-
6
-
-
33846126268
-
-
Sarma P.K.S., Tandon R., Gupta P., Dastidar S.G., Ray A., Das B., and Cliffe I.A. Expert Opin. Ther. Patents 17 (2007) 25
-
(2007)
Expert Opin. Ther. Patents
, vol.17
, pp. 25
-
-
Sarma, P.K.S.1
Tandon, R.2
Gupta, P.3
Dastidar, S.G.4
Ray, A.5
Das, B.6
Cliffe, I.A.7
-
9
-
-
49849098247
-
-
Piao W., Wang Y., Adachi Y., Yamamoto H., Li R., Imsumran A., Li H., Maehata T., Ii M., Arimura Y., Lee C.-T., Shinomura Y., Carbone D.P., and Imai K. Mol. Cancer Ther. 7 (2008) 1483
-
(2008)
Mol. Cancer Ther.
, vol.7
, pp. 1483
-
-
Piao, W.1
Wang, Y.2
Adachi, Y.3
Yamamoto, H.4
Li, R.5
Imsumran, A.6
Li, H.7
Maehata, T.8
Ii, M.9
Arimura, Y.10
Lee, C.-T.11
Shinomura, Y.12
Carbone, D.P.13
Imai, K.14
-
10
-
-
42249114184
-
-
Maiso P., Ocio E.M., Garayoa M., Montero J.C., Hofmann F., Garcia-Echeverria C., Zimmermann J., Pandiella A., and San Miguel J.F. Br. J. Haemetol. 141 (2008) 470
-
(2008)
Br. J. Haemetol.
, vol.141
, pp. 470
-
-
Maiso, P.1
Ocio, E.M.2
Garayoa, M.3
Montero, J.C.4
Hofmann, F.5
Garcia-Echeverria, C.6
Zimmermann, J.7
Pandiella, A.8
San Miguel, J.F.9
-
11
-
-
33947262154
-
-
Manara M.C., Landuzzi L., Nanni P., Nicoletti G., Zambelli D., Lollini P.L., Nanni C., Hofmann F., Garcia-Echeverria C., Picci P., and Scotlandi K. Clin. Cancer Res. 13 (2007) 1322
-
(2007)
Clin. Cancer Res.
, vol.13
, pp. 1322
-
-
Manara, M.C.1
Landuzzi, L.2
Nanni, P.3
Nicoletti, G.4
Zambelli, D.5
Lollini, P.L.6
Nanni, C.7
Hofmann, F.8
Garcia-Echeverria, C.9
Picci, P.10
Scotlandi, K.11
-
12
-
-
33845313289
-
-
Tanno B., Mancini C., Vitali R., Mancuso M., McDowell H.P., Dominici C., and Raschella G. Clin. Cancer Res. 12 (2006) 6772
-
(2006)
Clin. Cancer Res.
, vol.12
, pp. 6772
-
-
Tanno, B.1
Mancini, C.2
Vitali, R.3
Mancuso, M.4
McDowell, H.P.5
Dominici, C.6
Raschella, G.7
-
13
-
-
20944447905
-
-
Scotlandi K., Manara M.C., Nicoletti G., Lollini P.-L., Lukas S., Benini S., Croci S., Perdichizzi S., Zambelli D., Serra M., Garcia-Echeverria C., Hofmann F., and Picci P. Cancer Res. 65 (2005) 3868
-
(2005)
Cancer Res.
, vol.65
, pp. 3868
-
-
Scotlandi, K.1
Manara, M.C.2
Nicoletti, G.3
Lollini, P.-L.4
Lukas, S.5
Benini, S.6
Croci, S.7
Perdichizzi, S.8
Zambelli, D.9
Serra, M.10
Garcia-Echeverria, C.11
Hofmann, F.12
Picci, P.13
-
14
-
-
12144285705
-
-
Garcia-Echeverria C., Pearson M.A., Marti A., Meyer T., Mestan J., Zimmerman J., Gao J., Brueggen J., Capraro H.-G., Cozens R., Evans D.B., Fabbro D., Furet P., Porta D.G., Liebetanz J., Martiny-Baron G., Ruetz S., and Hofmann F. Cancer Cell 5 (2004) 231
-
(2004)
Cancer Cell
, vol.5
, pp. 231
-
-
Garcia-Echeverria, C.1
Pearson, M.A.2
Marti, A.3
Meyer, T.4
Mestan, J.5
Zimmerman, J.6
Gao, J.7
Brueggen, J.8
Capraro, H.-G.9
Cozens, R.10
Evans, D.B.11
Fabbro, D.12
Furet, P.13
Porta, D.G.14
Liebetanz, J.15
Martiny-Baron, G.16
Ruetz, S.17
Hofmann, F.18
-
15
-
-
12144290914
-
-
Mitsiades C.S., Mitsiades N.S., McMullan C.J., Poulaki V., Shringarpure R., Akiyama M., Hideshima T., Chauhan D., Joseph M., Libermann T.A., Garcia-Echeverria C., Pearson M.A., Hofmann F., Anderson K.C., and Kung A.L. Cancer Cell 5 (2004) 221
-
(2004)
Cancer Cell
, vol.5
, pp. 221
-
-
Mitsiades, C.S.1
Mitsiades, N.S.2
McMullan, C.J.3
Poulaki, V.4
Shringarpure, R.5
Akiyama, M.6
Hideshima, T.7
Chauhan, D.8
Joseph, M.9
Libermann, T.A.10
Garcia-Echeverria, C.11
Pearson, M.A.12
Hofmann, F.13
Anderson, K.C.14
Kung, A.L.15
-
16
-
-
31544464616
-
-
Haluska P., Carboni J.M., Loegering D.A., Lee F.Y., Wittman M., Saulnier M.G., Frennesson D.B., Kalli K.R., Conover C.A., Attar R.M., Kaufmann S.H., Gottardis M., and Erlichman C. Cancer Res. 66 (2006) 362
-
(2006)
Cancer Res.
, vol.66
, pp. 362
-
-
Haluska, P.1
Carboni, J.M.2
Loegering, D.A.3
Lee, F.Y.4
Wittman, M.5
Saulnier, M.G.6
Frennesson, D.B.7
Kalli, K.R.8
Conover, C.A.9
Attar, R.M.10
Kaufmann, S.H.11
Gottardis, M.12
Erlichman, C.13
-
17
-
-
47149115273
-
-
Zimmermann K., Wittman M.D., Saulnier M.G., Velaparthi U., Langley D.R., Sang X., Frennesson D., Carboni J., Li A., Greer A., Gottardis M., Attar R.M., Yang Z., Balimane P., Discenza L.N., and Vyas D. Bioorg. Med. Chem. Lett. 18 (2008) 4075
-
(2008)
Bioorg. Med. Chem. Lett.
, vol.18
, pp. 4075
-
-
Zimmermann, K.1
Wittman, M.D.2
Saulnier, M.G.3
Velaparthi, U.4
Langley, D.R.5
Sang, X.6
Frennesson, D.7
Carboni, J.8
Li, A.9
Greer, A.10
Gottardis, M.11
Attar, R.M.12
Yang, Z.13
Balimane, P.14
Discenza, L.N.15
Vyas, D.16
-
18
-
-
24744437999
-
-
Wittman M., Carboni J., Attar R., Balasubramanian B., Balimane P., Brassil P., Beaulieu F., Chang C., Clarke W., Dell J., Eummer J., Frennesson D., Gottardis M., Greer A., Hansel S., Hurlburt W., Jacobson B., Krishnananthan S., Lee F.Y., Li A., Lin T.-A., Liu P., Ouellet C., Sang X., Saulnier M.G., Stoffan K., Sun Y., Velaparthi U., Wong H., Yang Z., Zimmermann K., Zoeckler M., and Vyas D. J. Med. Chem. 48 (2005) 5639
-
(2005)
J. Med. Chem.
, vol.48
, pp. 5639
-
-
Wittman, M.1
Carboni, J.2
Attar, R.3
Balasubramanian, B.4
Balimane, P.5
Brassil, P.6
Beaulieu, F.7
Chang, C.8
Clarke, W.9
Dell, J.10
Eummer, J.11
Frennesson, D.12
Gottardis, M.13
Greer, A.14
Hansel, S.15
Hurlburt, W.16
Jacobson, B.17
Krishnananthan, S.18
Lee, F.Y.19
Li, A.20
Lin, T.-A.21
Liu, P.22
Ouellet, C.23
Sang, X.24
Saulnier, M.G.25
Stoffan, K.26
Sun, Y.27
Velaparthi, U.28
Wong, H.29
Yang, Z.30
Zimmermann, K.31
Zoeckler, M.32
Vyas, D.33
more..
-
19
-
-
34548058890
-
-
Ji Q.-S., Mulvihill M.J., Rosenfeld-Franklin M., Cooke A., Feng L., Mak G., O'Connor M., Yao Y., Pirritt C., Buck E., Eyzaguirre A., Arnold L.D., Gibson N.W., and Pachter J.A. Mol. Cancer Ther. 6 (2007) 2158
-
(2007)
Mol. Cancer Ther.
, vol.6
, pp. 2158
-
-
Ji, Q.-S.1
Mulvihill, M.J.2
Rosenfeld-Franklin, M.3
Cooke, A.4
Feng, L.5
Mak, G.6
O'Connor, M.7
Yao, Y.8
Pirritt, C.9
Buck, E.10
Eyzaguirre, A.11
Arnold, L.D.12
Gibson, N.W.13
Pachter, J.A.14
-
20
-
-
58549108840
-
-
Rosenfeld-Franklin, M.; Cooke, A.; Pirritt, C.; Landfair, D.; Silva, S.; Turton, R.; Feng, L.; Mulvihill, M. J.; Buck, E.; Pachter, J. A.; Ji, Q.-S.; Wild, R. Abstract of Papers, AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics, San Francisco, CA; American Association for Cancer Research: Philadelphia, PA, National Cancer Institute: Bethesda, MD, and European Organisation for Research and Treatment of Cancer: Brussels, Belgium, 2007; Abstract B244.
-
Rosenfeld-Franklin, M.; Cooke, A.; Pirritt, C.; Landfair, D.; Silva, S.; Turton, R.; Feng, L.; Mulvihill, M. J.; Buck, E.; Pachter, J. A.; Ji, Q.-S.; Wild, R. Abstract of Papers, AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics, San Francisco, CA; American Association for Cancer Research: Philadelphia, PA, National Cancer Institute: Bethesda, MD, and European Organisation for Research and Treatment of Cancer: Brussels, Belgium, 2007; Abstract B244.
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-
-
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21
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58549094354
-
-
note
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2; QPC, Hopkinton, MA) and 0.5 nM activated enzyme. Reactions were stopped after 1 h at room temperature with 33 μM EDTA. Peptide phosphorylation was measured by time resolved fluorescence with 7 nM streptavidin-Surelight™ allophycocyanin (Perkin-Elmer, Waltham, MA) and 1 nM Europium-conjugated phospho-tyrosine antibodies (Perkin-Elmer). Plates were read in a Victor X5 or Viewlux 1430 ultra HTS microplate imager (Perkin-Elmer).
-
-
-
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22
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58549091526
-
-
note
-
50 values were determined from inhibition curves using XLfit4 software (Guildford, UK).
-
-
-
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23
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33749409412
-
-
Girdler F., Gascoigne K.E., Eyers P.A., Hartmuth S., Crafter C., Foote K.M., Keen N.J., and Taylor S.S. J. Cell Sci. 119 (2006) 3664
-
(2006)
J. Cell Sci.
, vol.119
, pp. 3664
-
-
Girdler, F.1
Gascoigne, K.E.2
Eyers, P.A.3
Hartmuth, S.4
Crafter, C.5
Foote, K.M.6
Keen, N.J.7
Taylor, S.S.8
-
26
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58549087013
-
-
note
-
Low dose mouse PK studies were conducted with a 1% DMSO, 10% solution in water formulation. Composite sampling was used with three mice per time point. AUC was determined from 0 to 6 h.
-
-
-
-
30
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58549096154
-
-
note
-
Other kinases were screened using conditions and assays optimized for each.
-
-
-
-
31
-
-
58549100970
-
-
note
-
50 values using the Cheng-Prusoff relationship for ATP competitive inhibition.
-
-
-
-
32
-
-
58549101743
-
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note
-
IR protein was expressed and purified as previously described (Li, S.; Covino, N. D.; Stein, E. G.; Till, J. H.; Hubbard, S. R. J. Biol. Chem. 2003, 278, 26007). Protein at 10 mg/ml was complexed with a 3-fold molar excess of inhibitor for 1 h prior to crystallization. Crystals were grown by hanging drop vapor diffusion at 22° from 0.1 M MOPS, pH 7.0, 1.0 M trisodium citrate. Crystals were flash frozen in PFO prior to data collection. The structure was solved by molecular replacement using PDB:1P14 as a starting model.
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-
-
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34
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4644289313
-
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Wood E.R., Truesdale A.R., McDonald O.B., Yuan D., Hassell A., Dickerson S.H., Ellis B., Pennisi C., Horne E., Lackey K., Alligood K., Rusnak D.W., Gilmer T.M., and Shewchuk L. Cancer Res. 64 (2004) 6652
-
(2004)
Cancer Res.
, vol.64
, pp. 6652
-
-
Wood, E.R.1
Truesdale, A.R.2
McDonald, O.B.3
Yuan, D.4
Hassell, A.5
Dickerson, S.H.6
Ellis, B.7
Pennisi, C.8
Horne, E.9
Lackey, K.10
Alligood, K.11
Rusnak, D.W.12
Gilmer, T.M.13
Shewchuk, L.14
-
35
-
-
58549116954
-
-
note
-
50 values were determined from using a 4-parameter curve fit software package (XLfit4).
-
-
-
-
36
-
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58549095507
-
-
note
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® in saline (IV) or water (PO). The PO study in dogs was run as a partial suspension. IV doses ranged from 0.6 to 1.3 mg/kg, and PO doses ranged from 2.1 to 7.2 mg/kg depending on species. Rats were male Sprague-Dawleys. Dogs were male beagles. Monkeys were male cynomolgus. Reported data are for 0-24 h.
-
-
-
-
39
-
-
34248180625
-
-
Denley A., Carroll J.M., Brierley G.V., Cosgrove L., Wallace J., Forbes B., and Roberts Jr. C.T. Mol. Cell Biol. 27 (2007) 3569
-
(2007)
Mol. Cell Biol.
, vol.27
, pp. 3569
-
-
Denley, A.1
Carroll, J.M.2
Brierley, G.V.3
Cosgrove, L.4
Wallace, J.5
Forbes, B.6
Roberts Jr., C.T.7
-
40
-
-
33745924420
-
-
Jones H.E., Gee J.M.W., Barrow D., Tonge D., Holloway B., and Nicholson R.I. Br. J. Cancer 95 (2006) 172-180
-
(2006)
Br. J. Cancer
, vol.95
, pp. 172-180
-
-
Jones, H.E.1
Gee, J.M.W.2
Barrow, D.3
Tonge, D.4
Holloway, B.5
Nicholson, R.I.6
-
42
-
-
0036148531
-
-
Vella V., Pandini G., Sciacca L., Mineo R., Vigneri R., Pezzino V., and Belfiore A. J. Clin. Endocrinol. Metab. 87 (2002) 245
-
(2002)
J. Clin. Endocrinol. Metab.
, vol.87
, pp. 245
-
-
Vella, V.1
Pandini, G.2
Sciacca, L.3
Mineo, R.4
Vigneri, R.5
Pezzino, V.6
Belfiore, A.7
-
43
-
-
0036721496
-
-
Kalli K., Falowo O.I., Bale L.K., Zschunke M.A., Roche P.C., and Conover C.A. Endocrinology 143 (2002) 3259
-
(2002)
Endocrinology
, vol.143
, pp. 3259
-
-
Kalli, K.1
Falowo, O.I.2
Bale, L.K.3
Zschunke, M.A.4
Roche, P.C.5
Conover, C.A.6
-
44
-
-
0037191919
-
-
Sciacca L., Mineo R., Pandini G., Murabito A., Vigneri R., and Belfiore A. Oncogene 21 (2002) 8240
-
(2002)
Oncogene
, vol.21
, pp. 8240
-
-
Sciacca, L.1
Mineo, R.2
Pandini, G.3
Murabito, A.4
Vigneri, R.5
Belfiore, A.6
-
45
-
-
0037131385
-
-
Pandini G., Frasca F., Mineo R., Sciacca L., Vigneri R., and Belfiore A. J. Biol. Chem. 277 (2002) 39684
-
(2002)
J. Biol. Chem.
, vol.277
, pp. 39684
-
-
Pandini, G.1
Frasca, F.2
Mineo, R.3
Sciacca, L.4
Vigneri, R.5
Belfiore, A.6
-
46
-
-
0033561728
-
-
Sciacca L., Costantino A., Pandini G., Mineo R., Frasca F., Scalia P., Sbraccia P., Goldfine I.D., Vigneri R., and Belfiore A. Oncogene 18 (1999) 2471
-
(1999)
Oncogene
, vol.18
, pp. 2471
-
-
Sciacca, L.1
Costantino, A.2
Pandini, G.3
Mineo, R.4
Frasca, F.5
Scalia, P.6
Sbraccia, P.7
Goldfine, I.D.8
Vigneri, R.9
Belfiore, A.10
-
47
-
-
0032932822
-
-
Frasca F., Pandini G., Scalia P., Sciacca L., Mineo R., Costantino A., Goldfine I.D., Belfiore A., and Vigneri R. Mol. Cell Biol. 19 (1999) 3278
-
(1999)
Mol. Cell Biol.
, vol.19
, pp. 3278
-
-
Frasca, F.1
Pandini, G.2
Scalia, P.3
Sciacca, L.4
Mineo, R.5
Costantino, A.6
Goldfine, I.D.7
Belfiore, A.8
Vigneri, R.9
-
48
-
-
0032800850
-
-
Pandini G., Vigneri R., Costantino A., Frasca F., Ippolito A., Fujita-Yamaguchi Y., Siddle K., Goldfine I.D., and Belfiore A. Clin. Cancer Res. 5 (1999) 1935
-
(1999)
Clin. Cancer Res.
, vol.5
, pp. 1935
-
-
Pandini, G.1
Vigneri, R.2
Costantino, A.3
Frasca, F.4
Ippolito, A.5
Fujita-Yamaguchi, Y.6
Siddle, K.7
Goldfine, I.D.8
Belfiore, A.9
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