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Volumn 12, Issue 4, 2009, Pages 533-542

Is there a future for Aurora kinase inhibitors for anticancer therapy?

Author keywords

Aurora kinase; Mitosis; Small molecule inhibitor

Indexed keywords

2 [[3 [4 [5 [2 (3 FLUOROANILINO) 2 OXOETHYL] 1H PYRAZOL 3 YLAMINO] 7 QUINAZOLINYLOXY]PROPYL](ETHYL)AMINO]ETHYL DIHYDROGEN PHOSPHATE; 4 [[9 CHLORO 7 (2,6 DIFLUOROPHENYL) 5H PYRIMIDO[5,4 D][2]BENZAZEPIN 2 YL]AMINO]BENZOIC ACID; AMG 900; AS 703569; AT 9283; AURORA A KINASE; AURORA B KINASE; AURORA KINASE INHIBITOR; BI 811283; BMS 739562; CCT 129202; CTK 110; CYC 116; CYCLOPROPANECARBOXYLIC ACID [4 [4 (4 METHYL 1 PIPERAZINYL) 6 (5 METHYL 2H PYRAZOL 3 YLAMINO) 2 PYRIMIDINYLTHIO]PHENYL]AMIDE; DASATINIB; DOCETAXEL; ENMD 2076; GEMCITABINE; GSK 1070916; HESPERIDIN; IMATINIB; MK 5108; MK 6592; MLN 8237; MP 529; NILOTINIB; PF 3814735; PHA 739358; SNS 314; UNCLASSIFIED DRUG; UNINDEXED DRUG; VX 667; VX 689;

EID: 67649964383     PISSN: 13676733     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review
Times cited : (17)

References (76)
  • 1
    • 0035235736 scopus 로고    scopus 로고
    • Mitotic kinases as regulators of cell division and its checkpoints
    • Nigg EA: Mitotic kinases as regulators of cell division and its checkpoints. Nat Rev Mol Cell Biol (2001) 2(1):21-32.
    • (2001) Nat Rev Mol Cell Biol , vol.2 , Issue.1 , pp. 21-32
    • Nigg, E.A.1
  • 2
    • 0242551545 scopus 로고    scopus 로고
    • The cellular geography of Aurora kinases
    • An excellent review on the biology of Aurora kinases, ··
    • Carmena M, Earnshaw WC: The cellular geography of Aurora kinases. Nat Rev Mol Cell Biol (2003) 4(11):842-854. ·· An excellent review on the biology of Aurora kinases.
    • (2003) Nat Rev Mol Cell Biol , vol.4 , Issue.11 , pp. 842-854
    • Carmena, M.1    Earnshaw, W.C.2
  • 3
    • 0033106222 scopus 로고    scopus 로고
    • The conserved protein kinase Ipl1 regulates microtubule binding to kinetochores in budding yeast
    • Biggins S, Severin FF, Bhalla N, Sassoon I, Hyman AA, Murray AW: The conserved protein kinase Ipl1 regulates microtubule binding to kinetochores in budding yeast. Genes Dev (1999) 13(5):532-544.
    • (1999) Genes Dev , vol.13 , Issue.5 , pp. 532-544
    • Biggins, S.1    Severin, F.F.2    Bhalla, N.3    Sassoon, I.4    Hyman, A.A.5    Murray, A.W.6
  • 4
    • 11144225241 scopus 로고    scopus 로고
    • Marumoto T, Zhang D, Saya H: Aurora-A - A guardian of poles.Nat Rev Cancer (2005) 5(1):42-50. ·· A good introduction to the biology of Aurora A.
    • Marumoto T, Zhang D, Saya H: Aurora-A - A guardian of poles.Nat Rev Cancer (2005) 5(1):42-50. ·· A good introduction to the biology of Aurora A.
  • 5
    • 23744503085 scopus 로고    scopus 로고
    • Aurora kinases: Shining lights on the therapeutic horizon?
    • Andrews PD: Aurora kinases: Shining lights on the therapeutic horizon? Oncogene (2005) 24(32):5005-5015.
    • (2005) Oncogene , vol.24 , Issue.32 , pp. 5005-5015
    • Andrews, P.D.1
  • 6
    • 0032100685 scopus 로고    scopus 로고
    • A homologue of Drosophila Aurora kinase is oncogenic and amplified in human colorectal cancers
    • ·· Describes the mammalian Aurora A and Aurora B kinases and their overexpression in human colorectal tumors. Provides the first evidence that the overexpression of Aurora A is linked to cancer
    • Bischoff JR, Anderson L, Zhu Y, Mossie K, Ng L, Souza B, Schryver B, Flanagan P, Clairvoyant F, Ginther C, Chan CS et al: A homologue of Drosophila Aurora kinase is oncogenic and amplified in human colorectal cancers. EMBO J (1998) 17(11):3052-3065. ·· Describes the mammalian Aurora A and Aurora B kinases and their overexpression in human colorectal tumors. Provides the first evidence that the overexpression of Aurora A is linked to cancer.
    • (1998) EMBO J , vol.17 , Issue.11 , pp. 3052-3065
    • Bischoff, J.R.1    Anderson, L.2    Zhu, Y.3    Mossie, K.4    Ng, L.5    Souza, B.6    Schryver, B.7    Flanagan, P.8    Clairvoyant, F.9    Ginther, C.10    Chan, C.S.11
  • 7
    • 0033548619 scopus 로고    scopus 로고
    • Cell cycle-dependent expression and centrosome localization of a third human Aurora/Ipl1-related protein kinase, AIK3
    • Kimura M, Matsuda Y, Yoshioka T, Okano Y: Cell cycle-dependent expression and centrosome localization of a third human Aurora/Ipl1-related protein kinase, AIK3. J Biol Chem (1999) 274(11):7334-7340.
    • (1999) J Biol Chem , vol.274 , Issue.11 , pp. 7334-7340
    • Kimura, M.1    Matsuda, Y.2    Yoshioka, T.3    Okano, Y.4
  • 8
    • 8744313990 scopus 로고    scopus 로고
    • Direct association with inner centromere protein (INCENP) activates the novel chromosomal passenger protein, Aurora-C
    • Li X, Sakashita G, Matsuzaki H, Sugimoto K, Kimura K, Hanaoka F, Taniguchi H, Furukawa K, Urano T: Direct association with inner centromere protein (INCENP) activates the novel chromosomal passenger protein, Aurora-C. J Biol Chem (2004) 279(45):47201-47211.
    • (2004) J Biol Chem , vol.279 , Issue.45 , pp. 47201-47211
    • Li, X.1    Sakashita, G.2    Matsuzaki, H.3    Sugimoto, K.4    Kimura, K.5    Hanaoka, F.6    Taniguchi, H.7    Furukawa, K.8    Urano, T.9
  • 11
    • 0038341158 scopus 로고    scopus 로고
    • The Aurora kinases: Role in cell transformation and tumorigenesis
    • Katayama H, Brinkley WR, Sen S: The Aurora kinases: Role in cell transformation and tumorigenesis. Cancer Metastasis Rev(2003) 22(4):451-464.
    • (2003) Cancer Metastasis Rev , vol.22 , Issue.4 , pp. 451-464
    • Katayama, H.1    Brinkley, W.R.2    Sen, S.3
  • 12
    • 0842281498 scopus 로고    scopus 로고
    • Aurora kinases link chromosome segregation and cell division to cancer susceptibility
    • Meraldi P, Honda R, Nigg EA: Aurora kinases link chromosome segregation and cell division to cancer susceptibility.Curr Opin Genet Dev (2004) 14(1):29-36.
    • (2004) Curr Opin Genet Dev , vol.14 , Issue.1 , pp. 29-36
    • Meraldi, P.1    Honda, R.2    Nigg, E.A.3
  • 13
    • 10344236486 scopus 로고    scopus 로고
    • Aurora-kinase inhibitors as anticancer agents
    • A comprehensive review of the most well-characterized Aurora kinase inhibitors, ·
    • Keen N, Taylor S: Aurora-kinase inhibitors as anticancer agents. Nat Rev Cancer (2004) 4(12):927-936. · A comprehensive review of the most well-characterized Aurora kinase inhibitors.
    • (2004) Nat Rev Cancer , vol.4 , Issue.12 , pp. 927-936
    • Keen, N.1    Taylor, S.2
  • 14
    • 33845743957 scopus 로고    scopus 로고
    • Aurora kinases: New targets for cancer therapy
    • Carvajal RD, Tse A, Schwartz GK: Aurora kinases: New targets for cancer therapy. Clin Cancer Res (2006) 12(23):6869-6875.
    • (2006) Clin Cancer Res , vol.12 , Issue.23 , pp. 6869-6875
    • Carvajal, R.D.1    Tse, A.2    Schwartz, G.K.3
  • 15
    • 47949108203 scopus 로고    scopus 로고
    • Aurora kinases and their inhibitors: More than one target and one drug
    • Carpinelli P, Moll J: Aurora kinases and their inhibitors: More than one target and one drug. Adv Exp Med Biol (2008) 610:54-73.
    • (2008) Adv Exp Med Biol , vol.610 , pp. 54-73
    • Carpinelli, P.1    Moll, J.2
  • 17
    • 40649089661 scopus 로고    scopus 로고
    • Aurora kinases as targets for cancer therapy
    • Mountzios G, Terpos E, Dimopoulos MA: Aurora kinases as targets for cancer therapy. Cancer Treat Rev (2008) 34(2): 175-182.
    • (2008) Cancer Treat Rev , vol.34 , Issue.2 , pp. 175-182
    • Mountzios, G.1    Terpos, E.2    Dimopoulos, M.A.3
  • 19
    • 33749002867 scopus 로고    scopus 로고
    • Aurora sheds light on head and neck squamous cell carcinoma
    • Han H, Von Hoff DD: Aurora sheds light on head and neck squamous cell carcinoma. Clin Cancer Res (2006) 12(17): 5003-5004.
    • (2006) Clin Cancer Res , vol.12 , Issue.17 , pp. 5003-5004
    • Han, H.1    Von Hoff, D.D.2
  • 20
    • 38949203768 scopus 로고    scopus 로고
    • The centrosome index is a powerful prognostic marker in myeloma and identifies a cohort of patients that might benefit from Aurora kinase inhibition
    • Chng WJ, Braggio E, Mulligan G, Bryant B, Remstein E, Valdez R, Dogan A, Fonseca R: The centrosome index is a powerful prognostic marker in myeloma and identifies a cohort of patients that might benefit from Aurora kinase inhibition.Blood (2008) 111(3):1603-1609.
    • (2008) Blood , vol.111 , Issue.3 , pp. 1603-1609
    • Chng, W.J.1    Braggio, E.2    Mulligan, G.3    Bryant, B.4    Remstein, E.5    Valdez, R.6    Dogan, A.7    Fonseca, R.8
  • 23
    • 4444239881 scopus 로고    scopus 로고
    • The mitotic serine threonine kinase, Aurora-2, is a potential target for drug development in human pancreatic cancer
    • Rojanala S, Han H, Muñoz RM, Browne W, Nagle R, Von Hoff DD, Bearss DJ: The mitotic serine threonine kinase, Aurora-2, is a potential target for drug development in human pancreatic cancer. Mol Cancer Ther (2004) 3(4):451-457.
    • (2004) Mol Cancer Ther , vol.3 , Issue.4 , pp. 451-457
    • Rojanala, S.1    Han, H.2    Muñoz, R.M.3    Browne, W.4    Nagle, R.5    Von Hoff, D.D.6    Bearss, D.J.7
  • 24
    • 0028938482 scopus 로고
    • Mutations in Aurora prevent centrosome separation leading to the formation of monopolar spindles
    • First report describing the Aurora kinase and its functions in Drosophila, ··
    • Glover DM, Leibowitz MH, McLean DA, Parry H: Mutations in Aurora prevent centrosome separation leading to the formation of monopolar spindles. Cell (1995) 81(1):95-105. ·· First report describing the Aurora kinase and its functions in Drosophila.
    • (1995) Cell , vol.81 , Issue.1 , pp. 95-105
    • Glover, D.M.1    Leibowitz, M.H.2    McLean, D.A.3    Parry, H.4
  • 25
    • 0038746733 scopus 로고    scopus 로고
    • The small molecule hesperadin reveals a role for Aurora B in correcting kinetochore-microtubule attachment and in maintaining the spindle assembly checkpoint
    • Describes the first small-molecule Aurora kinase inhibitor, and the molecular and phenotypic effects of inhibition of this kinase, ·
    • Hauf S, Cole RW, LaTerra S, Zimmer C, Schnapp G, Walter R, Heckel A, van Meel J, Rieder CL, Peters JM: The small molecule hesperadin reveals a role for Aurora B in correcting kinetochore-microtubule attachment and in maintaining the spindle assembly checkpoint. J Cell Biol (2003) 161(2):281-294. · Describes the first small-molecule Aurora kinase inhibitor, and the molecular and phenotypic effects of inhibition of this kinase.
    • (2003) J Cell Biol , vol.161 , Issue.2 , pp. 281-294
    • Hauf, S.1    Cole, R.W.2    LaTerra, S.3    Zimmer, C.4    Schnapp, G.5    Walter, R.6    Heckel, A.7    van Meel, J.8    Rieder, C.L.9    Peters, J.M.10
  • 29
    • 67649940506 scopus 로고    scopus 로고
    • Gavai A, Norris D, Trainor G, Vite G, Zhao Y, Vyas D, Tokarski J, Han W, Wong T, Rupnow B: Pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of Aurora kinases. EJC Supplements (2008) 6(12): 93-94.
    • Gavai A, Norris D, Trainor G, Vite G, Zhao Y, Vyas D, Tokarski J, Han W, Wong T, Rupnow B: Pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of Aurora kinases. EJC Supplements (2008) 6(12): 93-94.
  • 30
    • 67649905538 scopus 로고    scopus 로고
    • Aurora kinase project/CTK110 series: Cetek Corporation, Marlborough, MA, USA (2009). www.cetek.com/ctk110.html
    • Aurora kinase project/CTK110 series: Cetek Corporation, Marlborough, MA, USA (2009). www.cetek.com/ctk110.html
  • 32
    • 33845367377 scopus 로고    scopus 로고
    • Fancelli D, Moll J, Varasi M, Bravo R, Artico R, Berta D, Bindi S, Cameron A, Candiani I, Cappella P, Carpinelli P et al: 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: Identification of a potent Aurora kinase inhibitor with a favorable antitumor kinase inhibition profile. J Med Chem (2006) 49(24):7247-7251. ·· Describes the first small-molecule inhibitor of Aurora kinase, danusertib, which has entered clinical development.
    • Fancelli D, Moll J, Varasi M, Bravo R, Artico R, Berta D, Bindi S, Cameron A, Candiani I, Cappella P, Carpinelli P et al: 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: Identification of a potent Aurora kinase inhibitor with a favorable antitumor kinase inhibition profile. J Med Chem (2006) 49(24):7247-7251. ·· Describes the first small-molecule inhibitor of Aurora kinase, danusertib, which has entered clinical development.
  • 35
    • 43249111278 scopus 로고    scopus 로고
    • Simultaneous targeting of Aurora kinases and Bcr-Abl kinase by the small molecule inhibitor PHA-739358 is effective against imatinib-resistant BCR-ABL mutations including T315I
    • Gontarewicz A, Balabanov S, Keller G, Colombo R, Graziano A, Pesenti E, Benten D, Bokemeyer C, Fiedler W, Moll J, Brümmendorf TH: Simultaneous targeting of Aurora kinases and Bcr-Abl kinase by the small molecule inhibitor PHA-739358 is effective against imatinib-resistant BCR-ABL mutations including T315I. Blood (2008) 111(8):4355-4364.
    • (2008) Blood , vol.111 , Issue.8 , pp. 4355-4364
    • Gontarewicz, A.1    Balabanov, S.2    Keller, G.3    Colombo, R.4    Graziano, A.5    Pesenti, E.6    Benten, D.7    Bokemeyer, C.8    Fiedler, W.9    Moll, J.10    Brümmendorf, T.H.11
  • 36
    • 0038780904 scopus 로고    scopus 로고
    • Chronic myelogenous leukemia as a paradigm of early cancer and possible curative strategies
    • Clarkson B, Strife A, Wisniewski D, Lambek CL, Liu C: Chronic myelogenous leukemia as a paradigm of early cancer and possible curative strategies. Leukemia (2003) 17(7):1211-1262.
    • (2003) Leukemia , vol.17 , Issue.7 , pp. 1211-1262
    • Clarkson, B.1    Strife, A.2    Wisniewski, D.3    Lambek, C.L.4    Liu, C.5
  • 38
    • 0031931662 scopus 로고    scopus 로고
    • RET/NTRK1 rearrangements in thyroid gland tumors of the papillary carcinoma family: Correlation with clinicopathological features
    • Bongarzone I, Vigneri P, Mariani L, Collini P, Pilotti S, Pierotti MA: RET/NTRK1 rearrangements in thyroid gland tumors of the papillary carcinoma family: Correlation with clinicopathological features. Clin Cancer Res (1998) 4(1): 223-228.
    • (1998) Clin Cancer Res , vol.4 , Issue.1 , pp. 223-228
    • Bongarzone, I.1    Vigneri, P.2    Mariani, L.3    Collini, P.4    Pilotti, S.5    Pierotti, M.A.6
  • 42
    • 39049166077 scopus 로고    scopus 로고
    • Aurora kinase inhibitors: Identification and preclinical validation of their biomarkers
    • Carpinelli P, Moll J: Aurora kinase inhibitors: Identification and preclinical validation of their biomarkers. Expert Opin Ther Targets (2008) 12(1):69-80.
    • (2008) Expert Opin Ther Targets , vol.12 , Issue.1 , pp. 69-80
    • Carpinelli, P.1    Moll, J.2
  • 44
    • 59349101062 scopus 로고    scopus 로고
    • HA: Phase I study of the pan aurora kinases (AKs) inhibitor PHA-739358 administered as a 24 h infusion without/with G-CSF in a 14-day cycle in patients with advanced solid tumors
    • Abs
    • Cohen B, Jones SF, von Mehren M, Cheng J, Spiegel DM, Laffranchi B, Mariani M, Spinelli R, Magazzu D, and A. Burris HA: Phase I study of the pan aurora kinases (AKs) inhibitor PHA-739358 administered as a 24 h infusion without/with G-CSF in a 14-day cycle in patients with advanced solid tumors. J Clin Oncol (2008) 26:Abs 2520.
    • (2008) J Clin Oncol , vol.26 , pp. 2520
    • Cohen, B.1    Jones, S.F.2    von Mehren, M.3    Cheng, J.4    Spiegel, D.M.5    Laffranchi, B.6    Mariani, M.7    Spinelli, R.8    Magazzu, D.9    Burris, A.10
  • 46
    • 2342639645 scopus 로고    scopus 로고
    • VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo
    • The first report of the activity of an Aurora kinase inhibitor (VX-680) in animal tumor models, ·
    • Harrington EA, Bebbington D, Moore J, Rasmussen RK, Ajose-Adeogun AO, Nakayama T, Graham JA, Demur C, Hercend T, Diu-Hercend A, Su M et al: VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo. Nat Med (2004) 10(3): 262-267. · The first report of the activity of an Aurora kinase inhibitor (VX-680) in animal tumor models.
    • (2004) Nat Med , vol.10 , Issue.3 , pp. 262-267
    • Harrington, E.A.1    Bebbington, D.2    Moore, J.3    Rasmussen, R.K.4    Ajose-Adeogun, A.O.5    Nakayama, T.6    Graham, J.A.7    Demur, C.8    Hercend, T.9    Diu-Hercend, A.10    Su, M.11
  • 48
    • 67649897709 scopus 로고    scopus 로고
    • Rubin EH, Shapiro GI, Stein MN, Watson P, Bergstrom D, Xiao A, Clark JB, Freedman SJ, Eder JP: A phase I clinical and pharmacokinetic (PK) trial of the Aurora kinase (AK) inhibitor MK-0457 in cancer patients. J Clin Oncol (2006) 24(June 20 Suppl):Abs 3009.
    • Rubin EH, Shapiro GI, Stein MN, Watson P, Bergstrom D, Xiao A, Clark JB, Freedman SJ, Eder JP: A phase I clinical and pharmacokinetic (PK) trial of the Aurora kinase (AK) inhibitor MK-0457 in cancer patients. J Clin Oncol (2006) 24(June 20 Suppl):Abs 3009.
  • 49
    • 33846878294 scopus 로고    scopus 로고
    • New blood cancer therapies under study
    • Hampton T: New blood cancer therapies under study.J Am Med Assoc (2007) 297(5):457-458.
    • (2007) J Am Med Assoc , vol.297 , Issue.5 , pp. 457-458
    • Hampton, T.1
  • 50
    • 33846240316 scopus 로고    scopus 로고
    • MK-0457, a novel kinase inhibitor, is active in patients with chronic myeloid leukemia or acute lymphocytic leukemia with the T315I BCR-ABL mutation
    • Giles FJ, Cortes J, Jones D, Bergstrom D, Kantarjian H, Freedman SJ: MK-0457, a novel kinase inhibitor, is active in patients with chronic myeloid leukemia or acute lymphocytic leukemia with the T315I BCR-ABL mutation. Blood (2007) 109(2):500-502.
    • (2007) Blood , vol.109 , Issue.2 , pp. 500-502
    • Giles, F.J.1    Cortes, J.2    Jones, D.3    Bergstrom, D.4    Kantarjian, H.5    Freedman, S.J.6
  • 51
    • 33947174540 scopus 로고    scopus 로고
    • Vertex Pharmaceuticals Inc: Vertex's collaborator Merck suspends patient enrollment in clinical trials of MK-0457 (VX-680) pending full analysis of clinical data, November 20
    • Vertex Pharmaceuticals Inc: Vertex's collaborator Merck suspends patient enrollment in clinical trials of MK-0457 (VX-680) pending full analysis of clinical data. Press Release(2007): November 20.
    • (2007) Press Release
  • 52
    • 34247603906 scopus 로고    scopus 로고
    • Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of Aurora B kinase
    • The first report of a selective Aurora B kinase inhibitor, AZD-1152, that entered clinical trials, ·
    • Mortlock AA, Foote KM, Heron NM, Jung FH, Pasquet G, Lohmann JJ, Warin N, Renaud F, De Savi C, Roberts NJ, Johnson T et al: Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of Aurora B kinase. J Med Chem (2007) 50(9):2213-2224. · The first report of a selective Aurora B kinase inhibitor, AZD-1152, that entered clinical trials.
    • (2007) J Med Chem , vol.50 , Issue.9 , pp. 2213-2224
    • Mortlock, A.A.1    Foote, K.M.2    Heron, N.M.3    Jung, F.H.4    Pasquet, G.5    Lohmann, J.J.6    Warin, N.7    Renaud, F.8    De Savi, C.9    Roberts, N.J.10    Johnson, T.11
  • 54
    • 67649895327 scopus 로고    scopus 로고
    • Schellens JH, Boss D, Witteveen PO, Zandvliet A, Beijnen JH, Voogel-Fuchs M, Morris C, Wilson D, Voest EE: Phase I and pharmacological study of the novel Aurora kinase inhibitor AZD1152. J Clin Oncol (2006) 24(18S):3008.
    • Schellens JH, Boss D, Witteveen PO, Zandvliet A, Beijnen JH, Voogel-Fuchs M, Morris C, Wilson D, Voest EE: Phase I and pharmacological study of the novel Aurora kinase inhibitor AZD1152. J Clin Oncol (2006) 24(18S):3008.
  • 55
    • 34247259822 scopus 로고    scopus 로고
    • Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase
    • Describes the in vitro and in vivo characterization of MLN-8054, the first selective Aurora A inhibitor to undergo clinical development, ·
    • Manfredi MG, Ecsedy JA, Meetze KA, Balani SK, Burenkova O, Chen W, Galvin KM, Hoar KM, Huck JJ, LeRoy PJ, Ray ET et al: Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase. Proc Natl Acad Sci USA (2007) 104(10):4106-4111. · Describes the in vitro and in vivo characterization of MLN-8054, the first selective Aurora A inhibitor to undergo clinical development.
    • (2007) Proc Natl Acad Sci USA , vol.104 , Issue.10 , pp. 4106-4111
    • Manfredi, M.G.1    Ecsedy, J.A.2    Meetze, K.A.3    Balani, S.K.4    Burenkova, O.5    Chen, W.6    Galvin, K.M.7    Hoar, K.M.8    Huck, J.J.9    LeRoy, P.J.10    Ray, E.T.11
  • 59
    • 65649086159 scopus 로고    scopus 로고
    • Phase I study of the safety, pharmacokinetics (PK), and pharmacodynamics (PD) of MLN8237, a selective Aurora A kinase inhibitor, in the United States
    • Infante J, Dees EC, Cohen RB, Burris H, O'Neil B, Murphy P, Lee Y, Pappas J, Ecsedy JA, Eton O: Phase I study of the safety, pharmacokinetics (PK), and pharmacodynamics (PD) of MLN8237, a selective Aurora A kinase inhibitor, in the United States. EJC Supplements (2008) 6(12):90-91.
    • (2008) EJC Supplements , vol.6 , Issue.12 , pp. 90-91
    • Infante, J.1    Dees, E.C.2    Cohen, R.B.3    Burris, H.4    O'Neil, B.5    Murphy, P.6    Lee, Y.7    Pappas, J.8    Ecsedy, J.A.9    Eton, O.10
  • 63
    • 67649610475 scopus 로고    scopus 로고
    • ENMD-2076, an oral Aurora-A and angiogenesis kinase inhibitor
    • April
    • Bray MR: ENMD-2076, an oral Aurora-A and angiogenesis kinase inhibitor. Proceedings of the AACR Annual Meeting (2008) 99: 13 April.
    • (2008) Proceedings of the AACR Annual Meeting , vol.99 , Issue.13
    • Bray, M.R.1
  • 65
    • 67649943593 scopus 로고    scopus 로고
    • An open-label, dose-escalation, safety, and pharmacokinetic study of ENMD-2076 administered orally to patients with advanced cancer
    • Abs
    • Bastos BR, Diamond J, Hansen R et al: An open-label, dose-escalation, safety, and pharmacokinetic study of ENMD-2076 administered orally to patients with advanced cancer. J Clin Oncol (2009) 27:Abs 3520
    • (2009) J Clin Oncol , vol.27 , pp. 3520
    • Bastos, B.R.1    Diamond, J.2    Hansen, R.3
  • 66
    • 67649955245 scopus 로고
    • The novel Aurora kinase inhibitor AS703569 shows potent anti-tumor activity in acute myelogenous leukemia (AML)
    • Abs
    • Romanelli A, Shaw J, Spooner E, Ma J, Clark A: The novel Aurora kinase inhibitor AS703569 shows potent anti-tumor activity in acute myelogenous leukemia (AML). Proceedings of the AACR Annual Meeting (2007) 98: Abs 1817.
    • (1817) Proceedings of the AACR Annual Meeting , vol.98
    • Romanelli, A.1    Shaw, J.2    Spooner, E.3    Ma, J.4    Clark, A.5
  • 67
    • 67649893048 scopus 로고    scopus 로고
    • Preclinical evaluation of the orally available Aurora kinase inhibitor AS703569 to support the selection of tumor indications for clinical studies
    • Abs
    • Maier A, Schuler J, Bausch N, Fiebig H, Romanelli A, Gianella-Borradori A: Preclinical evaluation of the orally available Aurora kinase inhibitor AS703569 to support the selection of tumor indications for clinical studies.Proceedings of the AACR Annual Meeting (2007) 98: Abs 3264.
    • (2007) Proceedings of the AACR Annual Meeting , vol.98 , pp. 3264
    • Maier, A.1    Schuler, J.2    Bausch, N.3    Fiebig, H.4    Romanelli, A.5    Gianella-Borradori, A.6
  • 68
    • 67649905530 scopus 로고    scopus 로고
    • Phase I, dose-escalation study of 2 dosing regimens of AS703569, an inhibitor of Aurora and other kinases, administered orally in patients with advanced hematological malignancies
    • Sonet A, Graux C, Maertens J, Hartog CM, Duyster J, Götze K, Greiner J, Hütter ML, Gratwohl A, Heim D, Hess D et al: Phase I, dose-escalation study of 2 dosing regimens of AS703569, an inhibitor of Aurora and other kinases, administered orally in patients with advanced hematological malignancies. Blood (2008) 112(11):2963.
    • (2008) Blood , vol.112 , Issue.11 , pp. 2963
    • Sonet, A.1    Graux, C.2    Maertens, J.3    Hartog, C.M.4    Duyster, J.5    Götze, K.6    Greiner, J.7    Hütter, M.L.8    Gratwohl, A.9    Heim, D.10    Hess, D.11
  • 69
    • 33947174540 scopus 로고    scopus 로고
    • Rigel Pharmaceuticals Inc: Rigel announces start of phase 1 combination therapy study of R763/AS703569 in advanced malignancies, July 12
    • Rigel Pharmaceuticals Inc: Rigel announces start of phase 1 combination therapy study of R763/AS703569 in advanced malignancies. Press Release (2007): July 12.
    • (2007) Press Release
  • 70
    • 65649154573 scopus 로고    scopus 로고
    • Preliminary results of a phase I accelerated dose-escalation, pharmacokinetic and pharmacodynamic study of PF-03814735, an oral Aurora kinase A and B inhibitor, in patients with advanced solid tumors
    • Schöffski P, Dumez H, Jones SF, Fowst C, Gerletti P, Xu H, Jakubczak J, Infante J, Mellaerts N, Burris HA: Preliminary results of a phase I accelerated dose-escalation, pharmacokinetic and pharmacodynamic study of PF-03814735, an oral Aurora kinase A and B inhibitor, in patients with advanced solid tumors. EJC Supplements (2008) 6(12):91.
    • (2008) EJC Supplements , vol.6 , Issue.12 , pp. 91
    • Schöffski, P.1    Dumez, H.2    Jones, S.F.3    Fowst, C.4    Gerletti, P.5    Xu, H.6    Jakubczak, J.7    Infante, J.8    Mellaerts, N.9    Burris, H.A.10
  • 72
    • 67649920285 scopus 로고    scopus 로고
    • Hajduch M, Vydra D, Dzubak P, Dziechciarkova M, Stuart I, Zheleva D: In vivo mode of action of CYC116, a novel small molecule inhibitor of Aurora kinases and VEGFR2. Proceedings of the AACR Annual Meeting (2008) 99: Abs 5645.
    • Hajduch M, Vydra D, Dzubak P, Dziechciarkova M, Stuart I, Zheleva D: In vivo mode of action of CYC116, a novel small molecule inhibitor of Aurora kinases and VEGFR2. Proceedings of the AACR Annual Meeting (2008) 99: Abs 5645.
  • 73
    • 67649943599 scopus 로고    scopus 로고
    • Taverna P, Hogan J, Kumer J, Arbitrano J, Hoch U, Silverman J, Howlett A: SNS-314, a potent inhibitor of Aurora kinases, shows broad anti-tumor activity and dosing flexibility in vivo. Ann Oncol (2007) 18(Suppl 4):iv33.
    • Taverna P, Hogan J, Kumer J, Arbitrano J, Hoch U, Silverman J, Howlett A: SNS-314, a potent inhibitor of Aurora kinases, shows broad anti-tumor activity and dosing flexibility in vivo. Ann Oncol (2007) 18(Suppl 4):iv33.
  • 76
    • 44949157910 scopus 로고    scopus 로고
    • Girdler F, Sessa F, Patercoli S, Villa F, Musacchio A, Taylor S: Molecular basis of drug resistance in Aurora kinases.Chem Biol (2008) 15(6):552-562. · Reports the first observed resistance against Aurora kinase inhibitors caused by mutations in Aurora B.
    • Girdler F, Sessa F, Patercoli S, Villa F, Musacchio A, Taylor S: Molecular basis of drug resistance in Aurora kinases.Chem Biol (2008) 15(6):552-562. · Reports the first observed resistance against Aurora kinase inhibitors caused by mutations in Aurora B.


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