-
1
-
-
0028929803
-
Angiogenesis in Cancer, Vascular, Rheumatoid and Other Disease
-
Folkman, J. Angiogenesis in Cancer, Vascular, Rheumatoid and Other Disease. Nat. Med. 1995, 1, 27-31.
-
(1995)
Nat. Med.
, vol.1
, pp. 27-31
-
-
Folkman, J.1
-
2
-
-
0034648765
-
Angiogenesis in Cancer and Other Diseases
-
Carmeliet, P.; Jain, R. K. Angiogenesis in Cancer and Other Diseases. Nature 2000, 407, 249-257.
-
(2000)
Nature
, vol.407
, pp. 249-257
-
-
Carmeliet, P.1
Jain, R.K.2
-
3
-
-
82755183572
-
Comparative Effectiveness of Axitinib Versus Sorafenib in Advanced Renal Cell Carcinoma (AXIS): A Randomised Phase 3 Trial
-
Rini, B. I.; Escudier, B.; Tomczak, P.; Kaprin, A.; Szczylik, C.; Hutson, T. E.; Michaelson, M. D.; Gorbunova, V. A.; Gore, M. E.; Rusakov, I. G.; Negrier, S.; Ou, Y.-C.; Castellano, D.; Lim, H. Y.; Uemura, H.; Tarazi, J.; Cella, D.; Chen, C.; Rosbrook, B.; Kim, S.; Motzer, R. J. Comparative Effectiveness of Axitinib Versus Sorafenib in Advanced Renal Cell Carcinoma (AXIS): A Randomised Phase 3 Trial. Lancet 2011, 378, 1931-1939.
-
(2011)
Lancet
, vol.378
, pp. 1931-1939
-
-
Rini, B.I.1
Escudier, B.2
Tomczak, P.3
Kaprin, A.4
Szczylik, C.5
Hutson, T.E.6
Michaelson, M.D.7
Gorbunova, V.A.8
Gore, M.E.9
Rusakov, I.G.10
Negrier, S.11
Ou, Y.-C.12
Castellano, D.13
Lim, H.Y.14
Uemura, H.15
Tarazi, J.16
Cella, D.17
Chen, C.18
Rosbrook, B.19
Kim, S.20
Motzer, R.J.21
more..
-
4
-
-
47949116252
-
Sorafenib in Advanced Hepatocellular Carcinoma
-
Llovet, J. M.; Ricci, S.; Mazzaferro, V.; Hilgard, P.; Gane, E.; Blanc, J. F.; de Oliveira, A. C.; Santoro, A.; Raoul, J. L.; Forner, A.; Schwartz, M.; Porta, C.; Zeuzem, S.; Bolondi, L.; Greten, T. F.; Galle, P. R.; Seitz, J. F.; Borbath, I.; Haussinger, D.; Giannaris, T.; Shan, M.; Moscovici, M.; Voliotis, D.; Bruix, J. Sorafenib in Advanced Hepatocellular Carcinoma. N. Engl. J. Med. 2008, 359, 378-390.
-
(2008)
N. Engl. J. Med.
, vol.359
, pp. 378-390
-
-
Llovet, J.M.1
Ricci, S.2
Mazzaferro, V.3
Hilgard, P.4
Gane, E.5
Blanc, J.F.6
De Oliveira, A.C.7
Santoro, A.8
Raoul, J.L.9
Forner, A.10
Schwartz, M.11
Porta, C.12
Zeuzem, S.13
Bolondi, L.14
Greten, T.F.15
Galle, P.R.16
Seitz, J.F.17
Borbath, I.18
Haussinger, D.19
Giannaris, T.20
Shan, M.21
Moscovici, M.22
Voliotis, D.23
Bruix, J.24
more..
-
5
-
-
84872921660
-
Regorafenib Monotherapy for Previously Treated Metastatic Colorectal Cancer (CORRECT): An International, Multicentre, Randomised, Placebo-Controlled, Phase 3 Trial
-
Grothey, A.; Van Cutsem, E.; Sobrero, A.; Siena, S.; Falcone, A.; Ychou, M.; Humblet, Y.; Bouche, O.; Mineur, L.; Barone, C.; Adenis, A.; Tabernero, J.; Yoshino, T.; Lenz, H. J.; Goldberg, R. M.; Sargent, D. J.; Cihon, F.; Cupit, L.; Wagner, A.; Laurent, D. Regorafenib Monotherapy for Previously Treated Metastatic Colorectal Cancer (CORRECT): An International, Multicentre, Randomised, Placebo-Controlled, Phase 3 Trial. Lancet 2013, 381, 303-312.
-
(2013)
Lancet
, vol.381
, pp. 303-312
-
-
Grothey, A.1
Van Cutsem, E.2
Sobrero, A.3
Siena, S.4
Falcone, A.5
Ychou, M.6
Humblet, Y.7
Bouche, O.8
Mineur, L.9
Barone, C.10
Adenis, A.11
Tabernero, J.12
Yoshino, T.13
Lenz, H.J.14
Goldberg, R.M.15
Sargent, D.J.16
Cihon, F.17
Cupit, L.18
Wagner, A.19
Laurent, D.20
more..
-
6
-
-
33745298429
-
Rational Design of Inhibitors That Bind to Inactive Kinase Conformations
-
Liu, Y.; Gray, N. S. Rational Design of Inhibitors That Bind to Inactive Kinase Conformations. Nat. Chem. Biol. 2006, 2, 358-364.
-
(2006)
Nat. Chem. Biol.
, vol.2
, pp. 358-364
-
-
Liu, Y.1
Gray, N.S.2
-
7
-
-
44049103958
-
Residence Time of Receptor-Ligand Complexes and Its Effect on Biological Function
-
Tummino, P. J.; Copeland, R. A. Residence Time of Receptor-Ligand Complexes and Its Effect on Biological Function. Biochemistry 2008, 47, 5481-5492.
-
(2008)
Biochemistry
, vol.47
, pp. 5481-5492
-
-
Tummino, P.J.1
Copeland, R.A.2
-
8
-
-
33749623857
-
Can Binding Kinetics Translate to a Clinically Differentiated Drug? From Theory to Practice
-
Swinney, D. C. Can Binding Kinetics Translate to a Clinically Differentiated Drug? From Theory to Practice. Lett. Drug Des. Discovery 2006, 3, 569-574.
-
(2006)
Lett. Drug Des. Discovery
, vol.3
, pp. 569-574
-
-
Swinney, D.C.1
-
9
-
-
33748325882
-
Drug-Target Residence Time and Its Implications for Lead Optimization
-
Copeland, R. A.; Pompliano, D. L.; Meek, T. D. Drug-Target Residence Time and Its Implications for Lead Optimization. Nat. Rev. Drug Discovery 2006, 5, 730-739.
-
(2006)
Nat. Rev. Drug Discovery
, vol.5
, pp. 730-739
-
-
Copeland, R.A.1
Pompliano, D.L.2
Meek, T.D.3
-
10
-
-
37349105704
-
E7080, a Novel Inhibitor That Targets Multiple Kinases, Has Potent Antitumor Activities against Stem Cell Factor Producing Human Small Cell Lung Cancer H146, Based on Angiogenesis Inhibition
-
Matsui, J.; Yamamoto, Y.; Funahashi, Y.; Tsuruoka, A.; Watanabe, T.; Wakabayashi, T.; Uenaka, T.; Asada, M. E7080, a Novel Inhibitor That Targets Multiple Kinases, Has Potent Antitumor Activities against Stem Cell Factor Producing Human Small Cell Lung Cancer H146, Based on Angiogenesis Inhibition. Int. J. Cancer 2008, 122, 664-671.
-
(2008)
Int. J. Cancer
, vol.122
, pp. 664-671
-
-
Matsui, J.1
Yamamoto, Y.2
Funahashi, Y.3
Tsuruoka, A.4
Watanabe, T.5
Wakabayashi, T.6
Uenaka, T.7
Asada, M.8
-
11
-
-
53049085556
-
Multi-Kinase Inhibitor E7080 Suppresses Lymph Node and Lung Metastases of Human Mammary Breast Tumor MDA-MB-231 Via Inhibition of Vascular Endothelial Growth Factor-Receptor (VEGF-R) 2 and VEGF-R3 Kinase
-
Matsui, J.; Funahashi, Y.; Uenaka, T.; Watanabe, T.; Tsuruoka, A.; Asada, M. Multi-Kinase Inhibitor E7080 Suppresses Lymph Node and Lung Metastases of Human Mammary Breast Tumor MDA-MB-231 Via Inhibition of Vascular Endothelial Growth Factor-Receptor (VEGF-R) 2 and VEGF-R3 Kinase. Clin. Cancer Res. 2008, 14, 5459-5465.
-
(2008)
Clin. Cancer Res.
, vol.14
, pp. 5459-5465
-
-
Matsui, J.1
Funahashi, Y.2
Uenaka, T.3
Watanabe, T.4
Tsuruoka, A.5
Asada, M.6
-
12
-
-
84883811272
-
Antitumor Activities of the Targeted Multi-Tyrosine Kinase Inhibitor Lenvatinib (E7080) against RET Gene Fusion-Driven Tumor Models
-
Okamoto, K.; Kodama, K.; Takase, K.; Sugi, N. H.; Yamamoto, Y.; Iwata, M.; Tsuruoka, A. Antitumor Activities of the Targeted Multi-Tyrosine Kinase Inhibitor Lenvatinib (E7080) against RET Gene Fusion-Driven Tumor Models. Cancer Lett. 2013, 340, 97-103.
-
(2013)
Cancer Lett.
, vol.340
, pp. 97-103
-
-
Okamoto, K.1
Kodama, K.2
Takase, K.3
Sugi, N.H.4
Yamamoto, Y.5
Iwata, M.6
Tsuruoka, A.7
-
13
-
-
84910633715
-
A Phase 3, Multicenter, Double-Blind, Placebo-Controlled Trial of Lenvatinib (E7080) in Patients with 131I-Refractory Differentiated Thyroid Cancer (SELECT)
-
Schlumberger, M.; Tahara, M.; Wirth, L. J.; Robinson, B.; Brose, M. S.; Elisei, R.; Dutcus, C. E.; de las Heras, B.; Zhu, J.; Habra, M. A.; Newbold, K.; Shah, M. H.; Hoff, A. O.; Gianoukakis, A. G.; Kiyota, N.; Taylor, M. H.; Kim, S.-B.; Krzyzanowska, M. K.; Sherman, S. I. A Phase 3, Multicenter, Double-Blind, Placebo-Controlled Trial of Lenvatinib (E7080) in Patients with 131I-Refractory Differentiated Thyroid Cancer (SELECT). ASCO Meet. Abstr. 2014, 32, LBA6008.
-
(2014)
ASCO Meet. Abstr.
, vol.32
, pp. LBA6008
-
-
Schlumberger, M.1
Tahara, M.2
Wirth, L.J.3
Robinson, B.4
Brose, M.S.5
Elisei, R.6
Dutcus, C.E.7
De Las Heras, B.8
Zhu, J.9
Habra, M.A.10
Newbold, K.11
Shah, M.H.12
Hoff, A.O.13
Gianoukakis, A.G.14
Kiyota, N.15
Taylor, M.H.16
Kim, S.-B.17
Krzyzanowska, M.K.18
Sherman, S.I.19
-
14
-
-
67650960664
-
Fragment-Based Lead Generation: Identification of Seed Fragments by a Highly Efficient Fragment Screening Technology
-
Neumann, L.; Ritscher, A.; Müller, G.; Hafenbradl, D. Fragment-Based Lead Generation: Identification of Seed Fragments by a Highly Efficient Fragment Screening Technology. J. Comput.-Aided Mol. Des. 2009, 23, 501-511.
-
(2009)
J. Comput.-Aided Mol. Des.
, vol.23
, pp. 501-511
-
-
Neumann, L.1
Ritscher, A.2
Müller, G.3
Hafenbradl, D.4
-
15
-
-
79952096135
-
Biochemical Characterization of TAK-593, a Novel VEGFR/PDGFR Inhibitor with a Two-Step Slow Binding Mechanism
-
Iwata, H.; Imamura, S.; Hori, A.; Hixon, M. S.; Kimura, H.; Miki, H. Biochemical Characterization of TAK-593, a Novel VEGFR/PDGFR Inhibitor with a Two-Step Slow Binding Mechanism. Biochemistry 2011, 50, 738-751.
-
(2011)
Biochemistry
, vol.50
, pp. 738-751
-
-
Iwata, H.1
Imamura, S.2
Hori, A.3
Hixon, M.S.4
Kimura, H.5
Miki, H.6
-
16
-
-
80052579653
-
Biochemical Characterization of a Novel Type-II VEGFR2 Kinase Inhibitor: Comparison of Binding to Non-Phosphorylated and Phosphorylated VEGFR2
-
Iwata, H.; Imamura, S.; Hori, A.; Hixon, M. S.; Kimura, H.; Miki, H. Biochemical Characterization of a Novel Type-II VEGFR2 Kinase Inhibitor: Comparison of Binding to Non-Phosphorylated and Phosphorylated VEGFR2. Bioorg. Med. Chem. 2011, 19, 5342-5351.
-
(2011)
Bioorg. Med. Chem.
, vol.19
, pp. 5342-5351
-
-
Iwata, H.1
Imamura, S.2
Hori, A.3
Hixon, M.S.4
Kimura, H.5
Miki, H.6
-
17
-
-
0033026444
-
Strategies toward the Design of Novel and Selective Protein Tyrosine Kinase Inhibitors
-
Traxler, P.; Furet, P. Strategies toward the Design of Novel and Selective Protein Tyrosine Kinase Inhibitors. Pharmacol. Ther. 1999, 82, 195-206.
-
(1999)
Pharmacol. Ther.
, vol.82
, pp. 195-206
-
-
Traxler, P.1
Furet, P.2
-
18
-
-
84867816311
-
Molecular Conformations, Interactions, and Properties Associated with Drug Efficiency and Clinical Performance among VEGFR TK Inhibitors
-
McTigue, M.; Murray, B. W.; Chen, J. H.; Deng, Y. L.; Solowiej, J.; Kania, R. S. Molecular Conformations, Interactions, and Properties Associated with Drug Efficiency and Clinical Performance among VEGFR TK Inhibitors. Proc. Natl. Acad. Sci. U.S.A. 2012, 109, 18281-18289.
-
(2012)
Proc. Natl. Acad. Sci. U.S.A.
, vol.109
, pp. 18281-18289
-
-
McTigue, M.1
Murray, B.W.2
Chen, J.H.3
Deng, Y.L.4
Solowiej, J.5
Kania, R.S.6
-
19
-
-
84888757762
-
-
John Wiley & Sons, Inc.: Hoboken, NJ
-
Copeland, R. A. Evaluation of Enzyme Inhibitors in Drug Discovery: A Guide for Medicinal Chemists and Pharmacologists, 2nd ed.; John Wiley & Sons, Inc.: Hoboken, NJ, 2013; pp 294-299.
-
(2013)
Evaluation of Enzyme Inhibitors in Drug Discovery: A Guide for Medicinal Chemists and Pharmacologists, 2nd Ed.
, pp. 294-299
-
-
Copeland, R.A.1
-
20
-
-
84877853315
-
Structure-Kinetic Relationship Study of CDK8/CycC Specific Compounds
-
Schneider, E. V.; Bottcher, J.; Huber, R.; Maskos, K.; Neumann, L. Structure-Kinetic Relationship Study of CDK8/CycC Specific Compounds. Proc. Natl. Acad. Sci. U.S.A. 2013, 110, 8081-8086.
-
(2013)
Proc. Natl. Acad. Sci. U.S.A.
, vol.110
, pp. 8081-8086
-
-
Schneider, E.V.1
Bottcher, J.2
Huber, R.3
Maskos, K.4
Neumann, L.5
-
21
-
-
33846899405
-
Molecular Recognition of Protein Kinase Binding Pockets for Design of Potent and Selective Kinase Inhibitors
-
Liao, J. J. Molecular Recognition of Protein Kinase Binding Pockets for Design of Potent and Selective Kinase Inhibitors. J. Med. Chem. 2007, 50, 409-424.
-
(2007)
J. Med. Chem.
, vol.50
, pp. 409-424
-
-
Liao, J.J.1
-
22
-
-
4544344125
-
CH/Pai Hydrogen Bonds in Crystals
-
Nishio, M. CH/Pai Hydrogen Bonds in Crystals. CrystEngComm 2004, 6, 130.
-
(2004)
CrystEngComm
, vol.6
, pp. 130
-
-
Nishio, M.1
-
23
-
-
57649159085
-
Structure-Activity Relationship Studies of 5-Benzylaminoimidazo-[1,2-C]Pyrimidine-8-Carboxamide Derivatives as Potent, Highly Selective ZAP-70 Kinase Inhibitors
-
Hirabayashi, A.; Mukaiyama, H.; Kobayashi, H.; Shiohara, H.; Nakayama, S.; Ozawa, M.; Miyazawa, K.; Misawa, K.; Ohnota, H.; Isaji, M. Structure-Activity Relationship Studies of 5-Benzylaminoimidazo-[1,2-C]Pyrimidine-8-Carboxamide Derivatives as Potent, Highly Selective ZAP-70 Kinase Inhibitors. Bioorg. Med. Chem. 2009, 17, 284-294.
-
(2009)
Bioorg. Med. Chem.
, vol.17
, pp. 284-294
-
-
Hirabayashi, A.1
Mukaiyama, H.2
Kobayashi, H.3
Shiohara, H.4
Nakayama, S.5
Ozawa, M.6
Miyazawa, K.7
Misawa, K.8
Ohnota, H.9
Isaji, M.10
-
24
-
-
84920725625
-
Antitumor Activity of Lenvatinib (E7080): An Angiogenesis Inhibitor That Targets Multiple Receptor Tyrosine Kinases in Preclinical Human Thyroid Cancer Models
-
Tohyama, O.; Matsui, J.; Kodama, K.; Hata-Sugi, N.; Kimura, T.; Okamoto, K.; Minoshima, Y.; Iwata, M.; Funahashi, Y. Antitumor Activity of Lenvatinib (E7080): An Angiogenesis Inhibitor That Targets Multiple Receptor Tyrosine Kinases in Preclinical Human Thyroid Cancer Models. J. Thyroid Res. 2014, 2014, 638747.
-
(2014)
J. Thyroid Res.
, vol.2014
, pp. 638747
-
-
Tohyama, O.1
Matsui, J.2
Kodama, K.3
Hata-Sugi, N.4
Kimura, T.5
Okamoto, K.6
Minoshima, Y.7
Iwata, M.8
Funahashi, Y.9
-
25
-
-
67349094019
-
A New Screening Assay for Allosteric Inhibitors of cSrc
-
Simard, J. R.; Klüter, S.; Grütter, C.; Getlik, M.; Rabiller, M.; Rode, H. B.; Rauh, D. A New Screening Assay for Allosteric Inhibitors of cSrc. Nat. Chem. Biol. 2009, 5, 394-396.
-
(2009)
Nat. Chem. Biol.
, vol.5
, pp. 394-396
-
-
Simard, J.R.1
Klüter, S.2
Grütter, C.3
Getlik, M.4
Rabiller, M.5
Rode, H.B.6
Rauh, D.7
-
26
-
-
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
-
27
-
-
84880177115
-
Type II Kinase Inhibitors: An Opportunity in Cancer for Rational Design
-
Blanc, J.; Geney, R.; Menet, C. Type II Kinase Inhibitors: An Opportunity in Cancer for Rational Design. Anticancer Agents Med. Chem. 2013, 13, 731-747.
-
(2013)
Anticancer Agents Med. Chem.
, vol.13
, pp. 731-747
-
-
Blanc, J.1
Geney, R.2
Menet, C.3
|