-
1
-
-
21144435503
-
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
-
Alvi AJ, Austen B, Weston VJ, Fegan C, MacCallum D, Gianella-Borradori A, Lane DP, Hubank M, Powell JE, Wei W, Taylor AMR, Moss PAH, Tatjana Stankovic T (2005) 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. Blood 105: 4484-4491
-
(2005)
Blood
, vol.105
, pp. 4484-4491
-
-
Alvi, A.J.1
Austen, B.2
Weston, V.J.3
Fegan, C.4
MacCallum, D.5
Gianella-Borradori, A.6
Lane, D.P.7
Hubank, M.8
Powell, J.E.9
Wei, W.10
Taylor, A.M.R.11
Moss, P.A.H.12
Tatjana Stankovic, T.13
-
2
-
-
24744437350
-
Roscovitine targets: Protein kinase and pyridoxal kinase
-
Bach S, Knockaert M, Reinhardt J, Lozach O, Schmitt S, Baratte B, Koken M, Coburn SP, Tang L, Jiang T, Liang DC, Galons H, Dierick JF, Pinna LA, Meggio F, Tozke F, Schachtele C, Lerman AS, Carno A, Wan Y, Gray N, Meijer L (2005) Roscovitine targets: protein kinase and pyridoxal kinase. J Biol Chem 280: 31208-31219
-
(2005)
J Biol Chem
, vol.280
, pp. 31208-31219
-
-
Bach, S.1
Knockaert, M.2
Reinhardt, J.3
Lozach, O.4
Schmitt, S.5
Baratte, B.6
Koken, M.7
Coburn, S.P.8
Tang, L.9
Jiang, T.10
Liang, D.C.11
Galons, H.12
Dierick, J.F.13
Pinna, L.A.14
Meggio, F.15
Tozke, F.16
Schachtele, C.17
Lerman, A.S.18
Carno, A.19
Wan, Y.20
Gray, N.21
Meijer, L.22
more..
-
3
-
-
13244268318
-
Clinical anticancer drug development: Targeting the cyclin dependent kinase
-
Benson B, Kaye S, Workman P, Garrett M, Walton M, de Bono J (2005) Clinical anticancer drug development: targeting the cyclin dependent kinase. Br J Cancer 92: 7-12
-
(2005)
Br J Cancer
, vol.92
, pp. 7-12
-
-
Benson, B.1
Kaye, S.2
Workman, P.3
Garrett, M.4
Walton, M.5
de Bono, J.6
-
4
-
-
0031028163
-
Inhibition of cyclin-dependent kinases by purine analogues: Crystal structure of human cdk2 complexed with roscovitine
-
De Azevedo WF, Leclerc S, Meijer L, Havlicek L, Strnad M, Kim SH (1997) Inhibition of cyclin-dependent kinases by purine analogues: crystal structure of human cdk2 complexed with roscovitine. Eur J Biochem 243: 518-526
-
(1997)
Eur J Biochem
, vol.243
, pp. 518-526
-
-
De Azevedo, W.F.1
Leclerc, S.2
Meijer, L.3
Havlicek, L.4
Strnad, M.5
Kim, S.H.6
-
5
-
-
1842637406
-
Pharmacokinetic model of R-roscovitine and its metabolite in healthy male subjects
-
De la Motte S, Gianella-Borradori A (2004) Pharmacokinetic model of R-roscovitine and its metabolite in healthy male subjects. Int J Clin Pharmacol Ther 42: 232-239
-
(2004)
Int J Clin Pharmacol Ther
, vol.42
, pp. 232-239
-
-
De la Motte, S.1
Gianella-Borradori, A.2
-
6
-
-
0032563315
-
Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors
-
Gray NS, Wodicka L, Thunnissen AM, Norman TC, Kwon S, Espinoza FH, Morgan DO, Barnes G, LeClerc S, Meijer L, Kim SH, Lockhart DJ, Schultz PG (1998) Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors. Science 281: 533-538
-
(1998)
Science
, vol.281
, pp. 533-538
-
-
Gray, N.S.1
Wodicka, L.2
Thunnissen, A.M.3
Norman, T.C.4
Kwon, S.5
Espinoza, F.H.6
Morgan, D.O.7
Barnes, G.8
LeClerc, S.9
Meijer, L.10
Kim, S.H.11
Lockhart, D.J.12
Schultz, P.G.13
-
7
-
-
0034973788
-
Activation of p53 by roscovitine-mediated suppression of MDM2 expression
-
Lu W, Chen L, Peng Y, Chen J (2001) Activation of p53 by roscovitine-mediated suppression of MDM2 expression. Oncogene 20: 3206-3216
-
(2001)
Oncogene
, vol.20
, pp. 3206-3216
-
-
Lu, W.1
Chen, L.2
Peng, Y.3
Chen, J.4
-
8
-
-
20444477948
-
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
-
MacCallum DE, Melville J, Frame S, Watt K, Anderson S, Gianella-Borradori A, Lane DP, Green SR (2005) 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. Cancer Res 65: 5399-5407
-
(2005)
Cancer Res
, vol.65
, pp. 5399-5407
-
-
MacCallum, D.E.1
Melville, J.2
Frame, S.3
Watt, K.4
Anderson, S.5
Gianella-Borradori, A.6
Lane, D.P.7
Green, S.R.8
-
9
-
-
0035754080
-
To cycle or not to cycle: A critical decision in cancer
-
Malumbres M, Barbacid M (2001) To cycle or not to cycle: a critical decision in cancer. Nat Rev Cancer 1: 222-231
-
(2001)
Nat Rev Cancer
, vol.1
, pp. 222-231
-
-
Malumbres, M.1
Barbacid, M.2
-
10
-
-
4444247138
-
Mammalian cells cycle without the D-type cyclin-dependent kinases Cdk4 and Cdk6
-
Malumbres M, Sotillo R, Santamaria D, Galan J, Cerezo A, Ortega S, Dubus P, Barbacid M (2004) Mammalian cells cycle without the D-type cyclin-dependent kinases Cdk4 and Cdk6. Cell 118: 493-504
-
(2004)
Cell
, vol.118
, pp. 493-504
-
-
Malumbres, M.1
Sotillo, R.2
Santamaria, D.3
Galan, J.4
Cerezo, A.5
Ortega, S.6
Dubus, P.7
Barbacid, M.8
-
11
-
-
0037058678
-
In vitro and in vivo antitumor properties of the cyclin dependent kinase inhibitor CYC202 (R-roscovitine)
-
McClue SJ, Blake D, Clarke R, Cowan A, Cummings L, Fischer PM, MacKenzie M, Melville J, Stewart K, Wang S, Zhelev N, Zheleva D, Lane DP (2002) In vitro and in vivo antitumor properties of the cyclin dependent kinase inhibitor CYC202 (R-roscovitine). Int J Cancer 102: 463-468
-
(2002)
Int J Cancer
, vol.102
, pp. 463-468
-
-
McClue, S.J.1
Blake, D.2
Clarke, R.3
Cowan, A.4
Cummings, L.5
Fischer, P.M.6
MacKenzie, M.7
Melville, J.8
Stewart, K.9
Wang, S.10
Zhelev, N.11
Zheleva, D.12
Lane, D.P.13
-
12
-
-
0031037714
-
Biochemical and cellular effects of roscovitine, a potent and selective inhibitor of the cyclin-dependent kinases cdc2, cdk2 and cdk5
-
Meijer L, Borgne A, Mulner O, Chong JP, Blow JJ, Inagaki N, Inagaki M, Delcros JG, Moulinoux JP (1997) Biochemical and cellular effects of roscovitine, a potent and selective inhibitor of the cyclin-dependent kinases cdc2, cdk2 and cdk5. Eur J Biochem 243: 527-536
-
(1997)
Eur J Biochem
, vol.243
, pp. 527-536
-
-
Meijer, L.1
Borgne, A.2
Mulner, O.3
Chong, J.P.4
Blow, J.J.5
Inagaki, N.6
Inagaki, M.7
Delcros, J.G.8
Moulinoux, J.P.9
-
13
-
-
0037665145
-
Roscovitine and other purines as kinase inhibitors. From starfish oocytes to clinical trials
-
Meijer L, Raymond E (2003) Roscovitine and other purines as kinase inhibitors. From starfish oocytes to clinical trials. Acc Chem Res 36: 417-425
-
(2003)
Acc Chem Res
, vol.36
, pp. 417-425
-
-
Meijer, L.1
Raymond, E.2
-
14
-
-
14044274202
-
Metabolism and pharmacokinetics of the cyclin-dependent kinase inhibitor R-Roscovitine in the mouse
-
Nutley BP, Raynaud FI, Wilson SC, Fischer PM, Hayes A, Goddard PM, McClue SJ, Jarman M, Lane DP, Workman P (2005) Metabolism and pharmacokinetics of the cyclin-dependent kinase inhibitor R-Roscovitine in the mouse. Mol Cancer Ther 4: 125-139
-
(2005)
Mol Cancer Ther
, vol.4
, pp. 125-139
-
-
Nutley, B.P.1
Raynaud, F.I.2
Wilson, S.C.3
Fischer, P.M.4
Hayes, A.5
Goddard, P.M.6
McClue, S.J.7
Jarman, M.8
Lane, D.P.9
Workman, P.10
-
15
-
-
0041854279
-
Cyclin-dependent kinase 2 is essential for meiosis but not for mitotic cell division in mice
-
Ortega S, Prieto I, Odajima J, Martin A, Dubus P, Sotillo R, Barbero JL, Malumbres M, Barbacid M (2003) Cyclin-dependent kinase 2 is essential for meiosis but not for mitotic cell division in mice. Nat Genet 35: 25-31
-
(2003)
Nat Genet
, vol.35
, pp. 25-31
-
-
Ortega, S.1
Prieto, I.2
Odajima, J.3
Martin, A.4
Dubus, P.5
Sotillo, R.6
Barbero, J.L.7
Malumbres, M.8
Barbacid, M.9
-
16
-
-
33846249367
-
-
Pierga J, Faivre S, Vera K, Laurence V, Delbaldo C, Bekradda M, Armand JP, Gianella-Borradori A, Dieras V, Raymond E (2003) A phase I and pharmacokinetic (PK) trial of CYC202, a novel oral cyclin-dependent kinase (CDK) inhibitor, in patients (pts) with advanced solid tumors. Proc Am Soc Clin Oncol 22: Abstr. 210
-
Pierga J, Faivre S, Vera K, Laurence V, Delbaldo C, Bekradda M, Armand JP, Gianella-Borradori A, Dieras V, Raymond E (2003) A phase I and pharmacokinetic (PK) trial of CYC202, a novel oral cyclin-dependent kinase (CDK) inhibitor, in patients (pts) with advanced solid tumors. Proc Am Soc Clin Oncol 22: Abstr. 210
-
-
-
-
17
-
-
23044439051
-
Seliciclib (CYC202 or R-roscovitine), a small-molecule cyclin-dependent kinase inhibitor, mediates activity via down-regulation of Mcl-1 in multiple myeloma
-
Raje N, Kumar S, Hideshima T, Roccaro A, Ishitsuka K, Yasui H, Shiraishi N, Chauhan D, Munshi NC, Green SR, Anderson KC (2005) Seliciclib (CYC202 or R-roscovitine), a small-molecule cyclin-dependent kinase inhibitor, mediates activity via down-regulation of Mcl-1 in multiple myeloma. Blood 106: 1042-1047
-
(2005)
Blood
, vol.106
, pp. 1042-1047
-
-
Raje, N.1
Kumar, S.2
Hideshima, T.3
Roccaro, A.4
Ishitsuka, K.5
Yasui, H.6
Shiraishi, N.7
Chauhan, D.8
Munshi, N.C.9
Green, S.R.10
Anderson, K.C.11
-
18
-
-
4444334494
-
Cassette dosing pharmacokinetics of a library of 2, 6, 9-trisubstituted purine cyclin-dependent kinase 2 inhibitors by parallel synthesis
-
Raynaud FI, Fischer PM, Nutley BP, Goddard PM, Lane DP, Workman P (2004) Cassette dosing pharmacokinetics of a library of 2, 6, 9-trisubstituted purine cyclin-dependent kinase 2 inhibitors by parallel synthesis. Mol Cancer Ther 3: 353-362
-
(2004)
Mol Cancer Ther
, vol.3
, pp. 353-362
-
-
Raynaud, F.I.1
Fischer, P.M.2
Nutley, B.P.3
Goddard, P.M.4
Lane, D.P.5
Workman, P.6
-
19
-
-
27644591251
-
In vitro and in vivo pharmacokinetic-pharmacodynamic relationships for the trisubstituted aminopurine cyclin-dependent kinase inhibitors olomoucine, bohemine and CYC202
-
Raynaud FI, Whittaker SR, Fischer PM, McClue S, Walton MI, Barrie SE, Garrett MD, Rogers P, Clarke SJ, Kelland LR, Valenti M, Brunton L, Eccles S, Lane DP, Workman P (2005) In vitro and in vivo pharmacokinetic-pharmacodynamic relationships for the trisubstituted aminopurine cyclin-dependent kinase inhibitors olomoucine, bohemine and CYC202. Clin Cancer Res 11: 4875-4887
-
(2005)
Clin Cancer Res
, vol.11
, pp. 4875-4887
-
-
Raynaud, F.I.1
Whittaker, S.R.2
Fischer, P.M.3
McClue, S.4
Walton, M.I.5
Barrie, S.E.6
Garrett, M.D.7
Rogers, P.8
Clarke, S.J.9
Kelland, L.R.10
Valenti, M.11
Brunton, L.12
Eccles, S.13
Lane, D.P.14
Workman, P.15
-
20
-
-
0036220822
-
Complexities in the development of cyclin-dependent kinase inhibitor drugs
-
Sausville EA (2002) Complexities in the development of cyclin-dependent kinase inhibitor drugs. Trends Mol Med 8(Suppl 4): S32-S37
-
(2002)
Trends Mol Med
, vol.8
, Issue.SUPPL. 4
-
-
Sausville, E.A.1
-
21
-
-
0035871444
-
Phase I trial of 72-h continuous infusion UCN-01 in patients with refractory neoplasms
-
Sausville EA, Arbuck SG, Messmann R, Headlee D, Bauer KS, Lush RM, Murgo A, Figg WD, Lahusen T, Jaken S, Jing X, Roberge M, Fuse E, Kuwabara T, Senderowicz AM (2001) Phase I trial of 72-h continuous infusion UCN-01 in patients with refractory neoplasms. J Clin Oncol 19: 2319-2333
-
(2001)
J Clin Oncol
, vol.19
, pp. 2319-2333
-
-
Sausville, E.A.1
Arbuck, S.G.2
Messmann, R.3
Headlee, D.4
Bauer, K.S.5
Lush, R.M.6
Murgo, A.7
Figg, W.D.8
Lahusen, T.9
Jaken, S.10
Jing, X.11
Roberge, M.12
Fuse, E.13
Kuwabara, T.14
Senderowicz, A.M.15
-
22
-
-
0031563780
-
The effect of the cyclin-dependent kinase inhibitor olomoucine on cell cycle kinetics
-
Schutte B, Nieland L, van Engeland M, Henfling ME, Meijer L, Ramaekers FC (1997) The effect of the cyclin-dependent kinase inhibitor olomoucine on cell cycle kinetics. Exp Cell Res 236: 4-15
-
(1997)
Exp Cell Res
, vol.236
, pp. 4-15
-
-
Schutte, B.1
Nieland, L.2
van Engeland, M.3
Henfling, M.E.4
Meijer, L.5
Ramaekers, F.C.6
-
23
-
-
0031670668
-
Phase I trial of continuous infusion flavopiridol, a novel cyclin-dependent kinase inhibitor, in patients with refractory neoplasms
-
Senderowicz AM, Headlee D, Stinson SF, Lush RM, Kalil N, Villalba L, Hill K, Steinberg SM, Figg WD, Tompkins A, Arbuck SG, Sausville EA (1998) Phase I trial of continuous infusion flavopiridol, a novel cyclin-dependent kinase inhibitor, in patients with refractory neoplasms. J Clin Oncol 16: 2986-2999
-
(1998)
J Clin Oncol
, vol.16
, pp. 2986-2999
-
-
Senderowicz, A.M.1
Headlee, D.2
Stinson, S.F.3
Lush, R.M.4
Kalil, N.5
Villalba, L.6
Hill, K.7
Steinberg, S.M.8
Figg, W.D.9
Tompkins, A.10
Arbuck, S.G.11
Sausville, E.A.12
-
24
-
-
4143122204
-
Phase I trial of the cyclin-dependent kinase inhibitor flavopiridol in combination with docetaxel in patients with metastatic breast cancer
-
Tan AR, Yang X, Berman A, Zhai S, Sparreboom A, Parr AL, Chow C, Brahim JS, Steinberg SM, Figg WD, Swain SM (2004) Phase I trial of the cyclin-dependent kinase inhibitor flavopiridol in combination with docetaxel in patients with metastatic breast cancer. Clin Cancer Res 10: 5038-5047
-
(2004)
Clin Cancer Res
, vol.10
, pp. 5038-5047
-
-
Tan, A.R.1
Yang, X.2
Berman, A.3
Zhai, S.4
Sparreboom, A.5
Parr, A.L.6
Chow, C.7
Brahim, J.S.8
Steinberg, S.M.9
Figg, W.D.10
Swain, S.M.11
-
25
-
-
24744461692
-
Crystal structure of pyridoxal kinase in complex with roscovitine and derivatives
-
Tang L, Li MH, Cao P, Wang F, Chang WR, Bach S, Reinhardt J, Ferandin Y, Galons H, Wan Y, Gray N, Meijer L, Jiang T, Liang DC (2005) Crystal structure of pyridoxal kinase in complex with roscovitine and derivatives. J Biol Chem 280: 31220-31229
-
(2005)
J Biol Chem
, vol.280
, pp. 31220-31229
-
-
Tang, L.1
Li, M.H.2
Cao, P.3
Wang, F.4
Chang, W.R.5
Bach, S.6
Reinhardt, J.7
Ferandin, Y.8
Galons, H.9
Wan, Y.10
Gray, N.11
Meijer, L.12
Jiang, T.13
Liang, D.C.14
-
26
-
-
0041327168
-
Proliferation of cancer cells despite CDK2 inhibition
-
Tetsu O, McCormick F (2003) Proliferation of cancer cells despite CDK2 inhibition. Cancer Cell 3: 233-245
-
(2003)
Cancer Cell
, vol.3
, pp. 233-245
-
-
Tetsu, O.1
McCormick, F.2
-
27
-
-
0036450831
-
Phase I clinical and pharmacokinetic trial of the cyclin-dependent kinase inhibitor flavopiridol
-
Thomas JP, Tutsch KD, Cleary JF, Bailey HH, Arzoomanian R, Alberti D, Simon K, Feierabend C, Binger K, Marnoch R, Dresen A, Wilding G (2002) Phase I clinical and pharmacokinetic trial of the cyclin-dependent kinase inhibitor flavopiridol. Cancer Chemother Pharmacol 50: 465-472
-
(2002)
Cancer Chemother Pharmacol
, vol.50
, pp. 465-472
-
-
Thomas, J.P.1
Tutsch, K.D.2
Cleary, J.F.3
Bailey, H.H.4
Arzoomanian, R.5
Alberti, D.6
Simon, K.7
Feierabend, C.8
Binger, K.9
Marnoch, R.10
Dresen, A.11
Wilding, G.12
-
28
-
-
20344371466
-
Stability, pKa and plasma protein binding of roscovitine
-
Vita M, Abdel-Rehim M, Nilsson C, Hassan Z, Skansen P, Wan H, Meurling L, Hassan M (2005) Stability, pKa and plasma protein binding of roscovitine. J Chromatogr B Analyt Technol Biomed Life Sci 821: 75-80
-
(2005)
J Chromatogr B Analyt Technol Biomed Life Sci
, vol.821
, pp. 75-80
-
-
Vita, M.1
Abdel-Rehim, M.2
Nilsson, C.3
Hassan, Z.4
Skansen, P.5
Wan, H.6
Meurling, L.7
Hassan, M.8
-
29
-
-
1642494839
-
The cyclin-dependent kinase inhibitor CYC202 (R-roscovitine) inhibits RB phosphorylation, causes loss of cyclin D1 and activates the mitogen activated protein kinase pathway
-
Whittaker SR, Walton MI, Garrett MD, Workman P (2004) The cyclin-dependent kinase inhibitor CYC202 (R-roscovitine) inhibits RB phosphorylation, causes loss of cyclin D1 and activates the mitogen activated protein kinase pathway. Cancer Res 64: 262-272
-
(2004)
Cancer Res
, vol.64
, pp. 262-272
-
-
Whittaker, S.R.1
Walton, M.I.2
Garrett, M.D.3
Workman, P.4
|