-
2
-
-
24944497371
-
Features of selective kinase inhibitors
-
Knight Z.A., Shokat K.M. (2005) Features of selective kinase inhibitors. Chem Biol 12 : 621 637.
-
(2005)
Chem Biol
, vol.12
, pp. 621-637
-
-
Knight, Z.A.1
Shokat, K.M.2
-
4
-
-
17644371341
-
Exosite-driven substrate specificity and function in coagulation
-
DOI 10.1111/j.1538-7836.2004.01021.x
-
Krishnaswamy S. (2005) Exosite-driven substrate specificity and function in coagulation. J Thromb Haemost 3 : 54 67. (Pubitemid 41647115)
-
(2005)
Journal of Thrombosis and Haemostasis
, vol.3
, Issue.1
, pp. 54-67
-
-
Krishnaswamy, S.1
-
5
-
-
0016796849
-
The refined crystal structure of bovine beta-trypsin at 1.8 A resolution. II. Crystallographic refinement, calcium binding site, benzamidine binding site and active site at pH 7.0
-
Bode W., Schwager P. (1975) The refined crystal structure of bovine beta-trypsin at 1.8 A resolution. II. Crystallographic refinement, calcium binding site, benzamidine binding site and active site at pH 7.0. J Mol Biol 98 : 693 717.
-
(1975)
J Mol Biol
, vol.98
, pp. 693-717
-
-
Bode, W.1
Schwager, P.2
-
6
-
-
0030767267
-
Exosites determine macromolecular substrate recognition by prothrombinase
-
DOI 10.1021/bi970979+
-
Krishnaswamy S., Betz A. (1997) Exosites determine macromolecular substrate recognition by prothrombinase. Biochemistry 36 : 12080 12086. (Pubitemid 27440946)
-
(1997)
Biochemistry
, vol.36
, Issue.40
, pp. 12080-12086
-
-
Krishnaswamy, S.1
Betz, A.2
-
7
-
-
0037088606
-
The contribution of factor Xa to exosite-dependent substrate recognition by prothrombinase
-
DOI 10.1074/jbc.M110848200
-
Wilkens M., Krishnaswamy S. (2002) The contribution of factor Xa to exosite-dependent substrate recognition by prothrombinase. J Biol Chem 277 : 9366 9374. (Pubitemid 34953021)
-
(2002)
Journal of Biological Chemistry
, vol.277
, Issue.11
, pp. 9366-9374
-
-
Wilkens, M.1
Krishnaswamy, S.2
-
8
-
-
0034665994
-
Exosite interactions determine the affinity of factor X for the extrinsic Xase complex
-
Baugh R.J., Dickinson C.D., Ruf W., Krishnaswamy S. (2000) Exosite interactions determine the affinity of factor X for the extrinsic Xase complex. J Biol Chem 275 : 28826 28833.
-
(2000)
J Biol Chem
, vol.275
, pp. 28826-28833
-
-
Baugh, R.J.1
Dickinson, C.D.2
Ruf, W.3
Krishnaswamy, S.4
-
9
-
-
4644273599
-
Substrate-dependent modulation of the mechanism of factor XIa inhibition
-
DOI 10.1021/bi048964g
-
Pedicord D.L., Seiffert D., Blat Y. (2004) Substrate-dependent modulation of the mechanism of factor XIa inhibition. Biochemistry 43 : 11883 11888. (Pubitemid 39277635)
-
(2004)
Biochemistry
, vol.43
, Issue.37
, pp. 11883-11888
-
-
Pedicord, D.L.1
Seiffert, D.2
Blat, Y.3
-
10
-
-
0029826460
-
Identification of a factor IX binding site on the third apple domain of activated factor XI
-
DOI 10.1074/jbc.271.46.29023
-
Sun Y., Gailani D. (1996) Identification of a factor IX binding site on the third apple domain of activated factor XI. J Biol Chem 271 : 29023 29028. (Pubitemid 26382607)
-
(1996)
Journal of Biological Chemistry
, vol.271
, Issue.46
, pp. 29023-29028
-
-
Sun, Y.1
Gailani, D.2
-
11
-
-
0037200036
-
Linear non-competitive inhibition of solubilized human γ-secretase by pepstatin A methylester, L685458, sulfonamides, and benzodiazepines
-
DOI 10.1074/jbc.M112328200
-
Tian G., Sobotka-Briner C.D., Zysk J., Liu X., Birr C., Sylvester M.A., Edwards P.D., Scott C.D., Greenberg B.D. (2002) Linear non-competitive inhibition of solubilized human gamma-secretase by pepstatin A methylester, L685458, sulfonamides, and benzodiazepines. J Biol Chem 277 : 31499 31505. (Pubitemid 34968951)
-
(2002)
Journal of Biological Chemistry
, vol.277
, Issue.35
, pp. 31499-31505
-
-
Tian, G.1
Sobotka-Briner, C.D.2
Zysk, J.3
Liu, X.4
Birr, C.5
Sylvester, M.A.6
Edwards, P.D.7
Scott, C.D.8
Greenberg, B.D.9
-
12
-
-
0037022644
-
Activity-dependent isolation of the presenilin- γ-secretase complex reveals nicastrin and a γ substrate
-
DOI 10.1073/pnas.052436599
-
Esler W.P., Kimberly W.T., Ostaszewski B.L., Ye W., Diehl T.S., Selkoe D.J., Wolfe M.S. (2002) Activity-dependent isolation of the presenilin- gamma -secretase complex reveals nicastrin and a gamma substrate. Proc Natl Acad Sci U S A 99 : 2720 2725. (Pubitemid 34240527)
-
(2002)
Proceedings of the National Academy of Sciences of the United States of America
, vol.99
, Issue.5
, pp. 2720-2725
-
-
Esler, W.P.1
Taylor Kimberly, W.2
Ostaszewski, B.L.3
Ye, W.4
Diehl, T.S.5
Selkoe, D.J.6
Wolfe, M.S.7
-
14
-
-
0028106180
-
Kinetics of enzymes with iso-mechanisms: Dead-end inhibition of fumarase and carbonic anhydrase II
-
Rebholz K.L., Northrop D.B. (1994) Kinetics of enzymes with iso-mechanisms: dead-end inhibition of fumarase and carbonic anhydrase II. Arch Biochem Biophys 312 : 227 233.
-
(1994)
Arch Biochem Biophys
, vol.312
, pp. 227-233
-
-
Rebholz, K.L.1
Northrop, D.B.2
-
15
-
-
0038136955
-
Kinetic studies on β-site amyloid precursor protein-cleaving enzyme (BACE): Confirmation of an iso-mechanism
-
DOI 10.1074/jbc.M210471200
-
Toulokhonova L., Metzler W.J., Witmer M.R., Copeland R.A., Marcinkeviciene J. (2003) Kinetic studies on beta-site amyloid precursor protein-cleaving enzyme (BACE). Confirmation of an iso mechanism. J Biol Chem 278 : 4582 4589. (Pubitemid 36800955)
-
(2003)
Journal of Biological Chemistry
, vol.278
, Issue.7
, pp. 4582-4589
-
-
Toulokhonova, L.1
Metzler, W.J.2
Witmer, M.R.3
Copeland, R.A.4
Marcinkeviciene, J.5
-
16
-
-
4544381198
-
Biochemical mechanisms of drug action: What does it take for success?
-
Swinney D.C. (2004) Biochemical mechanisms of drug action: what does it take for success? Nat Rev Drug Discov 3 : 801 808.
-
(2004)
Nat Rev Drug Discov
, vol.3
, pp. 801-808
-
-
Swinney, D.C.1
-
17
-
-
44049103958
-
Residence time of receptor-ligand complexes and its effect on biological function
-
Tummino P.J., Copeland R.A. (2008) Residence time of receptor-ligand complexes and its effect on biological function. Biochemistry 47 : 5481 5492.
-
(2008)
Biochemistry
, vol.47
, pp. 5481-5492
-
-
Tummino, P.J.1
Copeland, R.A.2
-
18
-
-
0035425205
-
A three-step kinetic mechanism for selective inhibition of cyclo-oxygenase-2 by diarylheterocyclic inhibitors
-
DOI 10.1042/0264-6021:3570709
-
Walker M.C., Kurumbail R.G., Kiefer J.R., Moreland K.T., Koboldt C.M., Isakson P.C., Seibert K., Gierse J.K. (2001) A three-step kinetic mechanism for selective inhibition of cyclo-oxygenase-2 by diarylheterocyclic inhibitors. Biochem J 357 : 709 718. (Pubitemid 32735151)
-
(2001)
Biochemical Journal
, vol.357
, Issue.3
, pp. 709-718
-
-
Walker, M.C.1
Kurumbail, R.G.2
Kiefer, J.R.3
Moreland, K.T.4
Koboldt, C.M.5
Isakson, P.C.6
Seibert, K.7
Gierse, J.K.8
-
19
-
-
0032585605
-
17α by abiraterone (17-(3-pyridyl)androsta-5,16- dien-3β- ol) and related steroidal inhibitors
-
DOI 10.1021/jm981017j
-
Jarman M., Barrie S.E., Llera J.M. (1998) The 16,17-double bond is needed for irreversible inhibition of human cytochrome p45017alpha by abiraterone (17-(3-pyridyl)androsta-5, 16-dien-3beta-ol) and related steroidal inhibitors. J Med Chem 41 : 5375 5381. (Pubitemid 29031321)
-
(1998)
Journal of Medicinal Chemistry
, vol.41
, Issue.27
, pp. 5375-5381
-
-
Jarman, M.1
Barrie, E.2
Llera, J.M.3
-
20
-
-
58049206736
-
Targeting inactive enzyme conformation: Aryl diketoacid derivatives as a new class of PTP1B inhibitors
-
Liu S., Zeng L.F., Wu L., Yu X., Xue T., Gunawan A.M., Long Y.Q., Zhang Z.Y. (2008) Targeting inactive enzyme conformation: aryl diketoacid derivatives as a new class of PTP1B inhibitors. J Am Chem Soc 130 : 17075 17084.
-
(2008)
J Am Chem Soc
, vol.130
, pp. 17075-17084
-
-
Liu, S.1
Zeng, L.F.2
Wu, L.3
Yu, X.4
Xue, T.5
Gunawan, A.M.6
Long, Y.Q.7
Zhang, Z.Y.8
-
21
-
-
34547817154
-
A new paradigm for protein kinase inhibition: Blocking phosphorylation without directly targeting ATP binding
-
Bogoyevitch M.A., Fairlie D.P. (2007) A new paradigm for protein kinase inhibition: blocking phosphorylation without directly targeting ATP binding. Drug Discov Today 12 : 622 633.
-
(2007)
Drug Discov Today
, vol.12
, pp. 622-633
-
-
Bogoyevitch, M.A.1
Fairlie, D.P.2
-
22
-
-
0026077176
-
Kinetic studies on rat liver 11 beta-hydroxysteroid dehydrogenase
-
Monder C., Lakshmi V., Miroff Y. (1991) Kinetic studies on rat liver 11 beta-hydroxysteroid dehydrogenase. Biochim Biophys Acta 1115 : 23 29.
-
(1991)
Biochim Biophys Acta
, vol.1115
, pp. 23-29
-
-
Monder, C.1
Lakshmi, V.2
Miroff, Y.3
-
23
-
-
34548268002
-
Cofactor-specific modulation of 11β-hydroxysteroid dehydrogenase 1 inhibitor potency
-
DOI 10.1016/j.bbapap.2007.07.005, PII S1570963907001574
-
Sahni-Arya B., Flynn M.J., Bergeron L., Salyan M.E., Pedicord D.L., Golla R., Ma Z. et al. (2007) Cofactor-specific modulation of 11beta-hydroxysteroid dehydrogenase 1 inhibitor potency. Biochim Biophys Acta 1774 : 1184 1191. (Pubitemid 47333258)
-
(2007)
Biochimica et Biophysica Acta - Proteins and Proteomics
, vol.1774
, Issue.9
, pp. 1184-1191
-
-
Sahni-Arya, B.1
Flynn, M.J.2
Bergeron, L.3
Salyan, M.E.K.4
Pedicord, D.L.5
Golla, R.6
Ma, Z.7
Wang, H.8
Seethala, R.9
Wu, S.C.10
Li, J.J.11
Nayeem, A.12
Gates, C.13
Hamann, L.G.14
Gordon, D.A.15
Blat, Y.16
-
24
-
-
52949108814
-
Distinctive molecular inhibition mechanisms for selective inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1
-
Tu H., Powers J.P., Liu J., Ursu S., Sudom A., Yan X., Xu H. et al. (2008) Distinctive molecular inhibition mechanisms for selective inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1. Bioorg Med Chem 16 : 8922 8931.
-
(2008)
Bioorg Med Chem
, vol.16
, pp. 8922-8931
-
-
Tu, H.1
Powers, J.P.2
Liu, J.3
Ursu, S.4
Sudom, A.5
Yan, X.6
Xu, H.7
-
25
-
-
0027378377
-
Refined 1.8 A structure of human aldose reductase complexed with the potent inhibitor zopolrestat
-
DOI 10.1073/pnas.90.21.9847
-
Wilson D.K., Tarle I., Petrash J.M., Quiocho F.A. (1993) Refined 1.8 A structure of human aldose reductase complexed with the potent inhibitor zopolrestat. Proc Natl Acad Sci U S A 90 : 9847 9851. (Pubitemid 23328207)
-
(1993)
Proceedings of the National Academy of Sciences of the United States of America
, vol.90
, Issue.21
, pp. 9847-9851
-
-
Wilson, D.K.1
Tarle, I.2
Petrash, J.M.3
Quiocho, F.A.4
-
26
-
-
0034521429
-
Efficient identification of inhibitors targeting the closed active site conformation of the HPRT from Trypanosoma cruzi
-
DOI 10.1016/S1074-5521(00)00045-4
-
Freymann D.M., Wenck M.A., Engel J.C., Feng J., Focia P.J., Eakin A.E., Craig S.P. (2000) Efficient identification of inhibitors targeting the closed active site conformation of the HPRT from Trypanosoma cruzi. Chem Biol 7 : 957 968. (Pubitemid 32046424)
-
(2000)
Chemistry and Biology
, vol.7
, Issue.12
, pp. 957-968
-
-
Freymann, D.M.1
Wenck, M.A.2
Engel, J.C.3
Feng, J.4
Focia, P.J.5
Eakin, A.E.6
Craig III, S.P.7
-
27
-
-
0026501290
-
Steady-state kinetics of the schistosomal hypoxanthine-guanine phosphoribosyltransferase
-
Yuan L., Craig S.P. III., McKerrow J.H., Wang C.C. (1992) Steady-state kinetics of the schistosomal hypoxanthine-guanine phosphoribosyltransferase. Biochemistry 31 : 806 810.
-
(1992)
Biochemistry
, vol.31
, pp. 806-810
-
-
Yuan, L.1
Craig, III.S.P.2
McKerrow, J.H.3
Wang, C.C.4
-
28
-
-
0030736715
-
The catalytic mechanism of mammalian adenylyl cyclase. Equilibrium binding and kinetic analysis of P-site inhibition
-
Dessauer C.W., Gilman A.G. (1997) The catalytic mechanism of mammalian adenylyl cyclase. Equilibrium binding and kinetic analysis of P-site inhibition. J Biol Chem 272 : 27787 27795.
-
(1997)
J Biol Chem
, vol.272
, pp. 27787-27795
-
-
Dessauer, C.W.1
Gilman, A.G.2
-
29
-
-
0026548701
-
Kinetic analysis of protein kinase C inhibition by staurosporine: Evidence that inhibition entails inhibitor binding at a conserved region of the catalytic domain but not competition with substrates
-
Ward N.E., O'Brian C.A. (1992) Kinetic analysis of protein kinase C inhibition by staurosporine: evidence that inhibition entails inhibitor binding at a conserved region of the catalytic domain but not competition with substrates. Mol Pharmacol 41 : 387 392.
-
(1992)
Mol Pharmacol
, vol.41
, pp. 387-392
-
-
Ward, N.E.1
O'Brian, C.A.2
-
30
-
-
9644264028
-
Catalytic domain crystal structure of protein kinase C-θ (PKCθ)
-
DOI 10.1074/jbc.M409216200
-
Xu Z.B., Chaudhary D., Olland S., Wolfrom S., Czerwinski R., Malakian K., Lin L., Stahl M.L., Joseph-McCarthy D., Benander C., Fitz L., Greco R., Somers W.S., Mosyak L. (2004) Catalytic domain crystal structure of protein kinase C-theta (PKCtheta). J Biol Chem 279 : 50401 50409. (Pubitemid 39577858)
-
(2004)
Journal of Biological Chemistry
, vol.279
, Issue.48
, pp. 50401-50409
-
-
Xu, Z.-B.1
Chaudhary, D.2
Olland, S.3
Wolfrom, S.4
Czerwinski, R.5
Malakian, K.6
Lin, L.7
Stahl, M.L.8
Joseph-McCarthy, D.9
Benander, C.10
Fitz, L.11
Greco, R.12
Somers, W.S.13
Mosyak, L.14
-
31
-
-
0031574365
-
Staurosporine-induced conformational changes of cAMP-dependent protein kinase catalytic subunit explain inhibitory potential
-
Prade L., Engh R.A., Girod A., Kinzel V., Huber R., Bossemeyer D. (1997) Staurosporine-induced conformational changes of cAMP-dependent protein kinase catalytic subunit explain inhibitory potential. Structure 5 : 1627 1637. (Pubitemid 28051976)
-
(1997)
Structure
, vol.5
, Issue.12
, pp. 1627-1637
-
-
Prade, L.1
Engh, R.A.2
Girod, A.3
Kinzel, V.4
Huber, R.5
Bossemeyer, D.6
-
32
-
-
0027408171
-
Crystal structure of the catalytic subunit of cAMP-dependent protein kinase complexed with MgATP and peptide inhibitor
-
Zheng J., Trafny E.A., Knighton D.R., Xuong N.H., Taylor S.S., Ten Eyck L.F., Sowadski J.M. (1993) 2.2 A refined crystal structure of the catalytic subunit of cAMP-dependent protein kinase complexed with MnATP and a peptide inhibitor. Acta Crystallogr D Biol Crystallogr 49 : 362 365. (Pubitemid 23094874)
-
(1993)
Biochemistry
, vol.32
, Issue.9
, pp. 2154-2161
-
-
Zheng, J.1
Knighton, D.R.2
Ten Eyck, L.F.3
Karlsson, R.4
Xuong, N.-H.5
Taylor, S.S.6
Sowadski, J.M.7
-
33
-
-
0037468159
-
c-Src inhibitor PP1 is non-competitive against ATP
-
DOI 10.1016/S0014-5793(03)00069-3
-
Karni R., Mizrachi S., Reiss-Sklan E., Gazit A., Livnah O., Levitzki A. (2003) The pp60c-Src inhibitor PP1 is non-competitive against ATP. FEBS Lett 537 : 47 52. (Pubitemid 36246674)
-
(2003)
FEBS Letters
, 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
-
34
-
-
0033063429
-
Crystal structure of Hck in complex with a Src family-selective tyrosine kinase inhibitor
-
DOI 10.1016/S1097-2765(00)80357-3
-
Schindler T., Sicheri F., Pico A., Gazit A., Levitzki A., Kuriyan J. (1999) Crystal structure of Hck in complex with a Src family-selective tyrosine kinase inhibitor. Mol Cell 3 : 639 648. (Pubitemid 29268447)
-
(1999)
Molecular Cell
, vol.3
, Issue.5
, pp. 639-648
-
-
Schindler, T.1
Sicheri, F.2
Pico, A.3
Gazit, A.4
Levitzki, A.5
Kuriyan, J.6
-
35
-
-
0342546626
-
Phosphorylation site-specific inhibition of platelet-derived growth factor β-receptor autophosphorylation by the receptor blocking tyrphostin AG1296
-
DOI 10.1021/bi962553l
-
Kovalenko M., Ronnstrand L., Heldin C.H., Loubtchenkov M., Gazit A., Levitzki A., Bohmer F.D. (1997) Phosphorylation site-specific inhibition of platelet-derived growth factor beta-receptor autophosphorylation by the receptor blocking tyrphostin AG1296. Biochemistry 36 : 6260 6269. (Pubitemid 27231382)
-
(1997)
Biochemistry
, vol.36
, Issue.21
, pp. 6260-6269
-
-
Kovalenko, M.1
Ronnstrand, L.2
Heldin, C.-H.3
Loubtchenkov, M.4
Gazit, A.5
Levitzki, A.6
Bohmer, F.D.7
|