-
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 (5600), 1912-34
-
(2002)
Science
, vol.298
, Issue.5600
, pp. 1912-1934
-
-
Manning, G.1
Whyte, D.B.2
Martinez, R.3
Hunter, T.4
Sudarsanam, S.5
-
2
-
-
0026342401
-
Crystal structure of the catalytic subunit of cyclic adenosine monophosphate-dependent protein kinase
-
Knighton, D. R.; Zheng, J. H.; Ten Eyck, L. F.; Ashford, V. A.; Xuong, N. H.; Taylor, S. S.; Sowadski, J. M. Crystal structure of the catalytic subunit of cyclic adenosine monophosphate-dependent protein kinase. Science, 1991, 253 (5018), 407-14.
-
(1991)
Science
, vol.253
, Issue.5018
, pp. 407-414
-
-
Knighton, D.R.1
Zheng, J.H.2
Ten Eyck, L.F.3
Ashford, V.A.4
Xuong, N.H.5
Taylor, S.S.6
Sowadski, J.M.7
-
3
-
-
77249164281
-
The (Un)targeted cancer kinome
-
Fedorov, O.; Muller, S.; Knapp, S. The (un)targeted cancer kinome. Nat. Chem. Boil., 2010, 6 (3), 166-169.
-
(2010)
Nat. Chem. Boil.
, vol.6
, Issue.3
, pp. 166-169
-
-
Fedorov, O.1
Muller, S.2
Knapp, S.3
-
4
-
-
84929941558
-
25 years of small molecular weight kinase inhibitors: Potentials and limitations
-
Fabbro, D., 25 years of small molecular weight kinase inhibitors: potentials and limitations. Mol. Pharmacol., 2015, 87 (5), 766-75.
-
(2015)
Mol. Pharmacol.
, vol.87
, Issue.5
, pp. 766-775
-
-
Fabbro, D.1
-
5
-
-
84863619884
-
The secret life of kinases: Functions beyond catalysis
-
Rauch, J.; Volinsky, N.; Romano, D.; Kolch, W. The secret life of kinases: functions beyond catalysis. Cell communication and signaling: CCS 2011, 9 (1), 23.
-
(2011)
Cell Communication and Signaling: CCS
, vol.9
, Issue.1
, pp. 23
-
-
Rauch, J.1
Volinsky, N.2
Romano, D.3
Kolch, W.4
-
6
-
-
84896920166
-
Novel approaches for targeting kinases: Allosteric inhibition, allosteric activation and pseudokinases
-
Cowan-Jacob, S. W.; Jahnke, W.; Knapp, S. Novel approaches for targeting kinases: allosteric inhibition, allosteric activation and pseudokinases. Future Med. Chem., 2014, 6 (5), 541-61.
-
(2014)
Future Med. Chem.
, vol.6
, Issue.5
, pp. 541-561
-
-
Cowan-Jacob, S.W.1
Jahnke, W.2
Knapp, S.3
-
7
-
-
0030815562
-
Osmotic activation of the HOG MAPK pathway via Ste11p MAPKKK: Scaffold role of Pbs2p MAPKK
-
Posas, F.; Saito, H. Osmotic activation of the HOG MAPK pathway via Ste11p MAPKKK: scaffold role of Pbs2p MAPKK. Science, 1997, 276 (5319), 1702-5.
-
(1997)
Science
, vol.276
, Issue.5319
, pp. 1702-1705
-
-
Posas, F.1
Saito, H.2
-
8
-
-
84874938176
-
Discovery and characterization of novel allosteric FAK inhibitors
-
Iwatani, M.; Iwata, H.; Okabe, A.; Skene, R. J.; Tomita, N.; Hayashi, Y.; Aramaki, Y.; Hosfield, D. J.; Hori, A.; Baba, A.; Miki, H., Discovery and characterization of novel allosteric FAK inhibitors. Euro. J. Med. Chem., 2013, 61, 49-60
-
(2013)
Euro. J. Med. Chem.
, vol.61
, pp. 49-60
-
-
Iwatani, M.1
Iwata, H.2
Okabe, A.3
Skene, R.J.4
Tomita, N.5
Hayashi, Y.6
Aramaki, Y.7
Hosfield, D.J.8
Hori, A.9
Baba, A.10
Miki, H.11
-
9
-
-
70349484472
-
An allosteric kinase inhibitor binds the p21-activated kinase autoregulatory domain covalently
-
Viaud, J.; Peterson, J. R. An allosteric kinase inhibitor binds the p21-activated kinase autoregulatory domain covalently. Mol. Cancer Ther., 2009, 8 (9), 2559-65
-
(2009)
Mol. Cancer Ther.
, vol.8
, Issue.9
, pp. 2559-2565
-
-
Viaud, J.1
Peterson, J.R.2
-
10
-
-
84938058345
-
Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor
-
Karpov, A. S.; Amiri, P.; Bellamacina, C.; Bellance, M. H.; Breitenstein, W.; Daniel, D.; Denay, R.; Fabbro, D.; Fernandez, C.; Galuba, I.; Guerro-Lagasse, S.; Gutmann, S.; Hinh, L.; Jahnke, W.; Klopp, J.; Lai, A.; Lindvall, M. K.; Ma, S.; Mobitz, H.; Pecchi, S.; Rummel, G.; Shoemaker, K.; Trappe, J.; Voliva, C.; Cowan-Jacob, S. W.; Marzinzik, A. L. Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor. ACS Med. Chem. Lett., 2015, 6 (7), 776-81
-
(2015)
ACS Med. Chem. Lett.
, vol.6
, Issue.7
, pp. 776-781
-
-
Karpov, A.S.1
Amiri, P.2
Bellamacina, C.3
Bellance, M.H.4
Breitenstein, W.5
Daniel, D.6
Denay, R.7
Fabbro, D.8
Fernandez, C.9
Galuba, I.10
Guerro-Lagasse, S.11
Gutmann, S.12
Hinh, L.13
Jahnke, W.14
Klopp, J.15
Lai, A.16
Lindvall, M.K.17
Ma, S.18
Mobitz, H.19
Pecchi, S.20
Rummel, G.21
Shoemaker, K.22
Trappe, J.23
Voliva, C.24
Cowan-Jacob, S.W.25
Marzinzik, A.L.26
more..
-
11
-
-
70350074904
-
Characterization of the CHK1 allosteric inhibitor binding site
-
Vanderpool, D.; Johnson, T. O.; Ping, C.; Bergqvist, S.; Alton, G.; Phonephaly, S.; Rui, E.; Luo, C.; Deng, Y. L.; Grant, S.; Quenzer, T.; Margosiak, S.; Register, J.; Brown, E.; Ermolieff, J. Characterization of the CHK1 allosteric inhibitor binding site. Biochemistry, 2009, 48 (41), 9823-30.
-
(2009)
Biochemistry
, vol.48
, Issue.41
, pp. 9823-9830
-
-
Vanderpool, D.1
Johnson, T.O.2
Ping, C.3
Bergqvist, S.4
Alton, G.5
Phonephaly, S.6
Rui, E.7
Luo, C.8
Deng, Y.L.9
Grant, S.10
Quenzer, T.11
Margosiak, S.12
Register, J.13
Brown, E.14
Ermolieff, J.15
-
12
-
-
84860538154
-
Structural biology and drug discovery for protein-protein interactions
-
Jubb, H.; Higueruelo, A. P.; Winter, A.; Blundell, T. L. Structural biology and drug discovery for protein-protein interactions. Trends in Pharmacol. Sci., 2012, 33 (5), 241-8.
-
(2012)
Trends in Pharmacol. Sci.
, vol.33
, Issue.5
, pp. 241-248
-
-
Jubb, H.1
Higueruelo, A.P.2
Winter, A.3
Blundell, T.L.4
-
13
-
-
77952575338
-
Binding or bending: Distinction of allosteric Abl kinase agonists from antagonists by an NMR-based conformational assay
-
Jahnke, W.; Grotzfeld, R. M.; Pelle, X.; Strauss, A.; Fendrich, G.; Cowan-Jacob, S. W.; Cotesta, S.; Fabbro, D.; Furet, P.; Mestan, J.; Marzinzik, A. L. Binding or bending: distinction of allosteric Abl kinase agonists from antagonists by an NMR-based conformational assay. J. Am. Chem. Soc., 2010, 132 (20), 7043-8.
-
(2010)
J. Am. Chem. Soc.
, vol.132
, Issue.20
, pp. 7043-7048
-
-
Jahnke, W.1
Grotzfeld, R.M.2
Pelle, X.3
Strauss, A.4
Fendrich, G.5
Cowan-Jacob, S.W.6
Cotesta, S.7
Fabbro, D.8
Furet, P.9
Mestan, J.10
Marzinzik, A.L.11
-
14
-
-
84876355112
-
Inhibition of tumor angiogenesis and growth by a small-molecule multi-FGF receptor blocker with allosteric properties
-
Bono, F.; De Smet, F.; Herbert, C.; De Bock, K.; Georgiadou, M.; Fons, P.; Tjwa, M.; Alcouffe, C.; Ny, A.; Bianciotto, M.; Jonckx, B.; Murakami, M.; Lanahan, A. A.; Michielsen, C.; Sibrac, D.; Dol-Gleizes, F.; Mazzone, M.; Zacchigna, S.; Herault, J. P.; Fischer, C.; Rigon, P.; Ruiz de Almodovar, C.; Claes, F.; Blanc, I.; Poesen, K.; Zhang, J.; Segura, I.; Gueguen, G.; Bordes, M. F.; Lambrechts, D.; Broussy, R.; van de Wouwer, M.; Michaux, C.; Shimada, T.; Jean, I.; Blacher, S.; Noel, A.; Motte, P.; Rom, E.; Rakic, J. M.; Katsuma, S.; Schaeffer, P.; Yayon, A.; Van Schepdael, A.; Schwalbe, H.; Gervasio, F. L.; Carmeliet, G.; Rozensky, J.; Dewerchin, M.; Simons, M.; Christopoulos, A.; Herbert, J. M.; Carmeliet, P. Inhibition of tumor angiogenesis and growth by a small-molecule multi-FGF receptor blocker with allosteric properties. Cancer cell, 2013, 23 (4), 477-88
-
(2013)
Cancer Cell
, vol.23
, Issue.4
, pp. 477-488
-
-
Bono, F.1
De Smet, F.2
Herbert, C.3
De Bock, K.4
Georgiadou, M.5
Fons, P.6
Tjwa, M.7
Alcouffe, C.8
Ny, A.9
Bianciotto, M.10
Jonckx, B.11
Murakami, M.12
Lanahan, A.A.13
Michielsen, C.14
Sibrac, D.15
Dol-Gleizes, F.16
Mazzone, M.17
Zacchigna, S.18
Herault, J.P.19
Fischer, C.20
Rigon, P.21
Ruiz De Almodovar, C.22
Claes, F.23
Blanc, I.24
Poesen, K.25
Zhang, J.26
Segura, I.27
Gueguen, G.28
Bordes, M.F.29
Lambrechts, D.30
Broussy, R.31
Van De Wouwer, M.32
Michaux, C.33
Shimada, T.34
Jean, I.35
Blacher, S.36
Noel, A.37
Motte, P.38
Rom, E.39
Rakic, J.M.40
Katsuma, S.41
Schaeffer, P.42
Yayon, A.43
Van Schepdael, A.44
Schwalbe, H.45
Gervasio, F.L.46
Carmeliet, G.47
Rozensky, J.48
Dewerchin, M.49
Simons, M.50
Christopoulos, A.51
Herbert, J.M.52
Carmeliet, P.53
more..
-
15
-
-
84863244750
-
Biophysical and mechanistic insights into novel allosteric inhibitor of spleen tyrosine kinase
-
Hall, J.; Aulabaugh, A.; Rajamohan, F.; Liu, S.; Kaila, N.; Wan, Z. K.; Ryan, M.; Magyar, R.; Qiu, X. Biophysical and mechanistic insights into novel allosteric inhibitor of spleen tyrosine kinase. J. Biol. Chem., 2012, 287 (10), 7717-27.
-
(2012)
J. Biol. Chem.
, vol.287
, Issue.10
, pp. 7717-7727
-
-
Hall, J.1
Aulabaugh, A.2
Rajamohan, F.3
Liu, S.4
Kaila, N.5
Wan, Z.K.6
Ryan, M.7
Magyar, R.8
Qiu, X.9
-
16
-
-
84941803293
-
The ABC of protein kinase conformations
-
Mobitz, H. The ABC of protein kinase conformations. Biochimica et biophysica acta, 2015, 1854 (10 Pt B), 1555-66.
-
(2015)
Biochimica Et Biophysica Acta
, vol.1854
, Issue.10
, pp. 1555-1566
-
-
Mobitz, H.1
-
17
-
-
84928021559
-
ABL001, a Potent Allosteric Inhibitor of BCR-ABL, Prevents Emergence of Re sistant Disease When Administered in Combination with Nilotinib in an in Vivo Murine Model of Chronic Myeloid Leukemia
-
Wylie, A.; Schoepfer, J.; Berellini, G.; Cai, H. B.; Caravatti, G.; Cotesta, S.; Dodd, S.; Donovan, J.; Erb, B.; Furet, P.; Gangal, G.; Grotzfeld, R.; Hassan, Q.; Hood, T.; Iyer, V.; Jacob, S.; Jahnke, W.; Lombardo, F.; Loo, A.; Manley, P. W.; Marzinzik, A.; Palmer, M.; Pelle, X.; Salem, B.; Sharma, S.; Thohan, S.; Zhu, S.; Keen, N.; Petruzzelli, L.; Vanasse, K. G.; Sellers, W. R. ABL001, a Potent Allosteric Inhibitor of BCR-ABL, Prevents Emergence of Re sistant Disease When Administered in Combination with Nilotinib in an in Vivo Murine Model of Chronic Myeloid Leukemia. Blood, 2014, 124 (21).
-
(2014)
Blood
, vol.124
, Issue.21
-
-
Wylie, A.1
Schoepfer, J.2
Berellini, G.3
Cai, H.B.4
Caravatti, G.5
Cotesta, S.6
Dodd, S.7
Donovan, J.8
Erb, B.9
Furet, P.10
Gangal, G.11
Grotzfeld, R.12
Hassan, Q.13
Hood, T.14
Iyer, V.15
Jacob, S.16
Jahnke, W.17
Lombardo, F.18
Loo, A.19
Manley, P.W.20
Marzinzik, A.21
Palmer, M.22
Pelle, X.23
Salem, B.24
Sharma, S.25
Thohan, S.26
Zhu, S.27
Keen, N.28
Petruzzelli, L.29
Vanasse, K.G.30
Sellers, W.R.31
more..
-
18
-
-
79955038588
-
Turning a protein kinase on or off from a single allosteric site via disulfide trapping
-
Sadowsky, J. D.; Burlingame, M. A.; Wolan, D. W.; McClendon, C. L.; Jacobson, M. P.; Wells, J. A. Turning a protein kinase on or off from a single allosteric site via disulfide trapping. Proc. Natl. Acad. Sci. U.S.A., 2011, 108 (15), 6056-61.
-
(2011)
Proc. Natl. Acad. Sci. U.S.A.
, vol.108
, Issue.15
, pp. 6056-6061
-
-
Sadowsky, J.D.1
Burlingame, M.A.2
Wolan, D.W.3
McClendon, C.L.4
Jacobson, M.P.5
Wells, J.A.6
-
19
-
-
84880047467
-
DEF pocket in p38alpha facilitates substrate selectivity and mediates autophosphorylation
-
Tzarum, N.; Komornik, N.; Ben Chetrit, D.; Engelberg, D.; Livnah, O. DEF pocket in p38alpha facilitates substrate selectivity and mediates autophosphorylation. J. Biol. Chem., 2013, 288 (27), 19537-47.
-
(2013)
J. Biol. Chem.
, vol.288
, Issue.27
, pp. 19537-19547
-
-
Tzarum, N.1
Komornik, N.2
Ben Chetrit, D.3
Engelberg, D.4
Livnah, O.5
-
20
-
-
85024110816
-
-
Pymol, The PyMOL Molecular Graphics System, Version 1.5.0.4 Schrödinger, LLC
-
Pymol, The PyMOL Molecular Graphics System, Version 1.5.0.4 Schrödinger, LLC.
-
-
-
-
21
-
-
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 (7), 358-64.
-
(2006)
Nat. Chem. Biol.
, vol.2
, Issue.7
, pp. 358-364
-
-
Liu, Y.1
Gray, N.S.2
-
22
-
-
77958576132
-
Crystal structure of human AKT1 with an allosteric inhibitor reveals a new mode of kinase inhibition
-
Wu, W. I.; Voegtli, W. C.; Sturgis, H. L.; Dizon, F. P.; Vigers, G. P.; Brandhuber, B. J. Crystal structure of human AKT1 with an allosteric inhibitor reveals a new mode of kinase inhibition. PloS one, 2010, 5 (9), e12913
-
(2010)
Plos One
, vol.5
, Issue.9
, pp. 12913
-
-
Wu, W.I.1
Voegtli, W.C.2
Sturgis, H.L.3
Dizon, F.P.4
Vigers, G.P.5
Brandhuber, B.J.6
-
23
-
-
84874860953
-
Structural basis of RIP1 inhibition by necrostatins
-
Xie, T.; Peng, W.; Liu, Y.; Yan, C.; Maki, J.; Degterev, A.; Yuan, J.; Shi, Y. Structural basis of RIP1 inhibition by necrostatins. Structure, 2013, 21 (3), 493-9.
-
(2013)
Structure
, vol.21
, Issue.3
, pp. 493-499
-
-
Xie, T.1
Peng, W.2
Liu, Y.3
Yan, C.4
Maki, J.5
Degterev, A.6
Yuan, J.7
Shi, Y.8
-
24
-
-
84941931457
-
Inhibitors Targeting CDK2
-
Alexander, L. T.; Mobitz, H.; Drueckes, P.; Savitsky, P.; Fedorov, O.; Elkins, J. M.; Deane, C. M.; Cowan-Jacob, S. W.; Knapp, S. Type II Inhibitors Targeting CDK2. ACS Chem. Biol., 2015, 10 (9), 2116-25.
-
(2015)
ACS Chem. Biol.
, vol.10
, Issue.9
, pp. 2116-2125
-
-
Alexander, L.T.1
Mobitz, H.2
Drueckes, P.3
Savitsky, P.4
Fedorov, O.5
Elkins, J.M.6
Deane, C.M.7
Cowan-Jacob, S.W.8
Knapp, S.9
Type, I.I.10
-
25
-
-
84903208494
-
Exploration of type II binding mode: A privileged approach for kinase inhibitor focused drug discovery?
-
Zhao, Z.; Wu, H.; Wang, L.; Liu, Y.; Knapp, S.; Liu, Q.; Gray, N. S. Exploration of type II binding mode: A privileged approach for kinase inhibitor focused drug discovery? ACS Chem. Biol., 2014, 9 (6), 1230-41.
-
(2014)
ACS Chem. Biol.
, vol.9
, Issue.6
, pp. 1230-1241
-
-
Zhao, Z.1
Wu, H.2
Wang, L.3
Liu, Y.4
Knapp, S.5
Liu, Q.6
Gray, N.S.7
-
26
-
-
0036295728
-
Molecular mechanism for the regulation of protein kinase B/Akt by hydrophobic motif phosphorylation
-
Yang, J.; Cron, P.; Thompson, V.; Good, V. M.; Hess, D.; Hemmings, B. A.; Barford, D. Molecular mechanism for the regulation of protein kinase B/Akt by hydrophobic motif phosphorylation. Mol. Cell, 2002, 9 (6), 1227-40.
-
(2002)
Mol. Cell
, vol.9
, Issue.6
, pp. 1227-1240
-
-
Yang, J.1
Cron, P.2
Thompson, V.3
Good, V.M.4
Hess, D.5
Hemmings, B.A.6
Barford, D.7
-
27
-
-
59649092904
-
Development of thioquinazolinones, allosteric Chk1 kinase inhibitors
-
Converso, A.; Hartingh, T.; Garbaccio, R. M.; Tasber, E.; Rickert, K.; Fraley, M. E.; Yan, Y.; Kreatsoulas, C.; Stirdivant, S.; Drakas, B.; Walsh, E. S.; Hamilton, K.; Buser, C. A.; Mao, X.; Abrams, M. T.; Beck, S. C.; Tao, W.; Lobell, R.; Sepp-Lorenzino, L.; Zugay-Murphy, J.; Sardana, V.; Munshi, S. K.; Jezequel-Sur, S. M.; Zuck, P. D.; Hartman, G. D. Development of thioquinazolinones, allosteric Chk1 kinase inhibitors. Bioorg. Med. Chem. Lett., 2009, 19 (4), 1240-4.
-
(2009)
Bioorg. Med. Chem. Lett.
, vol.19
, Issue.4
, pp. 1240-1244
-
-
Converso, A.1
Hartingh, T.2
Garbaccio, R.M.3
Tasber, E.4
Rickert, K.5
Fraley, M.E.6
Yan, Y.7
Kreatsoulas, C.8
Stirdivant, S.9
Drakas, B.10
Walsh, E.S.11
Hamilton, K.12
Buser, C.A.13
Mao, X.14
Abrams, M.T.15
Beck, S.C.16
Tao, W.17
Lobell, R.18
Sepp-Lorenzino, L.19
Zugay-Murphy, J.20
Sardana, V.21
Munshi, S.K.22
Jezequel-Sur, S.M.23
Zuck, P.D.24
Hartman, G.D.25
more..
-
28
-
-
79955617610
-
Discovery and characterization of non-ATP site inhibitors of the mitogen activated protein (MAP) kinases
-
Comess, K. M.; Sun, C.; Abad-Zapatero, C.; Goedken, E. R.; Gum, R. J.; Borhani, D. W.; Argiriadi, M.; Groebe, D. R.; Jia, Y.; Clampit, J. E.; Haasch, D. L.; Smith, H. T.; Wang, S.; Song, D.; Coen, M. L.; Cloutier, T. E.; Tang, H.; Cheng, X.; Quinn, C.; Liu, B.; Xin, Z.; Liu, G.; Fry, E. H.; Stoll, V.; Ng, T. I.; Banach, D.; Marcotte, D.; Burns, D. J.; Calderwood, D. J.; Hajduk, P. J. Discovery and characterization of non-ATP site inhibitors of the mitogen activated protein (MAP) kinases. ACS Chem. Biol., 2011, 6 (3), 234-44.
-
(2011)
ACS Chem. Biol.
, vol.6
, Issue.3
, pp. 234-244
-
-
Comess, K.M.1
Sun, C.2
Abad-Zapatero, C.3
Goedken, E.R.4
Gum, R.J.5
Borhani, D.W.6
Argiriadi, M.7
Groebe, D.R.8
Jia, Y.9
Clampit, J.E.10
Haasch, D.L.11
Smith, H.T.12
Wang, S.13
Song, D.14
Coen, M.L.15
Cloutier, T.E.16
Tang, H.17
Cheng, X.18
Quinn, C.19
Liu, B.20
Xin, Z.21
Liu, G.22
Fry, E.H.23
Stoll, V.24
Ng, T.I.25
Banach, D.26
Marcotte, D.27
Burns, D.J.28
Calderwood, D.J.29
Hajduk, P.J.30
more..
-
29
-
-
79951816826
-
Discovery and characterization of a cell-permeable, small-molecule c-Abl kinase activator that binds to the myristoyl binding site
-
Yang, J.; Campobasso, N.; Biju, M. P.; Fisher, K.; Pan, X. Q.; Cottom, J.; Galbraith, S.; Ho, T.; Zhang, H.; Hong, X.; Ward, P.; Hofmann, G.; Siegfried, B.; Zappacosta, F.; Washio, Y.; Cao, P.; Qu, J.; Bertrand, S.; Wang, D. Y.; Head, M. S.; Li, H.; Moores, S.; Lai, Z.; Johanson, K.; Burton, G.; Erickson-Miller, C.; Simpson, G.; Tummino, P.; Copeland, R. A.; Oliff, A. Discovery and characterization of a cell-permeable, small-molecule c-Abl kinase activator that binds to the myristoyl binding site. Chem. Boil., 2011, 18 (2), 177-86.
-
(2011)
Chem. Boil.
, vol.18
, Issue.2
, pp. 177-186
-
-
Yang, J.1
Campobasso, N.2
Biju, M.P.3
Fisher, K.4
Pan, X.Q.5
Cottom, J.6
Galbraith, S.7
Ho, T.8
Zhang, H.9
Hong, X.10
Ward, P.11
Hofmann, G.12
Siegfried, B.13
Zappacosta, F.14
Washio, Y.15
Cao, P.16
Qu, J.17
Bertrand, S.18
Wang, D.Y.19
Head, M.S.20
Li, H.21
Moores, S.22
Lai, Z.23
Johanson, K.24
Burton, G.25
Erickson-Miller, C.26
Simpson, G.27
Tummino, P.28
Copeland, R.A.29
Oliff, A.30
more..
-
30
-
-
70349305603
-
Structure and allosteric effects of low-molecular-weight activators on the protein kinase PDK1
-
Hindie, V.; Stroba, A.; Zhang, H.; Lopez-Garcia, L. A.; Idrissova, L.; Zeuzem, S.; Hirschberg, D.; Schaeffer, F.; Jorgensen, T. J.; Engel, M.; Alzari, P. M.; Biondi, R. M. Structure and allosteric effects of low-molecular-weight activators on the protein kinase PDK1. Nat. Chem. Boil., 2009, 5 (10), 758-64.
-
(2009)
Nat. Chem. Boil.
, vol.5
, Issue.10
, pp. 758-764
-
-
Hindie, V.1
Stroba, A.2
Zhang, H.3
Lopez-Garcia, L.A.4
Idrissova, L.5
Zeuzem, S.6
Hirschberg, D.7
Schaeffer, F.8
Jorgensen, T.J.9
Engel, M.10
Alzari, P.M.11
Biondi, R.M.12
-
31
-
-
36348998521
-
Mechanism of action of A-769662, a valuable tool for activation of AMPactivated protein kinase
-
Goransson, O.; McBride, A.; Hawley, S. A.; Ross, F. A.; Shpiro, N.; Foretz, M.; Viollet, B.; Hardie, D. G.; Sakamoto, K. Mechanism of action of A-769662, a valuable tool for activation of AMPactivated protein kinase. J. Chem. Boil., 2007, 282 (45), 32549-60.
-
(2007)
J. Chem. Boil.
, vol.282
, Issue.45
, pp. 32549-32560
-
-
Goransson, O.1
McBride, A.2
Hawley, S.A.3
Ross, F.A.4
Shpiro, N.5
Foretz, M.6
Viollet, B.7
Hardie, D.G.8
Sakamoto, K.9
-
32
-
-
84890963021
-
Structural basis of AMPK regulation by small molecule activators
-
Xiao, B.; Sanders, M. J.; Carmena, D.; Bright, N. J.; Haire, L. F.; Underwood, E.; Patel, B. R.; Heath, R. B.; Walker, P. A.; Hallen, S.; Giordanetto, F.; Martin, S. R.; Carling, D.; Gamblin, S. J. Structural basis of AMPK regulation by small molecule activators. Nat. Commun., 2013, 4, 3017.
-
(2013)
Nat. Commun.
, vol.4
, pp. 3017
-
-
Xiao, B.1
Sanders, M.J.2
Carmena, D.3
Bright, N.J.4
Haire, L.F.5
Underwood, E.6
Patel, B.R.7
Heath, R.B.8
Walker, P.A.9
Hallen, S.10
Giordanetto, F.11
Martin, S.R.12
Carling, D.13
Gamblin, S.J.14
-
33
-
-
84905719900
-
Structural basis for AMPK activation: Natural and synthetic ligands regulate kinase activity from opposite poles by different molecular mechanisms
-
Calabrese, M. F.; Rajamohan, F.; Harris, M. S.; Caspers, N. L.; Magyar, R.; Withka, J. M.; Wang, H.; Borzilleri, K. A.; Sahasrabudhe, P. V.; Hoth, L. R.; Geoghegan, K. F.; Han, S.; Brown, J.; Subashi, T. A.; Reyes, A. R.; Frisbie, R. K.; Ward, J.; Miller, R. A.; Landro, J. A.; Londregan, A. T.; Carpino, P. A.; Cabral, S.; Smith, A. C.; Conn, E. L.; Cameron, K. O.; Qiu, X.; Kurumbail, R. G. Structural basis for AMPK activation: natural and synthetic ligands regulate kinase activity from opposite poles by different molecular mechanisms. Structure, 2014, 22 (8), 1161-72.
-
(2014)
Structure
, vol.22
, Issue.8
, pp. 1161-1172
-
-
Calabrese, M.F.1
Rajamohan, F.2
Harris, M.S.3
Caspers, N.L.4
Magyar, R.5
Withka, J.M.6
Wang, H.7
Borzilleri, K.A.8
Sahasrabudhe, P.V.9
Hoth, L.R.10
Geoghegan, K.F.11
Han, S.12
Brown, J.13
Subashi, T.A.14
Reyes, A.R.15
Frisbie, R.K.16
Ward, J.17
Miller, R.A.18
Landro, J.A.19
Londregan, A.T.20
Carpino, P.A.21
Cabral, S.22
Smith, A.C.23
Conn, E.L.24
Cameron, K.O.25
Qiu, X.26
Kurumbail, R.G.27
more..
-
34
-
-
84878085324
-
First structure of protein kinase CK2 catalytic subunit with an effective CK2beta-competitive ligand
-
Raaf, J.; Guerra, B.; Neundorf, I.; Bopp, B.; Issinger, O. G.; Jose, J.; Pietsch, M.; Niefind, K. First structure of protein kinase CK2 catalytic subunit with an effective CK2beta-competitive ligand. ACS Chem. Boil., 2013, 8 (5), 901-7.
-
(2013)
ACS Chem. Boil.
, vol.8
, Issue.5
, pp. 901-907
-
-
Raaf, J.1
Guerra, B.2
Neundorf, I.3
Bopp, B.4
Issinger, O.G.5
Jose, J.6
Pietsch, M.7
Niefind, K.8
-
35
-
-
84862282122
-
Discovery and optimization of a series of 3-(3-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amines: Orally bioavailable, selective, and potent ATP-independent Akt inhibitors
-
Ashwell, M. A.; Lapierre, J. M.; Brassard, C.; Bresciano, K.; Bull, C.; Cornell-Kennon, S.; Eathiraj, S.; France, D. S.; Hall, T.; Hill, J.; Kelleher, E.; Khanapurkar, S.; Kizer, D.; Koerner, S.; Link, J.; Liu, Y.; Makhija, S.; Moussa, M.; Namdev, N.; Nguyen, K.; Nicewonger, R.; Palma, R.; Szwaya, J.; Tandon, M.; Uppalapati, U.; Vensel, D.; Volak, L. P.; Volckova, E.; Westlund, N.; Wu, H.; Yang, R. Y.; Chan, T. C. Discovery and optimization of a series of 3-(3-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amines: orally bioavailable, selective, and potent ATP-independent Akt inhibitors. J. Med. Chem., 2012, 55 (11), 5291-310.
-
(2012)
J. Med. Chem.
, vol.55
, Issue.11
, pp. 5291-5310
-
-
Ashwell, M.A.1
Lapierre, J.M.2
Brassard, C.3
Bresciano, K.4
Bull, C.5
Cornell-Kennon, S.6
Eathiraj, S.7
France, D.S.8
Hall, T.9
Hill, J.10
Kelleher, E.11
Khanapurkar, S.12
Kizer, D.13
Koerner, S.14
Link, J.15
Liu, Y.16
Makhija, S.17
Moussa, M.18
Namdev, N.19
Nguyen, K.20
Nicewonger, R.21
Palma, R.22
Szwaya, J.23
Tandon, M.24
Uppalapati, U.25
Vensel, D.26
Volak, L.P.27
Volckova, E.28
Westlund, N.29
Wu, H.30
Yang, R.Y.31
Chan, T.C.32
more..
-
36
-
-
77956136788
-
Allosteric IGF-1R Inhibitors
-
Heinrich, T.; Gradler, U.; Bottcher, H.; Blaukat, A.; Shutes, A. Allosteric IGF-1R Inhibitors. ACS Med. Chem. Lett., 2010, 1 (5), 199-203.
-
(2010)
ACS Med. Chem. Lett.
, vol.1
, Issue.5
, pp. 199-203
-
-
Heinrich, T.1
Gradler, U.2
Bottcher, H.3
Blaukat, A.4
Shutes, A.5
-
37
-
-
79953774130
-
Crystal structures of ABL-related gene (ABL2) in complex with imatinib, tozasertib (VX-680), and a type I inhibitor of the triazole carbothioamide class
-
Salah, E.; Ugochukwu, E.; Barr, A. J.; von Delft, F.; Knapp, S.; Elkins, J. M., Crystal structures of ABL-related gene (ABL2) in complex with imatinib, tozasertib (VX-680), and a type I inhibitor of the triazole carbothioamide class. J. Med. Chem., 2011, 54 (7), 2359-67.
-
(2011)
J. Med. Chem.
, vol.54
, Issue.7
, pp. 2359-2367
-
-
Salah, E.1
Ugochukwu, E.2
Barr, A.J.3
Von Delft, F.4
Knapp, S.5
Elkins, J.M.6
-
38
-
-
84900491469
-
Selectively targeting an inactive conformation of interleukin-2-inducible T-cell kinase by allosteric inhibitors
-
Han, S.; Czerwinski, R. M.; Caspers, N. L.; Limburg, D. C.; Ding, W.; Wang, H.; Ohren, J. F.; Rajamohan, F.; McLellan, T. J.; Unwalla, R.; Choi, C.; Parikh, M. D.; Seth, N.; Edmonds, J.; Phillips, C.; Shakya, S.; Li, X.; Spaulding, V.; Hughes, S.; Cook, A.; Robinson, C.; Mathias, J. P.; Navratilova, I.; Medley, Q. G.; Anderson, D. R.; Kurumbail, R. G.; Aulabaugh, A., Selectively targeting an inactive conformation of interleukin-2-inducible T-cell kinase by allosteric inhibitors. Biochem. J., 2014, 460 (2), 211-22.
-
(2014)
Biochem. J.
, vol.460
, Issue.2
, pp. 211-222
-
-
Han, S.1
Czerwinski, R.M.2
Caspers, N.L.3
Limburg, D.C.4
Ding, W.5
Wang, H.6
Ohren, J.F.7
Rajamohan, F.8
McLellan, T.J.9
Unwalla, R.10
Choi, C.11
Parikh, M.D.12
Seth, N.13
Edmonds, J.14
Phillips, C.15
Shakya, S.16
Li, X.17
Spaulding, V.18
Hughes, S.19
Cook, A.20
Robinson, C.21
Mathias, J.P.22
Navratilova, I.23
Medley, Q.G.24
Anderson, D.R.25
Kurumbail, R.G.26
Aulabaugh, A.27
more..
-
39
-
-
33846834003
-
Thermodynamics of nucleotide and non-ATP-competitive inhibitor binding to MEK1 by circular dichroism and isothermal titration calorimetry
-
Smith, C. K.; Windsor, W. T., Thermodynamics of nucleotide and non-ATP-competitive inhibitor binding to MEK1 by circular dichroism and isothermal titration calorimetry. Biochem., 2007, 46 (5), 1358-67.
-
(2007)
Biochem.
, vol.46
, Issue.5
, pp. 1358-1367
-
-
Smith, C.K.1
Windsor, W.T.2
-
40
-
-
0037468159
-
The pp60c-Src inhibitor PP1 is non-competitive against ATP
-
Karni, R.; Mizrachi, S.; Reiss-Sklan, E.; Gazit, A.; Livnah, O.; Levitzki, A., The pp60c-Src inhibitor PP1 is non-competitive against ATP. FEBS Lett. 2003, 537 (1-3), 47-52.
-
(2003)
FEBS Lett
, vol.537
, Issue.1-3
, pp. 47-52
-
-
Karni, R.1
Mizrachi, S.2
Reiss-Sklan, E.3
Gazit, A.4
Livnah, O.5
Levitzki, A.6
-
41
-
-
79958002291
-
A novel mode of protein kinase inhibition exploiting hydrophobic motifs of autoinhibited kinases: Discovery of ATP-independent inhibitors of fibroblast growth factor receptor
-
Eathiraj, S.; Palma, R.; Hirschi, M.; Volckova, E.; Nakuci, E.; Castro, J.; Chen, C. R.; Chan, T. C.; France, D. S.; Ashwell, M. A. A novel mode of protein kinase inhibition exploiting hydrophobic motifs of autoinhibited kinases: discovery of ATP-independent inhibitors of fibroblast growth factor receptor. J. Biol. Chem., 2011, 286 (23), 20677-87.
-
(2011)
J. Biol. Chem.
, vol.286
, Issue.23
, pp. 20677-20687
-
-
Eathiraj, S.1
Palma, R.2
Hirschi, M.3
Volckova, E.4
Nakuci, E.5
Castro, J.6
Chen, C.R.7
Chan, T.C.8
France, D.S.9
Ashwell, M.A.10
-
42
-
-
77951953170
-
Non-competitive inhibition by active site binders
-
Blat, Y. Non-competitive inhibition by active site binders. Chem. Biol. Drug Design, 2010, 75 (6), 535-40.
-
(2010)
Chem. Biol. Drug Design
, vol.75
, Issue.6
, pp. 535-540
-
-
Blat, Y.1
-
43
-
-
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. Clinical resistance to STI-571 cancer therapy caused by BCR-ABL gene mutation or amplification. Science, 2001, 293 (5531), 876-80.
-
(2001)
Science
, vol.293
, Issue.5531
, 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
-
44
-
-
2342629325
-
Imatinib (STI571) resistance in chronic myelogenous leukemia: Molecular basis of the underlying mechanisms and potential strategies for treatment
-
Cowan-Jacob, S. W.; Guez, V.; Fendrich, G.; Griffin, J. D.; Fabbro, D.; Furet, P.; Liebetanz, J.; Mestan, J.; Manley, P. W. Imatinib (STI571) resistance in chronic myelogenous leukemia: molecular basis of the underlying mechanisms and potential strategies for treatment. Mini Rev. Med. Chem., 2004, 4 (3), 285-99.
-
(2004)
Mini Rev. Med. Chem.
, vol.4
, Issue.3
, pp. 285-299
-
-
Cowan-Jacob, S.W.1
Guez, V.2
Fendrich, G.3
Griffin, J.D.4
Fabbro, D.5
Furet, P.6
Liebetanz, J.7
Mestan, J.8
Manley, P.W.9
-
45
-
-
0344626926
-
Structural basis for the autoinhibition of c-Abl tyrosine kinase
-
Nagar, B.; Hantschel, O.; Young, M. A.; Scheffzek, K.; Veach, D.; Bornmann, W.; Clarkson, B.; Superti-Furga, G.; Kuriyan, J. Structural basis for the autoinhibition of c-Abl tyrosine kinase. Cell, 2003, 112 (6), 859-71.
-
(2003)
Cell
, vol.112
, Issue.6
, pp. 859-871
-
-
Nagar, B.1
Hantschel, O.2
Young, M.A.3
Scheffzek, K.4
Veach, D.5
Bornmann, W.6
Clarkson, B.7
Superti-Furga, G.8
Kuriyan, J.9
-
46
-
-
0344626925
-
A myristoyl/phosphotyrosine switch regulates c-Abl
-
Hantschel, O.; Nagar, B.; Guettler, S.; Kretzschmar, J.; Dorey, K.; Kuriyan, J.; Superti-Furga, G. A myristoyl/phosphotyrosine switch regulates c-Abl. Cell, 2003, 112 (6), 845-57.
-
(2003)
Cell
, vol.112
, Issue.6
, pp. 845-857
-
-
Hantschel, O.1
Nagar, B.2
Guettler, S.3
Kretzschmar, J.4
Dorey, K.5
Kuriyan, J.6
Superti-Furga, G.7
-
47
-
-
33644889108
-
Allosteric inhibitors of Bcr-abl-dependent cell proliferation
-
Adrian, F. J.; Ding, Q.; Sim, T.; Velentza, A.; Sloan, C.; Liu, Y.; Zhang, G.; Hur, W.; Ding, S.; Manley, P.; Mestan, J.; Fabbro, D.; Gray, N. S. Allosteric inhibitors of Bcr-abl-dependent cell proliferation. Nat. Chem. Biol., 2006, 2 (2), 95-102.
-
(2006)
Nat. Chem. Biol.
, vol.2
, Issue.2
, pp. 95-102
-
-
Adrian, F.J.1
Ding, Q.2
Sim, T.3
Velentza, A.4
Sloan, C.5
Liu, Y.6
Zhang, G.7
Hur, W.8
Ding, S.9
Manley, P.10
Mestan, J.11
Fabbro, D.12
Gray, N.S.13
-
48
-
-
75749146563
-
Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors
-
Zhang, J.; Adrian, F. J.; Jahnke, W.; Cowan-Jacob, S. W.; Li, A. G.; Iacob, R. E.; Sim, T.; Powers, J.; Dierks, C.; Sun, F.; Guo, G. R.; Ding, Q.; Okram, B.; Choi, Y.; Wojciechowski, A.; Deng, X.; Liu, G.; Fendrich, G.; Strauss, A.; Vajpai, N.; Grzesiek, S.; Tuntland, T.; Liu, Y.; Bursulaya, B.; Azam, M.; Manley, P. W.; Engen, J. R.; Daley, G. Q.; Warmuth, M.; Gray, N. S. Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors. Nature, 2010, 463 (7280), 501-6.
-
(2010)
Nature
, vol.463
, Issue.7280
, pp. 501-506
-
-
Zhang, J.1
Adrian, F.J.2
Jahnke, W.3
Cowan-Jacob, S.W.4
Li, A.G.5
Iacob, R.E.6
Sim, T.7
Powers, J.8
Dierks, C.9
Sun, F.10
Guo, G.R.11
Ding, Q.12
Okram, B.13
Choi, Y.14
Wojciechowski, A.15
Deng, X.16
Liu, G.17
Fendrich, G.18
Strauss, A.19
Vajpai, N.20
Grzesiek, S.21
Tuntland, T.22
Liu, Y.23
Bursulaya, B.24
Azam, M.25
Manley, P.W.26
Engen, J.R.27
Daley, G.Q.28
Warmuth, M.29
Gray, N.S.30
more..
-
49
-
-
84937761544
-
Studying clonal dynamics in response to cancer therapy using highcomplexity barcoding
-
Bhang, H. E.; Ruddy, D. A.; Krishnamurthy Radhakrishna, V.; Caushi, J. X.; Zhao, R.; Hims, M. M.; Singh, A. P.; Kao, I.; Rakiec, D.; Shaw, P.; Balak, M.; Raza, A.; Ackley, E.; Keen, N.; Schlabach, M. R.; Palmer, M.; Leary, R. J.; Chiang, D. Y.; Sellers, W. R.; Michor, F.; Cooke, V. G.; Korn, J. M.; Stegmeier, F. Studying clonal dynamics in response to cancer therapy using highcomplexity barcoding. Nat. Med., 2015, 21 (5), 440-8.
-
(2015)
Nat. Med.
, vol.21
, Issue.5
, pp. 440-448
-
-
Bhang, H.E.1
Ruddy, D.A.2
Krishnamurthy Radhakrishna, V.3
Caushi, J.X.4
Zhao, R.5
Hims, M.M.6
Singh, A.P.7
Kao, I.8
Rakiec, D.9
Shaw, P.10
Balak, M.11
Raza, A.12
Ackley, E.13
Keen, N.14
Schlabach, M.R.15
Palmer, M.16
Leary, R.J.17
Chiang, D.Y.18
Sellers, W.R.19
Michor, F.20
Cooke, V.G.21
Korn, J.M.22
Stegmeier, F.23
more..
-
50
-
-
84928427103
-
Inhibitors of p21-activated kinases (PAKs)
-
Rudolph, J.; Crawford, J. J.; Hoeflich, K. P.; Wang, W. Inhibitors of p21-activated kinases (PAKs). J. Med. Chem., 2015, 58 (1), 111-29.
-
(2015)
J. Med. Chem.
, vol.58
, Issue.1
, pp. 111-129
-
-
Rudolph, J.1
Crawford, J.J.2
Hoeflich, K.P.3
Wang, W.4
-
51
-
-
48349123894
-
UnPAKing the class differences among p21-activated kinases
-
Eswaran, J.; Soundararajan, M.; Kumar, R.; Knapp, S. UnPAKing the class differences among p21-activated kinases. Trends in Biochem. Sci., 2008, 33 (8), 394-403.
-
(2008)
Trends in Biochem. Sci.
, vol.33
, Issue.8
, pp. 394-403
-
-
Eswaran, J.1
Soundararajan, M.2
Kumar, R.3
Knapp, S.4
-
52
-
-
84907445756
-
Molecular pathways: Targeting RAC-p21-activated serine-threonine kinase signaling in RAS-driven cancers
-
Baker, N. M.; Yee Chow, H.; Chernoff, J.; Der, C. J. Molecular pathways: targeting RAC-p21-activated serine-threonine kinase signaling in RAS-driven cancers. Clin. Cancer Res., 2014, 20 (18), 4740-6.
-
(2014)
Clin. Cancer Res.
, vol.20
, Issue.18
, pp. 4740-4746
-
-
Baker, N.M.1
Yee Chow, H.2
Chernoff, J.3
Der, C.J.4
-
53
-
-
84890946972
-
PAK signalling during the development and progression of cancer
-
Radu, M.; Semenova, G.; Kosoff, R.; Chernoff, J. PAK signalling during the development and progression of cancer. Nat. Rev. Cancer, 2014, 14 (1), 13-25.
-
(2014)
Nat. Rev. Cancer
, vol.14
, Issue.1
, pp. 13-25
-
-
Radu, M.1
Semenova, G.2
Kosoff, R.3
Chernoff, J.4
-
54
-
-
77952720804
-
Smallmolecule p21-activated kinase inhibitor PF-3758309 is a potent inhibitor of oncogenic signaling and tumor growth
-
Murray, B. W.; Guo, C.; Piraino, J.; Westwick, J. K.; Zhang, C.; Lamerdin, J.; Dagostino, E.; Knighton, D.; Loi, C. M.; Zager, M.; Kraynov, E.; Popoff, I.; Christensen, J. G.; Martinez, R.; Kephart, S. E.; Marakovits, J.; Karlicek, S.; Bergqvist, S.; Smeal, T. Smallmolecule p21-activated kinase inhibitor PF-3758309 is a potent inhibitor of oncogenic signaling and tumor growth. Proc. Natl. Acad. Sci. U.S.A., 2010, 107 (20), 9446-51.
-
(2010)
Proc. Natl. Acad. Sci. U.S.A.
, vol.107
, Issue.20
, pp. 9446-9451
-
-
Murray, B.W.1
Guo, C.2
Piraino, J.3
Westwick, J.K.4
Zhang, C.5
Lamerdin, J.6
Dagostino, E.7
Knighton, D.8
Loi, C.M.9
Zager, M.10
Kraynov, E.11
Popoff, I.12
Christensen, J.G.13
Martinez, R.14
Kephart, S.E.15
Marakovits, J.16
Karlicek, S.17
Bergqvist, S.18
Smeal, T.19
-
55
-
-
84885117132
-
FRAX597, a small molecule inhibitor of the p21-activated kinases, inhibits tumorigenesis of neurofibromatosis type 2 (NF2)-associated Schwannomas
-
Licciulli, S.; Maksimoska, J.; Zhou, C.; Troutman, S.; Kota, S.; Liu, Q.; Duron, S.; Campbell, D.; Chernoff, J.; Field, J.; Marmorstein, R.; Kissil, J. L. FRAX597, a small molecule inhibitor of the p21-activated kinases, inhibits tumorigenesis of neurofibromatosis type 2 (NF2)-associated Schwannomas. J. Biol. Chem., 2013, 288 (40), 29105-14.
-
(2013)
J. Biol. Chem.
, vol.288
, Issue.40
, pp. 29105-29114
-
-
Licciulli, S.1
Maksimoska, J.2
Zhou, C.3
Troutman, S.4
Kota, S.5
Liu, Q.6
Duron, S.7
Campbell, D.8
Chernoff, J.9
Field, J.10
Marmorstein, R.11
Kissil, J.L.12
-
56
-
-
84894073762
-
Back pocket flexibility provides group II p21-activated kinase (PAK) selectivity for type I 1/2 kinase inhibitors
-
Staben, S. T.; Feng, J. A.; Lyle, K.; Belvin, M.; Boggs, J.; Burch, J. D.; Chua, C. C.; Cui, H.; DiPasquale, A. G.; Friedman, L. S.; Heise, C.; Koeppen, H.; Kotey, A.; Mintzer, R.; Oh, A.; Roberts, D. A.; Rouge, L.; Rudolph, J.; Tam, C.; Wang, W.; Xiao, Y.; Young, A.; Zhang, Y.; Hoeflich, K. P. Back pocket flexibility provides group II p21-activated kinase (PAK) selectivity for type I 1/2 kinase inhibitors. J. Med. Chem., 2014, 57 (3), 1033-45.
-
(2014)
J. Med. Chem.
, vol.57
, Issue.3
, pp. 1033-1045
-
-
Staben, S.T.1
Feng, J.A.2
Lyle, K.3
Belvin, M.4
Boggs, J.5
Burch, J.D.6
Chua, C.C.7
Cui, H.8
Dipasquale, A.G.9
Friedman, L.S.10
Heise, C.11
Koeppen, H.12
Kotey, A.13
Mintzer, R.14
Oh, A.15
Roberts, D.A.16
Rouge, L.17
Rudolph, J.18
Tam, C.19
Wang, W.20
Xiao, Y.21
Young, A.22
Zhang, Y.23
Hoeflich, K.P.24
more..
-
57
-
-
41949100602
-
An isoform-selective, smallmolecule inhibitor targets the autoregulatory mechanism of p21-activated kinase
-
Deacon, S. W.; Beeser, A.; Fukui, J. A.; Rennefahrt, U. E.; Myers, C.; Chernoff, J.; Peterson, J. R. An isoform-selective, smallmolecule inhibitor targets the autoregulatory mechanism of p21-activated kinase. Chem. Biol., 2008, 15 (4), 322-31.
-
(2008)
Chem. Biol.
, vol.15
, Issue.4
, pp. 322-331
-
-
Deacon, S.W.1
Beeser, A.2
Fukui, J.A.3
Rennefahrt, U.E.4
Myers, C.5
Chernoff, J.6
Peterson, J.R.7
-
58
-
-
0344395603
-
Bypassing a kinase activity with an ATP-competitive drug
-
Papa, F. R.; Zhang, C.; Shokat, K.; Walter, P. Bypassing a kinase activity with an ATP-competitive drug. Science, 2003, 302 (5650), 1533-7.
-
(2003)
Science
, vol.302
, Issue.5650
, pp. 1533-1537
-
-
Papa, F.R.1
Zhang, C.2
Shokat, K.3
Walter, P.4
-
59
-
-
84928387908
-
Tyrosine Kinase 2-mediated Signal Transduction in T Lymphocytes Is Blocked by Pharmacological Stabilization of Its Pseudokinase Domain
-
Tokarski, J. S.; Zupa-Fernandez, A.; Tredup, J. A.; Pike, K.; Chang, C.; Xie, D.; Cheng, L.; Pedicord, D.; Muckelbauer, J.; Johnson, S. R.; Wu, S.; Edavettal, S. C.; Hong, Y.; Witmer, M. R.; Elkin, L. L.; Blat, Y.; Pitts, W. J.; Weinstein, D. S.; Burke, J. R. Tyrosine Kinase 2-mediated Signal Transduction in T Lymphocytes Is Blocked by Pharmacological Stabilization of Its Pseudokinase Domain. J. Biol. Chem., 2015, 290 (17), 11061-74.
-
(2015)
J. Biol. Chem.
, vol.290
, Issue.17
, pp. 11061-11074
-
-
Tokarski, J.S.1
Zupa-Fernandez, A.2
Tredup, J.A.3
Pike, K.4
Chang, C.5
Xie, D.6
Cheng, L.7
Pedicord, D.8
Muckelbauer, J.9
Johnson, S.R.10
Wu, S.11
Edavettal, S.C.12
Hong, Y.13
Witmer, M.R.14
Elkin, L.L.15
Blat, Y.16
Pitts, W.J.17
Weinstein, D.S.18
Burke, J.R.19
-
60
-
-
84928136142
-
ATP binding to the pseudokinase domain of JAK2 is critical for pathogenic activation
-
Hammaren, H. M.; Ungureanu, D.; Grisouard, J.; Skoda, R. C.; Hubbard, S. R.; Silvennoinen, O. ATP binding to the pseudokinase domain of JAK2 is critical for pathogenic activation. Proc. Natl. Acad. Sci. U.S.A., 2015, 112 (15), 4642-7.
-
(2015)
Proc. Natl. Acad. Sci. U.S.A.
, vol.112
, Issue.15
, pp. 4642-4647
-
-
Hammaren, H.M.1
Ungureanu, D.2
Grisouard, J.3
Skoda, R.C.4
Hubbard, S.R.5
Silvennoinen, O.6
-
61
-
-
77956513286
-
Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma
-
Bollag, G.; Hirth, P.; Tsai, J.; Zhang, J.; Ibrahim, P. N.; Cho, H.; Spevak, W.; Zhang, C.; Zhang, Y.; Habets, G.; Burton, E. A.; Wong, B.; Tsang, G.; West, B. L.; Powell, B.; Shellooe, R.; Marimuthu, A.; Nguyen, H.; Zhang, K. Y.; Artis, D. R.; Schlessinger, J.; Su, F.; Higgins, B.; Iyer, R.; D'Andrea, K.; Koehler, A.; Stumm, M.; Lin, P. S.; Lee, R. J.; Grippo, J.; Puzanov, I.; Kim, K. B.; Ribas, A.; McArthur, G. A.; Sosman, J. A.; Chapman, P. B.; Flaherty, K. T.; Xu, X.; Nathanson, K. L.; Nolop, K. Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma. Nature, 2010, 467 (7315), 596-9.
-
(2010)
Nature
, vol.467
, Issue.7315
, pp. 596-599
-
-
Bollag, G.1
Hirth, P.2
Tsai, J.3
Zhang, J.4
Ibrahim, P.N.5
Cho, H.6
Spevak, W.7
Zhang, C.8
Zhang, Y.9
Habets, G.10
Burton, E.A.11
Wong, B.12
Tsang, G.13
West, B.L.14
Powell, B.15
Shellooe, R.16
Marimuthu, A.17
Nguyen, H.18
Zhang, K.Y.19
Artis, D.R.20
Schlessinger, J.21
Su, F.22
Higgins, B.23
Iyer, R.24
D'andrea, K.25
Koehler, A.26
Stumm, M.27
Lin, P.S.28
Lee, R.J.29
Grippo, J.30
Puzanov, I.31
Kim, K.B.32
Ribas, A.33
McArthur, G.A.34
Sosman, J.A.35
Chapman, P.B.36
Flaherty, K.T.37
Xu, X.38
Nathanson, K.L.39
Nolop, K.40
more..
-
62
-
-
84942323259
-
Inhibition of RAF Isoforms and Active Dimers by LY3009120 Leads to Anti-tumor Activities in RAS or BRAF Mutant Cancers
-
Peng, S. B.; Henry, J. R.; Kaufman, M. D.; Lu, W. P.; Smith, B. D.; Vogeti, S.; Rutkoski, T. J.; Wise, S.; Chun, L.; Zhang, Y.; Van Horn, R. D.; Yin, T.; Zhang, X.; Yadav, V.; Chen, S. H.; Gong, X.; Ma, X.; Webster, Y.; Buchanan, S.; Mochalkin, I.; Huber, L.; Kays, L.; Donoho, G. P.; Walgren, J.; McCann, D.; Patel, P.; Conti, I.; Plowman, G. D.; Starling, J. J.; Flynn, D. L. Inhibition of RAF Isoforms and Active Dimers by LY3009120 Leads to Anti-tumor Activities in RAS or BRAF Mutant Cancers. Cancer cell, 2015, 28 (3), 384-98.
-
(2015)
Cancer Cell
, vol.28
, Issue.3
, pp. 384-398
-
-
Peng, S.B.1
Henry, J.R.2
Kaufman, M.D.3
Lu, W.P.4
Smith, B.D.5
Vogeti, S.6
Rutkoski, T.J.7
Wise, S.8
Chun, L.9
Zhang, Y.10
Van Horn, R.D.11
Yin, T.12
Zhang, X.13
Yadav, V.14
Chen, S.H.15
Gong, X.16
Ma, X.17
Webster, Y.18
Buchanan, S.19
Mochalkin, I.20
Huber, L.21
Kays, L.22
Donoho, G.P.23
Walgren, J.24
McCann, D.25
Patel, P.26
Conti, I.27
Plowman, G.D.28
Starling, J.J.29
Flynn, D.L.30
more..
-
63
-
-
84942319957
-
BRAF Mutants Evade ERK-Dependent Feedback by Different Mechanisms that Determine Their Sensitivity to Pharmacologic Inhibition
-
Yao, Z.; Torres, N. M.; Tao, A.; Gao, Y.; Luo, L.; Li, Q.; de Stanchina, E.; Abdel-Wahab, O.; Solit, D. B.; Poulikakos, P. I.; Rosen, N. BRAF Mutants Evade ERK-Dependent Feedback by Different Mechanisms that Determine Their Sensitivity to Pharmacologic Inhibition. Cancer cell, 2015, 28 (3), 370-83.
-
(2015)
Cancer Cell
, vol.28
, Issue.3
, pp. 370-383
-
-
Yao, Z.1
Torres, N.M.2
Tao, A.3
Gao, Y.4
Luo, L.5
Li, Q.6
De Stanchina, E.7
Abdel-Wahab, O.8
Solit, D.B.9
Poulikakos, P.I.10
Rosen, N.11
-
64
-
-
84908664886
-
Structure of the BRAF-MEK complex reveals a kinase activity independent role for BRAF in MAPK signaling
-
Haling, J. R.; Sudhamsu, J.; Yen, I.; Sideris, S.; Sandoval, W.; Phung, W.; Bravo, B. J.; Giannetti, A. M.; Peck, A.; Masselot, A.; Morales, T.; Smith, D.; Brandhuber, B. J.; Hymowitz, S. G.; Malek, S. Structure of the BRAF-MEK complex reveals a kinase activity independent role for BRAF in MAPK signaling. Cancer cell, 2014, 26 (3), 402-13.
-
(2014)
Cancer Cell
, vol.26
, Issue.3
, pp. 402-413
-
-
Haling, J.R.1
Sudhamsu, J.2
Yen, I.3
Sideris, S.4
Sandoval, W.5
Phung, W.6
Bravo, B.J.7
Giannetti, A.M.8
Peck, A.9
Masselot, A.10
Morales, T.11
Smith, D.12
Brandhuber, B.J.13
Hymowitz, S.G.14
Malek, S.15
-
65
-
-
83455254767
-
RAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF(V600E)
-
Poulikakos, P. I.; Persaud, Y.; Janakiraman, M.; Kong, X.; Ng, C.; Moriceau, G.; Shi, H.; Atefi, M.; Titz, B.; Gabay, M. T.; Salton, M.; Dahlman, K. B.; Tadi, M.; Wargo, J. A.; Flaherty, K. T.; Kelley, M. C.; Misteli, T.; Chapman, P. B.; Sosman, J. A.; Graeber, T. G.; Ribas, A.; Lo, R. S.; Rosen, N.; Solit, D. B. RAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF(V600E). Nature, 2011, 480 (7377), 387-90.
-
(2011)
Nature
, vol.480
, Issue.7377
, pp. 387-390
-
-
Poulikakos, P.I.1
Persaud, Y.2
Janakiraman, M.3
Kong, X.4
Ng, C.5
Moriceau, G.6
Shi, H.7
Atefi, M.8
Titz, B.9
Gabay, M.T.10
Salton, M.11
Dahlman, K.B.12
Tadi, M.13
Wargo, J.A.14
Flaherty, K.T.15
Kelley, M.C.16
Misteli, T.17
Chapman, P.B.18
Sosman, J.A.19
Graeber, T.G.20
Ribas, A.21
Lo, R.S.22
Rosen, N.23
Solit, D.B.24
more..
-
66
-
-
84925283093
-
Crystal structure of a BRAF kinase domain monomer explains basis for allosteric regulation
-
Thevakumaran, N.; Lavoie, H.; Critton, D. A.; Tebben, A.; Marinier, A.; Sicheri, F.; Therrien, M. Crystal structure of a BRAF kinase domain monomer explains basis for allosteric regulation. Nat. Struct. Mol. Biol., 2015, 22 (1), 37-43.
-
(2015)
Nat. Struct. Mol. Biol.
, vol.22
, Issue.1
, pp. 37-43
-
-
Thevakumaran, N.1
Lavoie, H.2
Critton, D.A.3
Tebben, A.4
Marinier, A.5
Sicheri, F.6
Therrien, M.7
-
67
-
-
79957497448
-
Discovery of a potential allosteric ligand binding site in CDK2. ACS
-
Betzi, S.; Alam, R.; Martin, M.; Lubbers, D. J.; Han, H.; Jakkaraj, S. R.; Georg, G. I.; Schonbrunn, E. Discovery of a potential allosteric ligand binding site in CDK2. ACS Chem. Biol., 2011, 6 (5), 492-501.
-
(2011)
Chem. Biol.
, vol.6
, Issue.5
, pp. 492-501
-
-
Betzi, S.1
Alam, R.2
Martin, M.3
Lubbers, D.J.4
Han, H.5
Jakkaraj, S.R.6
Georg, G.I.7
Schonbrunn, E.8
-
68
-
-
77954385114
-
Structural and thermodynamic characterization of the TYK2 and JAK3 kinase domains in complex with CP-690550 and CMP-6
-
Chrencik, J. E.; Patny, A.; Leung, I. K.; Korniski, B.; Emmons, T. L.; Hall, T.; Weinberg, R. A.; Gormley, J. A.; Williams, J. M.; Day, J. E.; Hirsch, J. L.; Kiefer, J. R.; Leone, J. W.; Fischer, H. D.; Sommers, C. D.; Huang, H. C.; Jacobsen, E. J.; Tenbrink, R. E.; Tomasselli, A. G.; Benson, T. E. Structural and thermodynamic characterization of the TYK2 and JAK3 kinase domains in complex with CP-690550 and CMP-6. J. Mol. Biol., 2010, 400 (3), 413-33.
-
(2010)
J. Mol. Biol.
, vol.400
, Issue.3
, pp. 413-433
-
-
Chrencik, J.E.1
Patny, A.2
Leung, I.K.3
Korniski, B.4
Emmons, T.L.5
Hall, T.6
Weinberg, R.A.7
Gormley, J.A.8
Williams, J.M.9
Day, J.E.10
Hirsch, J.L.11
Kiefer, J.R.12
Leone, J.W.13
Fischer, H.D.14
Sommers, C.D.15
Huang, H.C.16
Jacobsen, E.J.17
Tenbrink, R.E.18
Tomasselli, A.G.19
Benson, T.E.20
more..
-
69
-
-
84920747143
-
Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation
-
Goodwin, N. C.; Cianchetta, G.; Burgoon, H. A.; Healy, J.; Mabon, R.; Strobel, E. D.; Allen, J.; Wang, S.; Hamman, B. D.; Rawlins, D. B. Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation. ACS Med. Chem. Lett., 2015, 6 (1), 53-7.
-
(2015)
ACS Med. Chem. Lett.
, vol.6
, Issue.1
, pp. 53-57
-
-
Goodwin, N.C.1
Cianchetta, G.2
Burgoon, H.A.3
Healy, J.4
Mabon, R.5
Strobel, E.D.6
Allen, J.7
Wang, S.8
Hamman, B.D.9
Rawlins, D.B.10
-
70
-
-
65249090229
-
Crystal structures of MEK1 binary and ternary complexes with nucleotides and inhibitors
-
Fischmann, T. O.; Smith, C. K.; Mayhood, T. W.; Myers, J. E.; Reichert, P.; Mannarino, A.; Carr, D.; Zhu, H.; Wong, J.; Yang, R. S.; Le, H. V.; Madison, V. S. Crystal structures of MEK1 binary and ternary complexes with nucleotides and inhibitors. Biochemistry, 2009, 48 (12), 2661-74.
-
(2009)
Biochemistry
, vol.48
, Issue.12
, pp. 2661-2674
-
-
Fischmann, T.O.1
Smith, C.K.2
Mayhood, T.W.3
Myers, J.E.4
Reichert, P.5
Mannarino, A.6
Carr, D.7
Zhu, H.8
Wong, J.9
Yang, R.S.10
Le, H.V.11
Madison, V.S.12
-
71
-
-
84871599677
-
Natural-product-derived fragments for fragmentbased ligand discovery
-
Over, B.; Wetzel, S.; Grutter, C.; Nakai, Y.; Renner, S.; Rauh, D.; Waldmann, H. Natural-product-derived fragments for fragmentbased ligand discovery. Nat. Chem., 2013, 5 (1), 21-8.
-
(2013)
Nat. Chem.
, vol.5
, Issue.1
, pp. 21-28
-
-
Over, B.1
Wetzel, S.2
Grutter, C.3
Nakai, Y.4
Renner, S.5
Rauh, D.6
Waldmann, H.7
|