-
1
-
-
64349099558
-
Kinase domain mutations in cancer: implications for small molecule drug design strategies
-
Bikker J.A., Brooijmans N., Wissner A., Mansour T.S. (2009) Kinase domain mutations in cancer: implications for small molecule drug design strategies. J Med Chem;52:1493-1509.
-
(2009)
J Med Chem
, vol.52
, pp. 1493-1509
-
-
Bikker, J.A.1
Brooijmans, N.2
Wissner, A.3
Mansour, T.S.4
-
2
-
-
13844317894
-
EGFR mutation and resistance of non-small-cell lung cancer to gefitinib
-
Kobayashi S., Boggon T.J., Dayaram T., Janne P.A., Kocher O., Meyerson M., Johnson B.E., Eck M.J., Tenen D.G., Halmos B. (2005) EGFR mutation and resistance of non-small-cell lung cancer to gefitinib. N Engl J Med;352:786-792.
-
(2005)
N Engl J Med
, vol.352
, pp. 786-792
-
-
Kobayashi, S.1
Boggon, T.J.2
Dayaram, T.3
Janne, P.A.4
Kocher, O.5
Meyerson, M.6
Johnson, B.E.7
Eck, M.J.8
Tenen, D.G.9
Halmos, B.10
-
3
-
-
73349105243
-
Resistance to Targeted Therapies: Refining Anticancer Therapy in the Era of Molecular Oncology
-
Ellis L.M., Hicklin D.J. (2009) Resistance to Targeted Therapies: Refining Anticancer Therapy in the Era of Molecular Oncology. Clin Cancer Res;15:7471-7478.
-
(2009)
Clin Cancer Res
, vol.15
, pp. 7471-7478
-
-
Ellis, L.M.1
Hicklin, D.J.2
-
4
-
-
0038780904
-
Chronic myelogenous leukemia as a paradigm of early cancer and possible curative strategies
-
Clarkson B., Strife A., Wisniewski D., Lambek C.L., Liu C. (2003) Chronic myelogenous leukemia as a paradigm of early cancer and possible curative strategies. Leukemia;17:1211-1262.
-
(2003)
Leukemia
, vol.17
, pp. 1211-1262
-
-
Clarkson, B.1
Strife, A.2
Wisniewski, D.3
Lambek, C.L.4
Liu, C.5
-
5
-
-
0347132269
-
Regulation of the c-Abl and Bcr-Abl tyrosine kinases
-
Hantschel O., Superti-Furga G. (2004) Regulation of the c-Abl and Bcr-Abl tyrosine kinases. Nat Rev Mol Cell Biol;5:33-44.
-
(2004)
Nat Rev Mol Cell Biol
, vol.5
, pp. 33-44
-
-
Hantschel, O.1
Superti-Furga, G.2
-
6
-
-
0033614446
-
Chronic myeloid leukemia
-
Sawyers C.L. (1999) Chronic myeloid leukemia. N Engl J Med;340:1330-1340.
-
(1999)
N Engl J Med
, vol.340
, pp. 1330-1340
-
-
Sawyers, C.L.1
-
7
-
-
15944404601
-
The development of imatinib as a therapeutic agent for chronic myeloid leukemia
-
Deininger M., Buchdunger E., Druker B.J. (2005) The development of imatinib as a therapeutic agent for chronic myeloid leukemia. Blood;105:2640-2653.
-
(2005)
Blood
, vol.105
, pp. 2640-2653
-
-
Deininger, M.1
Buchdunger, E.2
Druker, B.J.3
-
8
-
-
0035810147
-
Efficacy and safety of a specific inhibitor of the BCR-ABL tyrosine kinase in chronic myeloid leukemia
-
Druker B.J., Talpaz M., Resta D.J., Peng B., Buchdunger E., Ford J.M., Lydon N.B., Kantarjian H., Capdeville R., Ohno-Jones S., Sawyers C.L. (2001) Efficacy and safety of a specific inhibitor of the BCR-ABL tyrosine kinase in chronic myeloid leukemia. N Engl J Med;344:1031-1037.
-
(2001)
N Engl J Med
, vol.344
, pp. 1031-1037
-
-
Druker, B.J.1
Talpaz, M.2
Resta, D.J.3
Peng, B.4
Buchdunger, E.5
Ford, J.M.6
Lydon, N.B.7
Kantarjian, H.8
Capdeville, R.9
Ohno-Jones, S.10
Sawyers, C.L.11
-
9
-
-
0035800507
-
Clinical resistance to STI-571 cancer therapy caused by BCR-ABL gene mutation or amplification
-
Gorre M.E., Mohammed M., Ellwood K., Hsu N., Paquette R., Rao P.N., Sawyers C.L. (2001) Clinical resistance to STI-571 cancer therapy caused by BCR-ABL gene mutation or amplification. Science;293:876-880.
-
(2001)
Science
, vol.293
, pp. 876-880
-
-
Gorre, M.E.1
Mohammed, M.2
Ellwood, K.3
Hsu, N.4
Paquette, R.5
Rao, P.N.6
Sawyers, C.L.7
-
10
-
-
0037105560
-
A phase 2 study of imatinib in patients with relapsed or refractory Philadelphia chromosome-positive acute lymphoid leukemias
-
Ottmann O.G., Druker B.J., Sawyers C.L., Goldman J.M., Reiffers J., Silver R.T., Tura S. et al. (2002) A phase 2 study of imatinib in patients with relapsed or refractory Philadelphia chromosome-positive acute lymphoid leukemias. Blood;100:1965-1971.
-
(2002)
Blood
, vol.100
, pp. 1965-1971
-
-
Ottmann, O.G.1
Druker, B.J.2
Sawyers, C.L.3
Goldman, J.M.4
Reiffers, J.5
Silver, R.T.6
Tura, S.7
-
11
-
-
33745086350
-
Nilotinib in imatinib-resistant CML and Philadelphia chromosome-positive ALL
-
Kantarjian H., Giles F., Wunderle L., Bhalla K., O'Brien S., Wassmann B., Tanaka C. et al. (2006) Nilotinib in imatinib-resistant CML and Philadelphia chromosome-positive ALL. N Engl J Med;354:2542-2551.
-
(2006)
N Engl J Med
, vol.354
, pp. 2542-2551
-
-
Kantarjian, H.1
Giles, F.2
Wunderle, L.3
Bhalla, K.4
O'Brien, S.5
Wassmann, B.6
Tanaka, C.7
-
12
-
-
3142676436
-
Overriding imatinib resistance with a novel ABL kinase inhibitor
-
Shah N.P., Tran C., Lee F.Y., Chen P., Norris D., Sawyers C.L. (2004) Overriding imatinib resistance with a novel ABL kinase inhibitor. Science;305:399-401.
-
(2004)
Science
, vol.305
, pp. 399-401
-
-
Shah, N.P.1
Tran, C.2
Lee, F.Y.3
Chen, P.4
Norris, D.5
Sawyers, C.L.6
-
13
-
-
34247470836
-
Second generation inhibitors of BCR-ABL for the treatment of imatinib-resistant chronic myeloid leukaemia
-
Weisberg E., Manley P.W., Cowan-Jacob S.W., Hochhaus A., Griffin J.D. (2007) Second generation inhibitors of BCR-ABL for the treatment of imatinib-resistant chronic myeloid leukaemia. Nat Rev Cancer;7:345-356.
-
(2007)
Nat Rev Cancer
, vol.7
, pp. 345-356
-
-
Weisberg, E.1
Manley, P.W.2
Cowan-Jacob, S.W.3
Hochhaus, A.4
Griffin, J.D.5
-
14
-
-
34548825795
-
Bcr-Abl kinase domain mutations, drug resistance, and the road to a cure for chronic myeloid leukemia
-
O'Hare T., Eide C.A., Deininger M.W. (2007) Bcr-Abl kinase domain mutations, drug resistance, and the road to a cure for chronic myeloid leukemia. Blood;110:2242-2249.
-
(2007)
Blood
, vol.110
, pp. 2242-2249
-
-
O'Hare, T.1
Eide, C.A.2
Deininger, M.W.3
-
15
-
-
76249090055
-
Selecting optimal second-line tyrosine kinase inhibitor therapy for chronic myeloid leukemia patients after imatinib failure: does the BCR-ABL mutation status really matter?
-
Branford S., Melo J.V., Hughes T.P. (2009) Selecting optimal second-line tyrosine kinase inhibitor therapy for chronic myeloid leukemia patients after imatinib failure: does the BCR-ABL mutation status really matter? Blood;114:5426-5435.
-
(2009)
Blood
, vol.114
, pp. 5426-5435
-
-
Branford, S.1
Melo, J.V.2
Hughes, T.P.3
-
16
-
-
77950573400
-
Through the "gatekeeper door": exploiting the active kinase conformation
-
Zuccotto F., Ardini E., Casale E., Angiolini M. (2010) Through the "gatekeeper door": exploiting the active kinase conformation. J Med Chem;53:2681-2694.
-
(2010)
J Med Chem
, vol.53
, pp. 2681-2694
-
-
Zuccotto, F.1
Ardini, E.2
Casale, E.3
Angiolini, M.4
-
17
-
-
0036682301
-
Crystal structures of the kinase domain of c-Abl in complex with the small molecule inhibitors PD173955 and imatinib (STI-571)
-
Nagar B., Bornmann W.G., Pellicena P., Schindler T., Veach D.R., Miller W.T., Clarkson B., Kuriyan J. (2002) Crystal structures of the kinase domain of c-Abl in complex with the small molecule inhibitors PD173955 and imatinib (STI-571). Cancer Res;62:4236-4243.
-
(2002)
Cancer Res
, vol.62
, pp. 4236-4243
-
-
Nagar, B.1
Bornmann, W.G.2
Pellicena, P.3
Schindler, T.4
Veach, D.R.5
Miller, W.T.6
Clarkson, B.7
Kuriyan, J.8
-
18
-
-
33745283618
-
The structure of Dasatinib (BMS-354825) bound to activated ABL kinase domain elucidates its inhibitory activity against imatinib-resistant ABL mutants
-
Tokarski J.S., Newitt J.A., Chang C.Y., Cheng J.D., Wittekind M., Kiefer S.E., Kish K., Lee F.Y., Borzillerri R., Lombardo L.J., Xie D., Zhang Y., Klei H.E. (2006) The structure of Dasatinib (BMS-354825) bound to activated ABL kinase domain elucidates its inhibitory activity against imatinib-resistant ABL mutants. Cancer Res;66:5790-5797.
-
(2006)
Cancer Res
, vol.66
, pp. 5790-5797
-
-
Tokarski, J.S.1
Newitt, J.A.2
Chang, C.Y.3
Cheng, J.D.4
Wittekind, M.5
Kiefer, S.E.6
Kish, K.7
Lee, F.Y.8
Borzillerri, R.9
Lombardo, L.J.10
Xie, D.11
Zhang, Y.12
Klei, H.E.13
-
19
-
-
13844251975
-
Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl
-
Weisberg E., Manley P.W., Breitenstein W., Bruggen J., Cowan-Jacob S.W., Ray A., Huntly B. et al. (2005) Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl. Cancer Cell;7:129-141.
-
(2005)
Cancer Cell
, vol.7
, pp. 129-141
-
-
Weisberg, E.1
Manley, P.W.2
Breitenstein, W.3
Bruggen, J.4
Cowan-Jacob, S.W.5
Ray, A.6
Huntly, B.7
-
20
-
-
34548548332
-
Crystal structure of the T315I Abl mutant in complex with the aurora kinases inhibitor PHA-739358
-
Modugno M., Casale E., Soncini C., Rosettani P., Colombo R., Lupi R., Rusconi L., Fancelli D., Carpinelli P., Cameron A.D., Isacchi A., Moll J. (2007) Crystal structure of the T315I Abl mutant in complex with the aurora kinases inhibitor PHA-739358. Cancer Res;67:7987-7990.
-
(2007)
Cancer Res
, vol.67
, pp. 7987-7990
-
-
Modugno, M.1
Casale, E.2
Soncini, C.3
Rosettani, P.4
Colombo, R.5
Lupi, R.6
Rusconi, L.7
Fancelli, D.8
Carpinelli, P.9
Cameron, A.D.10
Isacchi, A.11
Moll, J.12
-
21
-
-
34548169642
-
Crystal structure of the T315I mutant of AbI kinase
-
Zhou T., Parillon L., Li F., Wang Y., Keats J., Lamore S., Xu Q., Shakespeare W., Dalgarno D., Zhu X. (2007) Crystal structure of the T315I mutant of AbI kinase. Chem Biol Drug Des;70:171-181.
-
(2007)
Chem Biol Drug Des
, vol.70
, pp. 171-181
-
-
Zhou, T.1
Parillon, L.2
Li, F.3
Wang, Y.4
Keats, J.5
Lamore, S.6
Xu, Q.7
Shakespeare, W.8
Dalgarno, D.9
Zhu, X.10
-
22
-
-
77953790762
-
Discovery of 3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpipera zin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (ponatinib), a Potent, Orally Active Pan-Inhibitor of Breakpoint Cluster Region-Abelson (BCR-ABL) Kinase Including the T315I Gatekeeper Mutant
-
Huang W.S., Metcalf C.A., Sundaramoorthi R., Wang Y., Zou D., Thomas R.M., Zhu X. et al. (2010) Discovery of 3-[2-(Imidazo[1, 2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpipera zin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (ponatinib), a Potent, Orally Active Pan-Inhibitor of Breakpoint Cluster Region-Abelson (BCR-ABL) Kinase Including the T315I Gatekeeper Mutant. J Med Chem;53:4701-4719.
-
(2010)
J Med Chem
, vol.53
, pp. 4701-4719
-
-
Huang, W.S.1
Metcalf, C.A.2
Sundaramoorthi, R.3
Wang, Y.4
Zou, D.5
Thomas, R.M.6
Zhu, X.7
-
23
-
-
70350507997
-
AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance
-
O'Hare T., Shakespeare W.C., Zhu X., Eide C.A., Rivera V.M., Wang F., Adrian L.T. et al. (2009) AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance. Cancer Cell;16:401-412.
-
(2009)
Cancer Cell
, vol.16
, pp. 401-412
-
-
O'Hare, T.1
Shakespeare, W.C.2
Zhu, X.3
Eide, C.A.4
Rivera, V.M.5
Wang, F.6
Adrian, L.T.7
-
24
-
-
21144451094
-
In vitro activity of Bcr-Abl inhibitors AMN107 and BMS-354825 against clinically relevant imatinib-resistant Abl kinase domain mutants
-
O'Hare T., Walters D.K., Stoffregen E.P., Jia T., Manley P.W., Mestan J., Cowan-Jacob S.W., Lee F.Y., Heinrich M.C., Deininger M.W., Druker B.J. (2005) In vitro activity of Bcr-Abl inhibitors AMN107 and BMS-354825 against clinically relevant imatinib-resistant Abl kinase domain mutants. Cancer Res;65:4500-4505.
-
(2005)
Cancer Res
, vol.65
, pp. 4500-4505
-
-
O'Hare, T.1
Walters, D.K.2
Stoffregen, E.P.3
Jia, T.4
Manley, P.W.5
Mestan, J.6
Cowan-Jacob, S.W.7
Lee, F.Y.8
Heinrich, M.C.9
Deininger, M.W.10
Druker, B.J.11
-
25
-
-
0031059866
-
Processing of X-ray diffraction data collected in oscillation mode
-
Otwinowski Z., Minor W. (1997) Processing of X-ray diffraction data collected in oscillation mode. Methods Enzymol;276:307-326.
-
(1997)
Methods Enzymol
, vol.276
, pp. 307-326
-
-
Otwinowski, Z.1
Minor, W.2
|