-
1
-
-
0037032835
-
The protein kinase complement of the human genome
-
Manning, G.; Whyte, D. B.; Martinez, R.; Hunter, T.; Sudarsanam, S. The protein kinase complement of the human genome Science 2002, 298, 1912-1934
-
(2002)
Science
, vol.298
, pp. 1912-1934
-
-
Manning, G.1
Whyte, D.B.2
Martinez, R.3
Hunter, T.4
Sudarsanam, S.5
-
2
-
-
77950573400
-
Through the "gatekeeper door": Exploiting the active kinase conformation
-
Zuccotto, F.; Ardini, E.; Casale, E.; Angiolini, M. Through the "gatekeeper door": exploiting the active kinase conformation J. Med. Chem. 2010, 53, 2681-2694
-
(2010)
J. Med. Chem.
, vol.53
, pp. 2681-2694
-
-
Zuccotto, F.1
Ardini, E.2
Casale, E.3
Angiolini, M.4
-
3
-
-
57749188299
-
Targeting cancer with small molecule kinase inhibitors
-
Zhang, J.; Yang, P. L.; Gray, N. S. Targeting cancer with small molecule kinase inhibitors Nature Rev. Cancer 2009, 9, 28-39
-
(2009)
Nature Rev. Cancer
, vol.9
, pp. 28-39
-
-
Zhang, J.1
Yang, P.L.2
Gray, N.S.3
-
4
-
-
0037013143
-
The conformational plasticity of protein kinases
-
Huse, M.; Kuriyan, J. The conformational plasticity of protein kinases Cell 2002, 109, 275-282
-
(2002)
Cell
, vol.109
, pp. 275-282
-
-
Huse, M.1
Kuriyan, J.2
-
5
-
-
34249818791
-
C-Abl tyrosine kinase and inhibition by the cancer drug imatinib (Gleevec/STI-571)
-
Nagar, B. c-Abl tyrosine kinase and inhibition by the cancer drug imatinib (Gleevec/STI-571) J. Nutr. 2007, 137, 1518S-1523S
-
(2007)
J. Nutr.
, vol.137
-
-
Nagar, B.1
-
6
-
-
0030766163
-
Crystal structure of the activated insulin receptor tyrosine kinase in complex with peptide substrate and ATP analog
-
Hubbard, S. R. Crystal structure of the activated insulin receptor tyrosine kinase in complex with peptide substrate and ATP analog EMBO J. 1997, 16, 5572-5581
-
(1997)
EMBO J.
, vol.16
, pp. 5572-5581
-
-
Hubbard, S.R.1
-
7
-
-
0028582185
-
Crystal structure of the tyrosine kinase domain of the human insulin receptor
-
Hubbard, S. R.; Wei, L.; Ellis, L.; Hendrickson, W. A. Crystal structure of the tyrosine kinase domain of the human insulin receptor Nature 1994, 372, 746-754
-
(1994)
Nature
, vol.372
, pp. 746-754
-
-
Hubbard, S.R.1
Wei, L.2
Ellis, L.3
Hendrickson, W.A.4
-
8
-
-
0031034930
-
Crystal structure of the Src family tyrosine kinase Hck
-
Sicheri, F.; Moarefi, I.; Kuriyan, J. Crystal structure of the Src family tyrosine kinase Hck Nature 1997, 385, 602-609
-
(1997)
Nature
, vol.385
, pp. 602-609
-
-
Sicheri, F.1
Moarefi, I.2
Kuriyan, J.3
-
9
-
-
9444287030
-
Common and distinct elements in cellular signaling via EGF and FGF receptors
-
Schlessinger, J. Common and distinct elements in cellular signaling via EGF and FGF receptors Science 2004, 306, 1506-1507
-
(2004)
Science
, vol.306
, pp. 1506-1507
-
-
Schlessinger, J.1
-
10
-
-
63749086305
-
ErbB receptors and signaling pathways in cancer
-
Hynes, N. E.; MacDonald, G. ErbB receptors and signaling pathways in cancer Curr. Opin. Cell Biol. 2009, 21, 177-184
-
(2009)
Curr. Opin. Cell Biol.
, vol.21
, pp. 177-184
-
-
Hynes, N.E.1
MacDonald, G.2
-
11
-
-
0035144559
-
Mistletoe for cancer?
-
Ernst, E. Mistletoe for cancer? Eur. J. Cancer 2001, 37, 9-11
-
(2001)
Eur. J. Cancer
, vol.37
, pp. 9-11
-
-
Ernst, E.1
-
12
-
-
0033992633
-
Biochemical and clinical implications of the ErbB/HER signaling network of growth factor receptors
-
Klapper, L. N.; Kirschbaum, M. H.; Sela, M.; Yarden, Y. Biochemical and clinical implications of the ErbB/HER signaling network of growth factor receptors Adv. Cancer Res. 2000, 77, 25-79
-
(2000)
Adv. Cancer Res.
, vol.77
, pp. 25-79
-
-
Klapper, L.N.1
Kirschbaum, M.H.2
Sela, M.3
Yarden, Y.4
-
13
-
-
0034600849
-
The ErbB signaling network: Receptor heterodimerization in development and cancer
-
Olayioye, M. A.; Neve, R. M.; Lane, H. A.; Hynes, N. E. The ErbB signaling network: receptor heterodimerization in development and cancer EMBO J. 2000, 19, 3159-3167
-
(2000)
EMBO J.
, vol.19
, pp. 3159-3167
-
-
Olayioye, M.A.1
Neve, R.M.2
Lane, H.A.3
Hynes, N.E.4
-
14
-
-
0141599428
-
Structure of the epidermal growth factor receptor kinase domain alone and in complex with a 4-anilinoquinazoline inhibitor
-
Stamos, J.; Sliwkowski, M. X.; Eigenbrot, C. Structure of the epidermal growth factor receptor kinase domain alone and in complex with a 4-anilinoquinazoline inhibitor J. Biol. Chem. 2002, 277, 46265-46272
-
(2002)
J. Biol. Chem.
, vol.277
, pp. 46265-46272
-
-
Stamos, J.1
Sliwkowski, M.X.2
Eigenbrot, C.3
-
15
-
-
31544434945
-
Cetuximab and irinotecan interact synergistically to inhibit the growth of orthotopic anaplastic thyroid carcinoma xenografts in nude mice
-
Kim, S.; Prichard, C. N.; Younes, M. N.; Yazici, Y. D.; Jasser, S. A.; Bekele, B. N.; Myers, J. N. Cetuximab and irinotecan interact synergistically to inhibit the growth of orthotopic anaplastic thyroid carcinoma xenografts in nude mice Clin. Cancer Res. 2006, 12, 600-607
-
(2006)
Clin. Cancer Res.
, vol.12
, pp. 600-607
-
-
Kim, S.1
Prichard, C.N.2
Younes, M.N.3
Yazici, Y.D.4
Jasser, S.A.5
Bekele, B.N.6
Myers, J.N.7
-
16
-
-
0033763084
-
ZD1839 ('Iressa') as an anticancer agent
-
Baselga, J.; Averbuch, S. D. ZD1839 ('Iressa') as an anticancer agent Drugs 2000, 60, 33-40
-
(2000)
Drugs
, vol.60
, pp. 33-40
-
-
Baselga, J.1
Averbuch, S.D.2
-
17
-
-
33847406095
-
Structures of lung cancer-derived EGFR mutants and inhibitor complexes: Mechanism of activation and insights into differential inhibitor sensitivity
-
Yun, C. H.; Boggon, T. J.; Li, Y.; Woo, M. S.; Greulich, H.; Meyerson, M.; Eck, M. J. Structures of lung cancer-derived EGFR mutants and inhibitor complexes: mechanism of activation and insights into differential inhibitor sensitivity Cancer Cell 2007, 11, 217-227
-
(2007)
Cancer Cell
, vol.11
, pp. 217-227
-
-
Yun, C.H.1
Boggon, T.J.2
Li, Y.3
Woo, M.S.4
Greulich, H.5
Meyerson, M.6
Eck, M.J.7
-
18
-
-
0035553174
-
The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo
-
Rusnak, D. W.; Lackey, K.; Affleck, K.; Wood, E. R.; Alligood, K. J.; Rhodes, N.; Keith, B. R.; Murray, D. M.; Knight, W. B.; Mullin, R. J.; Gilmer, T. M. The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo Mol. Cancer Ther. 2001, 1, 85-94
-
(2001)
Mol. Cancer Ther.
, vol.1
, pp. 85-94
-
-
Rusnak, D.W.1
Lackey, K.2
Affleck, K.3
Wood, E.R.4
Alligood, K.J.5
Rhodes, N.6
Keith, B.R.7
Murray, D.M.8
Knight, W.B.9
Mullin, R.J.10
Gilmer, T.M.11
-
19
-
-
4644289313
-
A unique structure for epidermal growth factor receptor bound to GW572016 (Lapatinib): Relationships among protein conformation, inhibitor off-rate, and receptor activity in tumor cells
-
Wood, E. R.; Truesdale, A. T.; McDonald, O. B.; Yuan, D.; Hassell, A.; Dickerson, S. H.; Ellis, B.; Pennisi, C.; Horne, E.; Lackey, K.; Alligood, K. J.; Rusnak, D. W.; Gilmer, T. M.; Shewchuk, L. A unique structure for epidermal growth factor receptor bound to GW572016 (Lapatinib): relationships among protein conformation, inhibitor off-rate, and receptor activity in tumor cells Cancer Res. 2004, 64, 6652-6659
-
(2004)
Cancer Res.
, vol.64
, pp. 6652-6659
-
-
Wood, E.R.1
Truesdale, A.T.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.J.11
Rusnak, D.W.12
Gilmer, T.M.13
Shewchuk, L.14
-
20
-
-
20944433324
-
Dual inhibition of epidermal growth factor receptor and vascular endothelial growth factor receptor phosphorylation by AEE788 reduces growth and metastasis of human colon carcinoma in an orthotopic nude mouse model
-
Yokoi, K.; Thaker, P. H.; Yazici, S.; Rebhun, R. R.; Nam, D. H.; He, J.; Kim, S. J.; Abbruzzese, J. L.; Hamilton, S. R.; Fidler, I. J. Dual inhibition of epidermal growth factor receptor and vascular endothelial growth factor receptor phosphorylation by AEE788 reduces growth and metastasis of human colon carcinoma in an orthotopic nude mouse model Cancer Res. 2005, 65, 3716-3725
-
(2005)
Cancer Res.
, vol.65
, pp. 3716-3725
-
-
Yokoi, K.1
Thaker, P.H.2
Yazici, S.3
Rebhun, R.R.4
Nam, D.H.5
He, J.6
Kim, S.J.7
Abbruzzese, J.L.8
Hamilton, S.R.9
Fidler, I.J.10
-
21
-
-
33750708563
-
Preclinical antitumor activity of BMS-599626, a pan-HER kinase inhibitor that inhibits HER1/HER2 homodimer and heterodimer signaling
-
Wong, T. W.; Lee, F. Y.; Yu, C.; Luo, F. R.; Oppenheimer, S.; Zhang, H.; Smykla, R. A.; Mastalerz, H.; Fink, B. E.; Hunt, J. T.; Gavai, A. V.; Vite, G. D. Preclinical antitumor activity of BMS-599626, a pan-HER kinase inhibitor that inhibits HER1/HER2 homodimer and heterodimer signaling Clin. Cancer Res. 2006, 12, 6186-6193
-
(2006)
Clin. Cancer Res.
, vol.12
, pp. 6186-6193
-
-
Wong, T.W.1
Lee, F.Y.2
Yu, C.3
Luo, F.R.4
Oppenheimer, S.5
Zhang, H.6
Smykla, R.A.7
Mastalerz, H.8
Fink, B.E.9
Hunt, J.T.10
Gavai, A.V.11
Vite, G.D.12
-
22
-
-
79956310563
-
Structural analysis of the mechanism of inhibition and allosteric activation of the kinase domain of HER2 protein
-
Aertgeerts, K.; Skene, R.; Yano, J.; Sang, B. C.; Zou, H.; Snell, G.; Jennings, A.; Iwamoto, K.; Habuka, N.; Hirokawa, A.; Ishikawa, T.; Tanaka, T.; Miki, H.; Ohta, Y.; Sogabe, S. Structural analysis of the mechanism of inhibition and allosteric activation of the kinase domain of HER2 protein J. Biol. Chem. 2011, 286, 18756-18765
-
(2011)
J. Biol. Chem.
, vol.286
, pp. 18756-18765
-
-
Aertgeerts, K.1
Skene, R.2
Yano, J.3
Sang, B.C.4
Zou, H.5
Snell, G.6
Jennings, A.7
Iwamoto, K.8
Habuka, N.9
Hirokawa, A.10
Ishikawa, T.11
Tanaka, T.12
Miki, H.13
Ohta, Y.14
Sogabe, S.15
-
23
-
-
82555187407
-
Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2- d ]pyrimidine scaffold
-
Ishikawa, T.; Seto, M.; Banno, H.; Kawakita, Y.; Oorui, M.; Taniguchi, T.; Ohta, Y.; Tamura, T.; Nakayama, A.; Miki, H.; Kamiguchi, H.; Tanaka, T.; Habuka, N.; Sogabe, S.; Yano, J.; Aertgeerts, K.; Kamiyama, K. Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2- d ]pyrimidine scaffold J. Med. Chem. 2011, 54, 8030-8050
-
(2011)
J. Med. Chem.
, vol.54
, pp. 8030-8050
-
-
Ishikawa, T.1
Seto, M.2
Banno, H.3
Kawakita, Y.4
Oorui, M.5
Taniguchi, T.6
Ohta, Y.7
Tamura, T.8
Nakayama, A.9
Miki, H.10
Kamiguchi, H.11
Tanaka, T.12
Habuka, N.13
Sogabe, S.14
Yano, J.15
Aertgeerts, K.16
Kamiyama, K.17
-
24
-
-
2542582261
-
Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase
-
Rabindran, S. K.; Discafani, C. M.; Rosfjord, E. C.; Baxter, M.; Floyd, M. B.; Golas, J.; Hallett, W. A.; Johnson, B. D.; Nilakantan, R.; Overbeek, E.; Reich, M. F.; Shen, R.; Shi, X.; Tsou, H. R.; Wang, Y. F.; Wissner, A. Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase Cancer Res. 2004, 64, 3958-3965
-
(2004)
Cancer Res.
, vol.64
, pp. 3958-3965
-
-
Rabindran, S.K.1
Discafani, C.M.2
Rosfjord, E.C.3
Baxter, M.4
Floyd, M.B.5
Golas, J.6
Hallett, W.A.7
Johnson, B.D.8
Nilakantan, R.9
Overbeek, E.10
Reich, M.F.11
Shen, R.12
Shi, X.13
Tsou, H.R.14
Wang, Y.F.15
Wissner, A.16
-
25
-
-
40049099220
-
The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP
-
Yun, C. H.; Mengwasser, K. E.; Toms, A. V.; Woo, M. S.; Greulich, H.; Wong, K. K.; Meyerson, M.; Eck, M. J. The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP Proc. Natl. Acad. Sci. U S A. 2008, 105, 2070-2075
-
(2008)
Proc. Natl. Acad. Sci. U S A.
, vol.105
, pp. 2070-2075
-
-
Yun, C.H.1
Mengwasser, K.E.2
Toms, A.V.3
Woo, M.S.4
Greulich, H.5
Wong, K.K.6
Meyerson, M.7
Eck, M.J.8
-
26
-
-
72949092456
-
Novel mutant-selective EGFR kinase inhibitors against EGFR T790M
-
Zhou, W.; Ercan, D.; Chen, L.; Yun, C. H.; Li, D.; Capelletti, M.; Cortot, A. B.; Chirieac, L.; Iacob, R. E.; Padera, R.; Engen, J. R.; Wong, K. K.; Eck, M. J.; Gray, N. S.; Janne, P. A. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M Nature 2009, 462, 1070-1074
-
(2009)
Nature
, vol.462
, pp. 1070-1074
-
-
Zhou, W.1
Ercan, D.2
Chen, L.3
Yun, C.H.4
Li, D.5
Capelletti, M.6
Cortot, A.B.7
Chirieac, L.8
Iacob, R.E.9
Padera, R.10
Engen, J.R.11
Wong, K.K.12
Eck, M.J.13
Gray, N.S.14
Janne, P.A.15
-
27
-
-
38049038935
-
A phase i dose escalation study of BIBW 2992, an irreversible dual inhibitor of epidermal growth factor receptor 1 (EGFR) and 2 (HER2) tyrosine kinase in a 2-week on, 2-week off schedule in patients with advanced solid tumours
-
Eskens, F. A.; Mom, C. H.; Planting, A. S.; Gietema, J. A.; Amelsberg, A.; Huisman, H.; van Doorn, L.; Burger, H.; Stopfer, P.; Verweij, J.; de Vries, E. G. A phase I dose escalation study of BIBW 2992, an irreversible dual inhibitor of epidermal growth factor receptor 1 (EGFR) and 2 (HER2) tyrosine kinase in a 2-week on, 2-week off schedule in patients with advanced solid tumours Br. J. Cancer 2008, 98, 80-85
-
(2008)
Br. J. Cancer
, vol.98
, pp. 80-85
-
-
Eskens, F.A.1
Mom, C.H.2
Planting, A.S.3
Gietema, J.A.4
Amelsberg, A.5
Huisman, H.6
Van Doorn, L.7
Burger, H.8
Stopfer, P.9
Verweij, J.10
De Vries, E.G.11
-
28
-
-
84867621201
-
Target Binding Properties and Cellular Activity of Afatinib (BIBW 2992), an Irreversible ErbB Family Blocker
-
Solca, F.; Dahl, G.; Zoephel, A.; Bader, G.; Sanderson, M.; Klein, C.; Kraemer, O.; Himmelsbach, F.; Haaksma, E.; Adolf, G. R. Target Binding Properties and Cellular Activity of Afatinib (BIBW 2992), an Irreversible ErbB Family Blocker J. Pharmacol. Exp. Ther. 2012, 343, 342-350
-
(2012)
J. Pharmacol. Exp. Ther.
, vol.343
, pp. 342-350
-
-
Solca, F.1
Dahl, G.2
Zoephel, A.3
Bader, G.4
Sanderson, M.5
Klein, C.6
Kraemer, O.7
Himmelsbach, F.8
Haaksma, E.9
Adolf, G.R.10
-
29
-
-
84866133032
-
Dacomitinib (PF-00299804), an irreversible Pan-HER inhibitor, inhibits proliferation of HER2-amplified breast cancer cell lines resistant to trastuzumab and lapatinib
-
Kalous, O.; Conklin, D.; Desai, A. J.; O'Brien, N. A.; Ginther, C.; Anderson, L.; Cohen, D. J.; Britten, C. D.; Taylor, I.; Christensen, J. G.; Slamon, D. J.; Finn, R. S. Dacomitinib (PF-00299804), an irreversible Pan-HER inhibitor, inhibits proliferation of HER2-amplified breast cancer cell lines resistant to trastuzumab and lapatinib Mol. Cancer Ther. 2012, 11, 1978-1987
-
(2012)
Mol. Cancer Ther.
, vol.11
, pp. 1978-1987
-
-
Kalous, O.1
Conklin, D.2
Desai, A.J.3
O'Brien, N.A.4
Ginther, C.5
Anderson, L.6
Cohen, D.J.7
Britten, C.D.8
Taylor, I.9
Christensen, J.G.10
Slamon, D.J.11
Finn, R.S.12
-
30
-
-
84866255620
-
Randomized phase II study of dacomitinib (PF-00299804), an irreversible pan-human epidermal growth factor receptor inhibitor, versus erlotinib in patients with advanced non-small-cell lung cancer
-
Ramalingam, S. S.; Blackhall, F.; Krzakowski, M.; Barrios, C. H.; Park, K.; Bover, I.; Seog Heo, D.; Rosell, R.; Talbot, D. C.; Frank, R.; Letrent, S. P.; Ruiz-Garcia, A.; Taylor, I.; Liang, J. Q.; Campbell, A. K.; O'Connell, J.; Boyer, M. Randomized phase II study of dacomitinib (PF-00299804), an irreversible pan-human epidermal growth factor receptor inhibitor, versus erlotinib in patients with advanced non-small-cell lung cancer J. Clin. Oncol. 2012, 30, 3337-3344
-
(2012)
J. Clin. Oncol.
, vol.30
, pp. 3337-3344
-
-
Ramalingam, S.S.1
Blackhall, F.2
Krzakowski, M.3
Barrios, C.H.4
Park, K.5
Bover, I.6
Seog Heo, D.7
Rosell, R.8
Talbot, D.C.9
Frank, R.10
Letrent, S.P.11
Ruiz-Garcia, A.12
Taylor, I.13
Liang, J.Q.14
Campbell, A.K.15
O'Connell, J.16
Boyer, M.17
-
31
-
-
84871553618
-
Gefitinib-Related Interstitial Lung Disease in Taiwanese Patients with Non-Small-Cell Lung Cancer
-
Chang, S. C.; Chang, C. Y.; Chang, S. J.; Yuan, M. K.; Lai, Y. C.; Liu, Y. C.; Chen, C. Y.; Kuo, L. C.; Yu, C. J. Gefitinib-Related Interstitial Lung Disease in Taiwanese Patients With Non-Small-Cell Lung Cancer Clin. Lung Cancer 2012, 14, 55-61
-
(2012)
Clin. Lung Cancer
, vol.14
, pp. 55-61
-
-
Chang, S.C.1
Chang, C.Y.2
Chang, S.J.3
Yuan, M.K.4
Lai, Y.C.5
Liu, Y.C.6
Chen, C.Y.7
Kuo, L.C.8
Yu, C.J.9
-
32
-
-
38049025794
-
Review: Side effects of approved molecular targeted therapies in solid cancers
-
Widakowich, C.; de Castro, G., Jr.; de Azambuja, E.; Dinh, P.; Awada, A. Review: side effects of approved molecular targeted therapies in solid cancers Oncologist 2007, 12, 1443-1455
-
(2007)
Oncologist
, vol.12
, pp. 1443-1455
-
-
Widakowich, C.1
De Castro Jr., G.2
De Azambuja, E.3
Dinh, P.4
Awada, A.5
-
33
-
-
84455171485
-
Human metabolism of lapatinib, a dual kinase inhibitor: Implications for hepatotoxicity
-
Castellino, S.; O'Mara, M.; Koch, K.; Borts, D. J.; Bowers, G. D.; MacLauchlin, C. Human metabolism of lapatinib, a dual kinase inhibitor: implications for hepatotoxicity Drug Metab. Dispos. 2012, 40, 139-150
-
(2012)
Drug Metab. Dispos.
, vol.40
, pp. 139-150
-
-
Castellino, S.1
O'Mara, M.2
Koch, K.3
Borts, D.J.4
Bowers, G.D.5
MacLauchlin, C.6
-
34
-
-
84870840686
-
Strategies for Overcoming EGFR Resistance in the Treatment of Advanced-Stage NSCLC
-
Lovly, C. M.; Horn, L. Strategies for Overcoming EGFR Resistance in the Treatment of Advanced-Stage NSCLC Curr. Treat. Options Oncol. 2012, 13, 516-526
-
(2012)
Curr. Treat. Options Oncol.
, vol.13
, pp. 516-526
-
-
Lovly, C.M.1
Horn, L.2
-
35
-
-
80051974226
-
Off-target serine/threonine kinase 10 inhibition by erlotinib enhances lymphocytic activity leading to severe skin disorders
-
Yamamoto, N.; Honma, M.; Suzuki, H. Off-target serine/threonine kinase 10 inhibition by erlotinib enhances lymphocytic activity leading to severe skin disorders Mol. Pharmacol. 2011, 80, 466-475
-
(2011)
Mol. Pharmacol.
, vol.80
, pp. 466-475
-
-
Yamamoto, N.1
Honma, M.2
Suzuki, H.3
-
36
-
-
13944262091
-
Optimization of 6,7-disubstituted-4-(arylamino)quinoline-3-carbonitriles as orally active, irreversible inhibitors of human epidermal growth factor receptor-2 kinase activity
-
Tsou, H. R.; Overbeek-Klumpers, E. G.; Hallett, W. A.; Reich, M. F.; Floyd, M. B.; Johnson, B. D.; Michalak, R. S.; Nilakantan, R.; Discafani, C.; Golas, J.; Rabindran, S. K.; Shen, R.; Shi, X.; Wang, Y. F.; Upeslacis, J.; Wissner, A. Optimization of 6,7-disubstituted-4-(arylamino)quinoline-3- carbonitriles as orally active, irreversible inhibitors of human epidermal growth factor receptor-2 kinase activity J. Med. Chem. 2005, 48, 1107-1131
-
(2005)
J. Med. Chem.
, vol.48
, pp. 1107-1131
-
-
Tsou, H.R.1
Overbeek-Klumpers, E.G.2
Hallett, W.A.3
Reich, M.F.4
Floyd, M.B.5
Johnson, B.D.6
Michalak, R.S.7
Nilakantan, R.8
Discafani, C.9
Golas, J.10
Rabindran, S.K.11
Shen, R.12
Shi, X.13
Wang, Y.F.14
Upeslacis, J.15
Wissner, A.16
-
37
-
-
4644289313
-
A unique structure for epidermal growth factor receptor bound to GW572016 (Lapatinib): Relationships among protein conformation, inhibitor off-rate, and receptor activity in tumor cells
-
Wood, E. R.; Truesdale, A. T.; McDonald, O. B.; Yuan, D.; Hassell, A.; Dickerson, S. H.; Ellis, B.; Pennisi, C.; Horne, E.; Lackey, K.; Alligood, K. J.; Rusnak, D. W.; Gilmer, T. M.; Shewchuk, L. A unique structure for epidermal growth factor receptor bound to GW572016 (Lapatinib): relationships among protein conformation, inhibitor off-rate, and receptor activity in tumor cells Cancer Res. 2004, 64, 6652-6659
-
(2004)
Cancer Res.
, vol.64
, pp. 6652-6659
-
-
Wood, E.R.1
Truesdale, A.T.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.J.11
Rusnak, D.W.12
Gilmer, T.M.13
Shewchuk, L.14
-
38
-
-
77954325013
-
Fast-forwarding hit to lead: Aurora and epidermal growth factor receptor kinase inhibitor lead identification
-
Coumar, M. S.; Chu, C. Y.; Lin, C. W.; Shiao, H. Y.; Ho, Y. L.; Reddy, R.; Lin, W. H.; Chen, C. H.; Peng, Y. H.; Leou, J. S.; Lien, T. W.; Huang, C. T.; Fang, M. Y.; Wu, S. H.; Wu, J. S.; Chittimalla, S. K.; Song, J. S.; Hsu, J. T.; Wu, S. Y.; Liao, C. C.; Chao, Y. S.; Hsieh, H. P. Fast-forwarding hit to lead: aurora and epidermal growth factor receptor kinase inhibitor lead identification J. Med. Chem. 2010, 53, 4980-4988
-
(2010)
J. Med. Chem.
, vol.53
, pp. 4980-4988
-
-
Coumar, M.S.1
Chu, C.Y.2
Lin, C.W.3
Shiao, H.Y.4
Ho, Y.L.5
Reddy, R.6
Lin, W.H.7
Chen, C.H.8
Peng, Y.H.9
Leou, J.S.10
Lien, T.W.11
Huang, C.T.12
Fang, M.Y.13
Wu, S.H.14
Wu, J.S.15
Chittimalla, S.K.16
Song, J.S.17
Hsu, J.T.18
Wu, S.Y.19
Liao, C.C.20
Chao, Y.S.21
Hsieh, H.P.22
more..
-
39
-
-
19944426858
-
High frequency of epidermal growth factor receptor mutations with complex patterns in non-small cell lung cancers related to gefitinib responsiveness in Taiwan
-
Huang, S. F.; Liu, H. P.; Li, L. H.; Ku, Y. C.; Fu, Y. N.; Tsai, H. Y.; Chen, Y. T.; Lin, Y. F.; Chang, W. C.; Kuo, H. P.; Wu, Y. C.; Chen, Y. R.; Tsai, S. F. High frequency of epidermal growth factor receptor mutations with complex patterns in non-small cell lung cancers related to gefitinib responsiveness in Taiwan Clin. Cancer Res. 2004, 10, 8195-8203
-
(2004)
Clin. Cancer Res.
, vol.10
, pp. 8195-8203
-
-
Huang, S.F.1
Liu, H.P.2
Li, L.H.3
Ku, Y.C.4
Fu, Y.N.5
Tsai, H.Y.6
Chen, Y.T.7
Lin, Y.F.8
Chang, W.C.9
Kuo, H.P.10
Wu, Y.C.11
Chen, Y.R.12
Tsai, S.F.13
-
40
-
-
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. Crystal structures of the kinase domain of c-Abl in complex with the small molecule inhibitors PD173955 and imatinib (STI-571) Cancer Res. 2002, 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
-
41
-
-
84866334399
-
Development of o -chlorophenyl substituted pyrimidines as exceptionally potent aurora kinase inhibitors
-
Lawrence, H. R.; Martin, M. P.; Luo, Y.; Pireddu, R.; Yang, H.; Gevariya, H.; Ozcan, S.; Zhu, J. Y.; Kendig, R.; Rodriguez, M.; Elias, R.; Cheng, J. Q.; Sebti, S. M.; Schonbrunn, E.; Lawrence, N. J. Development of o -chlorophenyl substituted pyrimidines as exceptionally potent aurora kinase inhibitors J. Med. Chem. 2012, 55, 7392-7416
-
(2012)
J. Med. Chem.
, vol.55
, pp. 7392-7416
-
-
Lawrence, H.R.1
Martin, M.P.2
Luo, Y.3
Pireddu, R.4
Yang, H.5
Gevariya, H.6
Ozcan, S.7
Zhu, J.Y.8
Kendig, R.9
Rodriguez, M.10
Elias, R.11
Cheng, J.Q.12
Sebti, S.M.13
Schonbrunn, E.14
Lawrence, N.J.15
-
42
-
-
77955664248
-
X-ray crystal structure of JNK2 complexed with the p38alpha inhibitor BIRB796: Insights into the rational design of DFG-out binding MAP kinase inhibitors
-
Kuglstatter, A.; Ghate, M.; Tsing, S.; Villasenor, A. G.; Shaw, D.; Barnett, J. W.; Browner, M. F. X-ray crystal structure of JNK2 complexed with the p38alpha inhibitor BIRB796: insights into the rational design of DFG-out binding MAP kinase inhibitors Bioorg. Med. Chem. Lett. 2010, 20, 5217-5220
-
(2010)
Bioorg. Med. Chem. Lett.
, vol.20
, pp. 5217-5220
-
-
Kuglstatter, A.1
Ghate, M.2
Tsing, S.3
Villasenor, A.G.4
Shaw, D.5
Barnett, J.W.6
Browner, M.F.7
-
43
-
-
18344395134
-
Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site
-
Pargellis, C.; Tong, L.; Churchill, L.; Cirillo, P. F.; Gilmore, T.; Graham, A. G.; Grob, P. M.; Hickey, E. R.; Moss, N.; Pav, S.; Regan, J. Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site Nature Struct. Biol. 2002, 9, 268-272
-
(2002)
Nature Struct. Biol.
, vol.9
, pp. 268-272
-
-
Pargellis, C.1
Tong, L.2
Churchill, L.3
Cirillo, P.F.4
Gilmore, T.5
Graham, A.G.6
Grob, P.M.7
Hickey, E.R.8
Moss, N.9
Pav, S.10
Regan, J.11
-
44
-
-
84870520781
-
IL-13-induced airway mucus production is attenuated by MAPK13 inhibition
-
Alevy, Y. G.; Patel, A. C.; Romero, A. G.; Patel, D. A.; Tucker, J.; Roswit, W. T.; Miller, C. A.; Heier, R. F.; Byers, D. E.; Brett, T. J.; Holtzman, M. J. IL-13-induced airway mucus production is attenuated by MAPK13 inhibition J. Clin. Invest. 2012, 122, 4555-4568
-
(2012)
J. Clin. Invest.
, vol.122
, pp. 4555-4568
-
-
Alevy, Y.G.1
Patel, A.C.2
Romero, A.G.3
Patel, D.A.4
Tucker, J.5
Roswit, W.T.6
Miller, C.A.7
Heier, R.F.8
Byers, D.E.9
Brett, T.J.10
Holtzman, M.J.11
-
45
-
-
65549152514
-
Equally potent inhibition of c-Src and Abl by compounds that recognize inactive kinase conformations
-
Seeliger, M. A.; Ranjitkar, P.; Kasap, C.; Shan, Y.; Shaw, D. E.; Shah, N. P.; Kuriyan, J.; Maly, D. J. Equally potent inhibition of c-Src and Abl by compounds that recognize inactive kinase conformations Cancer Res. 2009, 69, 2384-2392
-
(2009)
Cancer Res.
, vol.69
, pp. 2384-2392
-
-
Seeliger, M.A.1
Ranjitkar, P.2
Kasap, C.3
Shan, Y.4
Shaw, D.E.5
Shah, N.P.6
Kuriyan, J.7
Maly, D.J.8
-
46
-
-
33847659183
-
C-Src binds to the cancer drug imatinib with an inactive Abl/c-Kit conformation and a distributed thermodynamic penalty
-
Seeliger, M. A.; Nagar, B.; Frank, F.; Cao, X.; Henderson, M. N.; Kuriyan, J. c-Src binds to the cancer drug imatinib with an inactive Abl/c-Kit conformation and a distributed thermodynamic penalty Structure 2007, 15, 299-311
-
(2007)
Structure
, vol.15
, pp. 299-311
-
-
Seeliger, M.A.1
Nagar, B.2
Frank, F.3
Cao, X.4
Henderson, M.N.5
Kuriyan, J.6
-
47
-
-
34247370247
-
Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors
-
Hodous, B. L.; Geuns-Meyer, S. D.; Hughes, P. E.; Albrecht, B. K.; Bellon, S.; Caenepeel, S.; Cee, V. J.; Chaffee, S. C.; Emery, M.; Fretland, J.; Gallant, P.; Gu, Y.; Johnson, R. E.; Kim, J. L.; Long, A. M.; Morrison, M.; Olivieri, P. R.; Patel, V. F.; Polverino, A.; Rose, P.; Wang, L.; Zhao, H. Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors Bioorg. Med. Chem. Lett. 2007, 17, 2886-2889
-
(2007)
Bioorg. Med. Chem. Lett.
, vol.17
, pp. 2886-2889
-
-
Hodous, B.L.1
Geuns-Meyer, S.D.2
Hughes, P.E.3
Albrecht, B.K.4
Bellon, S.5
Caenepeel, S.6
Cee, V.J.7
Chaffee, S.C.8
Emery, M.9
Fretland, J.10
Gallant, P.11
Gu, Y.12
Johnson, R.E.13
Kim, J.L.14
Long, A.M.15
Morrison, M.16
Olivieri, P.R.17
Patel, V.F.18
Polverino, A.19
Rose, P.20
Wang, L.21
Zhao, H.22
more..
-
48
-
-
33847377928
-
Evolution of a highly selective and potent 2-(pyridin-2-yl)-1,3,5- triazine Tie-2 kinase inhibitor
-
Hodous, B. L.; Geuns-Meyer, S. D.; Hughes, P. E.; Albrecht, B. K.; Bellon, S.; Bready, J.; Caenepeel, S.; Cee, V. J.; Chaffee, S. C.; Coxon, A.; Emery, M.; Fretland, J.; Gallant, P.; Gu, Y.; Hoffman, D.; Johnson, R. E.; Kendall, R.; Kim, J. L.; Long, A. M.; Morrison, M.; Olivieri, P. R.; Patel, V. F.; Polverino, A.; Rose, P.; Tempest, P.; Wang, L.; Whittington, D. A.; Zhao, H. Evolution of a highly selective and potent 2-(pyridin-2-yl)-1,3,5-triazine Tie-2 kinase inhibitor J. Med. Chem. 2007, 50, 611-626
-
(2007)
J. Med. Chem.
, vol.50
, pp. 611-626
-
-
Hodous, B.L.1
Geuns-Meyer, S.D.2
Hughes, P.E.3
Albrecht, B.K.4
Bellon, S.5
Bready, J.6
Caenepeel, S.7
Cee, V.J.8
Chaffee, S.C.9
Coxon, A.10
Emery, M.11
Fretland, J.12
Gallant, P.13
Gu, Y.14
Hoffman, D.15
Johnson, R.E.16
Kendall, R.17
Kim, J.L.18
Long, A.M.19
Morrison, M.20
Olivieri, P.R.21
Patel, V.F.22
Polverino, A.23
Rose, P.24
Tempest, P.25
Wang, L.26
Whittington, D.A.27
Zhao, H.28
more..
-
49
-
-
84869087642
-
Crystal structure of human CDC7 kinase in complex with its activator DBF4
-
Hughes, S.; Elustondo, F.; Di Fonzo, A.; Leroux, F. G.; Wong, A. C.; Snijders, A. P.; Matthews, S. J.; Cherepanov, P. Crystal structure of human CDC7 kinase in complex with its activator DBF4 Nature Struct. Mol. Biol. 2012, 19, 1101-1107
-
(2012)
Nature Struct. Mol. Biol.
, vol.19
, pp. 1101-1107
-
-
Hughes, S.1
Elustondo, F.2
Di Fonzo, A.3
Leroux, F.G.4
Wong, A.C.5
Snijders, A.P.6
Matthews, S.J.7
Cherepanov, P.8
-
50
-
-
84865527163
-
An integrated chemical biology approach provides insight into Cdk2 functional redundancy and inhibitor sensitivity
-
Echalier, A.; Cot, E.; Camasses, A.; Hodimont, E.; Hoh, F.; Jay, P.; Sheinerman, F.; Krasinska, L.; Fisher, D. An integrated chemical biology approach provides insight into Cdk2 functional redundancy and inhibitor sensitivity Chem. Biol. 2012, 19, 1028-1040
-
(2012)
Chem. Biol.
, vol.19
, pp. 1028-1040
-
-
Echalier, A.1
Cot, E.2
Camasses, A.3
Hodimont, E.4
Hoh, F.5
Jay, P.6
Sheinerman, F.7
Krasinska, L.8
Fisher, D.9
-
51
-
-
84873908358
-
Comparative Structural and Functional Studies of 4-(Thiazol-5-yl)-2- (phenylamino)pyrimidine-5-carbonitrile CDK9 Inhibitors Suggest the Basis for Isotype Selectivity
-
Hole, A. J.; Baumli, S.; Shao, H.; Shi, S.; Huang, S.; Pepper, C.; Fischer, P. M.; Wang, S.; Endicott, J. A.; Noble, M. E. Comparative Structural and Functional Studies of 4-(Thiazol-5-yl)-2-(phenylamino)pyrimidine-5- carbonitrile CDK9 Inhibitors Suggest the Basis for Isotype Selectivity J. Med. Chem. 2013, 56, 660-670
-
(2013)
J. Med. Chem.
, vol.56
, pp. 660-670
-
-
Hole, A.J.1
Baumli, S.2
Shao, H.3
Shi, S.4
Huang, S.5
Pepper, C.6
Fischer, P.M.7
Wang, S.8
Endicott, J.A.9
Noble, M.E.10
-
52
-
-
84872309000
-
Optimization of inhibitors of the tyrosine kinase EphB4. 2. Cellular potency improvement and binding mode validation by X-ray crystallography
-
Lafleur, K.; Dong, J.; Huang, D.; Caflisch, A.; Nevado, C. Optimization of inhibitors of the tyrosine kinase EphB4. 2. Cellular potency improvement and binding mode validation by X-ray crystallography J. Med. Chem. 2013, 56, 84-96
-
(2013)
J. Med. Chem.
, vol.56
, pp. 84-96
-
-
Lafleur, K.1
Dong, J.2
Huang, D.3
Caflisch, A.4
Nevado, C.5
-
53
-
-
84861190659
-
The design, synthesis, and biological evaluation of PIM kinase inhibitors
-
Tsuhako, A. L.; Brown, D. S.; Koltun, E. S.; Aay, N.; Arcalas, A.; Chan, V.; Du, H.; Engst, S.; Franzini, M.; Galan, A.; Huang, P.; Johnston, S.; Kane, B.; Kim, M. H.; Laird, A. D.; Lin, R.; Mock, L.; Ngan, I.; Pack, M.; Stott, G.; Stout, T. J.; Yu, P.; Zaharia, C.; Zhang, W.; Zhou, P.; Nuss, J. M.; Kearney, P. C.; Xu, W. The design, synthesis, and biological evaluation of PIM kinase inhibitors Bioorg. Med. Chem. Lett. 2012, 22, 3732-3738
-
(2012)
Bioorg. Med. Chem. Lett.
, vol.22
, pp. 3732-3738
-
-
Tsuhako, A.L.1
Brown, D.S.2
Koltun, E.S.3
Aay, N.4
Arcalas, A.5
Chan, V.6
Du, H.7
Engst, S.8
Franzini, M.9
Galan, A.10
Huang, P.11
Johnston, S.12
Kane, B.13
Kim, M.H.14
Laird, A.D.15
Lin, R.16
Mock, L.17
Ngan, I.18
Pack, M.19
Stott, G.20
Stout, T.J.21
Yu, P.22
Zaharia, C.23
Zhang, W.24
Zhou, P.25
Nuss, J.M.26
Kearney, P.C.27
Xu, W.28
more..
-
54
-
-
79958698832
-
Structure-based design of thienobenzoxepin inhibitors of PI3-kinase
-
Staben, S. T.; Siu, M.; Goldsmith, R.; Olivero, A. G.; Do, S.; Burdick, D. J.; Heffron, T. P.; Dotson, J.; Sutherlin, D. P.; Zhu, B. Y.; Tsui, V.; Le, H.; Lee, L.; Lesnick, J.; Lewis, C.; Murray, J. M.; Nonomiya, J.; Pang, J.; Prior, W. W.; Salphati, L.; Rouge, L.; Sampath, D.; Sideris, S.; Wiesmann, C.; Wu, P. Structure-based design of thienobenzoxepin inhibitors of PI3-kinase Bioorg. Med. Chem. Lett. 2011, 21, 4054-4058
-
(2011)
Bioorg. Med. Chem. Lett.
, vol.21
, pp. 4054-4058
-
-
Staben, S.T.1
Siu, M.2
Goldsmith, R.3
Olivero, A.G.4
Do, S.5
Burdick, D.J.6
Heffron, T.P.7
Dotson, J.8
Sutherlin, D.P.9
Zhu, B.Y.10
Tsui, V.11
Le, H.12
Lee, L.13
Lesnick, J.14
Lewis, C.15
Murray, J.M.16
Nonomiya, J.17
Pang, J.18
Prior, W.W.19
Salphati, L.20
Rouge, L.21
Sampath, D.22
Sideris, S.23
Wiesmann, C.24
Wu, P.25
more..
-
55
-
-
84872298847
-
3,6-Diamino-4-(2-halophenyl)-2-benzoylthieno[2,3- b ]pyridine-5- carbonitriles are selective inhibitors of Plasmodium falciparum glycogen synthase kinase-3
-
Fugel, W.; Oberholzer, A. E.; Gschloessl, B.; Dzikowski, R.; Pressburger, N.; Preu, L.; Pearl, L. H.; Baratte, B.; Ratin, M.; Okun, I.; Doerig, C.; Kruggel, S.; Lemcke, T.; Meijer, L.; Kunick, C. 3,6-Diamino-4-(2-halophenyl)-2- benzoylthieno[2,3- b ]pyridine-5-carbonitriles are selective inhibitors of Plasmodium falciparum glycogen synthase kinase-3 J. Med. Chem. 2013, 56, 264-275
-
(2013)
J. Med. Chem.
, vol.56
, pp. 264-275
-
-
Fugel, W.1
Oberholzer, A.E.2
Gschloessl, B.3
Dzikowski, R.4
Pressburger, N.5
Preu, L.6
Pearl, L.H.7
Baratte, B.8
Ratin, M.9
Okun, I.10
Doerig, C.11
Kruggel, S.12
Lemcke, T.13
Meijer, L.14
Kunick, C.15
-
56
-
-
84870244642
-
Identification of novel series of pyrazole and indole-urea based DFG-out PYK2 inhibitors
-
Bhattacharya, S. K.; Aspnes, G. E.; Bagley, S. W.; Boehm, M.; Brosius, A. D.; Buckbinder, L.; Chang, J. S.; Dibrino, J.; Eng, H.; Frederick, K. S.; Griffith, D. A.; Griffor, M. C.; Guimaraes, C. R.; Guzman-Perez, A.; Han, S.; Kalgutkar, A. S.; Klug-McLeod, J.; Garcia-Irizarry, C.; Li, J.; Lippa, B.; Price, D. A.; Southers, J. A.; Walker, D. P.; Wei, L.; Xiao, J.; Zawistoski, M. P.; Zhao, X. Identification of novel series of pyrazole and indole-urea based DFG-out PYK2 inhibitors Bioorg. Med. Chem. Lett. 2012, 22, 7523-7529
-
(2012)
Bioorg. Med. Chem. Lett.
, vol.22
, pp. 7523-7529
-
-
Bhattacharya, S.K.1
Aspnes, G.E.2
Bagley, S.W.3
Boehm, M.4
Brosius, A.D.5
Buckbinder, L.6
Chang, J.S.7
Dibrino, J.8
Eng, H.9
Frederick, K.S.10
Griffith, D.A.11
Griffor, M.C.12
Guimaraes, C.R.13
Guzman-Perez, A.14
Han, S.15
Kalgutkar, A.S.16
Klug-Mcleod, J.17
Garcia-Irizarry, C.18
Li, J.19
Lippa, B.20
Price, D.A.21
Southers, J.A.22
Walker, D.P.23
Wei, L.24
Xiao, J.25
Zawistoski, M.P.26
Zhao, X.27
more..
-
57
-
-
84870249023
-
SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors
-
Forsyth, T.; Kearney, P. C.; Kim, B. G.; Johnson, H. W.; Aay, N.; Arcalas, A.; Brown, D. S.; Chan, V.; Chen, J.; Du, H.; Epshteyn, S.; Galan, A. A.; Huynh, T. P.; Ibrahim, M. A.; Kane, B.; Koltun, E. S.; Mann, G.; Meyr, L. E.; Lee, M. S.; Lewis, G. L.; Noguchi, R. T.; Pack, M.; Ridgway, B. H.; Shi, X.; Takeuchi, C. S.; Zu, P.; Leahy, J. W.; Nuss, J. M.; Aoyama, R.; Engst, S.; Gendreau, S. B.; Kassees, R.; Li, J.; Lin, S. H.; Martini, J. F.; Stout, T.; Tong, P.; Woolfrey, J.; Zhang, W.; Yu, P. SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors Bioorg. Med. Chem. Lett. 2012, 22, 7653-7658
-
(2012)
Bioorg. Med. Chem. Lett.
, vol.22
, pp. 7653-7658
-
-
Forsyth, T.1
Kearney, P.C.2
Kim, B.G.3
Johnson, H.W.4
Aay, N.5
Arcalas, A.6
Brown, D.S.7
Chan, V.8
Chen, J.9
Du, H.10
Epshteyn, S.11
Galan, A.A.12
Huynh, T.P.13
Ibrahim, M.A.14
Kane, B.15
Koltun, E.S.16
Mann, G.17
Meyr, L.E.18
Lee, M.S.19
Lewis, G.L.20
Noguchi, R.T.21
Pack, M.22
Ridgway, B.H.23
Shi, X.24
Takeuchi, C.S.25
Zu, P.26
Leahy, J.W.27
Nuss, J.M.28
Aoyama, R.29
Engst, S.30
Gendreau, S.B.31
Kassees, R.32
Li, J.33
Lin, S.H.34
Martini, J.F.35
Stout, T.36
Tong, P.37
Woolfrey, J.38
Zhang, W.39
Yu, P.40
more..
-
58
-
-
84866350285
-
Pyrazolopyridine inhibitors of B-Raf(V600E). Part 4: Rational design and kinase selectivity profile of cell potent type II inhibitors
-
Wenglowsky, S.; Moreno, D.; Laird, E. R.; Gloor, S. L.; Ren, L.; Risom, T.; Rudolph, J.; Sturgis, H. L.; Voegtli, W. C. Pyrazolopyridine inhibitors of B-Raf(V600E). Part 4: rational design and kinase selectivity profile of cell potent type II inhibitors Bioorg. Med. Chem. Lett. 2012, 22, 6237-6241
-
(2012)
Bioorg. Med. Chem. Lett.
, vol.22
, pp. 6237-6241
-
-
Wenglowsky, S.1
Moreno, D.2
Laird, E.R.3
Gloor, S.L.4
Ren, L.5
Risom, T.6
Rudolph, J.7
Sturgis, H.L.8
Voegtli, W.C.9
-
59
-
-
84870005710
-
Covalent inhibitors of interleukin-2 inducible T cell kinase (itk) with nanomolar potency in a whole-blood assay
-
Zapf, C. W.; Gerstenberger, B. S.; Xing, L.; Limburg, D. C.; Anderson, D. R.; Caspers, N.; Han, S.; Aulabaugh, A.; Kurumbail, R.; Shakya, S.; Li, X.; Spaulding, V.; Czerwinski, R. M.; Seth, N.; Medley, Q. G. Covalent inhibitors of interleukin-2 inducible T cell kinase (itk) with nanomolar potency in a whole-blood assay J. Med. Chem. 2012, 55, 10047-10063
-
(2012)
J. Med. Chem.
, vol.55
, pp. 10047-10063
-
-
Zapf, C.W.1
Gerstenberger, B.S.2
Xing, L.3
Limburg, D.C.4
Anderson, D.R.5
Caspers, N.6
Han, S.7
Aulabaugh, A.8
Kurumbail, R.9
Shakya, S.10
Li, X.11
Spaulding, V.12
Czerwinski, R.M.13
Seth, N.14
Medley, Q.G.15
-
60
-
-
84869453987
-
Affinity-based probes based on type II kinase inhibitors
-
Ranjitkar, P.; Perera, B. G.; Swaney, D. L.; Hari, S. B.; Larson, E. T.; Krishnamurty, R.; Merritt, E. A.; Villen, J.; Maly, D. J. Affinity-based probes based on type II kinase inhibitors J. Am. Chem. Soc. 2012, 134, 19017-19025
-
(2012)
J. Am. Chem. Soc.
, vol.134
, pp. 19017-19025
-
-
Ranjitkar, P.1
Perera, B.G.2
Swaney, D.L.3
Hari, S.B.4
Larson, E.T.5
Krishnamurty, R.6
Merritt, E.A.7
Villen, J.8
Maly, D.J.9
-
61
-
-
33947706654
-
Flipped out: Structure-guided design of selective pyrazolylpyrrole ERK inhibitors
-
Aronov, A. M.; Baker, C.; Bemis, G. W.; Cao, J.; Chen, G.; Ford, P. J.; Germann, U. A.; Green, J.; Hale, M. R.; Jacobs, M.; Janetka, J. W.; Maltais, F.; Martinez-Botella, G.; Namchuk, M. N.; Straub, J.; Tang, Q.; Xie, X. Flipped out: structure-guided design of selective pyrazolylpyrrole ERK inhibitors J. Med. Chem. 2007, 50, 1280-1287
-
(2007)
J. Med. Chem.
, vol.50
, pp. 1280-1287
-
-
Aronov, A.M.1
Baker, C.2
Bemis, G.W.3
Cao, J.4
Chen, G.5
Ford, P.J.6
Germann, U.A.7
Green, J.8
Hale, M.R.9
Jacobs, M.10
Janetka, J.W.11
Maltais, F.12
Martinez-Botella, G.13
Namchuk, M.N.14
Straub, J.15
Tang, Q.16
Xie, X.17
-
62
-
-
61349149899
-
Dissecting specificity in the Janus kinases: The structures of JAK-specific inhibitors complexed to the JAK1 and JAK2 protein tyrosine kinase domains
-
Williams, N. K.; Bamert, R. S.; Patel, O.; Wang, C.; Walden, P. M.; Wilks, A. F.; Fantino, E.; Rossjohn, J.; Lucet, I. S. Dissecting specificity in the Janus kinases: the structures of JAK-specific inhibitors complexed to the JAK1 and JAK2 protein tyrosine kinase domains J. Mol. Biol. 2009, 387, 219-232
-
(2009)
J. Mol. Biol.
, vol.387
, pp. 219-232
-
-
Williams, N.K.1
Bamert, R.S.2
Patel, O.3
Wang, C.4
Walden, P.M.5
Wilks, A.F.6
Fantino, E.7
Rossjohn, J.8
Lucet, I.S.9
-
63
-
-
77950473958
-
Kinase selectivity potential for inhibitors targeting the ATP binding site: A network analysis
-
Huang, D.; Zhou, T.; Lafleur, K.; Nevado, C.; Caflisch, A. Kinase selectivity potential for inhibitors targeting the ATP binding site: a network analysis Bioinformatics 2010, 26, 198-204
-
(2010)
Bioinformatics
, vol.26
, pp. 198-204
-
-
Huang, D.1
Zhou, T.2
Lafleur, K.3
Nevado, C.4
Caflisch, A.5
-
64
-
-
0029029617
-
Mechanism of CDK activation revealed by the structure of a cyclinA-CDK2 complex
-
Jeffrey, P. D.; Russo, A. A.; Polyak, K.; Gibbs, E.; Hurwitz, J.; Massague, J.; Pavletich, N. P. Mechanism of CDK activation revealed by the structure of a cyclinA-CDK2 complex Nature 1995, 376, 313-320
-
(1995)
Nature
, vol.376
, pp. 313-320
-
-
Jeffrey, P.D.1
Russo, A.A.2
Polyak, K.3
Gibbs, E.4
Hurwitz, J.5
Massague, J.6
Pavletich, N.P.7
-
65
-
-
43049098940
-
A cell-based high-throughput screen for epidermal growth factor receptor pathway inhibitors
-
Lin, W. H.; Song, J. S.; Chang, T. Y.; Chang, C. Y.; Fu, Y. N.; Yeh, C. L.; Wu, S. H.; Huang, Y. W.; Fang, M. Y.; Lien, T. W.; Hsieh, H. P.; Chao, Y. S.; Huang, S. F.; Tsai, S. F.; Wang, L. M.; Hsu, J. T.; Chen, Y. R. A cell-based high-throughput screen for epidermal growth factor receptor pathway inhibitors Anal. Biochem. 2008, 377, 89-94
-
(2008)
Anal. Biochem.
, vol.377
, pp. 89-94
-
-
Lin, W.H.1
Song, J.S.2
Chang, T.Y.3
Chang, C.Y.4
Fu, Y.N.5
Yeh, C.L.6
Wu, S.H.7
Huang, Y.W.8
Fang, M.Y.9
Lien, T.W.10
Hsieh, H.P.11
Chao, Y.S.12
Huang, S.F.13
Tsai, S.F.14
Wang, L.M.15
Hsu, J.T.16
Chen, Y.R.17
-
66
-
-
0000560808
-
MOLREP: An automated program for molecular replacement
-
Vagin, A.; Teplyakov, A. MOLREP: an automated program for molecular replacement J. Appl. Crystallogr. 1997, 30, 1022-1025
-
(1997)
J. Appl. Crystallogr.
, vol.30
, pp. 1022-1025
-
-
Vagin, A.1
Teplyakov, A.2
-
68
-
-
0030924992
-
Refinement of macromolecular structures by the maximum-likelihood method
-
Murshudov, G. N.; Vagin, A. A.; Dodson, E. J. Refinement of macromolecular structures by the maximum-likelihood method Acta Crystallogr., Sect. D: Biol. Crystallogr. 1997, 53, 240-255
-
(1997)
Acta Crystallogr., Sect. D: Biol. Crystallogr.
, vol.53
, pp. 240-255
-
-
Murshudov, G.N.1
Vagin, A.A.2
Dodson, E.J.3
-
69
-
-
84889120137
-
Improved methods for building protein models in electron density maps and the location of errors in these models
-
Jones, T. A.; Zou, J. Y.; Cowan, S. W.; Kjeldgaard, M. Improved methods for building protein models in electron density maps and the location of errors in these models Acta Crystallogr., Sect. A: Found. Crystallogr. 1991, 47, 110-119
-
(1991)
Acta Crystallogr., Sect. A: Found. Crystallogr.
, vol.47
, pp. 110-119
-
-
Jones, T.A.1
Zou, J.Y.2
Cowan, S.W.3
Kjeldgaard, M.4
-
70
-
-
66249103704
-
PDB-REDO: Automated re-refinement of X-ray structure models in the PDB
-
Joosten, R. P.; Salzemann, J.; Bloch, V.; Stockinger, H.; Berglund, A.-C.; Blanchet, C.; Bongcam-Rudloff, E.; Combet, C.; Da Costa, A. L.; Deleage, G.; Diarena, M.; Fabbretti, R.; Fettahi, G.; Flegel, V.; Gisel, A.; Kasam, V.; Kervinen, T.; Korpelainen, E.; Mattila, K.; Pagni, M.; Reichstadt, M.; Breton, V.; Tickle, I. J.; Vriend, G. PDB-REDO: automated re-refinement of X-ray structure models in the PDB J. Appl. Crystallogr. 2009, 42, 376-384
-
(2009)
J. Appl. Crystallogr.
, vol.42
, pp. 376-384
-
-
Joosten, R.P.1
Salzemann, J.2
Bloch, V.3
Stockinger, H.4
Berglund, A.-C.5
Blanchet, C.6
Bongcam-Rudloff, E.7
Combet, C.8
Da Costa, A.L.9
Deleage, G.10
Diarena, M.11
Fabbretti, R.12
Fettahi, G.13
Flegel, V.14
Gisel, A.15
Kasam, V.16
Kervinen, T.17
Korpelainen, E.18
Mattila, K.19
Pagni, M.20
Reichstadt, M.21
Breton, V.22
Tickle, I.J.23
Vriend, G.24
more..
-
71
-
-
74549178560
-
MolProbity: All-atom structure validation for macromolecular crystallography
-
Chen, V. B.; Arendall, W. B., III; Headd, J. J.; Keedy, D. A.; Immormino, R. M.; Kapral, G. J.; Murray, L. W.; Richardson, J. S.; Richardson, D. C. MolProbity: all-atom structure validation for macromolecular crystallography Acta Crystallogr., Sect. D: Biol. Crystallogr. 2010, 66, 12-21
-
(2010)
Acta Crystallogr., Sect. D: Biol. Crystallogr.
, vol.66
, pp. 12-21
-
-
Chen, V.B.1
Arendall III, W.B.2
Headd, J.J.3
Keedy, D.A.4
Immormino, R.M.5
Kapral, G.J.6
Murray, L.W.7
Richardson, J.S.8
Richardson, D.C.9
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