-
1
-
-
0037032835
-
The protein kinase complement of the human genome
-
Manning, G., Whyte, D. B., Martinez, R., Hunter, T., and Sudarsanam, S. (2002) The protein kinase complement of the human genome Science 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
-
-
0035413606
-
Kinetic and catalytic mechanisms of protein kinases
-
Adams, J. A. (2001) Kinetic and catalytic mechanisms of protein kinases Chem. Rev. 101, 2271-2290
-
(2001)
Chem. Rev.
, vol.101
, pp. 2271-2290
-
-
Adams, J.A.1
-
3
-
-
1642323740
-
Protein kinase inhibitors: Insights into drug design from structure
-
Noble, M. E., Endicott, J. A., and Johnson, L. N. (2004) Protein kinase inhibitors: insights into drug design from structure Science 303, 1800-1805
-
(2004)
Science
, vol.303
, pp. 1800-1805
-
-
Noble, M.E.1
Endicott, J.A.2
Johnson, L.N.3
-
4
-
-
84861859600
-
The structural basis for control of eukaryotic protein kinases
-
Endicott, J. A., Noble, M. E., and Johnson, L. N. (2012) The structural basis for control of eukaryotic protein kinases Annu. Rev. Biochem. 81, 587-613
-
(2012)
Annu. Rev. Biochem.
, vol.81
, pp. 587-613
-
-
Endicott, J.A.1
Noble, M.E.2
Johnson, L.N.3
-
5
-
-
84896920166
-
Novel approaches for targeting kinases: Allosteric inhibition, allosteric activation and pseudokinases
-
Cowan-Jacob, S. W., Jahnke, W., and Knapp, S. (2014) Novel approaches for targeting kinases: allosteric inhibition, allosteric activation and pseudokinases Future Med. Chem. 6, 541-561
-
(2014)
Future Med. Chem.
, vol.6
, pp. 541-561
-
-
Cowan-Jacob, S.W.1
Jahnke, W.2
Knapp, S.3
-
6
-
-
84905815719
-
Recently targeted kinases and their inhibitors-the path to clinical trials
-
Knapp, S. and Sundstrom, M. (2014) Recently targeted kinases and their inhibitors-the path to clinical trials Curr. Opin Pharmacol. 17, 58-63
-
(2014)
Curr. Opin Pharmacol.
, vol.17
, pp. 58-63
-
-
Knapp, S.1
Sundstrom, M.2
-
8
-
-
0034665713
-
Structural mechanism for STI-571 inhibition of abelson tyrosine kinase
-
Schindler, T., Bornmann, W., Pellicena, P., Miller, W. T., Clarkson, B., and Kuriyan, J. (2000) Structural mechanism for STI-571 inhibition of abelson tyrosine kinase Science 289, 1938-1942
-
(2000)
Science
, vol.289
, pp. 1938-1942
-
-
Schindler, T.1
Bornmann, W.2
Pellicena, P.3
Miller, W.T.4
Clarkson, B.5
Kuriyan, J.6
-
9
-
-
0036635291
-
Glivec (STI571, imatinib), a rationally developed, targeted anticancer drug
-
Capdeville, R., Buchdunger, E., Zimmermann, J., and Matter, A. (2002) Glivec (STI571, imatinib), a rationally developed, targeted anticancer drug Nat. Rev. Drug Discovery 1, 493-502
-
(2002)
Nat. Rev. Drug Discovery
, vol.1
, pp. 493-502
-
-
Capdeville, R.1
Buchdunger, E.2
Zimmermann, J.3
Matter, A.4
-
10
-
-
57749188299
-
Targeting cancer with small molecule kinase inhibitors
-
Zhang, J., Yang, P. L., and Gray, N. S. (2009) Targeting cancer with small molecule kinase inhibitors Nat. Rev. Cancer 9, 28-39
-
(2009)
Nat. Rev. Cancer
, vol.9
, pp. 28-39
-
-
Zhang, J.1
Yang, P.L.2
Gray, N.S.3
-
11
-
-
80755125565
-
Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity
-
Anastassiadis, T., Deacon, S. W., Devarajan, K., Ma, H., and Peterson, J. R. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity Nat. Biotechnol. 29, 1039-1045
-
(2011)
Nat. Biotechnol.
, vol.29
, pp. 1039-1045
-
-
Anastassiadis, T.1
Deacon, S.W.2
Devarajan, K.3
Ma, H.4
Peterson, J.R.5
-
12
-
-
80755125575
-
Comprehensive analysis of kinase inhibitor selectivity
-
Davis, M. I., Hunt, J. P., Herrgard, S., Ciceri, P., Wodicka, L. M., Pallares, G., Hocker, M., Treiber, D. K., and Zarrinkar, P. P. (2011) Comprehensive analysis of kinase inhibitor selectivity Nat. Biotechnol. 29, 1046-1051
-
(2011)
Nat. Biotechnol.
, vol.29
, pp. 1046-1051
-
-
Davis, M.I.1
Hunt, J.P.2
Herrgard, S.3
Ciceri, P.4
Wodicka, L.M.5
Pallares, G.6
Hocker, M.7
Treiber, D.K.8
Zarrinkar, P.P.9
-
13
-
-
33745298429
-
Rational design of inhibitors that bind to inactive kinase conformations
-
Liu, Y. and Gray, N. S. (2006) Rational design of inhibitors that bind to inactive kinase conformations Nat. Chem. Biol. 2, 358-364
-
(2006)
Nat. Chem. Biol.
, vol.2
, pp. 358-364
-
-
Liu, Y.1
Gray, N.S.2
-
14
-
-
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., and Gray, N. S. (2014) Exploration of type II binding mode: A privileged approach for kinase inhibitor focused drug discovery? ACS Chem. Biol. 9, 1230-1241
-
(2014)
ACS Chem. Biol.
, vol.9
, 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
-
15
-
-
77958160823
-
Dynamics connect substrate recognition to catalysis in protein kinase A
-
Masterson, L. R., Cheng, C., Yu, T., Tonelli, M., Kornev, A., Taylor, S. S., and Veglia, G. (2010) Dynamics connect substrate recognition to catalysis in protein kinase A Nat. Chem. Biol. 6, 821-828
-
(2010)
Nat. Chem. Biol.
, vol.6
, pp. 821-828
-
-
Masterson, L.R.1
Cheng, C.2
Yu, T.3
Tonelli, M.4
Kornev, A.5
Taylor, S.S.6
Veglia, G.7
-
16
-
-
0037013143
-
The conformational plasticity of protein kinases
-
Huse, M. and Kuriyan, J. (2002) The conformational plasticity of protein kinases Cell 109, 275-282
-
(2002)
Cell
, vol.109
, pp. 275-282
-
-
Huse, M.1
Kuriyan, J.2
-
17
-
-
79959476700
-
The evolution of protein kinase inhibitors from antagonists to agonists of cellular signaling
-
Dar, A. C. and Shokat, K. M. (2011) The evolution of protein kinase inhibitors from antagonists to agonists of cellular signaling Annu. Rev. Biochem. 80, 769-795
-
(2011)
Annu. Rev. Biochem.
, vol.80
, pp. 769-795
-
-
Dar, A.C.1
Shokat, K.M.2
-
18
-
-
84901330713
-
Modulating noncatalytic function with kinase inhibitors
-
Agius, M. P. and Soellner, M. B. (2014) Modulating noncatalytic function with kinase inhibitors Chem. Biol. 21, 569-571
-
(2014)
Chem. Biol.
, vol.21
, pp. 569-571
-
-
Agius, M.P.1
Soellner, M.B.2
-
19
-
-
19944431003
-
Allosteric Akt (PKB) inhibitors: Discovery and SAR of isozyme selective inhibitors
-
Lindsley, C. W., Zhao, Z., Leister, W. H., Robinson, R. G., Barnett, S. F., Defeo-Jones, D., Jones, R. E., Hartman, G. D., Huff, J. R., Huber, H. E., and Duggan, M. E. (2005) Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors Bioorg. Med. Chem. Lett. 15, 761-764
-
(2005)
Bioorg. Med. Chem. Lett.
, vol.15
, pp. 761-764
-
-
Lindsley, C.W.1
Zhao, Z.2
Leister, W.H.3
Robinson, R.G.4
Barnett, S.F.5
Defeo-Jones, D.6
Jones, R.E.7
Hartman, G.D.8
Huff, J.R.9
Huber, H.E.10
Duggan, M.E.11
-
20
-
-
79951967029
-
Principles of early drug discovery
-
Hughes, J. P., Rees, S., Kalindjian, S. B., and Philpott, K. L. (2011) Principles of early drug discovery Br. J. Pharmacol. 162, 1239-1249
-
(2011)
Br. J. Pharmacol.
, vol.162
, pp. 1239-1249
-
-
Hughes, J.P.1
Rees, S.2
Kalindjian, S.B.3
Philpott, K.L.4
-
21
-
-
37549000580
-
Development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved physical properties and cell activity
-
Zhao, Z., Robinson, R. G., Barnett, S. F., Defeo-Jones, D., Jones, R. E., Hartman, G. D., Huber, H. E., Duggan, M. E., and Lindsley, C. W. (2008) Development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved physical properties and cell activity Bioorg. Med. Chem. Lett. 18, 49-53
-
(2008)
Bioorg. Med. Chem. Lett.
, vol.18
, pp. 49-53
-
-
Zhao, Z.1
Robinson, R.G.2
Barnett, S.F.3
Defeo-Jones, D.4
Jones, R.E.5
Hartman, G.D.6
Huber, H.E.7
Duggan, M.E.8
Lindsley, C.W.9
-
22
-
-
19944433628
-
Identification and characterization of pleckstrin-homology-domain-dependent and isoenzyme-specific Akt inhibitors
-
Barnett, S. F., Defeo-Jones, D., Fu, S., Hancock, P. J., Haskell, K. M., Jones, R. E., Kahana, J. A., Kral, A. M., Leander, K., Lee, L. L., Malinowski, J., McAvoy, E. M., Nahas, D. D., Robinson, R. G., and Huber, H. E. (2005) Identification and characterization of pleckstrin-homology-domain-dependent and isoenzyme-specific Akt inhibitors Biochem. J. 385, 399-408
-
(2005)
Biochem. J.
, vol.385
, pp. 399-408
-
-
Barnett, S.F.1
Defeo-Jones, D.2
Fu, S.3
Hancock, P.J.4
Haskell, K.M.5
Jones, R.E.6
Kahana, J.A.7
Kral, A.M.8
Leander, K.9
Lee, L.L.10
Malinowski, J.11
McAvoy, E.M.12
Nahas, D.D.13
Robinson, R.G.14
Huber, H.E.15
-
23
-
-
78149473070
-
Allostery and population shift in drug discovery
-
Kar, G., Keskin, O., Gursoy, A., and Nussinov, R. (2010) Allostery and population shift in drug discovery Curr. Opin Pharmacol. 10, 715-722
-
(2010)
Curr. Opin Pharmacol.
, vol.10
, pp. 715-722
-
-
Kar, G.1
Keskin, O.2
Gursoy, A.3
Nussinov, R.4
-
24
-
-
84862726767
-
ERK inhibition overcomes acquired resistance to MEK inhibitors
-
Hatzivassiliou, G., Liu, B., OBrien, C., Spoerke, J. M., Hoeflich, K. P., Haverty, P. M., Soriano, R., Forrest, W. F., Heldens, S., Chen, H., Toy, K., Ha, C., Zhou, W., Song, K., Friedman, L. S., Amler, L. C., Hampton, G. M., Moffat, J., Belvin, M., and Lackner, M. R. (2012) ERK inhibition overcomes acquired resistance to MEK inhibitors Mol. Cancer Ther. 11, 1143-1154
-
(2012)
Mol. Cancer Ther.
, vol.11
, pp. 1143-1154
-
-
Hatzivassiliou, G.1
Liu, B.2
Obrien, C.3
Spoerke, J.M.4
Hoeflich, K.P.5
Haverty, P.M.6
Soriano, R.7
Forrest, W.F.8
Heldens, S.9
Chen, H.10
Toy, K.11
Ha, C.12
Zhou, W.13
Song, K.14
Friedman, L.S.15
Amler, L.C.16
Hampton, G.M.17
Moffat, J.18
Belvin, M.19
Lackner, M.R.20
more..
-
25
-
-
84919832780
-
Activation pathway of Src kinase reveals intermediate states as targets for drug design
-
Shukla, D., Meng, Y., Roux, B., and Pande, V. S. (2014) Activation pathway of Src kinase reveals intermediate states as targets for drug design Nat. Commun. 5, 3397
-
(2014)
Nat. Commun.
, vol.5
, pp. 3397
-
-
Shukla, D.1
Meng, Y.2
Roux, B.3
Pande, V.S.4
-
26
-
-
84903899364
-
Molecular basis for pseudokinase-dependent autoinhibition of JAK2 tyrosine kinase
-
Shan, Y., Gnanasambandan, K., Ungureanu, D., Kim, E. T., Hammaren, H., Yamashita, K., Silvennoinen, O., Shaw, D. E., and Hubbard, S. R. (2014) Molecular basis for pseudokinase-dependent autoinhibition of JAK2 tyrosine kinase Nat. Struct Mol. Biol. 21, 579-584
-
(2014)
Nat. Struct Mol. Biol.
, vol.21
, pp. 579-584
-
-
Shan, Y.1
Gnanasambandan, K.2
Ungureanu, D.3
Kim, E.T.4
Hammaren, H.5
Yamashita, K.6
Silvennoinen, O.7
Shaw, D.E.8
Hubbard, S.R.9
-
27
-
-
79959275847
-
How does a drug molecule find its target binding site?
-
Shan, Y., Kim, E. T., Eastwood, M. P., Dror, R. O., Seeliger, M. A., and Shaw, D. E. (2011) How does a drug molecule find its target binding site? J. Am. Chem. Soc. 133, 9181-9183
-
(2011)
J. Am. Chem. Soc.
, vol.133
, pp. 9181-9183
-
-
Shan, Y.1
Kim, E.T.2
Eastwood, M.P.3
Dror, R.O.4
Seeliger, M.A.5
Shaw, D.E.6
-
28
-
-
33748325882
-
Drug-target residence time and its implications for lead optimization
-
Copeland, R. A., Pompliano, D. L., and Meek, T. D. (2006) Drug-target residence time and its implications for lead optimization Nat. Rev. Drug Discovery 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
-
29
-
-
64049102289
-
Binding of small-molecule ligands to proteins: "what you see" is not always "what you get"
-
Mobley, D. L. and Dill, K. A. (2009) Binding of small-molecule ligands to proteins: "what you see" is not always "what you get" Structure 17, 489-498
-
(2009)
Structure
, vol.17
, pp. 489-498
-
-
Mobley, D.L.1
Dill, K.A.2
-
31
-
-
77950482089
-
Global consequences of activation loop phosphorylation on protein kinase A
-
Steichen, J. M., Iyer, G. H., Li, S., Saldanha, S. A., Deal, M. S., Woods, V. L., Jr., and Taylor, S. S. (2010) Global consequences of activation loop phosphorylation on protein kinase A J. Biol. Chem. 285, 3825-3832
-
(2010)
J. Biol. Chem.
, vol.285
, pp. 3825-3832
-
-
Steichen, J.M.1
Iyer, G.H.2
Li, S.3
Saldanha, S.A.4
Deal, M.S.5
Woods, V.L.6
Taylor, S.S.7
-
32
-
-
84860369376
-
Structural basis for the regulation of protein kinase A by activation loop phosphorylation
-
Steichen, J. M., Kuchinskas, M., Keshwani, M. M., Yang, J., Adams, J. A., and Taylor, S. S. (2012) Structural basis for the regulation of protein kinase A by activation loop phosphorylation J. Biol. Chem. 287, 14672-14680
-
(2012)
J. Biol. Chem.
, vol.287
, pp. 14672-14680
-
-
Steichen, J.M.1
Kuchinskas, M.2
Keshwani, M.M.3
Yang, J.4
Adams, J.A.5
Taylor, S.S.6
-
33
-
-
84872511666
-
Strategies for the selective regulation of kinases with allosteric modulators: Exploiting exclusive structural features
-
Fang, Z., Grutter, C., and Rauh, D. (2013) Strategies for the selective regulation of kinases with allosteric modulators: exploiting exclusive structural features ACS Chem. Biol. 8, 58-70
-
(2013)
ACS Chem. Biol.
, vol.8
, pp. 58-70
-
-
Fang, Z.1
Grutter, C.2
Rauh, D.3
-
34
-
-
33845197964
-
Surface comparison of active and inactive protein kinases identifies a conserved activation mechanism
-
Kornev, A. P., Haste, N. M., Taylor, S. S., and Eyck, L. F. (2006) Surface comparison of active and inactive protein kinases identifies a conserved activation mechanism Proc. Natl. Acad. Sci. U. S. A. 103, 17783-17788
-
(2006)
Proc. Natl. Acad. Sci. U. S. A.
, vol.103
, pp. 17783-17788
-
-
Kornev, A.P.1
Haste, N.M.2
Taylor, S.S.3
Eyck, L.F.4
-
35
-
-
55749102720
-
A helix scaffold for the assembly of active protein kinases
-
Kornev, A. P., Taylor, S. S., and Ten Eyck, L. F. (2008) A helix scaffold for the assembly of active protein kinases Proc. Natl. Acad. Sci. U. S. A. 105, 14377-14382
-
(2008)
Proc. Natl. Acad. Sci. U. S. A.
, vol.105
, pp. 14377-14382
-
-
Kornev, A.P.1
Taylor, S.S.2
Ten Eyck, L.F.3
-
36
-
-
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., and Eck, M. J. (2007) Structures of lung cancer-derived EGFR mutants and inhibitor complexes: mechanism of activation and insights into differential inhibitor sensitivity Cancer Cell 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
-
37
-
-
0141599428
-
Structure of the epidermal growth factor receptor kinase domain alone and in complex with a 4-anilinoquinazoline inhibitor
-
Stamos, J., Sliwkowski, M. X., and Eigenbrot, C. (2002) Structure of the epidermal growth factor receptor kinase domain alone and in complex with a 4-anilinoquinazoline inhibitor J. Biol. Chem. 277, 46265-46272
-
(2002)
J. Biol. Chem.
, vol.277
, pp. 46265-46272
-
-
Stamos, J.1
Sliwkowski, M.X.2
Eigenbrot, C.3
-
38
-
-
84921278792
-
A unique inhibitor binding site in ERK1/2 is associated with slow binding kinetics
-
Chaikuad, A., Tacconi, E. M., Zimmer, J., Liang, Y., Gray, N. S., Tarsounas, M., and Knapp, S. (2014) A unique inhibitor binding site in ERK1/2 is associated with slow binding kinetics Nat. Chem. Biol. 10, 853-860
-
(2014)
Nat. Chem. Biol.
, vol.10
, pp. 853-860
-
-
Chaikuad, A.1
Tacconi, E.M.2
Zimmer, J.3
Liang, Y.4
Gray, N.S.5
Tarsounas, M.6
Knapp, S.7
-
39
-
-
84880254869
-
Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors
-
Morris, E. J., Jha, S., Restaino, C. R., Dayananth, P., Zhu, H., Cooper, A., Carr, D., Deng, Y., Jin, W., Black, S., Long, B., Liu, J., Dinunzio, E., Windsor, W., Zhang, R., Zhao, S., Angagaw, M. H., Pinheiro, E. M., Desai, J., Xiao, L., Shipps, G., Hruza, A., Wang, J., Kelly, J., Paliwal, S., Gao, X., Babu, B. S., Zhu, L., Daublain, P., Zhang, L., Lutterbach, B. A., Pelletier, M. R., Philippar, U., Siliphaivanh, P., Witter, D., Kirschmeier, P., Bishop, W. R., Hicklin, D., Gilliland, D. G., Jayaraman, L., Zawel, L., Fawell, S., and Samatar, A. A. (2013) Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors Cancer Discovery 3, 742-750
-
(2013)
Cancer Discovery
, vol.3
, pp. 742-750
-
-
Morris, E.J.1
Jha, S.2
Restaino, C.R.3
Dayananth, P.4
Zhu, H.5
Cooper, A.6
Carr, D.7
Deng, Y.8
Jin, W.9
Black, S.10
Long, B.11
Liu, J.12
Dinunzio, E.13
Windsor, W.14
Zhang, R.15
Zhao, S.16
Angagaw, M.H.17
Pinheiro, E.M.18
Desai, J.19
Xiao, L.20
Shipps, G.21
Hruza, A.22
Wang, J.23
Kelly, J.24
Paliwal, S.25
Gao, X.26
Babu, B.S.27
Zhu, L.28
Daublain, P.29
Zhang, L.30
Lutterbach, B.A.31
Pelletier, M.R.32
Philippar, U.33
Siliphaivanh, P.34
Witter, D.35
Kirschmeier, P.36
Bishop, W.R.37
Hicklin, D.38
Gilliland, D.G.39
Jayaraman, L.40
Zawel, L.41
Fawell, S.42
Samatar, A.A.43
more..
-
40
-
-
84873406911
-
Insights into the aberrant activity of mutant EGFR kinase domain and drug recognition
-
Gajiwala, K. S., Feng, J., Ferre, R., Ryan, K., Brodsky, O., Weinrich, S., Kath, J. C., and Stewart, A. (2013) Insights into the aberrant activity of mutant EGFR kinase domain and drug recognition Structure 21, 209-219
-
(2013)
Structure
, vol.21
, pp. 209-219
-
-
Gajiwala, K.S.1
Feng, J.2
Ferre, R.3
Ryan, K.4
Brodsky, O.5
Weinrich, S.6
Kath, J.C.7
Stewart, A.8
-
41
-
-
53549104402
-
Activation of tyrosine kinases by mutation of the gatekeeper threonine
-
Azam, M., Seeliger, M. A., Gray, N. S., Kuriyan, J., and Daley, G. Q. (2008) Activation of tyrosine kinases by mutation of the gatekeeper threonine Nat. Struct. Mol. Biol. 15, 1109-1118
-
(2008)
Nat. Struct. Mol. Biol.
, vol.15
, pp. 1109-1118
-
-
Azam, M.1
Seeliger, M.A.2
Gray, N.S.3
Kuriyan, J.4
Daley, G.Q.5
-
42
-
-
0031025991
-
Three-dimensional structure of the tyrosine kinase c-Src
-
Xu, W., Harrison, S. C., and Eck, M. J. (1997) Three-dimensional structure of the tyrosine kinase c-Src Nature 385, 595-602
-
(1997)
Nature
, vol.385
, pp. 595-602
-
-
Xu, W.1
Harrison, S.C.2
Eck, M.J.3
-
43
-
-
33646755174
-
A Src-like inactive conformation in the abl tyrosine kinase domain
-
Levinson, N. M., Kuchment, O., Shen, K., Young, M. A., Koldobskiy, M., Karplus, M., Cole, P. A., and Kuriyan, J. (2006) A Src-like inactive conformation in the abl tyrosine kinase domain PLoS Biol. 4, e144
-
(2006)
PLoS Biol.
, vol.4
, pp. 144
-
-
Levinson, N.M.1
Kuchment, O.2
Shen, K.3
Young, M.A.4
Koldobskiy, M.5
Karplus, M.6
Cole, P.A.7
Kuriyan, J.8
-
44
-
-
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., and Kuriyan, J. (2007) c-Src binds to the cancer drug imatinib with an inactive Abl/c-Kit conformation and a distributed thermodynamic penalty Structure 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
-
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., and Maly, D. J. (2009) Equally potent inhibition of c-Src and Abl by compounds that recognize inactive kinase conformations Cancer Res. 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
-
-
77955792293
-
In vitro selection of a DNA-templated small-molecule library reveals a class of macrocyclic kinase inhibitors
-
Kleiner, R. E., Dumelin, C. E., Tiu, G. C., Sakurai, K., and Liu, D. R. (2010) In vitro selection of a DNA-templated small-molecule library reveals a class of macrocyclic kinase inhibitors J. Am. Chem. Soc. 132, 11779-11791
-
(2010)
J. Am. Chem. Soc.
, vol.132
, pp. 11779-11791
-
-
Kleiner, R.E.1
Dumelin, C.E.2
Tiu, G.C.3
Sakurai, K.4
Liu, D.R.5
-
47
-
-
84862777996
-
Highly specific, bisubstrate-competitive Src inhibitors from DNA-templated macrocycles
-
Georghiou, G., Kleiner, R. E., Pulkoski-Gross, M., Liu, D. R., and Seeliger, M. A. (2012) Highly specific, bisubstrate-competitive Src inhibitors from DNA-templated macrocycles Nat. Chem. Biol. 8, 366-374
-
(2012)
Nat. Chem. Biol.
, vol.8
, pp. 366-374
-
-
Georghiou, G.1
Kleiner, R.E.2
Pulkoski-Gross, M.3
Liu, D.R.4
Seeliger, M.A.5
-
48
-
-
33846228789
-
Contribution of ABL kinase domain mutations to imatinib resistance in different subsets of Philadelphia-positive patients: By the GIMEMA Working Party on Chronic Myeloid Leukemia
-
Soverini, S., Colarossi, S., Gnani, A., Rosti, G., Castagnetti, F., Poerio, A., Iacobucci, I., Amabile, M., Abruzzese, E., Orlandi, E., Radaelli, F., Ciccone, F., Tiribelli, M., di Lorenzo, R., Caracciolo, C., Izzo, B., Pane, F., Saglio, G., Baccarani, M., Martinelli, G., and Leukemia, G. W. P. o. C. M. (2006) Contribution of ABL kinase domain mutations to imatinib resistance in different subsets of Philadelphia-positive patients: by the GIMEMA Working Party on Chronic Myeloid Leukemia Clin. Cancer Res. 12 (-) 7374-7379
-
(2006)
Clin. Cancer Res.
, vol.1
, Issue.2
, pp. 7374-7379
-
-
Soverini, S.1
Colarossi, S.2
Gnani, A.3
Rosti, G.4
Castagnetti, F.5
Poerio, A.6
Iacobucci, I.7
Amabile, M.8
Abruzzese, E.9
Orlandi, E.10
Radaelli, F.11
Ciccone, F.12
Tiribelli, M.13
Di Lorenzo, R.14
Caracciolo, C.15
Izzo, B.16
Pane, F.17
Saglio, G.18
Baccarani, M.19
Martinelli, G.20
Leukemia, O.P.W.G.C.M.21
more..
-
49
-
-
15744380263
-
Structures of human MAP kinase kinase 1 (MEK1) and MEK2 describe novel noncompetitive kinase inhibition
-
Ohren, J. F., Chen, H., Pavlovsky, A., Whitehead, C., Zhang, E., Kuffa, P., Yan, C., McConnell, P., Spessard, C., Banotai, C., Mueller, W. T., Delaney, A., Omer, C., Sebolt-Leopold, J., Dudley, D. T., Leung, I. K., Flamme, C., Warmus, J., Kaufman, M., Barrett, S., Tecle, H., and Hasemann, C. A. (2004) Structures of human MAP kinase kinase 1 (MEK1) and MEK2 describe novel noncompetitive kinase inhibition Nat. Struct. Mol. Biol. 11, 1192-1197
-
(2004)
Nat. Struct. Mol. Biol.
, vol.11
, pp. 1192-1197
-
-
Ohren, J.F.1
Chen, H.2
Pavlovsky, A.3
Whitehead, C.4
Zhang, E.5
Kuffa, P.6
Yan, C.7
McConnell, P.8
Spessard, C.9
Banotai, C.10
Mueller, W.T.11
Delaney, A.12
Omer, C.13
Sebolt-Leopold, J.14
Dudley, D.T.15
Leung, I.K.16
Flamme, C.17
Warmus, J.18
Kaufman, M.19
Barrett, S.20
Tecle, H.21
Hasemann, C.A.22
more..
-
50
-
-
56549093146
-
The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901
-
Barrett, S. D., Bridges, A. J., Dudley, D. T., Saltiel, A. R., Fergus, J. H., Flamme, C. M., Delaney, A. M., Kaufman, M., LePage, S., Leopold, W. R., Przybranowski, S. A., Sebolt-Leopold, J., Van Becelaere, K., Doherty, A. M., Kennedy, R. M., Marston, D., Howard, W. A., Jr., Smith, Y., Warmus, J. S., and Tecle, H. (2008) The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901 Bioorg. Med. Chem. Lett. 18, 6501-6504
-
(2008)
Bioorg. Med. Chem. Lett.
, vol.18
, pp. 6501-6504
-
-
Barrett, S.D.1
Bridges, A.J.2
Dudley, D.T.3
Saltiel, A.R.4
Fergus, J.H.5
Flamme, C.M.6
Delaney, A.M.7
Kaufman, M.8
Lepage, S.9
Leopold, W.R.10
Przybranowski, S.A.11
Sebolt-Leopold, J.12
Van Becelaere, K.13
Doherty, A.M.14
Kennedy, R.M.15
Marston, D.16
Howard, W.A.17
Smith, Y.18
Warmus, J.S.19
Tecle, H.20
more..
-
51
-
-
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., and Shewchuk, L. (2004) 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. 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
-
52
-
-
40049099848
-
Mechanism of activation and inhibition of the HER4/ErbB4 kinase
-
Qiu, C., Tarrant, M. K., Choi, S. H., Sathyamurthy, A., Bose, R., Banjade, S., Pal, A., Bornmann, W. G., Lemmon, M. A., Cole, P. A., and Leahy, D. J. (2008) Mechanism of activation and inhibition of the HER4/ErbB4 kinase Structure 16, 460-467
-
(2008)
Structure
, vol.16
, pp. 460-467
-
-
Qiu, C.1
Tarrant, M.K.2
Choi, S.H.3
Sathyamurthy, A.4
Bose, R.5
Banjade, S.6
Pal, A.7
Bornmann, W.G.8
Lemmon, M.A.9
Cole, P.A.10
Leahy, D.J.11
-
53
-
-
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., and Regan, J. (2002) Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site Nat. Struct. Biol. 9, 268-272
-
(2002)
Nat. 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
-
54
-
-
0042020196
-
The kinetics of binding to p38MAP kinase by analogues of BIRB 796
-
Regan, J., Pargellis, C. A., Cirillo, P. F., Gilmore, T., Hickey, E. R., Peet, G. W., Proto, A., Swinamer, A., and Moss, N. (2003) The kinetics of binding to p38MAP kinase by analogues of BIRB 796 Bioorg. Med. Chem. Lett. 13, 3101-3104
-
(2003)
Bioorg. Med. Chem. Lett.
, vol.13
, pp. 3101-3104
-
-
Regan, J.1
Pargellis, C.A.2
Cirillo, P.F.3
Gilmore, T.4
Hickey, E.R.5
Peet, G.W.6
Proto, A.7
Swinamer, A.8
Moss, N.9
-
55
-
-
77950573400
-
Through the "gatekeeper door": Exploiting the active kinase conformation
-
Zuccotto, F., Ardini, E., Casale, E., and Angiolini, M. (2010) Through the "gatekeeper door": exploiting the active kinase conformation J. Med. Chem. 53, 2681-2694
-
(2010)
J. Med. Chem.
, vol.53
, pp. 2681-2694
-
-
Zuccotto, F.1
Ardini, E.2
Casale, E.3
Angiolini, M.4
-
56
-
-
84879377486
-
Sequence determinants of a specific inactive protein kinase conformation
-
Hari, S. B., Merritt, E. A., and Maly, D. J. (2013) Sequence determinants of a specific inactive protein kinase conformation Chem. Biol. 20, 806-815
-
(2013)
Chem. Biol.
, vol.20
, pp. 806-815
-
-
Hari, S.B.1
Merritt, E.A.2
Maly, D.J.3
-
57
-
-
33749238553
-
Discovery and development of sorafenib: A multikinase inhibitor for treating cancer
-
Wilhelm, S., Carter, C., Lynch, M., Lowinger, T., Dumas, J., Smith, R. A., Schwartz, B., Simantov, R., and Kelley, S. (2006) Discovery and development of sorafenib: a multikinase inhibitor for treating cancer Nat. Rev. Drug Discovery 5, 835-844
-
(2006)
Nat. Rev. Drug Discovery
, vol.5
, pp. 835-844
-
-
Wilhelm, S.1
Carter, C.2
Lynch, M.3
Lowinger, T.4
Dumas, J.5
Smith, R.A.6
Schwartz, B.7
Simantov, R.8
Kelley, S.9
-
58
-
-
77951689893
-
Analysis of imatinib and sorafenib binding to p38alpha compared with c-Abl and b-Raf provides structural insights for understanding the selectivity of inhibitors targeting the DFG-out form of protein kinases
-
Namboodiri, H. V., Bukhtiyarova, M., Ramcharan, J., Karpusas, M., Lee, Y., and Springman, E. B. (2010) Analysis of imatinib and sorafenib binding to p38alpha compared with c-Abl and b-Raf provides structural insights for understanding the selectivity of inhibitors targeting the DFG-out form of protein kinases Biochemistry 49, 3611-3618
-
(2010)
Biochemistry
, vol.49
, pp. 3611-3618
-
-
Namboodiri, H.V.1
Bukhtiyarova, M.2
Ramcharan, J.3
Karpusas, M.4
Lee, Y.5
Springman, E.B.6
-
59
-
-
67649995940
-
Development of a fluorescent-tagged kinase assay system for the detection and characterization of allosteric kinase inhibitors
-
Simard, J. R., Getlik, M., Grutter, C., Pawar, V., Wulfert, S., Rabiller, M., and Rauh, D. (2009) Development of a fluorescent-tagged kinase assay system for the detection and characterization of allosteric kinase inhibitors J. Am. Chem. Soc. 131, 13286-13296
-
(2009)
J. Am. Chem. Soc.
, vol.131
, pp. 13286-13296
-
-
Simard, J.R.1
Getlik, M.2
Grutter, C.3
Pawar, V.4
Wulfert, S.5
Rabiller, M.6
Rauh, D.7
-
60
-
-
73249153398
-
High-throughput screening to identify inhibitors which stabilize inactive kinase conformations in p38alpha
-
Simard, J. R., Grutter, C., Pawar, V., Aust, B., Wolf, A., Rabiller, M., Wulfert, S., Robubi, A., Kluter, S., Ottmann, C., and Rauh, D. (2009) High-throughput screening to identify inhibitors which stabilize inactive kinase conformations in p38alpha J. Am. Chem. Soc. 131, 18478-18488
-
(2009)
J. Am. Chem. Soc.
, vol.131
, pp. 18478-18488
-
-
Simard, J.R.1
Grutter, C.2
Pawar, V.3
Aust, B.4
Wolf, A.5
Rabiller, M.6
Wulfert, S.7
Robubi, A.8
Kluter, S.9
Ottmann, C.10
Rauh, D.11
-
61
-
-
67349094019
-
A new screening assay for allosteric inhibitors of cSrc
-
Simard, J. R., Kluter, S., Grutter, C., Getlik, M., Rabiller, M., Rode, H. B., and Rauh, D. (2009) A new screening assay for allosteric inhibitors of cSrc Nat. Chem. Biol. 5, 394-396
-
(2009)
Nat. Chem. Biol.
, vol.5
, pp. 394-396
-
-
Simard, J.R.1
Kluter, S.2
Grutter, C.3
Getlik, M.4
Rabiller, M.5
Rode, H.B.6
Rauh, D.7
-
62
-
-
84863634917
-
Fluorophore labeled kinase detects ligands that bind within the MAPK insert of p38alpha kinase
-
Getlik, M., Simard, J. R., Termathe, M., Grutter, C., Rabiller, M., van Otterlo, W. A., and Rauh, D. (2012) Fluorophore labeled kinase detects ligands that bind within the MAPK insert of p38alpha kinase PLoS One 7, e39713
-
(2012)
PLoS One
, vol.7
, pp. 39713
-
-
Getlik, M.1
Simard, J.R.2
Termathe, M.3
Grutter, C.4
Rabiller, M.5
Van Otterlo, W.A.6
Rauh, D.7
-
63
-
-
84861854598
-
Direct binding assay for the detection of type IV allosteric inhibitors of Abl
-
Schneider, R., Becker, C., Simard, J. R., Getlik, M., Bohlke, N., Janning, P., and Rauh, D. (2012) Direct binding assay for the detection of type IV allosteric inhibitors of Abl J. Am. Chem. Soc. 134, 9138-9141
-
(2012)
J. Am. Chem. Soc.
, vol.134
, pp. 9138-9141
-
-
Schneider, R.1
Becker, C.2
Simard, J.R.3
Getlik, M.4
Bohlke, N.5
Janning, P.6
Rauh, D.7
-
64
-
-
84921367741
-
Discovery of Inter-Domain Stabilizers-A Novel Assay System for Allosteric Akt Inhibitors
-
Fang, Z., Simard, J. R., Plenker, D., Nguyen, H. D., Phan, T., Wolle, P., Baumeister, S., and Rauh, D. (2014) Discovery of Inter-Domain Stabilizers-A Novel Assay System for Allosteric Akt Inhibitors Acs Chem. Biol. 10.1021/cb500355c
-
(2014)
Acs Chem. Biol.
-
-
Fang, Z.1
Simard, J.R.2
Plenker, D.3
Nguyen, H.D.4
Phan, T.5
Wolle, P.6
Baumeister, S.7
Rauh, D.8
-
65
-
-
84856298523
-
Biosensor-based approach to the identification of protein kinase ligands with dual-site modes of action
-
Navratilova, I., Macdonald, G., Robinson, C., Hughes, S., Mathias, J., Phillips, C., and Cook, A. (2012) Biosensor-based approach to the identification of protein kinase ligands with dual-site modes of action J. Biomol. Screening 17, 183-193
-
(2012)
J. Biomol. Screening
, vol.17
, pp. 183-193
-
-
Navratilova, I.1
Macdonald, G.2
Robinson, C.3
Hughes, S.4
Mathias, J.5
Phillips, C.6
Cook, A.7
-
66
-
-
84893873004
-
Quick evaluation of kinase inhibitors by surface plasmon resonance using single-site specifically biotinylated kinases
-
Kitagawa, D., Gouda, M., and Kirii, Y. (2014) Quick evaluation of kinase inhibitors by surface plasmon resonance using single-site specifically biotinylated kinases J. Biomol. Screening 19, 453-461
-
(2014)
J. Biomol. Screening
, vol.19
, pp. 453-461
-
-
Kitagawa, D.1
Gouda, M.2
Kirii, Y.3
-
67
-
-
33747597796
-
Detection of protein conformational change by optical second-harmonic generation
-
Salafsky, J. S. (2006) Detection of protein conformational change by optical second-harmonic generation J. Chem. Phys. 125, 074701
-
(2006)
J. Chem. Phys.
, vol.125
, pp. 074701
-
-
Salafsky, J.S.1
-
68
-
-
35448970955
-
Second-harmonic generation for studying structural motion of biological molecules in real time and space
-
Salafsky, J. S. (2007) Second-harmonic generation for studying structural motion of biological molecules in real time and space Phys. Chem. Chem. Phys. 9, 5704-5711
-
(2007)
Phys. Chem. Chem. Phys.
, vol.9
, pp. 5704-5711
-
-
Salafsky, J.S.1
-
69
-
-
77952411548
-
Probing myosin structural conformation in vivo by second-harmonic generation microscopy
-
Nucciotti, V., Stringari, C., Sacconi, L., Vanzi, F., Fusi, L., Linari, M., Piazzesi, G., Lombardi, V., and Pavone, F. S. (2010) Probing myosin structural conformation in vivo by second-harmonic generation microscopy Proc. Natl. Acad. Sci. U. S. A. 107, 7763-7768
-
(2010)
Proc. Natl. Acad. Sci. U. S. A.
, vol.107
, pp. 7763-7768
-
-
Nucciotti, V.1
Stringari, C.2
Sacconi, L.3
Vanzi, F.4
Fusi, L.5
Linari, M.6
Piazzesi, G.7
Lombardi, V.8
Pavone, F.S.9
-
70
-
-
84880806523
-
Cracking the molecular origin of intrinsic tyrosine kinase activity through analysis of pathogenic gain-of-function mutations
-
Chen, H., Huang, Z., Dutta, K., Blais, S., Neubert, T. A., Li, X., Cowburn, D., Traaseth, N. J., and Mohammadi, M. (2013) Cracking the molecular origin of intrinsic tyrosine kinase activity through analysis of pathogenic gain-of-function mutations Cell Rep. 4, 376-384
-
(2013)
Cell Rep.
, vol.4
, pp. 376-384
-
-
Chen, H.1
Huang, Z.2
Dutta, K.3
Blais, S.4
Neubert, T.A.5
Li, X.6
Cowburn, D.7
Traaseth, N.J.8
Mohammadi, M.9
-
71
-
-
32044462537
-
NMR characterization of kinase p38 dynamics in free and ligand-bound forms
-
Vogtherr, M., Saxena, K., Hoelder, S., Grimme, S., Betz, M., Schieborr, U., Pescatore, B., Robin, M., Delarbre, L., Langer, T., Wendt, K. U., and Schwalbe, H. (2006) NMR characterization of kinase p38 dynamics in free and ligand-bound forms Angew. Chem., Int. Ed. Engl. 45, 993-997
-
(2006)
Angew. Chem., Int. Ed. Engl.
, vol.45
, pp. 993-997
-
-
Vogtherr, M.1
Saxena, K.2
Hoelder, S.3
Grimme, S.4
Betz, M.5
Schieborr, U.6
Pescatore, B.7
Robin, M.8
Delarbre, L.9
Langer, T.10
Wendt, K.U.11
Schwalbe, H.12
-
72
-
-
84898003608
-
Extracellular-regulated kinase 2 is activated by the enhancement of hinge flexibility
-
Sours, K. M., Xiao, Y., and Ahn, N. G. (2014) Extracellular-regulated kinase 2 is activated by the enhancement of hinge flexibility J. Mol. Biol. 426, 1925-1935
-
(2014)
J. Mol. Biol.
, vol.426
, pp. 1925-1935
-
-
Sours, K.M.1
Xiao, Y.2
Ahn, N.G.3
-
73
-
-
84894379546
-
Phosphorylation releases constraints to domain motion in ERK2
-
Xiao, Y., Lee, T., Latham, M. P., Warner, L. R., Tanimoto, A., Pardi, A., and Ahn, N. G. (2014) Phosphorylation releases constraints to domain motion in ERK2 Proc. Natl. Acad. Sci. U. S. A. 111, 2506-2511
-
(2014)
Proc. Natl. Acad. Sci. U. S. A.
, vol.111
, pp. 2506-2511
-
-
Xiao, Y.1
Lee, T.2
Latham, M.P.3
Warner, L.R.4
Tanimoto, A.5
Pardi, A.6
Ahn, N.G.7
-
74
-
-
49649108911
-
Solution conformations and dynamics of ABL kinase-inhibitor complexes determined by NMR substantiate the different binding modes of imatinib/nilotinib and dasatinib
-
Vajpai, N., Strauss, A., Fendrich, G., Cowan-Jacob, S. W., Manley, P. W., Grzesiek, S., and Jahnke, W. (2008) Solution conformations and dynamics of ABL kinase-inhibitor complexes determined by NMR substantiate the different binding modes of imatinib/nilotinib and dasatinib J. Biol. Chem. 283, 18292-18302
-
(2008)
J. Biol. Chem.
, vol.283
, pp. 18292-18302
-
-
Vajpai, N.1
Strauss, A.2
Fendrich, G.3
Cowan-Jacob, S.W.4
Manley, P.W.5
Grzesiek, S.6
Jahnke, W.7
-
75
-
-
79952283168
-
Structure of the Ire1 autophosphorylation complex and implications for the unfolded protein response
-
Ali, M. M., Bagratuni, T., Davenport, E. L., Nowak, P. R., Silva-Santisteban, M. C., Hardcastle, A., McAndrews, C., Rowlands, M. G., Morgan, G. J., Aherne, W., Collins, I., Davies, F. E., and Pearl, L. H. (2011) Structure of the Ire1 autophosphorylation complex and implications for the unfolded protein response EMBO J. 30, 894-905
-
(2011)
EMBO J.
, vol.30
, pp. 894-905
-
-
Ali, M.M.1
Bagratuni, T.2
Davenport, E.L.3
Nowak, P.R.4
Silva-Santisteban, M.C.5
Hardcastle, A.6
McAndrews, C.7
Rowlands, M.G.8
Morgan, G.J.9
Aherne, W.10
Collins, I.11
Davies, F.E.12
Pearl, L.H.13
-
76
-
-
84870357261
-
Divergent allosteric control of the IRE1alpha endoribonuclease using kinase inhibitors
-
Wang, L., Perera, B. G., Hari, S. B., Bhhatarai, B., Backes, B. J., Seeliger, M. A., Schurer, S. C., Oakes, S. A., Papa, F. R., and Maly, D. J. (2012) Divergent allosteric control of the IRE1alpha endoribonuclease using kinase inhibitors Nat. Chem. Biol. 8, 982-989
-
(2012)
Nat. Chem. Biol.
, vol.8
, pp. 982-989
-
-
Wang, L.1
Perera, B.G.2
Hari, S.B.3
Bhhatarai, B.4
Backes, B.J.5
Seeliger, M.A.6
Schurer, S.C.7
Oakes, S.A.8
Papa, F.R.9
Maly, D.J.10
-
77
-
-
84921403151
-
Druggable sensors of the unfolded protein response
-
Maly, D. J. and Papa, F. R. (2014) Druggable sensors of the unfolded protein response Nat. Chem. Biol. 10, 892-901
-
(2014)
Nat. Chem. Biol.
, vol.10
, pp. 892-901
-
-
Maly, D.J.1
Papa, F.R.2
-
78
-
-
84905492694
-
Allosteric inhibition of the IRE1alpha RNase preserves cell viability and function during endoplasmic reticulum stress
-
Ghosh, R., Wang, L., Wang, E. S., Perera, B. G., Igbaria, A., Morita, S., Prado, K., Thamsen, M., Caswell, D., Macias, H., Weiberth, K. F., Gliedt, M. J., Alavi, M. V., Hari, S. B., Mitra, A. K., Bhhatarai, B., Schurer, S. C., Snapp, E. L., Gould, D. B., German, M. S., Backes, B. J., Maly, D. J., Oakes, S. A., and Papa, F. R. (2014) Allosteric inhibition of the IRE1alpha RNase preserves cell viability and function during endoplasmic reticulum stress Cell 158, 534-548
-
(2014)
Cell
, vol.158
, pp. 534-548
-
-
Ghosh, R.1
Wang, L.2
Wang, E.S.3
Perera, B.G.4
Igbaria, A.5
Morita, S.6
Prado, K.7
Thamsen, M.8
Caswell, D.9
Macias, H.10
Weiberth, K.F.11
Gliedt, M.J.12
Alavi, M.V.13
Hari, S.B.14
Mitra, A.K.15
Bhhatarai, B.16
Schurer, S.C.17
Snapp, E.L.18
Gould, D.B.19
German, M.S.20
Backes, B.J.21
Maly, D.J.22
Oakes, S.A.23
Papa, F.R.24
more..
-
79
-
-
59649111087
-
The unfolded protein response signals through high-order assembly of Ire1
-
Korennykh, A. V., Egea, P. F., Korostelev, A. A., Finer-Moore, J., Zhang, C., Shokat, K. M., Stroud, R. M., and Walter, P. (2009) The unfolded protein response signals through high-order assembly of Ire1 Nature 457, 687-693
-
(2009)
Nature
, vol.457
, pp. 687-693
-
-
Korennykh, A.V.1
Egea, P.F.2
Korostelev, A.A.3
Finer-Moore, J.4
Zhang, C.5
Shokat, K.M.6
Stroud, R.M.7
Walter, P.8
-
80
-
-
84858236398
-
Working without kinase activity: Phosphotransfer-independent functions of extracellular signal-regulated kinases
-
Rodriguez, J. and Crespo, P. (2011) Working without kinase activity: phosphotransfer-independent functions of extracellular signal-regulated kinases Sci. Signal 4, re3
-
(2011)
Sci. Signal
, vol.4
, pp. 3
-
-
Rodriguez, J.1
Crespo, P.2
-
81
-
-
84901295552
-
Conformation-selective ATP-competitive inhibitors control regulatory interactions and noncatalytic functions of mitogen-activated protein kinases
-
Hari, S. B., Merritt, E. A., and Maly, D. J. (2014) Conformation-selective ATP-competitive inhibitors control regulatory interactions and noncatalytic functions of mitogen-activated protein kinases Chem. Biol. 21, 628-635
-
(2014)
Chem. Biol.
, vol.21
, pp. 628-635
-
-
Hari, S.B.1
Merritt, E.A.2
Maly, D.J.3
-
82
-
-
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., and Gray, N. S. (2010) Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors Nature 463, 501-506
-
(2010)
Nature
, vol.463
, 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..
-
83
-
-
84888104464
-
NMR reveals the allosteric opening and closing of Abelson tyrosine kinase by ATP-site and myristoyl pocket inhibitors
-
Skora, L., Mestan, J., Fabbro, D., Jahnke, W., and Grzesiek, S. (2013) NMR reveals the allosteric opening and closing of Abelson tyrosine kinase by ATP-site and myristoyl pocket inhibitors Proc. Natl. Acad. Sci. U. S. A. 110, E4437-4445
-
(2013)
Proc. Natl. Acad. Sci. U. S. A.
, vol.110
, pp. 4437-4445
-
-
Skora, L.1
Mestan, J.2
Fabbro, D.3
Jahnke, W.4
Grzesiek, S.5
-
84
-
-
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., and Wissner, A. (2004) Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase Cancer Res. 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
-
85
-
-
33144464795
-
EKB-569, a new irreversible epidermal growth factor receptor tyrosine kinase inhibitor, with clinical activity in patients with non-small cell lung cancer with acquired resistance to gefitinib
-
Yoshimura, N., Kudoh, S., Kimura, T., Mitsuoka, S., Matsuura, K., Hirata, K., Matsui, K., Negoro, S., Nakagawa, K., and Fukuoka, M. (2006) EKB-569, a new irreversible epidermal growth factor receptor tyrosine kinase inhibitor, with clinical activity in patients with non-small cell lung cancer with acquired resistance to gefitinib Lung Cancer 51, 363-368
-
(2006)
Lung Cancer
, vol.51
, pp. 363-368
-
-
Yoshimura, N.1
Kudoh, S.2
Kimura, T.3
Mitsuoka, S.4
Matsuura, K.5
Hirata, K.6
Matsui, K.7
Negoro, S.8
Nakagawa, K.9
Fukuoka, M.10
-
86
-
-
77955625479
-
The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy
-
Honigberg, L. A., Smith, A. M., Sirisawad, M., Verner, E., Loury, D., Chang, B., Li, S., Pan, Z., Thamm, D. H., Miller, R. A., and Buggy, J. J. (2010) The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy Proc. Natl. Acad. Sci. U. S. A. 107, 13075-13080
-
(2010)
Proc. Natl. Acad. Sci. U. S. A.
, vol.107
, pp. 13075-13080
-
-
Honigberg, L.A.1
Smith, A.M.2
Sirisawad, M.3
Verner, E.4
Loury, D.5
Chang, B.6
Li, S.7
Pan, Z.8
Thamm, D.H.9
Miller, R.A.10
Buggy, J.J.11
-
87
-
-
84874301754
-
Developing irreversible inhibitors of the protein kinase cysteinome
-
Liu, Q., Sabnis, Y., Zhao, Z., Zhang, T., Buhrlage, S. J., Jones, L. H., and Gray, N. S. (2013) Developing irreversible inhibitors of the protein kinase cysteinome Chem. Biol. 20, 146-159
-
(2013)
Chem. Biol.
, vol.20
, pp. 146-159
-
-
Liu, Q.1
Sabnis, Y.2
Zhao, Z.3
Zhang, T.4
Buhrlage, S.J.5
Jones, L.H.6
Gray, N.S.7
-
88
-
-
58549114067
-
A conserved protonation-dependent switch controls drug binding in the Abl kinase
-
Shan, Y., Seeliger, M. A., Eastwood, M. P., Frank, F., Xu, H., Jensen, M. O., Dror, R. O., Kuriyan, J., and Shaw, D. E. (2009) A conserved protonation-dependent switch controls drug binding in the Abl kinase Proc. Natl. Acad. Sci. U. S. A. 106, 139-144
-
(2009)
Proc. Natl. Acad. Sci. U. S. A.
, vol.106
, pp. 139-144
-
-
Shan, Y.1
Seeliger, M.A.2
Eastwood, M.P.3
Frank, F.4
Xu, H.5
Jensen, M.O.6
Dror, R.O.7
Kuriyan, J.8
Shaw, D.E.9
-
89
-
-
84877853315
-
Structure-kinetic relationship study of CDK8/CycC specific compounds
-
Schneider, E. V., Bottcher, J., Huber, R., Maskos, K., and Neumann, L. (2013) Structure-kinetic relationship study of CDK8/CycC specific compounds Proc. Natl. Acad. Sci. U. S. A. 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
-
90
-
-
84859388604
-
Investigation of the effect of molecular properties on the binding kinetics of a ligand to its biological target
-
Miller, D. C., Lunn, G., Jones, P., Sabnis, Y., Davies, N. L., and Driscoll, P. (2012) Investigation of the effect of molecular properties on the binding kinetics of a ligand to its biological target Medchemcomm 3, 449-452
-
(2012)
Medchemcomm
, vol.3
, pp. 449-452
-
-
Miller, D.C.1
Lunn, G.2
Jones, P.3
Sabnis, Y.4
Davies, N.L.5
Driscoll, P.6
-
91
-
-
0023364022
-
Computer simulations of the diffusion of a substrate to an active site of an enzyme
-
Sharp, K., Fine, R., and Honig, B. (1987) Computer simulations of the diffusion of a substrate to an active site of an enzyme Science 236, 1460-1463
-
(1987)
Science
, vol.236
, pp. 1460-1463
-
-
Sharp, K.1
Fine, R.2
Honig, B.3
-
92
-
-
84872837570
-
Solvent fluctuations in hydrophobic cavity-ligand binding kinetics
-
Setny, P., Baron, R., Michael Kekenes-Huskey, P., McCammon, J. A., and Dzubiella, J. (2013) Solvent fluctuations in hydrophobic cavity-ligand binding kinetics Proc. Natl. Acad. Sci. U. S. A. 110, 1197-1202
-
(2013)
Proc. Natl. Acad. Sci. U. S. A.
, vol.110
, pp. 1197-1202
-
-
Setny, P.1
Baron, R.2
Michael Kekenes-Huskey, P.3
McCammon, J.A.4
Dzubiella, J.5
-
93
-
-
77952921531
-
A lipid pathway for ligand binding is necessary for a cannabinoid G protein-coupled receptor
-
Hurst, D. P., Grossfield, A., Lynch, D. L., Feller, S., Romo, T. D., Gawrisch, K., Pitman, M. C., and Reggio, P. H. (2010) A lipid pathway for ligand binding is necessary for a cannabinoid G protein-coupled receptor J. Biol. Chem. 285, 17954-17964
-
(2010)
J. Biol. Chem.
, vol.285
, pp. 17954-17964
-
-
Hurst, D.P.1
Grossfield, A.2
Lynch, D.L.3
Feller, S.4
Romo, T.D.5
Gawrisch, K.6
Pitman, M.C.7
Reggio, P.H.8
-
94
-
-
84885131303
-
Computational analysis of the binding specificity of Gleevec to Abl, c-Kit, Lck, and c-Src tyrosine kinases
-
Lin, Y. L. and Roux, B. (2013) Computational analysis of the binding specificity of Gleevec to Abl, c-Kit, Lck, and c-Src tyrosine kinases J. Am. Chem. Soc. 135, 14741-14753
-
(2013)
J. Am. Chem. Soc.
, vol.135
, pp. 14741-14753
-
-
Lin, Y.L.1
Roux, B.2
-
95
-
-
84873135773
-
Explaining why Gleevec is a specific and potent inhibitor of Abl kinase
-
Lin, Y. L., Meng, Y., Jiang, W., and Roux, B. (2013) Explaining why Gleevec is a specific and potent inhibitor of Abl kinase Proc. Natl. Acad. Sci. U. S. A. 110, 1664-1669
-
(2013)
Proc. Natl. Acad. Sci. U. S. A.
, vol.110
, pp. 1664-1669
-
-
Lin, Y.L.1
Meng, Y.2
Jiang, W.3
Roux, B.4
-
96
-
-
77951557992
-
Molecular dynamics simulations show that conformational selection governs the binding preferences of imatinib for several tyrosine kinases
-
Aleksandrov, A. and Simonson, T. (2010) Molecular dynamics simulations show that conformational selection governs the binding preferences of imatinib for several tyrosine kinases J. Biol. Chem. 285, 13807-13815
-
(2010)
J. Biol. Chem.
, vol.285
, pp. 13807-13815
-
-
Aleksandrov, A.1
Simonson, T.2
-
97
-
-
84890823201
-
Conformation-selective inhibitors reveal differences in the activation and phosphate-binding loops of the tyrosine kinases Abl and Src
-
Hari, S. B., Perera, B. G., Ranjitkar, P., Seeliger, M. A., and Maly, D. J. (2013) Conformation-selective inhibitors reveal differences in the activation and phosphate-binding loops of the tyrosine kinases Abl and Src ACS Chem. Biol. 8, 2734-2743
-
(2013)
ACS Chem. Biol.
, vol.8
, pp. 2734-2743
-
-
Hari, S.B.1
Perera, B.G.2
Ranjitkar, P.3
Seeliger, M.A.4
Maly, D.J.5
-
98
-
-
79957497448
-
Discovery of a potential allosteric ligand binding site in CDK2
-
Betzi, S., Alam, R., Martin, M., Lubbers, D. J., Han, H., Jakkaraj, S. R., Georg, G. I., and Schonbrunn, E. (2011) Discovery of a potential allosteric ligand binding site in CDK2 ACS Chem. Biol. 6, 492-501
-
(2011)
ACS Chem. Biol.
, vol.6
, 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
-
99
-
-
84866449140
-
A novel approach to the discovery of small-molecule ligands of CDK2
-
Martin, M. P., Alam, R., Betzi, S., Ingles, D. J., Zhu, J. Y., and Schonbrunn, E. (2012) A novel approach to the discovery of small-molecule ligands of CDK2 Chembiochem 13, 2128-2136
-
(2012)
Chembiochem
, vol.13
, pp. 2128-2136
-
-
Martin, M.P.1
Alam, R.2
Betzi, S.3
Ingles, D.J.4
Zhu, J.Y.5
Schonbrunn, E.6
-
100
-
-
84921364228
-
A dynamically coupled allosteric network underlies binding cooperativity in Src kinase
-
(In press)
-
Foda, Z. H., Shan, Y., Kim, E., Shaw, D. E., and Seeliger, M. A. (In press) A dynamically coupled allosteric network underlies binding cooperativity in Src kinase, Nat. Commun.
-
Nat. Commun.
-
-
Foda, Z.H.1
Shan, Y.2
Kim, E.3
Shaw, D.E.4
Seeliger, M.A.5
-
101
-
-
37649004940
-
Structure of the dual enzyme Ire1 reveals the basis for catalysis and regulation in nonconventional RNA splicing
-
Lee, K. P., Dey, M., Neculai, D., Cao, C., Dever, T. E., and Sicheri, F. (2008) Structure of the dual enzyme Ire1 reveals the basis for catalysis and regulation in nonconventional RNA splicing Cell 132, 89-100
-
(2008)
Cell
, vol.132
, pp. 89-100
-
-
Lee, K.P.1
Dey, M.2
Neculai, D.3
Cao, C.4
Dever, T.E.5
Sicheri, F.6
|