메뉴 건너뛰기




Volumn 18, Issue 3, 2008, Pages 253-274

Therapeutic potential of mitotic kinesin inhibitors in cancer

Author keywords

Antimitotic; Cancer; CENP E; Centromere associated protein E; Eg5; Inhibitor; Kinesin spindle protein; KSP; Mitotic kinesin

Indexed keywords

1,2,4 OXADIAZIN 5(6H) ONE; 1,2,4 OXADIAZOL 5 ONE; 4H PYRANO[2,3 B]PYRIDINE 4 ONE; 5 OXOHEXAHYDROPYRANO[4,3 D]PYRIMIDIN 2 THIONE; 5 OXOHEXAHYDROPYRIDO[4,3 D]PYRIMIDIN 2 THIONE; ADENOSINE TRIPHOSPHATASE; ANTINEOPLASTIC AGENT; ARRY 520; CENTROMERE PROTEIN E; EMD 534085; ENASTRON; GSK 923295; IMIDAZOLIN 2 ONE; ISOQUINOLIN 1 ONE; ISOXAZOLO[4,5 D]PYRIMIDINE DERIVATIVE; ISPINESIB; KINESIN; KINESIN SPINDLE PROTEIN; MITOTIC KINESIN INHIBITOR; MK 0731; MON 97; MONASTROL; OXAZOLIN 2 ONE; PROTEIN INHIBITOR; PYRIDO[1,2 A]PYRIMIDIN 4 ONE; SB 743921; TETRAHYDROPYRIDO[1,2 A]PYRIMIDIN 4 ONE; THIENO[3,2 D]PYRIMIDIN 4 ONE; UNCLASSIFIED DRUG; UNINDEXED DRUG; VS 83;

EID: 42549100037     PISSN: 13543776     EISSN: None     Source Type: Journal    
DOI: 10.1517/13543776.18.3.253     Document Type: Review
Times cited : (21)

References (186)
  • 1
    • 24344465919 scopus 로고    scopus 로고
    • Analysis of the kinesin superfamily: Insights into structure and function
    • Miki H, Okada Y, Hirokawa N. Analysis of the kinesin superfamily: insights into structure and function. Trends Cell Biol 2005;15:467-76
    • (2005) Trends Cell Biol , vol.15 , pp. 467-476
    • Miki, H.1    Okada, Y.2    Hirokawa, N.3
  • 3
    • 0035146128 scopus 로고    scopus 로고
    • The spindle: A dynamic assembly of microtubules and motors
    • Wittmann T, Hyman A, Desai A. The spindle: a dynamic assembly of microtubules and motors. Nat Cell Biol 2001;3:E28-34
    • (2001) Nat Cell Biol , vol.3
    • Wittmann, T.1    Hyman, A.2    Desai, A.3
  • 4
    • 0034682703 scopus 로고    scopus 로고
    • Motor function in the mitotic spindle
    • Heald R. Motor function in the mitotic spindle. Cell 2000;102:399-402
    • (2000) Cell , vol.102 , pp. 399-402
    • Heald, R.1
  • 6
    • 33646380571 scopus 로고    scopus 로고
    • Mitotic kinesins as targets for anticancer therapy
    • Belmont LD. Mitotic kinesins as targets for anticancer therapy. AACR Educ Book 2005;173-7
    • (2005) AACR Educ Book , pp. 173-177
    • Belmont, L.D.1
  • 7
    • 34548814434 scopus 로고    scopus 로고
    • Mitotic drug targets and the development of novel anti-mitotic anticancer drugs
    • Schmidt M, Bastians H. Mitotic drug targets and the development of novel anti-mitotic anticancer drugs. Drug Resist Update 2007;10:162-81
    • (2007) Drug Resist Update , vol.10 , pp. 162-181
    • Schmidt, M.1    Bastians, H.2
  • 8
    • 0026739078 scopus 로고
    • Mitotic spindle organization by a plus-end-directed microtubule motor
    • Sawin KE, Leguellec K, Philippe M, Mitchison TJ. Mitotic spindle organization by a plus-end-directed microtubule motor. Nature 1992;359:540-3
    • (1992) Nature , vol.359 , pp. 540-543
    • Sawin, K.E.1    Leguellec, K.2    Philippe, M.3    Mitchison, T.J.4
  • 10
    • 0029417238 scopus 로고
    • Phosphorylation by p34cdc2 regulates spindle association of human Eg5, a kinesin-related motor essential for bipolar spindle formation in vivo
    • Blangy A, Lane HA, D'Herin P, et al. Phosphorylation by p34cdc2 regulates spindle association of human Eg5, a kinesin-related motor essential for bipolar spindle formation in vivo. Cell 1995;83:1159-69
    • (1995) Cell , vol.83 , pp. 1159-1169
    • Blangy, A.1    Lane, H.A.2    D'Herin, P.3
  • 11
    • 18344371892 scopus 로고    scopus 로고
    • The bipolar mitotic kinesin Eg5 moves on both microtubules that it crosslinks
    • Kapitein LC, Peterman EJ, Kwok BH, et al. The bipolar mitotic kinesin Eg5 moves on both microtubules that it crosslinks. Nature 2005;435:114-8
    • (2005) Nature , vol.435 , pp. 114-118
    • Kapitein, L.C.1    Peterman, E.J.2    Kwok, B.H.3
  • 12
    • 22244459880 scopus 로고    scopus 로고
    • Induction of apoptosis by an inhibitor of the mitotic kinesin KSP requires both activation of the spindle assembly checkpoint and mitotic slippage
    • Tao W, South VJ, Zhang Y, et al. Induction of apoptosis by an inhibitor of the mitotic kinesin KSP requires both activation of the spindle assembly checkpoint and mitotic slippage. Cancer Cell 2005;8:49-59
    • (2005) Cancer Cell , vol.8 , pp. 49-59
    • Tao, W.1    South, V.J.2    Zhang, Y.3
  • 13
    • 22244478043 scopus 로고    scopus 로고
    • Decoding the links between mitosis, cancer, and chemotherapy: The mitotic checkpoint, adaptation, and cell death
    • Weaver BA, Cleveland DW. Decoding the links between mitosis, cancer, and chemotherapy: the mitotic checkpoint, adaptation, and cell death. Cancer Cell 2005;8:7-12
    • (2005) Cancer Cell , vol.8 , pp. 7-12
    • Weaver, B.A.1    Cleveland, D.W.2
  • 14
    • 33846172672 scopus 로고    scopus 로고
    • An inhibitor of the kinesin spindle protein activates the intrinsic apoptotic pathway independently of p53 and de novo protein synthesis
    • Tao W, South VJ, Diehl RE, et al. An inhibitor of the kinesin spindle protein activates the intrinsic apoptotic pathway independently of p53 and de novo protein synthesis. Mol Cell Biol 2007;27:689-98
    • (2007) Mol Cell Biol , vol.27 , pp. 689-698
    • Tao, W.1    South, V.J.2    Diehl, R.E.3
  • 15
    • 0034605123 scopus 로고    scopus 로고
    • Probing spindle assembly mechanisms with monastrol, a small molecule inhibitor of the mitotic kinesin, Eg5
    • Kapoor TM, Mayer TU, Coughlin ML, Mitchison TJ. Probing spindle assembly mechanisms with monastrol, a small molecule inhibitor of the mitotic kinesin, Eg5. J Cell Biol 2000;150:975-88
    • (2000) J Cell Biol , vol.150 , pp. 975-988
    • Kapoor, T.M.1    Mayer, T.U.2    Coughlin, M.L.3    Mitchison, T.J.4
  • 16
    • 0025782910 scopus 로고
    • CENP-E, a novel human centromere-associated protein required for progression from metaphase to anaphase
    • Yen TJ, Compton DA, Wise D, et al. CENP-E, a novel human centromere-associated protein required for progression from metaphase to anaphase. EMBO J 1991;10:1245-54
    • (1991) EMBO J , vol.10 , pp. 1245-1254
    • Yen, T.J.1    Compton, D.A.2    Wise, D.3
  • 17
    • 0026767624 scopus 로고
    • CENP-E is a putative kinetochore motor that accumulates just before mitosis
    • Yen TJ, Li G, Schaar BT, et al. CENP-E is a putative kinetochore motor that accumulates just before mitosis. Nature 1992;359:536-9
    • (1992) Nature , vol.359 , pp. 536-539
    • Yen, T.J.1    Li, G.2    Schaar, B.T.3
  • 18
    • 0030665077 scopus 로고    scopus 로고
    • CENP-E is a plus end-directed kinetochore motor required for metaphase chromosome alignment
    • Wood KW, Sakowicz R, Goldstein LS, Cleveland DW. CENP-E is a plus end-directed kinetochore motor required for metaphase chromosome alignment. Cell 1997;91:357-66
    • (1997) Cell , vol.91 , pp. 357-366
    • Wood, K.W.1    Sakowicz, R.2    Goldstein, L.S.3    Cleveland, D.W.4
  • 19
    • 0030347061 scopus 로고    scopus 로고
    • Modulation of CENP-E organization at kinetochores by spindle microtubule attachment
    • Thrower DA, Jordan MA, Wilson L. Modulation of CENP-E organization at kinetochores by spindle microtubule attachment. Cell Motil Cytoskel 1996;35:121-33
    • (1996) Cell Motil Cytoskel , vol.35 , pp. 121-133
    • Thrower, D.A.1    Jordan, M.A.2    Wilson, L.3
  • 20
    • 0035958945 scopus 로고    scopus 로고
    • Purification and characterization of native conventional kinesin, HSET, and CENP-E from mitotic HeLa cells
    • Deluca JG, Newton CN, Himes RH, et al. Purification and characterization of native conventional kinesin, HSET, and CENP-E from mitotic HeLa cells. J Biol Chem 2001;276:28014-21
    • (2001) J Biol Chem , vol.276 , pp. 28014-28021
    • Deluca, J.G.1    Newton, C.N.2    Himes, R.H.3
  • 21
    • 3242771433 scopus 로고    scopus 로고
    • Crystal structure of the motor domain of the human kinetochore protein CENP-E
    • Garcia-Saez I, Yen T, Wade RH, Kozielski F. Crystal structure of the motor domain of the human kinetochore protein CENP-E. J Mol Biol 2004;340:1107-16
    • (2004) J Mol Biol , vol.340 , pp. 1107-1116
    • Garcia-Saez, I.1    Yen, T.2    Wade, R.H.3    Kozielski, F.4
  • 22
    • 33747805355 scopus 로고    scopus 로고
    • Human kinetochore-associated kinesin CENP-E visualized at 17 Å resolution bound to microtubules
    • Neumann I, Garcia-Saez S, Debonis R, et al. Human kinetochore-associated kinesin CENP-E visualized at 17 Å resolution bound to microtubules. J Mol Biol 2006;362:203-11
    • (2006) J Mol Biol , vol.362 , pp. 203-211
    • Neumann, I.1    Garcia-Saez, S.2    Debonis, R.3
  • 23
    • 0029903059 scopus 로고    scopus 로고
    • The kinesin-like protein CENP-E is kinetochoreassociated throughout poleward chromosome segregation during anaphase-A
    • Brown KD, Wood KW, Cleveland DW. The kinesin-like protein CENP-E is kinetochoreassociated throughout poleward chromosome segregation during anaphase-A. J Cell Sci 1996;109:961-9
    • (1996) J Cell Sci , vol.109 , pp. 961-969
    • Brown, K.D.1    Wood, K.W.2    Cleveland, D.W.3
  • 24
    • 0001665802 scopus 로고    scopus 로고
    • CENP-E forms a link between attachment of spindle microtubules to kinetochores and the mitotic checkpoint
    • Yao X, Abrieu A, Zheng Y, et al. CENP-E forms a link between attachment of spindle microtubules to kinetochores and the mitotic checkpoint. Nat Cell Biol 2000;2:484-91
    • (2000) Nat Cell Biol , vol.2 , pp. 484-491
    • Yao, X.1    Abrieu, A.2    Zheng, Y.3
  • 25
    • 0036744787 scopus 로고    scopus 로고
    • Unstable kinetochore-microtubule capture and chromosomal instability following deletion of CENP-E
    • Putkey FR, Cramer T, Morphew MK, et al. Unstable kinetochore-microtubule capture and chromosomal instability following deletion of CENP-E. Dev Cell 2002;3:351-65
    • (2002) Dev Cell , vol.3 , pp. 351-365
    • Putkey, F.R.1    Cramer, T.2    Morphew, M.K.3
  • 26
    • 0034664766 scopus 로고    scopus 로고
    • CENP-E as an essential component of the mitotic checkpoint in vitro
    • Abrieu A, Kahana JA, Wood KW, Cleveland DW. CENP-E as an essential component of the mitotic checkpoint in vitro. Cell 2000;102:817-26
    • (2000) Cell , vol.102 , pp. 817-826
    • Abrieu, A.1    Kahana, J.A.2    Wood, K.W.3    Cleveland, D.W.4
  • 27
    • 0038446875 scopus 로고    scopus 로고
    • Activating and silencing the mitotic checkpoint through CENP-E-dependent activation/inactivation of BubR1
    • Mao Y, Abrieu A, Cleveland DW. Activating and silencing the mitotic checkpoint through CENP-E-dependent activation/inactivation of BubR1. Cell 2003;114:87-98
    • (2003) Cell , vol.114 , pp. 87-98
    • Mao, Y.1    Abrieu, A.2    Cleveland, D.W.3
  • 28
    • 3343013148 scopus 로고    scopus 로고
    • Gene silencing of CENP-E by small interfering RNA in HeLa cells leads to missegregation of chromosomes after a mitotic delay
    • Tanudji M, Shoemaker J, L'Italien L, et al. Gene silencing of CENP-E by small interfering RNA in HeLa cells leads to missegregation of chromosomes after a mitotic delay. Mol Biol Cell 2004;15:3771-81
    • (2004) Mol Biol Cell , vol.15 , pp. 3771-3781
    • Tanudji, M.1    Shoemaker, J.2    L'Italien, L.3
  • 29
    • 0033615357 scopus 로고    scopus 로고
    • Small molecule inhibitor of mitotic spindle bipolarity identified in a phenotype-based screen
    • Mayer TU, Kapoor TM, Haggarty SJ, et al. Small molecule inhibitor of mitotic spindle bipolarity identified in a phenotype-based screen. Science 1999;286:971-4
    • (1999) Science , vol.286 , pp. 971-974
    • Mayer, T.U.1    Kapoor, T.M.2    Haggarty, S.J.3
  • 30
    • 10744220712 scopus 로고    scopus 로고
    • Inhibition of a mitotic motor protein: Where, how, and conformational consequences
    • Yan Y, Sardana V, Xu B, et al. Inhibition of a mitotic motor protein: where, how, and conformational consequences. J Mol Biol 2004;335:547-54
    • (2004) J Mol Biol , vol.335 , pp. 547-554
    • Yan, Y.1    Sardana, V.2    Xu, B.3
  • 31
    • 0037457808 scopus 로고    scopus 로고
    • Interaction of the mitotic inhibitor monastrol with human kinesin Eg5
    • Debonis S, Simorre J-P, Crevel I, et al. Interaction of the mitotic inhibitor monastrol with human kinesin Eg5. Biochemistry 2003;42:338-49
    • (2003) Biochemistry , vol.42 , pp. 338-349
    • Debonis, S.1    Simorre, J.-P.2    Crevel, I.3
  • 32
    • 0036752261 scopus 로고    scopus 로고
    • Evidence that monastrol is an allosteric inhibitor of the mitotic kinesin Eg5
    • Maliga Z, Kapoor TM, Mitchison TJ. Evidence that monastrol is an allosteric inhibitor of the mitotic kinesin Eg5. Chem Biol 2002;9:989-96
    • (2002) Chem Biol , vol.9 , pp. 989-996
    • Maliga, Z.1    Kapoor, T.M.2    Mitchison, T.J.3
  • 33
    • 17144405643 scopus 로고    scopus 로고
    • Mitotic kinesins: Prospects for antimitotic drug discovery
    • Bergnes G, Brejc K, Belmont L. Mitotic kinesins: prospects for antimitotic drug discovery. Curr Top Med Chem 2005;5:127-45
    • (2005) Curr Top Med Chem , vol.5 , pp. 127-145
    • Bergnes, G.1    Brejc, K.2    Belmont, L.3
  • 34
    • 21444449874 scopus 로고    scopus 로고
    • Inhibitors of kinesin motor proteins: Research and clinical progress
    • Duhl DM, Renhowe PA. Inhibitors of kinesin motor proteins: research and clinical progress. Curr Opin Drug Discov Dev 2005;8:431-6
    • (2005) Curr Opin Drug Discov Dev , vol.8 , pp. 431-436
    • Duhl, D.M.1    Renhowe, P.A.2
  • 35
    • 20344403500 scopus 로고    scopus 로고
    • New cytotoxic agents: A review of the literature
    • Hotta K, Ueoka H. New cytotoxic agents: a review of the literature. Crit Rev Oncol Hematol 2005;55:45-65
    • (2005) Crit Rev Oncol Hematol , vol.55 , pp. 45-65
    • Hotta, K.1    Ueoka, H.2
  • 36
    • 25444501831 scopus 로고    scopus 로고
    • Development of a high-throughput robotic fluorescence-based assay for HsEg5 inhibitor screening
    • Zhang B, Senator D, Wilson CJ, Ng SC. Development of a high-throughput robotic fluorescence-based assay for HsEg5 inhibitor screening. Anal Biochem 2005;345:326-35
    • (2005) Anal Biochem , vol.345 , pp. 326-335
    • Zhang, B.1    Senator, D.2    Wilson, C.J.3    Ng, S.C.4
  • 37
    • 33645023929 scopus 로고    scopus 로고
    • Increased therapeutic potential of an experimental anti-mitotic inhibitor SB715992 by genistein in PC-3 human prostate cancer cell line
    • Davis DA, Sarkar SH, Hussain M, et al. Increased therapeutic potential of an experimental anti-mitotic inhibitor SB715992 by genistein in PC-3 human prostate cancer cell line. BMC Cancer 2006;6:22-32
    • (2006) BMC Cancer , vol.6 , pp. 22-32
    • Davis, D.A.1    Sarkar, S.H.2    Hussain, M.3
  • 38
    • 42549151864 scopus 로고    scopus 로고
    • Chu Q, Holen KD, Rowinsky EK, et al. A phase I study to determine the safety and pharmacokinetics of IV administered SB-715992, a novel kinesin spindle protein (KSP) inhibitor, in patients (pts) with solid tumors. Proc Am Soc Clin Oncol 2003;22:[Abstract 525]
    • Chu Q, Holen KD, Rowinsky EK, et al. A phase I study to determine the safety and pharmacokinetics of IV administered SB-715992, a novel kinesin spindle protein (KSP) inhibitor, in patients (pts) with solid tumors. Proc Am Soc Clin Oncol 2003;22:[Abstract 525]
  • 39
    • 42549104865 scopus 로고    scopus 로고
    • Rodon J, Till E, Patnaik A, et al. Phase I study of ispinesib (SB-715992), a kinesin spindle protein inhibitor, in combination with capecitabine in patients with advanced solid tumors. Eur J Cancer 2006;4:[Abstract 640]
    • Rodon J, Till E, Patnaik A, et al. Phase I study of ispinesib (SB-715992), a kinesin spindle protein inhibitor, in combination with capecitabine in patients with advanced solid tumors. Eur J Cancer 2006;4:[Abstract 640]
  • 40
    • 42549086102 scopus 로고    scopus 로고
    • A phase II study of ispinesib in patients (pts) with recurrent and/or metastatic head and neck squamous cell carcinoma (RMHNSC)
    • Abstract 600P
    • Tang P, Siu LL, Chen EX, et al. A phase II study of ispinesib in patients (pts) with recurrent and/or metastatic head and neck squamous cell carcinoma (RMHNSC). Ann Oncol 2006;17(S):[Abstract 600P]
    • (2006) Ann Oncol , vol.17 , Issue.S
    • Tang, P.1    Siu, L.L.2    Chen, E.X.3
  • 41
    • 42549139623 scopus 로고    scopus 로고
    • A second generation KSP inhibitor, SB-743921, is a highly potent and active therapeutic in preclinical models of cancer
    • Abstract B11
    • Jackson JR, Gilmartin A, Dhanak D, et al. A second generation KSP inhibitor, SB-743921, is a highly potent and active therapeutic in preclinical models of cancer. First Mol Diagn Cancer Ther Dev 2006;[Abstract B11]
    • (2006) First Mol Diagn Cancer Ther Dev
    • Jackson, J.R.1    Gilmartin, A.2    Dhanak, D.3
  • 42
    • 42549103528 scopus 로고    scopus 로고
    • Belmont LD, Wood KW, Sutton D, et al. Sequence dependent anti-tumor activity of bortezomib and the KSP inhibitor, SB743921, in a solid tumor xenograft model. Eur J Cancer 2006;4:[Abstract 378]
    • Belmont LD, Wood KW, Sutton D, et al. Sequence dependent anti-tumor activity of bortezomib and the KSP inhibitor, SB743921, in a solid tumor xenograft model. Eur J Cancer 2006;4:[Abstract 378]
  • 43
    • 42549137741 scopus 로고    scopus 로고
    • Holen KD, Belani CP, Wilding G, et al. Phase I study to determine tolerability and pharmacokinetics (PK) of SB-743921, a novel kinesin spindle protein (KSP) inhibitor. J Clin Oncol 2006;24:[Abstract 2000]
    • Holen KD, Belani CP, Wilding G, et al. Phase I study to determine tolerability and pharmacokinetics (PK) of SB-743921, a novel kinesin spindle protein (KSP) inhibitor. J Clin Oncol 2006;24:[Abstract 2000]
  • 44
    • 42549143895 scopus 로고    scopus 로고
    • A Phase I-II study to determine the safety and pharmacokinetics of intravenous administration of SB-743921 on days 1 and 15 of a 28 day cycle in patients with non-Hodgkin's lymphoma NCT00343564, ChnicalTrials.gov. 21 June 2006. Available at:, Last accessed 14 November 2007
    • A Phase I-II study to determine the safety and pharmacokinetics of intravenous administration of SB-743921 on days 1 and 15 of a 28 day cycle in patients with non-Hodgkin's lymphoma (NCT00343564). ChnicalTrials.gov. 21 June 2006. Available at: http://clinicaltrials.gov/ show/NCT00343564 [Last accessed 14 November 2007]
  • 45
    • 42549161334 scopus 로고    scopus 로고
    • Stein MN, Rubin EH, Scott PD, et al. Phase I clinical and pharmacokinetic (PK) trial of the kinesin spindle protein (KSP) inhibitor MK-0731 in cancer patients. J Clin Oncol 2006;24:[Abstract 2001]
    • Stein MN, Rubin EH, Scott PD, et al. Phase I clinical and pharmacokinetic (PK) trial of the kinesin spindle protein (KSP) inhibitor MK-0731 in cancer patients. J Clin Oncol 2006;24:[Abstract 2001]
  • 46
    • 42549132464 scopus 로고    scopus 로고
    • Stein MN, Tan A, Taber K, et al. Phase I clinical and pharmacokinetic (PK) trial of the kinesin spindle protein (KSP) inhibitor MK-0731 in patients with solid tumors. J Clin Oncol 2007;25:[Abstract 2548]
    • Stein MN, Tan A, Taber K, et al. Phase I clinical and pharmacokinetic (PK) trial of the kinesin spindle protein (KSP) inhibitor MK-0731 in patients with solid tumors. J Clin Oncol 2007;25:[Abstract 2548]
  • 47
    • 42549107262 scopus 로고    scopus 로고
    • A study of MK0731 in patients with advanced solid tumors (NCT104364). 25 February 2005. ClinicalTrials.gov. Available at: http://clinicaltrials.gov/ct2/show/NCT00104364?term=MK0731&rank=1 [Last accessed 14 November 2007]
    • A study of MK0731 in patients with advanced solid tumors (NCT104364). 25 February 2005. ClinicalTrials.gov. Available at: http://clinicaltrials.gov/ct2/show/NCT00104364?term=MK0731&rank=1 [Last accessed 14 November 2007]
  • 48
    • 42549161337 scopus 로고    scopus 로고
    • Array BioPharma reports full-year 2007 R&D highlights. Array Biopharma. press release. 6 August 2007. ClinicalTrials.gov. Available at: http://investor.arraybiopharma.com/phoenix.zhtml?c=123810&p= irol-newsArticle&[D=1037137&highlight [Last accessed 14 November 2007]
    • Array BioPharma reports full-year 2007 R&D highlights. Array Biopharma. press release. 6 August 2007. ClinicalTrials.gov. Available at: http://investor.arraybiopharma.com/phoenix.zhtml?c=123810&p= irol-newsArticle&[D=1037137&highlight [Last accessed 14 November 2007]
  • 49
    • 42549160307 scopus 로고    scopus 로고
    • Tolerability study of investigational agent, ARRY-520, in subjects with cancer (NCT00462358). 18 April 2007. ClinicalTrials.gov. Available at: http://clinicaltrials.gov/ct2/show/NCT00462358?term=ARRY-520&rank=1 [Last accessed 14 November 2007]
    • Tolerability study of investigational agent, ARRY-520, in subjects with cancer (NCT00462358). 18 April 2007. ClinicalTrials.gov. Available at: http://clinicaltrials.gov/ct2/show/NCT00462358?term=ARRY-520&rank=1 [Last accessed 14 November 2007]
  • 50
    • 42549143427 scopus 로고    scopus 로고
    • Merck KGaA reports Q3 2007 R&D highlights. Merck KGaA press release. 24 October 2007. Available at: http://www.merck.de/servlet/PB/show/ 1755050/Merck_Q3_2007_handout_portfolio_review.pdf [Last accessed 14 November 2007]
    • Merck KGaA reports Q3 2007 R&D highlights. Merck KGaA press release. 24 October 2007. Available at: http://www.merck.de/servlet/PB/show/ 1755050/Merck_Q3_2007_handout_portfolio_review.pdf [Last accessed 14 November 2007]
  • 51
    • 42549103030 scopus 로고    scopus 로고
    • Detailed biochemical analysis of the CENP-E inhibitor GSK923295A
    • Abstract 3179
    • Lad L, Luo L, Wood K, et al. Detailed biochemical analysis of the CENP-E inhibitor GSK923295A. Proc Am Assoc Cancer Res 2007;48:[Abstract 3179]
    • (2007) Proc Am Assoc Cancer Res , vol.48
    • Lad, L.1    Luo, L.2    Wood, K.3
  • 52
    • 70349844338 scopus 로고    scopus 로고
    • GSK923295A, a potent and selective CENP-E inhibitor, has broad spectrum activity against human tumor xenografts in nude mice
    • Abstract 1522
    • Sutton D, Diamond M, Faucette L, et al. GSK923295A, a potent and selective CENP-E inhibitor, has broad spectrum activity against human tumor xenografts in nude mice. Proc Am Assoc Cancer Res 2007;48:[Abstract 1522]
    • (2007) Proc Am Assoc Cancer Res , vol.48
    • Sutton, D.1    Diamond, M.2    Faucette, L.3
  • 53
    • 42549136326 scopus 로고    scopus 로고
    • Phase I study to assess the safety, pharmacokinetics & pharmacodynamics of GSK923295 in subjects with refractory cancer (NCT00504790). ClinicalTrials.gov. 18 July 2007. Available at: http://clinicaltrials.gov/ct2/show/NCT00504790?term=GSK923295&rank=1 [Last accessed 14 November 2007]
    • Phase I study to assess the safety, pharmacokinetics & pharmacodynamics of GSK923295 in subjects with refractory cancer (NCT00504790). ClinicalTrials.gov. 18 July 2007. Available at: http://clinicaltrials.gov/ct2/show/NCT00504790?term=GSK923295&rank=1 [Last accessed 14 November 2007]
  • 54
    • 10344242934 scopus 로고    scopus 로고
    • Inhibitors of the mitotic kinesin spindle protein
    • Coleman PJ, Fraley ME. Inhibitors of the mitotic kinesin spindle protein. Expert Opin Ther Patents 2004;14:1659-67
    • (2004) Expert Opin Ther Patents , vol.14 , pp. 1659-1667
    • Coleman, P.J.1    Fraley, M.E.2
  • 55
    • 33751222838 scopus 로고    scopus 로고
    • Kinesin spindle protein inhibitors as anticancer agents
    • Jiang C, You Q, Li Z, Guo Q. Kinesin spindle protein inhibitors as anticancer agents. Expert Opin Ther Patents 2006;16:1517-32
    • (2006) Expert Opin Ther Patents , vol.16 , pp. 1517-1532
    • Jiang, C.1    You, Q.2    Li, Z.3    Guo, Q.4
  • 56
    • 42549097294 scopus 로고    scopus 로고
    • Commissariat Á L'énergie Atomique. WO2006097617; 2006
    • Commissariat Á L'énergie Atomique. WO2006097617; 2006
  • 57
    • 34248158214 scopus 로고    scopus 로고
    • Structure of human Eg5 in complex with a new monastrol-based inhibitor bound in the R configuration
    • Garcia-Saez I, Debonis S, Lopez R, et al. Structure of human Eg5 in complex with a new monastrol-based inhibitor bound in the R configuration. J Biol Chem 2007;282:9740-7
    • (2007) J Biol Chem , vol.282 , pp. 9740-9747
    • Garcia-Saez, I.1    Debonis, S.2    Lopez, R.3
  • 58
    • 42549141038 scopus 로고    scopus 로고
    • Leipzig University/Max-Planck Institute. WO2006048308; 2006
    • Leipzig University/Max-Planck Institute. WO2006048308; 2006
  • 59
    • 22144463476 scopus 로고    scopus 로고
    • Development and biological evaluation of potent and specific inhibitors of mitotic kinesin Eg5
    • Gartner M, Sunder-Plassmann N, Seiler J, et al. Development and biological evaluation of potent and specific inhibitors of mitotic kinesin Eg5. Chem Biochem 2005;6:1173-7
    • (2005) Chem Biochem , vol.6 , pp. 1173-1177
    • Gartner, M.1    Sunder-Plassmann, N.2    Seiler, J.3
  • 60
    • 27744596104 scopus 로고    scopus 로고
    • Synthesis and biological evaluation of novel Eg5 inhibitors
    • Sarli V, Huemmer S, Sunder-Plassmann N, et al. Synthesis and biological evaluation of novel Eg5 inhibitors. Chem Biochem 2005;6:2005-13
    • (2005) Chem Biochem , vol.6 , pp. 2005-2013
    • Sarli, V.1    Huemmer, S.2    Sunder-Plassmann, N.3
  • 61
    • 42549164964 scopus 로고    scopus 로고
    • Harvard University. WO2006074293; 2006
    • Harvard University. WO2006074293; 2006
  • 63
    • 0037136153 scopus 로고    scopus 로고
    • Improved synthesis and preparative scale resolution of racemic monastrol
    • Dondoni A, Massi A, Sabbatini S. Improved synthesis and preparative scale resolution of racemic monastrol. Tetrahedron Lett 2002;43:5913-6
    • (2002) Tetrahedron Lett , vol.43 , pp. 5913-5916
    • Dondoni, A.1    Massi, A.2    Sabbatini, S.3
  • 64
    • 28444438118 scopus 로고    scopus 로고
    • Highly enantioseletive Biginelli reaction using a new chiral ytterbium catalyst: Asymmetric synthesis of dihydropyrimidines
    • Huang Y, Yang F, Zhu C. Highly enantioseletive Biginelli reaction using a new chiral ytterbium catalyst: asymmetric synthesis of dihydropyrimidines. J Am Chem Soc 2005;127:16386-7
    • (2005) J Am Chem Soc , vol.127 , pp. 16386-16387
    • Huang, Y.1    Yang, F.2    Zhu, C.3
  • 65
    • 33845205051 scopus 로고    scopus 로고
    • Highly enantioselective organocatalytic Biginelli reaction
    • Chen XH, Xu XY, Liu H, et al. Highly enantioselective organocatalytic Biginelli reaction. J Am Chem Soc 2006;128:14802-3
    • (2006) J Am Chem Soc , vol.128 , pp. 14802-14803
    • Chen, X.H.1    Xu, X.Y.2    Liu, H.3
  • 66
    • 34547700231 scopus 로고    scopus 로고
    • New chemical tools for investigating human mitotic kinesin Eg5
    • Klein E, Debonis S, Thiede B, et al. New chemical tools for investigating human mitotic kinesin Eg5. Bioorg Med Chem 2007;15:6474-88
    • (2007) Bioorg Med Chem , vol.15 , pp. 6474-6488
    • Klein, E.1    Debonis, S.2    Thiede, B.3
  • 67
    • 42549098877 scopus 로고    scopus 로고
    • Cytokinetics. WO2004100873; 2004
    • Cytokinetics. WO2004100873; 2004
  • 68
    • 42549166875 scopus 로고    scopus 로고
    • Cytokinetics. WO2004103282; 2004
    • Cytokinetics. WO2004103282; 2004
  • 69
    • 42549149193 scopus 로고    scopus 로고
    • Cytokinetics. WO2005013888; 2005
    • Cytokinetics. WO2005013888; 2005
  • 70
    • 42549137249 scopus 로고    scopus 로고
    • Cytokinetics. WO2004091547; 2004
    • Cytokinetics. WO2004091547; 2004
  • 71
    • 42549094402 scopus 로고    scopus 로고
    • Cytokinetics. WO2005061460; 2005
    • Cytokinetics. WO2005061460; 2005
  • 72
    • 42549142766 scopus 로고    scopus 로고
    • Cytokinetics. WO2005042697; 2005
    • Cytokinetics. WO2005042697; 2005
  • 73
    • 42549098237 scopus 로고    scopus 로고
    • Cytokinetics. WO2007067752; 2007
    • Cytokinetics. WO2007067752; 2007
  • 74
    • 42549106299 scopus 로고    scopus 로고
    • Chiron. WO2004111058; 2004
    • Chiron. WO2004111058; 2004
  • 75
    • 42549172217 scopus 로고    scopus 로고
    • Chiron. WO2004113335; 2004
    • Chiron. WO2004113335; 2004
  • 76
    • 42549164967 scopus 로고    scopus 로고
    • Chiron. WO2005100357; 2005
    • Chiron. WO2005100357; 2005
  • 77
    • 42549105837 scopus 로고    scopus 로고
    • Cytokinetics. WO2004064741; 2004
    • Cytokinetics. WO2004064741; 2004
  • 78
    • 42549109846 scopus 로고    scopus 로고
    • Chiron. WO2006002236; 2006
    • Chiron. WO2006002236; 2006
  • 79
    • 42549161801 scopus 로고    scopus 로고
    • Chiron. WO2006049835; 2006
    • Chiron. WO2006049835; 2006
  • 80
    • 42549136327 scopus 로고    scopus 로고
    • Takeda WO2006060737; 2006
    • Takeda WO2006060737; 2006
  • 81
    • 42549142440 scopus 로고    scopus 로고
    • AstraZeneca. WO2006018627; 2006
    • AstraZeneca. WO2006018627; 2006
  • 82
    • 42549085537 scopus 로고    scopus 로고
    • AstraZeneca. WO2006008523; 2006
    • AstraZeneca. WO2006008523; 2006
  • 83
    • 42549136799 scopus 로고    scopus 로고
    • AstraZeneca. WO2006018628; 2006
    • AstraZeneca. WO2006018628; 2006
  • 84
    • 2342563857 scopus 로고    scopus 로고
    • Antitumor activity of a kinesin inhibitor
    • Sakowicz R, Finer JT, Beraud C, et al. Antitumor activity of a kinesin inhibitor. Cancer Res 2004;64:3276-80
    • (2004) Cancer Res , vol.64 , pp. 3276-3280
    • Sakowicz, R.1    Finer, J.T.2    Beraud, C.3
  • 85
    • 42549171794 scopus 로고    scopus 로고
    • Merck KGaA. WO2006097176; 2006
    • Merck KGaA. WO2006097176; 2006
  • 86
    • 42549096369 scopus 로고    scopus 로고
    • BMS. WO2004106492; 2004
    • BMS. WO2004106492; 2004
  • 87
    • 42549149593 scopus 로고    scopus 로고
    • AstraZeneca. WO2004078758; 2004
    • AstraZeneca. WO2004078758; 2004
  • 88
    • 42549138714 scopus 로고    scopus 로고
    • BMS. WO2005077920; 2005
    • BMS. WO2005077920; 2005
  • 89
    • 42549167878 scopus 로고    scopus 로고
    • BMS. WO2003099286; 2003
    • BMS. WO2003099286; 2003
  • 90
    • 33745131839 scopus 로고    scopus 로고
    • Synthesis and SAR of pyrrolotriazine-4-one based Eg5 inhibitors
    • Kim KS, Lu S-F, Cornelius LA, et al. Synthesis and SAR of pyrrolotriazine-4-one based Eg5 inhibitors. Bioorg Med Chem Lett 2006;16:3937-42
    • (2006) Bioorg Med Chem Lett , vol.16 , pp. 3937-3942
    • Kim, K.S.1    Lu, S.-F.2    Cornelius, L.A.3
  • 91
    • 42549153198 scopus 로고    scopus 로고
    • Merck & Co. WO2005061518;
    • Merck & Co. WO2005061518; 2005
    • (2005)
  • 92
    • 42549166409 scopus 로고    scopus 로고
    • Merck & Co. WO2006078598;
    • Merck & Co. WO2006078598; 2006
    • (2006)
  • 93
    • 42549170911 scopus 로고    scopus 로고
    • Merck & Co. WO2006078575;
    • Merck & Co. WO2006078575; 2006
    • (2006)
  • 94
    • 42549170458 scopus 로고    scopus 로고
    • Merck & Co. WO2006078574;
    • Merck & Co. WO2006078574; 2006
    • (2006)
  • 95
    • 42549135290 scopus 로고    scopus 로고
    • AstraZeneca. WO2005041888; 2005
    • AstraZeneca. WO2005041888; 2005
  • 96
    • 42549159815 scopus 로고    scopus 로고
    • Cytokinetics. WO2004009036; 2004
    • Cytokinetics. WO2004009036; 2004
  • 97
    • 42549147816 scopus 로고    scopus 로고
    • Cytokinetics/GSK. WO2004055008; 2004
    • Cytokinetics/GSK. WO2004055008; 2004
  • 98
    • 42549083682 scopus 로고    scopus 로고
    • Merck & Co. WO2003039460;
    • Merck & Co. WO2003039460; 2003
    • (2003)
  • 99
    • 42549156976 scopus 로고    scopus 로고
    • Merck KGaA. WO2006125555; 2006
    • Merck KGaA. WO2006125555; 2006
  • 100
    • 42549096859 scopus 로고    scopus 로고
    • Chiron. WO2005051922; 2005
    • Chiron. WO2005051922; 2005
  • 101
    • 42549139234 scopus 로고    scopus 로고
    • Chiron. WO2007021794; 2007
    • Chiron. WO2007021794; 2007
  • 102
    • 20144388363 scopus 로고    scopus 로고
    • Kinesin spindle protein (KSP) inhibitors. Part 1: The discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of the mitotic kinesin KSP
    • Cox CD, Breslin MJ, Mariano BJ, et al. Kinesin spindle protein (KSP) inhibitors. Part 1: the discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of the mitotic kinesin KSP. Bioorg Med Chem Lett 2005;15:2041-5
    • (2005) Bioorg Med Chem Lett , vol.15 , pp. 2041-2045
    • Cox, C.D.1    Breslin, M.J.2    Mariano, B.J.3
  • 103
    • 33144468938 scopus 로고    scopus 로고
    • Kinesin spindle protein (KSP) inhibitors. Part 2: The design, synthesis, and characterization of 2,4-diaryl-2,5-dihydropyrrole inhibitors of the mitotic kinesin KSP
    • Fraley ME, Garbaccio RM, Arrington KL, et al. Kinesin spindle protein (KSP) inhibitors. Part 2: the design, synthesis, and characterization of 2,4-diaryl-2,5-dihydropyrrole inhibitors of the mitotic kinesin KSP. Bioorg Med Chem Lett 2006;16:1775-9
    • (2006) Bioorg Med Chem Lett , vol.16 , pp. 1775-1779
    • Fraley, M.E.1    Garbaccio, R.M.2    Arrington, K.L.3
  • 104
    • 33144455399 scopus 로고    scopus 로고
    • Kinesin spindle protein (KSP) inhibitors. Part 3: Synthesis and evaluation of phenolic 2,4-diaryl-2,5-dihydropyrroles with reduced hERG binding and employment of a phosphate prodrug strategy for aqueous solubility
    • Garbaccio RM, Fraley ME, Tasber ES, et al. Kinesin spindle protein (KSP) inhibitors. Part 3: synthesis and evaluation of phenolic 2,4-diaryl-2,5-dihydropyrroles with reduced hERG binding and employment of a phosphate prodrug strategy for aqueous solubility. Bioorg Med Chem Lett 2006;16:1780-3
    • (2006) Bioorg Med Chem Lett , vol.16 , pp. 1780-1783
    • Garbaccio, R.M.1    Fraley, M.E.2    Tasber, E.S.3
  • 105
    • 33646175956 scopus 로고    scopus 로고
    • Kinesin spindle protein (KSP) inhibitors. Part 4: Structure-based design of 5-alkylamino-3,5-diaryl-4,5-dihydropyrazoles as potent, water-soluble inhibitors of the mitotic kinesin KSP
    • Cox CD, Torrent M, Breslin MJ, et al. Kinesin spindle protein (KSP) inhibitors. Part 4: structure-based design of 5-alkylamino-3,5-diaryl-4,5-dihydropyrazoles as potent, water-soluble inhibitors of the mitotic kinesin KSP. Bioorg Med Chem Lett 2006;16:3175-9
    • (2006) Bioorg Med Chem Lett , vol.16 , pp. 3175-3179
    • Cox, C.D.1    Torrent, M.2    Breslin, M.J.3
  • 106
    • 34247379910 scopus 로고    scopus 로고
    • Kinesin spindle protein (KSP) inhibitors. Part 5: Discovery of 2-propylamino-2,4-diaryl-2,5-dihydropyrroles as potent, water-soluble KSP inhibitors, and modulation of their basicity by β-fluorination to overcome cellular efflux by P-glycoprotein
    • Cox CD, Breslin MJ, Whitman DB, et al. Kinesin spindle protein (KSP) inhibitors. Part 5: discovery of 2-propylamino-2,4-diaryl-2,5-dihydropyrroles as potent, water-soluble KSP inhibitors, and modulation of their basicity by β-fluorination to overcome cellular efflux by P-glycoprotein. Bioorg Med Chem Lett 2007;17:2697-702
    • (2007) Bioorg Med Chem Lett , vol.17 , pp. 2697-2702
    • Cox, C.D.1    Breslin, M.J.2    Whitman, D.B.3
  • 107
    • 34548561520 scopus 로고    scopus 로고
    • Kinesin spindle protein (KSP) inhibitors. Part 6:design and synthesis of 3,5-diaryl-4,5-dihydropyrazole amides as potent inhibitors of the mitotic kinesin KSP
    • Coleman PJ, Schreier JD, Cox CD, et al. Kinesin spindle protein (KSP) inhibitors. Part 6:design and synthesis of 3,5-diaryl-4,5-dihydropyrazole amides as potent inhibitors of the mitotic kinesin KSP. Bioorg Med Chem Lett 2007;17:5390-5
    • (2007) Bioorg Med Chem Lett , vol.17 , pp. 5390-5395
    • Coleman, P.J.1    Schreier, J.D.2    Cox, C.D.3
  • 108
    • 42549144407 scopus 로고    scopus 로고
    • Merck & Co. WO2006110390;
    • Merck & Co. WO2006110390; 2006
    • (2006)
  • 109
    • 42549104504 scopus 로고    scopus 로고
    • Merck & Co. WO2006101761;
    • Merck & Co. WO2006101761; 2006
    • (2006)
  • 110
    • 42549151862 scopus 로고    scopus 로고
    • Merck & Co. WO2006007496;
    • Merck & Co. WO2006007496; 2006
    • (2006)
  • 111
    • 42549141039 scopus 로고    scopus 로고
    • Merck & Co. WO2005017190;
    • Merck & Co. WO2005017190; 2005
    • (2005)
  • 112
    • 42549095937 scopus 로고    scopus 로고
    • Merck & Co. WO2005019205;
    • Merck & Co. WO2005019205; 2005
    • (2005)
  • 113
    • 42549150960 scopus 로고    scopus 로고
    • Merck & Co. WO2005019206;
    • Merck & Co. WO2005019206; 2005
    • (2005)
  • 114
    • 42549112909 scopus 로고    scopus 로고
    • Merck & Co. WO2006101780;
    • Merck & Co. WO2006101780; 2006
    • (2006)
  • 115
    • 42549088524 scopus 로고    scopus 로고
    • Merck & Co. WO2005018547;
    • Merck & Co. WO2005018547; 2005
    • (2005)
  • 116
    • 42549104864 scopus 로고    scopus 로고
    • Merck & Co. WO2006007501;
    • Merck & Co. WO2006007501; 2006
    • (2006)
  • 117
    • 42549083678 scopus 로고    scopus 로고
    • Kyowa Hakko/Fuji Film. WO2005035512; 2005
    • Kyowa Hakko/Fuji Film. WO2005035512; 2005
  • 118
    • 42549151410 scopus 로고    scopus 로고
    • Kyowa Hakko/Fuji Film. JP2005232016; 2005
    • Kyowa Hakko/Fuji Film. JP2005232016; 2005
  • 119
    • 42549105838 scopus 로고    scopus 로고
    • Merck & Co. WO2006031348;
    • Merck & Co. WO2006031348; 2006
    • (2006)
  • 120
    • 42549099806 scopus 로고    scopus 로고
    • Array Biopharma. WO2006044825; 2006
    • Array Biopharma. WO2006044825; 2006
  • 121
    • 42549118861 scopus 로고    scopus 로고
    • Merck & Co. WO2006023440;
    • Merck & Co. WO2006023440; 2006
    • (2006)
  • 122
    • 42549108050 scopus 로고    scopus 로고
    • Merck & Co. WO2004112699;
    • Merck & Co. WO2004112699; 2004
    • (2004)
  • 123
    • 42549109401 scopus 로고    scopus 로고
    • Merck & Co. WO2005018638;
    • Merck & Co. WO2005018638; 2005
    • (2005)
  • 124
    • 42549140564 scopus 로고    scopus 로고
    • Merck & Co. WO2006086358;
    • Merck & Co. WO2006086358; 2006
    • (2006)
  • 125
    • 42549098413 scopus 로고    scopus 로고
    • Merck & Co. WO2006007491;
    • Merck & Co. WO2006007491; 2006
    • (2006)
  • 126
    • 42549129076 scopus 로고    scopus 로고
    • Merck & Co. WO2006023083;
    • Merck & Co. WO2006023083; 2006
    • (2006)
  • 127
    • 34548591160 scopus 로고    scopus 로고
    • Kinesin spindle protein (KSP) inhibitors. Part 7: Design and synthesis of 3,3-disubstituted dihydropyrazolobenzoxazines as potent inhibitors of the mitotic kinesin KSP
    • Garbaccio RM, Tasber ES, Neilson LA, et al. Kinesin spindle protein (KSP) inhibitors. Part 7: design and synthesis of 3,3-disubstituted dihydropyrazolobenzoxazines as potent inhibitors of the mitotic kinesin KSP. Bioorg Med Chem Lett 2007;17:5671-6
    • (2007) Bioorg Med Chem Lett , vol.17 , pp. 5671-5676
    • Garbaccio, R.M.1    Tasber, E.S.2    Neilson, L.A.3
  • 128
    • 34548563725 scopus 로고    scopus 로고
    • Kinesin spindle protein (KSP) inhibitors. Part 8: Design and synthesis of 1,4-diaryl-4,5-dihydropyrazoles as potent inhibitors of the mitotic kinesin KSP
    • Roecker AJ, Coleman PJ, Mercer SP, et al. Kinesin spindle protein (KSP) inhibitors. Part 8: design and synthesis of 1,4-diaryl-4,5-dihydropyrazoles as potent inhibitors of the mitotic kinesin KSP. Bioorg Med Chem Lett 2007;17:5677-82
    • (2007) Bioorg Med Chem Lett , vol.17 , pp. 5677-5682
    • Roecker, A.J.1    Coleman, P.J.2    Mercer, S.P.3
  • 129
    • 42549110322 scopus 로고    scopus 로고
    • Merck & Co. WO2006068933;
    • Merck & Co. WO2006068933; 2006
    • (2006)
  • 130
    • 42549143425 scopus 로고    scopus 로고
    • Merck & Co. WO2004111193;
    • Merck & Co. WO2004111193; 2004
    • (2004)
  • 131
    • 42549157422 scopus 로고    scopus 로고
    • Merck & Co. WO2006007497;
    • Merck & Co. WO2006007497; 2006
    • (2006)
  • 132
    • 33644794320 scopus 로고    scopus 로고
    • Inhibitors of human mitotic kinesin Eg5: Characterization of the 4-phenyl-tetrahydroisoquinoline lead series
    • Tarby CM, Kaltenbach III RF, Huynh T, et al. Inhibitors of human mitotic kinesin Eg5: characterization of the 4-phenyl-tetrahydroisoquinoline lead series. Bioorg Med Chem Lett 2006;16:2095-100
    • (2006) Bioorg Med Chem Lett , vol.16 , pp. 2095-2100
    • Tarby, C.M.1    Kaltenbach III, R.F.2    Huynh, T.3
  • 133
    • 42549113838 scopus 로고    scopus 로고
    • GSK/Cytokinetics. WO2005060692; 2005
    • GSK/Cytokinetics. WO2005060692; 2005
  • 134
    • 42549116062 scopus 로고    scopus 로고
    • GSK. WO2005062847; 2005
    • GSK. WO2005062847; 2005
  • 135
    • 42549137746 scopus 로고    scopus 로고
    • GSK/Cytokinetics. WO2006020358; 2006
    • GSK/Cytokinetics. WO2006020358; 2006
  • 136
    • 34948846564 scopus 로고    scopus 로고
    • Novel ATP-competitive kinesin spindle protein inhibitors
    • Parrish CA, Adams ND, Auger KR, et al. Novel ATP-competitive kinesin spindle protein inhibitors. J Med Chem 2007;50:4939-52
    • (2007) J Med Chem , vol.50 , pp. 4939-4952
    • Parrish, C.A.1    Adams, N.D.2    Auger, K.R.3
  • 137
    • 42549092519 scopus 로고    scopus 로고
    • Jackson JR, Auger KR, Gilmartin AG, et al. A resistance mechanism for the KSP inhibitor ispinesib implicates point mutations in the compound binding site. Mol Targets Cancer Ther 2005:[Abstrart C207]
    • Jackson JR, Auger KR, Gilmartin AG, et al. A resistance mechanism for the KSP inhibitor ispinesib implicates point mutations in the compound binding site. Mol Targets Cancer Ther 2005:[Abstrart C207]
  • 138
    • 42549157875 scopus 로고    scopus 로고
    • GSK. WO2006113432; 2006
    • GSK. WO2006113432; 2006
  • 139
    • 42549129796 scopus 로고    scopus 로고
    • Merck KGaA. WO2005063735; 2005
    • Merck KGaA. WO2005063735; 2005
  • 140
    • 42549162725 scopus 로고    scopus 로고
    • Merck KGaA. WO2007054138; 2007
    • Merck KGaA. WO2007054138; 2007
  • 141
    • 42549119346 scopus 로고    scopus 로고
    • Merck KGaA. WO2006133805; 2006
    • Merck KGaA. WO2006133805; 2006
  • 142
    • 42549088526 scopus 로고    scopus 로고
    • Merck KGaA. WO2006002726; 2006
    • Merck KGaA. WO2006002726; 2006
  • 143
    • 42549154642 scopus 로고    scopus 로고
    • Merck KGaA. WO2006133821; 2006
    • Merck KGaA. WO2006133821; 2006
  • 144
    • 42549124963 scopus 로고    scopus 로고
    • Altana. WO2006018435; 2006
    • Altana. WO2006018435; 2006
  • 145
    • 42549108510 scopus 로고    scopus 로고
    • Nycomed. WO2007096393; 2007
    • Nycomed. WO2007096393; 2007
  • 146
    • 42549126260 scopus 로고    scopus 로고
    • Nycomed. WO2007096395; 2007
    • Nycomed. WO2007096395; 2007
  • 147
    • 42549144861 scopus 로고    scopus 로고
    • Chiron. WO2005070930; 2005
    • Chiron. WO2005070930; 2005
  • 148
    • 42549164965 scopus 로고    scopus 로고
    • Schering. WO2006098961; 2006
    • Schering. WO2006098961; 2006
  • 149
    • 42549098238 scopus 로고    scopus 로고
    • Schering. WO2006098962; 2006
    • Schering. WO2006098962; 2006
  • 150
    • 42549160804 scopus 로고    scopus 로고
    • Kalypsys. WO2007011721; 2007
    • Kalypsys. WO2007011721; 2007
  • 151
    • 42549152337 scopus 로고    scopus 로고
    • Kalypsys. WO2007011760; 2007
    • Kalypsys. WO2007011760; 2007
  • 152
    • 42549092520 scopus 로고    scopus 로고
    • Kalypsys. WO2007011759; 2007
    • Kalypsys. WO2007011759; 2007
  • 153
    • 42549138715 scopus 로고    scopus 로고
    • Kalypsys. WO2007011647; 2007
    • Kalypsys. WO2007011647; 2007
  • 154
    • 34250178457 scopus 로고    scopus 로고
    • Synthesis and SAR of thiophene containing kinesin spindle protein (KSP) inhibitors
    • Pinkerton AB, Lee TT, Hoffman TZ, et al. Synthesis and SAR of thiophene containing kinesin spindle protein (KSP) inhibitors. Bioorg Med Chem Lett 2007;17:3562-9
    • (2007) Bioorg Med Chem Lett , vol.17 , pp. 3562-3569
    • Pinkerton, A.B.1    Lee, T.T.2    Hoffman, T.Z.3
  • 155
    • 34250328223 scopus 로고    scopus 로고
    • Synthesis and biological evaluation of L-cysteine derivatives as mitotic kinesin Eg5 inhibitors
    • Ogo N, Oishi S, Matsuno K, et al. Synthesis and biological evaluation of L-cysteine derivatives as mitotic kinesin Eg5 inhibitors. Bioorg Med Chem Lett 2007;17:3921-4
    • (2007) Bioorg Med Chem Lett , vol.17 , pp. 3921-3924
    • Ogo, N.1    Oishi, S.2    Matsuno, K.3
  • 156
    • 33745867225 scopus 로고    scopus 로고
    • S-Trityl-L-cysteine is a reversible, tight binding inhibitor of the human kinesin Eg5 that specifically blocks mitotic progression
    • Skoufias DA, Debonis S, Saoudi Y, et al. S-Trityl-L-cysteine is a reversible, tight binding inhibitor of the human kinesin Eg5 that specifically blocks mitotic progression. J Biol Chem 2006;281:17559-69
    • (2006) J Biol Chem , vol.281 , pp. 17559-17569
    • Skoufias, D.A.1    Debonis, S.2    Saoudi, Y.3
  • 157
    • 42549158339 scopus 로고    scopus 로고
    • Merck KGaA. WO2006094602; 2006
    • Merck KGaA. WO2006094602; 2006
  • 158
    • 33747755812 scopus 로고    scopus 로고
    • Phenothiazine and carbazole-related compounds inhibit mitotic kinesin Eg5 and trigger apoptosis in transformed culture cells
    • Okumura H, Nakazawa J, Tsuganezawa K, et al. Phenothiazine and carbazole-related compounds inhibit mitotic kinesin Eg5 and trigger apoptosis in transformed culture cells. Toxicol Lett 2006;166:44-52
    • (2006) Toxicol Lett , vol.166 , pp. 44-52
    • Okumura, H.1    Nakazawa, J.2    Tsuganezawa, K.3
  • 159
    • 42549095444 scopus 로고    scopus 로고
    • Riken. JP2006348021; 2006
    • Riken. JP2006348021; 2006
  • 160
    • 42549103028 scopus 로고    scopus 로고
    • Cytokinetics. WO2002057244; 2002
    • Cytokinetics. WO2002057244; 2002
  • 161
    • 42549164966 scopus 로고    scopus 로고
    • Merck & Co. WO2004004652;
    • Merck & Co. WO2004004652; 2004
    • (2004)
  • 162
    • 33846216475 scopus 로고    scopus 로고
    • Pharmacophore identification of KSP inhibitors
    • Liu F, You Q, Chen Y. Pharmacophore identification of KSP inhibitors. Bioorg Med Chem Lett 2007;17:722-6
    • (2007) Bioorg Med Chem Lett , vol.17 , pp. 722-726
    • Liu, F.1    You, Q.2    Chen, Y.3
  • 163
    • 34547614098 scopus 로고    scopus 로고
    • Docking studies on kinesin spindle protein inhibitors: An important cooperative 'minor binding pocket' which increases the binding affinity significantly
    • Jiang C, Chen Y, Wang X, You Q. Docking studies on kinesin spindle protein inhibitors: an important cooperative 'minor binding pocket' which increases the binding affinity significantly. J Mol Model 2007;13:987-92
    • (2007) J Mol Model , vol.13 , pp. 987-992
    • Jiang, C.1    Chen, Y.2    Wang, X.3    You, Q.4
  • 164
    • 42549151409 scopus 로고    scopus 로고
    • Cytokinetics. WO2005107762; 2005
    • Cytokinetics. WO2005107762; 2005
  • 165
    • 42549124471 scopus 로고    scopus 로고
    • Cytokinetics. WO2007056056; 2007
    • Cytokinetics. WO2007056056; 2007
  • 166
    • 42549141525 scopus 로고    scopus 로고
    • Cytokinetics. WO2007056143; 2007
    • Cytokinetics. WO2007056143; 2007
  • 167
    • 42549093457 scopus 로고    scopus 로고
    • Cytokinetics. WO2007056078; 2007
    • Cytokinetics. WO2007056078; 2007
  • 168
    • 2442648857 scopus 로고    scopus 로고
    • SB-715992, a potent and selective inhibitor of the mitotic kinesin KSP, demonstrates broad-spectrum activity in advanced murine tumors and human tumor xenografts
    • Abstract 1335
    • Johnson RK, Mccabe FL, Caulder E, et al. SB-715992, a potent and selective inhibitor of the mitotic kinesin KSP, demonstrates broad-spectrum activity in advanced murine tumors and human tumor xenografts. Proc Am Assoc Cancer Res 2002;43:[Abstract 1335]
    • (2002) Proc Am Assoc Cancer Res , vol.43
    • Johnson, R.K.1    Mccabe, F.L.2    Caulder, E.3
  • 169
    • 20344406651 scopus 로고    scopus 로고
    • Phase I trial of novel kinesin spindle protein (KSP) inhibitor SB-715992 IV Q 21 days
    • Abstract 2078
    • Chu QS, Holen KD, Rowinsky EK, et al. Phase I trial of novel kinesin spindle protein (KSP) inhibitor SB-715992 IV Q 21 days. Proc Am Soc Clin Oncol 2004;23:[Abstract 2078]
    • (2004) Proc Am Soc Clin Oncol , vol.23
    • Chu, Q.S.1    Holen, K.D.2    Rowinsky, E.K.3
  • 170
    • 42549106301 scopus 로고    scopus 로고
    • Williams D, Kathman S, Chu Q, et al. A phase I study of SB-715992, a novel kinesin spindle protein (KSP) inhibitor: pharmacokinetic (PK)/ pharmacodynamic (PD) modelling of absolute neutrophil counts (ANC). Eur J Cancer Suppl 2004;2:[Abstract 55]
    • Williams D, Kathman S, Chu Q, et al. A phase I study of SB-715992, a novel kinesin spindle protein (KSP) inhibitor: pharmacokinetic (PK)/ pharmacodynamic (PD) modelling of absolute neutrophil counts (ANC). Eur J Cancer Suppl 2004;2:[Abstract 55]
  • 171
    • 13344275252 scopus 로고    scopus 로고
    • Phase I trial of novel kinesin spindle protein (KSP) inhibitor SB-715992 IV days 1, 8, 15 q 28 days
    • Abstract 2004
    • Burris HA, Lorusso P, Jones S, et al. Phase I trial of novel kinesin spindle protein (KSP) inhibitor SB-715992 IV days 1, 8, 15 q 28 days. Proc Am Soc Clin Oncol 2004;23:[Abstract 2004]
    • (2004) Proc Am Soc Clin Oncol , vol.23
    • Burris, H.A.1    Lorusso, P.2    Jones, S.3
  • 172
    • 42549141040 scopus 로고    scopus 로고
    • Study of ispinesib in subjects with breast cancer (NCT00089973). ClinicalTrials.gov. 18 August 2004. Available at http://clinicaltrials.gov/ct2/show/NCT00089973?id=NCT00089973&rank= 1 [Last accessed 14 November 2007]
    • Study of ispinesib in subjects with breast cancer (NCT00089973). ClinicalTrials.gov. 18 August 2004. Available at http://clinicaltrials.gov/ct2/show/NCT00089973?id=NCT00089973&rank= 1 [Last accessed 14 November 2007]
  • 173
    • 42549122436 scopus 로고    scopus 로고
    • Ispinesib in subjects with ptatinum-taxanerefractory or resistant relapsed ovarian cancer (NCT00097409). ClinicalTrials.gov. 23 November 2004. Available at http://clinicaltrials.gov/ct2/show/ NCT00097409?id=NCT00097409&rank=1 [Last accessed 14 November 2007]
    • Ispinesib in subjects with ptatinum-taxanerefractory or resistant relapsed ovarian cancer (NCT00097409). ClinicalTrials.gov. 23 November 2004. Available at http://clinicaltrials.gov/ct2/show/ NCT00097409?id=NCT00097409&rank=1 [Last accessed 14 November 2007]
  • 174
    • 42549113353 scopus 로고    scopus 로고
    • Ispinesib in patients with advanced or metastatic non-small cell lung cancer (NCT00085813). CtinicalTrials.gov. 14 June 2004. Available at: accessed] http://clinicaltrials.gov/ct2/show/ NCT00085813?id=NCT00085813&rank=1 [Last accessed 14 November 2007]
    • Ispinesib in patients with advanced or metastatic non-small cell lung cancer (NCT00085813). CtinicalTrials.gov. 14 June 2004. Available at: accessed] http://clinicaltrials.gov/ct2/show/ NCT00085813?id=NCT00085813&rank=1 [Last accessed 14 November 2007]
  • 175
    • 42549117005 scopus 로고    scopus 로고
    • SB-715992 in treating patients with recurrent or metastatic head and neck cancer NCT00095628, ClinicalTrials.gov. 5 November 2004. Available at [Last accessed 14 November 2007
    • SB-715992 in treating patients with recurrent or metastatic head and neck cancer (NCT00095628). ClinicalTrials.gov. 5 November 2004. Available at http://clinicaltrials.gov/ct2/show/ NCT00095628?id=NCT00095628&rank=1 [Last accessed 14 November 2007]
  • 176
    • 42549156975 scopus 로고    scopus 로고
    • SB-715992 in treating patients with acute leukemia, chronic myelogenous leukemia, or advanced myelodysplastic syndromes NCT00098826, ClinicalTrials.gov. 8 December 2004. Available at [Last accessed 14 November 2007
    • SB-715992 in treating patients with acute leukemia, chronic myelogenous leukemia, or advanced myelodysplastic syndromes (NCT00098826). ClinicalTrials.gov. 8 December 2004. Available at http://clinicaltrials.gov/ct2/show/NCT00098826?id=NCT00098826&rank=1 [Last accessed 14 November 2007]
  • 177
    • 42549135427 scopus 로고    scopus 로고
    • A phase II study of ispinesib (SB-715992) in patients with metastatic or recurrent malignant melanoma: A National Cancer Institute of Canada Clinical Trials Group trial
    • 26 October, doi:10.1007/ s10637-007-9097-9
    • Lee CW, Bélanger K, Rao SC, et al. A phase II study of ispinesib (SB-715992) in patients with metastatic or recurrent malignant melanoma: a National Cancer Institute of Canada Clinical Trials Group trial. Invest New Drugs 2007; published online 26 October 2007, doi:10.1007/ s10637-007-9097-9
    • (2007) Invest New Drugs 2007; published online
    • Lee, C.W.1    Bélanger, K.2    Rao, S.C.3
  • 178
    • 42549085099 scopus 로고    scopus 로고
    • Cytokinetics announces the initiation of Phase I/II clinical trial for SB-743921. Cytokinetics press release. 17 April 2006. Available at http://www.cytokinetics.com/cyto/pr_1145284422 [Last accessed 14 November 2007]
    • Cytokinetics announces the initiation of Phase I/II clinical trial for SB-743921. Cytokinetics press release. 17 April 2006. Available at http://www.cytokinetics.com/cyto/pr_1145284422 [Last accessed 14 November 2007]
  • 179
    • 42549108051 scopus 로고    scopus 로고
    • ARRY-520, a KSP inhibitor with efficacy and pharmacodynamic activity in animal models of solid tumors
    • Abstract 1433
    • Woessner RD, Corrette C, Allen S, et al. ARRY-520, a KSP inhibitor with efficacy and pharmacodynamic activity in animal models of solid tumors. Proc Am Assoc Cancer Res 2007;48:[Abstract 1433]
    • (2007) Proc Am Assoc Cancer Res , vol.48
    • Woessner, R.D.1    Corrette, C.2    Allen, S.3
  • 180
    • 75149163793 scopus 로고    scopus 로고
    • ARRY-520, a novel, highly selective KSP inhibitor with potent anti-proliferative activity
    • Abstract 5590
    • Lemieux C, Dewolf W, Voegtli W, et al. ARRY-520, a novel, highly selective KSP inhibitor with potent anti-proliferative activity. Proc Am Assoc Cancer Res 2007;48:[Abstract 5590]
    • (2007) Proc Am Assoc Cancer Res , vol.48
    • Lemieux, C.1    Dewolf, W.2    Voegtli, W.3
  • 181
    • 21444446863 scopus 로고    scopus 로고
    • Divide and conquer: New generation of drugs targets mitosis
    • GARBER K. Divide and conquer: new generation of drugs targets mitosis. J Natl Cancer Inst 2005;97:874-6
    • (2005) J Natl Cancer Inst , vol.97 , pp. 874-876
    • GARBER, K.1
  • 182
    • 15744404844 scopus 로고    scopus 로고
    • Mitotic kinesin inhibitors induce mitotic arrest and cell death in taxol-resistant and -sensitive cancer cells.)
    • Marcus AI, Peters U, Thomas SL, et al. Mitotic kinesin inhibitors induce mitotic arrest and cell death in taxol-resistant and -sensitive cancer cells.) J Biol Chem 2005;280:11569-77
    • (2005) J Biol Chem , vol.280 , pp. 11569-11577
    • Marcus, A.I.1    Peters, U.2    Thomas, S.L.3
  • 183
    • 0034605123 scopus 로고    scopus 로고
    • Probing spindle assembly mechanisms with monastrol, a small molecule inhibitor of the mitotic kinesin, Eg5
    • Kapoor TM, Mayer TU, Coughlin ML, Mitchison TJ. Probing spindle assembly mechanisms with monastrol, a small molecule inhibitor of the mitotic kinesin, Eg5. J Cell Biol 2000;150:975-88
    • (2000) J Cell Biol , vol.150 , pp. 975-988
    • Kapoor, T.M.1    Mayer, T.U.2    Coughlin, M.L.3    Mitchison, T.J.4
  • 184
    • 18444407796 scopus 로고    scopus 로고
    • Mammalian mitotic centromere-associated kinesin (MCAK)
    • Aoki S, Ohta K, Yamazaki T, et al. Mammalian mitotic centromere-associated kinesin (MCAK). FEBS J 2005;272:2132-40
    • (2005) FEBS J , vol.272 , pp. 2132-2140
    • Aoki, S.1    Ohta, K.2    Yamazaki, T.3
  • 185
    • 42549085539 scopus 로고    scopus 로고
    • Cytokinetics. WO2004026226; 2004
    • Cytokinetics. WO2004026226; 2004
  • 186
    • 42549103029 scopus 로고    scopus 로고
    • Max-Planck Institute. WO2006079478; 2006
    • Max-Planck Institute. WO2006079478; 2006


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.