Clinical anticancer drug development: targeting the cyclin-dependent kinases

Modulating Innate and Adaptive Immunity by (R)-Roscovitine: Potential Therapeutic Opportunity in Cystic Fibrosis

2016 • 4,824 citations

Biochemical and Cellular Effects of Roscovitine, a Potent and Selective Inhibitor of the Cyclin‐Dependent Kinases cdc2, cdk2 and cdk5

1997 • 1,324 citations

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

2003 • 781 citations

Preclinical and Clinical Development of Cyclin-Dependent Kinase Modulators

2000 • 501 citations

Proliferation of cancer cells despite CDK2 inhibition

2003 • 458 citations

UCN-01: a Potent Abrogator of G2 Checkpoint Function in Cancer Cells With Disrupted p53

1996 • 451 citations

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

1998 • 408 citations

Genomic-scale measurement of mRNA turnover and the mechanisms of action of the anti-cancer drug flavopiridol

2001 • 374 citations

In vitro and in vivo antitumor properties of the cyclin dependent kinase inhibitor CYC202 (R‐roscovitine)

2002 • 365 citations

The radiosensitizing agent 7-hydroxystaurosporine (UCN-01) inhibits the DNA damage checkpoint kinase hChk1.

2000 • 318 citations

Phase I Trial of 72-Hour Continuous Infusion UCN-01 in Patients With Refractory Neoplasms

2001 • 295 citations

Flavopiridol in Untreated or Relapsed Mantle-Cell Lymphoma: Results of a Phase II Study of the National Cancer Institute of Canada Clinical Trials Group

2003 • 279 citations

Cytotoxic synergy between flavopiridol (NSC 649890, L86-8275) and various antineoplastic agents: the importance of sequence of administration.

1997 • 261 citations

Down-regulation of cyclin D1 by transcriptional repression in MCF-7 human breast carcinoma cells induced by flavopiridol.

1999 • 255 citations

Flavopiridol, a novel cyclin-dependent kinase inhibitor, suppresses the growth of head and neck squamous cell carcinomas by inducing apoptosis.

1998 • 248 citations

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

2004 • 247 citations

Flavopiridol Induces Apoptosis of Normal Lymphoid Cells, Causes Immunosuppression, and Has Potent Antitumor Activity In Vivo Against Human Leukemia and Lymphoma Xenografts

1998 • 246 citations

Small-molecule cyclin-dependent kinase modulators

2003 • 235 citations

Flavopiridol, A Novel Cyclin-Dependent Kinase Inhibitor, in Metastatic Renal Cancer: A University of Chicago Phase II Consortium Study

2000 • 212 citations

Interference with PDK1-Akt survival signaling pathway by UCN-01 (7-hydroxystaurosporine)

2002 • 210 citations

Phase II Study of the Cyclin-Dependent Kinase Inhibitor Flavopiridol Administered to Patients With Advanced Gastric Carcinoma

2001 • 205 citations

Unpredicted clinical pharmacology of UCN-01 caused by specific binding to human alpha1-acid glycoprotein.

1998 • 198 citations

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

2004 • 190 citations

A phase II trial of the cyclin-dependent kinase inhibitor flavopiridol in patients with previously untreated stage IV non-small cell lung cancer.

2001 • 183 citations

Complexities in the development of cyclin-dependent kinase inhibitor drugs

2002 • 159 citations

Phase I Study of the Cyclin-Dependent Kinase Inhibitor Flavopiridol in Combination With Paclitaxel in Patients With Advanced Solid Tumors

2002 • 159 citations

G1 phase accumulation induced by UCN-01 is associated with dephosphorylation of Rb and CDK2 proteins as well as induction of CDK inhibitor p21/Cip1/WAF1/Sdi1 in p53-mutated human epidermoid carcinoma A431 cells.

1997 • 155 citations

UCN-01 inhibits p53 up-regulation and abrogates gamma-radiation-induced G(2)-M checkpoint independently of p53 by targeting both of the checkpoint kinases, Chk2 and Chk1.

2002 • 140 citations

E7070, a novel sulphonamide agent with potent antitumour activity in vitro and in vivo

2001 • 127 citations

Phase I Clinical and Pharmacokinetic Study of Flavopiridol Administered as a Daily 1-Hour Infusion in Patients With Advanced Neoplasms

2002 • 126 citations

Phase I clinical and pharmacokinetic trial of the cyclin-dependent kinase inhibitor flavopiridol

2002 • 121 citations

Activation of p53 by roscovitine-mediated suppression of MDM2 expression

2001 • 118 citations

Augmentation of apoptosis and tumor regression by flavopiridol in the presence of CPT-11 in Hct116 colon cancer monolayers and xenografts.

2001 • 114 citations

The Effect of the Cyclin-Dependent Kinase Inhibitor Olomoucine on Cell Cycle Kinetics

1997 • 110 citations

Flavopiridol down-regulates antiapoptotic proteins and sensitizes human breast cancer cells to epothilone B-induced apoptosis.

2003 • 109 citations

Clinical pharmacology of UCN-01: Initial observations and comparison to preclinical models

1998 • 90 citations

Seventy-Two Hour Continuous Infusion Flavopiridol in Relapsed and Refractory Mantle Cell Lymphoma

2002 • 78 citations

7-Hydroxystaurosporine (UCN-01) causes redistribution of proliferating cell nuclear antigen and abrogates cisplatin-induced S-phase arrest in Chinese hamster ovary cells.

1997 • 74 citations

Phase I and Pharmacokinetic Study of E7070, a Novel Chloroindolyl Sulfonamide Cell-Cycle Inhibitor, Administered as a One-Hour Infusion Every Three Weeks in Patients With Advanced Cancer

2002 • 60 citations

Phase I and pharmacokinetic study of E7070, a novel sulfonamide, given at a daily times five schedule in patients with solid tumors. A study by the EORTC-Early Clinical Studies Group (ECSG)

2001 • 56 citations

Phase II study of E7070 in patients with metastatic melanoma

2004 • 52 citations

Possible mechanisms of diarrheal side effects associated with the use of a novel chemotherapeutic agent, flavopiridol.

2001 • 44 citations

The Production of Tumors by Tobacco Tars.

1941 • 35 citations

Flavopiridol-related proinflammatory syndrome is associated with induction of interleukin-6.

2003 • 33 citations

A phase I trial of the oral cyclin dependent kinase inhibitor CYC202 in patients with advanced malignancy

2004 • 13 citations

Flavopiridol given as a 30-min intravenous (IV) bolus followed by 4-hr continuous IV infusion (CIVI) results in clinical activity and tumor lysis in refractory chronic lymphocytic leukemia (CLL)

2004 • 8 citations

PET as a biomarker of the antitumor effects of the CDK2 inhibitor BMS-387032

2004 • 2 citations