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Buckbinder L., Crawford D.T., Qi H., Ke H.K., Olson L.M., Long K.R., Bonnette P.C., Baumann A.P., Hambor J.E., Grasser W.A., Pan L.C., Owen T.A., Luzzio M.J., Hulford C.A., Gebhard D.F., Paralkar V.M., Simmons H.A., Kath J.C., Roberts W.G., Smock S.L., Guzman-Perez A., Brown T.A., and Li M. Proc. Natl. Acad. Sci. U.S.A. 104 (2007) 10619
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Pan, L.C.11
Owen, T.A.12
Luzzio, M.J.13
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Gebhard, D.F.15
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more..
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17
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68349129603
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Kim, T.-S.; Bauer, D.; Bellon, S.; Boezio, A.; Booker, S.; Choquette, D.; D'Amico, D. C.; D'Angelo, N.; Dominguez, C.; Fellows, I. M.; Germain, J.; Graceffa, R.; Harmange, J.-C.; Hirai, S.; La, D.; Lee, M.; Liu, L.; Norman, M. H.; Potashman, M.; Roveto, P.; Siegmund, A. C.; Xi, N.; Yang, K. US Patent Application 20080312232A1, 2008. Experimental procedures and cMet data for some of these compounds will be published in due course.
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Kim, T.-S.; Bauer, D.; Bellon, S.; Boezio, A.; Booker, S.; Choquette, D.; D'Amico, D. C.; D'Angelo, N.; Dominguez, C.; Fellows, I. M.; Germain, J.; Graceffa, R.; Harmange, J.-C.; Hirai, S.; La, D.; Lee, M.; Liu, L.; Norman, M. H.; Potashman, M.; Roveto, P.; Siegmund, A. C.; Xi, N.; Yang, K. US Patent Application 20080312232A1, 2008. Experimental procedures and cMet data for some of these compounds will be published in due course.
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19
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68349127739
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PDB entry 3CC6 (1.6 Å): Busam, R. D.; Lehtio, L.; Karlberg, T.; Arrowsmith, C. H.; Bountra, C.; Collins, R.; Dahlgren, L. G.; Edwards, A. M.; Flodin, S.; Flores, A.; Graslund, S.; Hammarstrom, M.; Helleday, T.; Herman, M. D.; Johansson, A.; Johansson, I.; Kallas, A.; Kotenyova, T.; Moche, M.; Nilsson, M. E.; Nordlund, P.; Nyman, T.; Persson, C.; Sagemark, J.; Svensson, L.; Thorsell, A. G.; Tresaugues, L.; Van den Berg, S.; Weigelt, J.; Welin, M.; Berglund, H.
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PDB entry 3CC6 (1.6 Å): Busam, R. D.; Lehtio, L.; Karlberg, T.; Arrowsmith, C. H.; Bountra, C.; Collins, R.; Dahlgren, L. G.; Edwards, A. M.; Flodin, S.; Flores, A.; Graslund, S.; Hammarstrom, M.; Helleday, T.; Herman, M. D.; Johansson, A.; Johansson, I.; Kallas, A.; Kotenyova, T.; Moche, M.; Nilsson, M. E.; Nordlund, P.; Nyman, T.; Persson, C.; Sagemark, J.; Svensson, L.; Thorsell, A. G.; Tresaugues, L.; Van den Berg, S.; Weigelt, J.; Welin, M.; Berglund, H.
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20
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34250026140
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PDB entry 2J0L (2.3 Å):
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PDB entry 2J0L (2.3 Å):. Lietha D., Cai X., Ceccarelli D.F.J., Li Y., Schaller M.D., and Eck M.J. Cell 129 (2007) 1177
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Lietha, D.1
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Eck, M.J.6
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21
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65749105992
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Han S., Mistry A., Chang J.S., Cunningham D., Giffor M., Bonnette P.C., Wang H., Chrunyk B.A., Aspnes G.E., Walker D.P., Brosius A.D., and Buckbinder L. J. Biol. Chem. 284 (2009) 13193
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Wang, H.7
Chrunyk, B.A.8
Aspnes, G.E.9
Walker, D.P.10
Brosius, A.D.11
Buckbinder, L.12
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22
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68349136330
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note
-
293T cells were stably transfected with plasmids expressing a tetracycline repressor protein and a human Pyk2 cDNA regulated by a tetracycline operator sequence (T-REx™ System, Invitrogen, Carlsbad CA). In the absence of tetracycline basal Pyk2 expression was very low; in the presence of 100 ng/ml tetracycline Pyk2 expression was induced and was associated with increased Y402 autophosphorylation. Cellular immunofluorescence using antibodies for total Pyk2 and Y402 phosphorylation was quantitated in 96-well format using an Odyssey Infrared Imaging System (Li-Cor Biosciences, Lincoln NE).
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23
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0031917388
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Zheng C., Xing Z., Bian C., Guo C., Akbay A., Warner L., and Guan J.-L. J. Biol. Chem. 273 (1998) 2384
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Warner, L.6
Guan, J.-L.7
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25
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68349134530
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note
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Pyk2 inhibitors from different chemical series also showed variable activity in this assay (data not shown).
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26
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60449088467
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Han C.-Y.E., Wang Y., Yu L., Powers D., Xiong X., Yu V., Nguyen Y., Jean D.J., and Babij P. Bioorg. Med. Chem. Lett. 19 (2009) 1442
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Yu, V.6
Nguyen, Y.7
Jean, D.J.8
Babij, P.9
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27
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68349151891
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note
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Selectivity profiling was not run on compound 2 for as many targets as compound 1 but Jak3, Tyk2 and Aurora-2 were all >1 μM.
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28
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55549143963
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Walker D.P., Bi F.C., Kalgutkar A.S., Bauman J.N., Zhao S.X., Soglia J.R., Aspnes G.E., Kung D.W., Klug-McLeod J., Zawistoski M.P., McGlynn M.A., Oliver R., Dunn M., Li J.-C., Richter D.T., Cooper B.A., Kath J.C., Hulford C.A., Autry C.L., Luzzio M.J., Ung E.J., Roberts W.G., Bonnette P.C., Buckbinder L., Mistry A., Griffor M.C., Han S., and Guzman-Perez A. Bioorg. Med. Chem. Lett. 18 (2008) 6071
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Walker, D.P.1
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Zhao, S.X.5
Soglia, J.R.6
Aspnes, G.E.7
Kung, D.W.8
Klug-McLeod, J.9
Zawistoski, M.P.10
McGlynn, M.A.11
Oliver, R.12
Dunn, M.13
Li, J.-C.14
Richter, D.T.15
Cooper, B.A.16
Kath, J.C.17
Hulford, C.A.18
Autry, C.L.19
Luzzio, M.J.20
Ung, E.J.21
Roberts, W.G.22
Bonnette, P.C.23
Buckbinder, L.24
Mistry, A.25
Griffor, M.C.26
Han, S.27
Guzman-Perez, A.28
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