 January 2018

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Mechanisms of action of flavopiridol

21 January 2018

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Flavopiridol, an inhibitor of transcription: implications, problems and solutions

21 January 2018

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Preclinical and clinical development of the cyclin-dependent kinase inhibitor flavopiridol

21 January 2018

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A novel liposomal formulation of flavopiridol

21 January 2018

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Potent induction of wild-type p53-dependent transcription in tumour cells by a synthetic inhibitor of cyclin-dependent kinases

21 January 2018

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In vitro activity of cyclin-dependent kinase inhibitor CYC202 (Seliciclib, R-roscovitine) in mantle cell lymphomas.

21 January 2018

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Activation of p53 by roscovitine-mediated suppression of MDM2 expression

21 January 2018

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The Cyclin-dependent kinase inhibitor CYC202 (R-roscovitine) inhibits retinoblastoma protein phosphorylation, causes loss of Cyclin D1, and activates the mitogen-activated protein kinase pathway

21 January 2018

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Roscovitine-induced up-regulation of p53AIP1 protein precedes the onset of apoptosis in human MCF-7 breast cancer cells

21 January 2018

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The cyclin-dependent kinase inhibitor seliciclib (R-roscovitine; CYC202) decreases the expression of mitotic control genes and prevents entry into mitosis

21 January 2018

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Seliciclib (CYC202, R-Roscovitine) induces cell death in multiple myeloma cells by inhibition of RNA polymerase II-dependent transcription and down-regulation of Mcl-1

21 January 2018

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Roscovitine sensitizes glioma cells to TRAIL-mediated apoptosis by downregulation of survivin and XIAP.

21 January 2018

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Seliciclib (CYC202 or R-roscovitine), a small-molecule cyclin-dependent kinase inhibitor, mediates activity via down-regulation of Mcl-1 in multiple myeloma

21 January 2018

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R-Roscovitine simultaneously targets both the p53 and NF-kappaB pathways and causes potentiation of apoptosis: implications in cancer therapy.

21 January 2018

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In vitro and in vivo pharmacokinetic-pharmacodynamic relationships for the trisubstituted aminopurine cyclin-dependent kinase inhibitors olomoucine, bohemine and CYC202.

21 January 2018

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Pharmacodynamic effects of seliciclib, an orally administered cell cycle modulator, in undifferentiated nasopharyngeal cancer

21 January 2018

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Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6.

21 January 2018

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A novel orally active small molecule potently induces G1 arrest in primary myeloma cells and prevents tumor growth by specific inhibition of cyclin-dependent kinase 4/6.

21 January 2018

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Pharmacologic inhibition of cyclin-dependent kinase 4/6 activity arrests proliferation in myoblasts and rhabdomyosarcoma-derived cells

21 January 2018

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Toward understanding the structural basis of cyclin-dependent kinase 6 specific inhibition

21 January 2018

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Mantle cell lymphoma cells express predominantly cyclin D1a isoform and are highly sensitive to selective inhibition of CDK4 kinase activity.

21 January 2018

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N-(cycloalkylamino)acyl-2-aminothiazole inhibitors of cyclin-dependent kinase 2. N-[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4- piperidinecarboxamide (BMS-387032), a highly efficacious and selective antitumor agent

21 January 2018

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SNS-032 is a potent and selective CDK 2, 7 and 9 inhibitor that drives target modulation in patient samples

21 January 2018

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Mechanism of action of SNS-032, a novel cyclin-dependent kinase inhibitor, in chronic lymphocytic leukemia

21 January 2018

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SNS-032 prevents tumor cell-induced angiogenesis by inhibiting vascular endothelial growth factor

21 January 2018

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A phase 1 study of SNS-032 (formerly BMS-387032), a potent inhibitor of cyclin-dependent kinases 2, 7 and 9 administered as a single oral dose and weekly infusion in patients with metastatic refractory solid tumors

21 January 2018

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P-glycoprotein plays a role in the oral absorption of BMS-387032, a potent cyclin-dependent kinase 2 inhibitor, in rats

21 January 2018

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Discovery of [4-Amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin-5-yl](2,3-difluoro-6- methoxyphenyl)methanone (R547), a potent and selective cyclin-dependent kinase inhibitor with significant in vivo antitumor activity

21 January 2018

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In vitro and in vivo activity of R547: a potent and selective cyclin-dependent kinase inhibitor currently in phase I clinical trials

21 January 2018

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In vitro antitumor properties of a novel cyclin-dependent kinase inhibitor, P276-00.

21 January 2018

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P276-00, a novel cyclin-dependent inhibitor induces G1-G2 arrest, shows antitumor activity on cisplatin-resistant cells and significant in vivo efficacy in tumor models.

21 January 2018

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Preclinical activity of P276-00, a novel small-molecule cyclin-dependent kinase inhibitor in the therapy of multiple myeloma

21 January 2018

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Molecular and pharmacodynamic characteristics of the novel multi-target tumor growth inhibitor ZK 304709.

21 January 2018

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A phase I dose escalation study of the pharmacokinetics and tolerability of ZK 304709, an oral multi-targeted growth inhibitor (MTGI), in patients with advanced solid tumours

21 January 2018

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Identification of N-(4-piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a novel cyclin dependent kinase inhibitor using fragment-based X-ray crystallography and structure based drug design

21 January 2018

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Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines

21 January 2018

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Peripheral white blood cell toxicity induced by broad spectrum cyclin-dependent kinase inhibitors.

21 January 2018

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Toxicity and toxicokinetics of the cyclin-dependent kinase inhibitor AG-024322 in cynomolgus monkeys following intravenous infusion

21 January 2018

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Imidazo[1,2-a]pyridines: a potent and selective class of cyclin-dependent kinase inhibitors identified through structure-based hybridisation

21 January 2018

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Imidazo[1,2-b]pyridazines: a potent and selective class of cyclin-dependent kinase inhibitors

21 January 2018

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Imidazo[1,2-a]pyridines. Part 2: SAR and optimisation of a potent and selective class of cyclin-dependent kinase inhibitors

21 January 2018

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Imidazoles: SAR and development of a potent class of cyclin-dependent kinase inhibitors

21 January 2018

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Cytokinin-derived cyclin-dependent kinase inhibitors: synthesis and cdc2 inhibitory activity of olomoucine and related compounds

21 January 2018

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CVT-313, a Specific and Potent Inhibitor of CDK2 That Prevents Neointimal Proliferation

21 January 2018

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Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors

21 January 2018

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Crystal structure of human cyclin-dependent kinase 2 in complex with the adenine-derived inhibitor H717

21 January 2018

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N-&-N, a new class of cell death-inducing kinase inhibitors derived from the purine roscovitine

21 January 2018

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Pyrazolo[1,5-a]-1,3,5-triazine as a purine bioisostere: access to potent cyclin-dependent kinase inhibitor (R)-roscovitine analogue.

21 January 2018

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Apoptosis-based therapies for hematologic malignancies

21 January 2018

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Bcl-2-family proteins and hematologic malignancies: history and future prospects

21 January 2018

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A novel CDK inhibitor, CYC202 (R-roscovitine), overcomes the defect in p53-dependent apoptosis in B-CLL by down-regulation of genes involved in transcription regulation and survival.

21 January 2018

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Cyclin-dependent kinase inhibitor Roscovitine induces apoptosis in chronic lymphocytic leukemia cells.

21 January 2018

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Cdk inhibitory nucleoside analogs prevent transcription from viral genomes

21 January 2018

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Functional p53 in cells contributes to the anticancer effect of the cyclin-dependent kinase inhibitor roscovitine

21 January 2018

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Strategies for optimizing combinations of molecularly targeted anticancer agents

21 January 2018

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A p34(cdc2) survival checkpoint in cancer

21 January 2018

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Efficacy of sequential treatment of HCT116 colon cancer monolayers and xenografts with docetaxel, flavopiridol, and 5-fluorouracil.

21 January 2018

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The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901.

21 January 2018

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MTAP homozygous deletion: an Achilles heel of human cancers ready for clinical use?

21 January 2018

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Apoptosis of metastatic prostate cancer cells by a combination of cyclin-dependent kinase and AKT inhibitors

21 January 2018

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Transformed Cells Require Continuous Activity Of RNA Polymerase II To Resist Oncogene-Induced Apoptosis

21 January 2018

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CDK inhibitors in cancer therapy: what is next?

21 January 2018

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Selective cyclin-dependent kinase inhibitors discriminating between cell cycle and transcriptional kinases: future reality or utopia?

21 January 2018

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The role of the Cdk5-p35 kinase in neuronal development

21 January 2018

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Roscovitine in B-chronic lymphocytic leukemia cells: high apoptosis-inducing efficacy and synergism with alemtuzumab independent of the patients' pretreatment status

21 January 2018

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21 January 2018

Identifiers

DOI

10.4155/FMC.09.110

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24 August 2017

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