메뉴 건너뛰기




Volumn 375, Issue 2, 2003, Pages 255-262

Structural basis for UCN-01 (7-hydroxystaurosporine) specificity and PDK1 (3-phosphoinositide-dependent protein kinase-1) inhibition

Author keywords

3 phosphoinositide dependent protein kinase 1 (PDK1); 7 hydroxystaurosporine (UCN 01); Kinase alignment; Kinase inhibitor specificity

Indexed keywords

CRYSTAL STRUCTURE; ENZYMES; HYDROGEN BONDS; INSULIN; OPTIMIZATION;

EID: 0142231577     PISSN: 02646021     EISSN: None     Source Type: Journal    
DOI: 10.1042/BJ20031119     Document Type: Article
Times cited : (118)

References (49)
  • 1
    • 0034653608 scopus 로고    scopus 로고
    • The PI3K-PDK1 connection: More than just a road to PKB
    • Vanhaesebroeck, B. and Alessi, D. R. (2000) The PI3K-PDK1 connection: more than just a road to PKB. Biochem. J. 346, 561-576
    • (2000) Biochem. J. , vol.346 , pp. 561-576
    • Vanhaesebroeck, B.1    Alessi, D.R.2
  • 2
    • 0033084143 scopus 로고    scopus 로고
    • Role of phosphatidylinositol 3,4,5-trisphosphate in regulating the activity and localization of 3-phosphoinositide-dependent protein kinase-1
    • Currie, R. A., Walker, K. S., Gray, A., Deak, M., Casamayor, A., Downes, C. P., Cohen, P., Alessi, D. R. and Lucocq, J. (1999) Role of phosphatidylinositol 3,4,5-trisphosphate in regulating the activity and localization of 3-phosphoinositide-dependent protein kinase-1. Biochem. J. 337, 575-583
    • (1999) Biochem. J. , vol.337 , pp. 575-583
    • Currie, R.A.1    Walker, K.S.2    Gray, A.3    Deak, M.4    Casamayor, A.5    Downes, C.P.6    Cohen, P.7    Alessi, D.R.8    Lucocq, J.9
  • 3
    • 85047681190 scopus 로고    scopus 로고
    • Discovery of PDK1, one of the missing links in insulin signal transduction
    • Alessi, D. R. (2001) Discovery of PDK1, one of the missing links in insulin signal transduction. Biochem. Soc. Trans. 29, 1-14
    • (2001) Biochem. Soc. Trans. , vol.29 , pp. 1-14
    • Alessi, D.R.1
  • 4
    • 0035499454 scopus 로고    scopus 로고
    • Ten years of protein kinase B signalling: A hard Akt to follow
    • Brazil, D. P and Hemmings, B. A. (2001) Ten years of protein kinase B signalling: a hard Akt to follow. Trends Biochem. Sci. 26, 657-664
    • (2001) Trends Biochem. Sci. , vol.26 , pp. 657-664
    • Brazil, D.P.1    Hemmings, B.A.2
  • 5
    • 0035489468 scopus 로고    scopus 로고
    • PKB/AKT Functional insights from genetic models
    • Scheid, M. P and Woodgett, J. R. (2001) PKB/AKT Functional insights from genetic models. Nat. Rev. Mol. Cell. Biol. 2, 760-768
    • (2001) Nat. Rev. Mol. Cell. Biol. , vol.2 , pp. 760-768
    • Scheid, M.P.1    Woodgett, J.R.2
  • 7
    • 0035856598 scopus 로고    scopus 로고
    • Regulation and physiological roles of serum-and glucocorticoid-induced protein kinase isoforms
    • Lang, F. and Cohen, P. (2001) Regulation and physiological roles of serum-and glucocorticoid-induced protein kinase isoforms, Sci. STKE, RE17
    • (2001) Sci. STKE , vol.RE17
    • Lang, F.1    Cohen, P.2
  • 8
    • 0040175067 scopus 로고    scopus 로고
    • Role and regulation of 90 kDa ribosomal S6 kinase (RSK) in signal transduction
    • Frodin, M. and Gammeltoft, S. (1999) Role and regulation of 90 kDa ribosomal S6 kinase (RSK) in signal transduction. Mol. Cell. Endocrinol. 151, 65-77
    • (1999) Mol. Cell. Endocrinol. , vol.151 , pp. 65-77
    • Frodin, M.1    Gammeltoft, S.2
  • 9
    • 0037954572 scopus 로고    scopus 로고
    • Signalling specificity of Ser/Thr protein kinases through docking-site-mediated interactions
    • Biondi, R. M. and Nebreda, A. R. (2003) Signalling specificity of Ser/ Thr protein kinases through docking-site-mediated interactions. Biochem. J. 372, 1-13
    • (2003) Biochem. J. , vol.372 , pp. 1-13
    • Biondi, R.M.1    Nebreda, A.R.2
  • 10
    • 0034161251 scopus 로고    scopus 로고
    • Identification of a pocket in the PDK1 kinase domain that interacts with PIF and the C-terminal residues of PKA
    • Biondi, R. M., Cheung, P. C. F., Casamayor, A., Deak, M., Currie, R. A. and Alessi, D. R. (2000) Identification of a pocket in the PDK1 kinase domain that interacts with PIF and the C-terminal residues of PKA. EMBO J. 19, 979-988
    • (2000) EMBO J. , vol.19 , pp. 979-988
    • Biondi, R.M.1    Cheung, P.C.F.2    Casamayor, A.3    Deak, M.4    Currie, R.A.5    Alessi, D.R.6
  • 11
    • 0037102153 scopus 로고    scopus 로고
    • High resolution crystal structure of the human PDK1 catalytic domain defines the regulatory phosphopeptide docking site
    • Biondi, R. M., Komander, D., Thomas, C. C., Lizcano, J. M., Deak, M., Alessi, D. R. and van Aalten, D. M. F. (2002) High resolution crystal structure of the human PDK1 catalytic domain defines the regulatory phosphopeptide docking site. EMBO J. 21, 4219-4228
    • (2002) EMBO J. , vol.21 , pp. 4219-4228
    • Biondi, R.M.1    Komander, D.2    Thomas, C.C.3    Lizcano, J.M.4    Deak, M.5    Alessi, D.R.6    Van Aalten, D.M.F.7
  • 12
    • 0036181869 scopus 로고    scopus 로고
    • PTEN: The down side of PI 3-kinase signalling
    • Leslie, N. R. and Downes, C. P. (2002) PTEN: the down side of PI 3-kinase signalling. Cell. Signal. 14, 285-295
    • (2002) Cell. Signal. , vol.14 , pp. 285-295
    • Leslie, N.R.1    Downes, C.P.2
  • 14
    • 0024394417 scopus 로고
    • Staurosporine, K-252 and UCN-01 -potent but nonspecific inhibitors of protein-kinases
    • Ruegg, U. T. and Burgess, G. M. (1989) Staurosporine, K-252 and UCN-01 -potent but nonspecific inhibitors of protein-kinases, Trends Pharmacol. Sci. 10, 218-220
    • (1989) Trends Pharmacol. Sci. , vol.10 , pp. 218-220
    • Ruegg, U.T.1    Burgess, G.M.2
  • 15
    • 0028242089 scopus 로고
    • Protein-kinase-C inhibitors induce apoptosis in human-malignant glioma cell-lines
    • Couldwell, W. T., Hinton, D. R., He, S. K., Chen, T. C., Sebat, I., Weiss, M. H. and Law, R. E. (1994) Protein-kinase-C inhibitors induce apoptosis in human-malignant glioma cell-lines. FEBS Lett. 345, 43-46
    • (1994) FEBS Lett. , vol.345 , pp. 43-46
    • Couldwell, W.T.1    Hinton, D.R.2    He, S.K.3    Chen, T.C.4    Sebat, I.5    Weiss, M.H.6    Law, R.E.7
  • 16
    • 0024542411 scopus 로고
    • Ucn-01 and ucn-02, new selective inhibitors of protein kinase-c. Purification, physicochemical properties, structural determination and biological-activities
    • Takahashi, I., Saitoh, Y., Yoshida, M., Sano, H., Nakano, H., Morimoto, M. and Tamaoki, T. (1989) Ucn-01 and ucn-02, new selective inhibitors of protein kinase-c. Purification, physicochemical properties, structural determination and biological-activities. J. Antibiot. 42, 571-576
    • (1989) J. Antibiot. , vol.42 , pp. 571-576
    • Takahashi, I.1    Saitoh, Y.2    Yoshida, M.3    Sano, H.4    Nakano, H.5    Morimoto, M.6    Tamaoki, T.7
  • 17
    • 0034306450 scopus 로고    scopus 로고
    • Specificity and mechanism of action of some commonly used protein kinase inhibitors
    • Davies, S. P., Reddy, H., Caivano, M. and Cohen, P. (2000) Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem. J. 351, 95-105
    • (2000) Biochem. J. , vol.351 , pp. 95-105
    • Davies, S.P.1    Reddy, H.2    Caivano, M.3    Cohen, P.4
  • 18
    • 0034013507 scopus 로고    scopus 로고
    • Staurosporine analogues - Pharmacological toys or useful antitumour agents?
    • Gescher, A. (2000) Staurosporine analogues - pharmacological toys or useful antitumour agents? Crit. Rev. Oncol. Hematol. 34, 127-133
    • (2000) Crit. Rev. Oncol. Hematol. , vol.34 , pp. 127-133
    • Gescher, A.1
  • 19
    • 0036057475 scopus 로고    scopus 로고
    • The cell cycle as a target for cancer therapy: Basic and clinical findings with the small molecule inhibitors flavopiridol and UCN-01
    • Senderowicz, A. M. (2002) The cell cycle as a target for cancer therapy: basic and clinical findings with the small molecule inhibitors flavopiridol and UCN-01. Oncologist 7, 9-12
    • (2002) Oncologist , vol.7 , pp. 9-12
    • Senderowicz, A.M.1
  • 21
    • 0037034928 scopus 로고    scopus 로고
    • Interference with PDK1-Akt survival signaling pathway by UCN-01 (7-hydroxystaurosporine)
    • Sato, S., Fujita, N. and Tsuruo, T. (2002) Interference with PDK1-Akt survival signaling pathway by UCN-01 (7-hydroxystaurosporine). Oncogene 21, 1727-1738
    • (2002) Oncogene , vol.21 , pp. 1727-1738
    • Sato, S.1    Fujita, N.2    Tsuruo, T.3
  • 22
    • 0031059866 scopus 로고    scopus 로고
    • Processing of X-ray diffraction data collected in oscillation mode
    • Otwinowski Z. and Minor, W. (1997) Processing of X-ray diffraction data collected in oscillation mode. Methods Enzymol. 276, 307-326
    • (1997) Methods Enzymol. , vol.276 , pp. 307-326
    • Otwinowski, Z.1    Minor, W.2
  • 24
    • 84889120137 scopus 로고
    • Improved methods for building protein models in electron density maps and the location of errors in these models
    • Jones, T. A., Zou, J. Y., Cowan, S. W. and Kjeldgaard, M. (1991) Improved methods for building protein models in electron density maps and the location of errors in these models. Acta Crystallogr. Sect. A: Found. Crystallogr. A47, 110-119
    • (1991) Acta Crystallogr. Sect. A: Found. Crystallogr. , vol.A47 , pp. 110-119
    • Jones, T.A.1    Zou, J.Y.2    Cowan, S.W.3    Kjeldgaard, M.4
  • 25
    • 0030158429 scopus 로고    scopus 로고
    • PRODRG, a program for generating molecular topologies and unique molecular descriptors from coordinates of small molecules
    • van Aalten, D. M. F., Bywater, R., Findlay, J. B. C., Hendlich, M., Hooft, R. W. W. and Vriend, G. (1996) PRODRG, a program for generating molecular topologies and unique molecular descriptors from coordinates of small molecules. J. Comput. Aided Mol. Des. 10, 255-262
    • (1996) J. Comput. Aided Mol. Des. , vol.10 , pp. 255-262
    • Van Aalten, D.M.F.1    Bywater, R.2    Findlay, J.B.C.3    Hendlich, M.4    Hooft, R.W.W.5    Vriend, G.6
  • 26
    • 0037392942 scopus 로고    scopus 로고
    • The specificities of protein kinase inhibitors: An update
    • Bain, J., McLauchlan, H., Elliott, M. and Cohen, P. (2003) The specificities of protein kinase inhibitors: an update, Biochem. J. 371, 199-204
    • (2003) Biochem. J. , vol.371 , pp. 199-204
    • Bain, J.1    McLauchlan, H.2    Elliott, M.3    Cohen, P.4
  • 27
    • 0026342401 scopus 로고
    • Crystal-structure of the catalytic subunit of cyclic adenosine monophosphate dependent protein-kinase
    • Knighton, D. R., Zheng, J. H., Teneyck, L. F., Ashford, V. A., Xuong, N. H., Taylor, S. S. and Sowadski, J. M. (1991) Crystal-structure of the catalytic subunit of cyclic adenosine monophosphate dependent protein-kinase. Science 253, 407-414
    • (1991) Science , vol.253 , pp. 407-414
    • Knighton, D.R.1    Zheng, J.H.2    Teneyck, L.F.3    Ashford, V.A.4    Xuong, N.H.5    Taylor, S.S.6    Sowadski, J.M.7
  • 29
    • 0031574365 scopus 로고    scopus 로고
    • 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. and Bossemeyer, D. (1997) Staurosporine-induced conformational changes of cAMP-dependent protein kinase catalytic subunit explain inhibitory potential. Structure 5, 1627-1637
    • (1997) Structure , vol.5 , pp. 1627-1637
    • Prade, L.1    Engh, R.A.2    Girod, A.3    Kinzel, V.4    Huber, R.5    Bossemeyer, D.6
  • 31
    • 0031253655 scopus 로고    scopus 로고
    • Protein kinase inhibition by staurosporine revealed in details of the molecular interaction with CDK2
    • Lawrie, A. M., Noble, M. E. M., Tunnah, P., Brown, N. R., Johnson, L. N. and Endicott, J. A. (1997) Protein kinase inhibition by staurosporine revealed in details of the molecular interaction with CDK2. Nat. Struct. Biol. 4, 796-801
    • (1997) Nat. Struct. Biol. , vol.4 , pp. 796-801
    • Lawrie, A.M.1    Noble, M.E.M.2    Tunnah, P.3    Brown, N.R.4    Johnson, L.N.5    Endicott, J.A.6
  • 32
    • 0027995683 scopus 로고
    • Detection, delineation, measurement and display of cavities in macromolecular structures
    • Kleywegt, G. J. and Jones, T. A. (1994) Detection, delineation, measurement and display of cavities in macromolecular structures. Acta Crystallogr. Sect D: Biol. Crystallogr. D50, 178-185
    • (1994) Acta Crystallogr. Sect D: Biol. Crystallogr. , vol.D50 , pp. 178-185
    • Kleywegt, G.J.1    Jones, T.A.2
  • 34
    • 0033516705 scopus 로고    scopus 로고
    • The packing density in proteins: Standard radii and volumes
    • Tsai, J., Taylor, R., Chothia, C. and Gerstein, M. (1999) The packing density in proteins: standard radii and volumes. J. Mol. Biol. 290, 253-266
    • (1999) J. Mol. Biol. , vol.290 , pp. 253-266
    • Tsai, J.1    Taylor, R.2    Chothia, C.3    Gerstein, M.4
  • 35
    • 0036304913 scopus 로고    scopus 로고
    • Molecular mimicry of carbohydrates by peptides
    • Johnson, M. A. and Pinto, B. M. (2002) Molecular mimicry of carbohydrates by peptides. Aust. J. Chem. 55, 13-25
    • (2002) Aust. J. Chem. , vol.55 , pp. 13-25
    • Johnson, M.A.1    Pinto, B.M.2
  • 36
    • 0025398721 scopus 로고
    • WHAT IF: A molecular modeling and drug design program
    • Vriend, G. (1990) WHAT IF: a molecular modeling and drug design program. J. Mol. Graph. 8, 52-56
    • (1990) J. Mol. Graph. , vol.8 , pp. 52-56
    • Vriend, G.1
  • 37
    • 0030442990 scopus 로고    scopus 로고
    • Positioning hydrogen atoms by optimizing hydrogen-bond networks in protein structures
    • Hooft, R. W. W., Sander, C. and Vriend, G. (1996) Positioning hydrogen atoms by optimizing hydrogen-bond networks in protein structures, Proteins 26, 363-376
    • (1996) Proteins , vol.26 , pp. 363-376
    • Hooft, R.W.W.1    Sander, C.2    Vriend, G.3
  • 38
    • 0034623005 scopus 로고    scopus 로고
    • T-Coffee: A novel method for fast and accurate multiple sequence alignment
    • Notredame, C., Higgins, D. G. and Heringa, J. (2000) T-Coffee: a novel method for fast and accurate multiple sequence alignment, J. Mol. Biol. 302, 205-217
    • (2000) J. Mol. Biol. , vol.302 , pp. 205-217
    • Notredame, C.1    Higgins, D.G.2    Heringa, J.3
  • 39
    • 0029644732 scopus 로고
    • Two structures of the catalytic domain of phosphorylase-kinase - An active protein-kinase complexed with substrate-analog and product
    • Owen, D. J., Noble, M. E. M., Garman, E. F., Papageorgiou, A. C. and Johnson, L. N. (1995) Two structures of the catalytic domain of phosphorylase-kinase - an active protein-kinase complexed with substrate-analog and product. Structure 3, 467-482
    • (1995) Structure , vol.3 , pp. 467-482
    • Owen, D.J.1    Noble, M.E.M.2    Garman, E.F.3    Papageorgiou, A.C.4    Johnson, L.N.5
  • 40
    • 0033152210 scopus 로고    scopus 로고
    • Structural analysis of the lymphocyte-specific kinase Lck in complex with non-selective and Src family selective kinase inhibitors
    • Zhu, X. T., Kim, J. L., Newcomb, J. R., Rose, P. E., Stover, D. R., Toledo, L. M., Zhao, H. L. and Morgenstern, K. A. (1999) Structural analysis of the lymphocyte-specific kinase Lck in complex with non-selective and Src family selective kinase inhibitors, Struct. Fold. Des. 7, 651-661
    • (1999) Struct. Fold. Des. , vol.7 , pp. 651-661
    • Zhu, X.T.1    Kim, J.L.2    Newcomb, J.R.3    Rose, P.E.4    Stover, D.R.5    Toledo, L.M.6    Zhao, H.L.7    Morgenstern, K.A.8
  • 41
    • 18744373865 scopus 로고    scopus 로고
    • Crystal structure of an activated Akt/protein kinase B ternary complex with GSK3-peptide and AMP-PNP
    • Yang, J., Cron, P., Good, V. M., Thompson, V., Hemmings, B. A. and Barford, D. (2002) Crystal structure of an activated Akt/protein kinase B ternary complex with GSK3-peptide and AMP-PNP. Nat. Struct. Biol. 9, 940-944
    • (2002) Nat. Struct. Biol. , vol.9 , pp. 940-944
    • Yang, J.1    Cron, P.2    Good, V.M.3    Thompson, V.4    Hemmings, B.A.5    Barford, D.6
  • 43
    • 0033555270 scopus 로고    scopus 로고
    • Structure of the protein tyrosine kinase domain of C-terminal Src kinase (CSK) in complex with staurosporine
    • Lamers, M. B. A. C., Antson, A. A., Hubbard, R. E., Scott, R. K. and Williams, D. H. (1999) Structure of the protein tyrosine kinase domain of C-terminal Src kinase (CSK) in complex with staurosporine. J. Mol. Biol., 285, 713-725
    • (1999) J. Mol. Biol. , vol.285 , pp. 713-725
    • Lamers, M.B.A.C.1    Antson, A.A.2    Hubbard, R.E.3    Scott, R.K.4    Williams, D.H.5
  • 44
    • 0033567706 scopus 로고    scopus 로고
    • The structure of phosphorylated P38 gamma is monomeric and reveals a conserved activation-loop conformation
    • Bellon, S., Fitzgibbon, M. J., Fox, T., Hsiao, H. M. and Wilson, K. P. (1999) The structure of phosphorylated P38 gamma is monomeric and reveals a conserved activation-loop conformation, Struct. Fold. Des. 7, 1057-1065
    • (1999) Struct. Fold. Des. , vol.7 , pp. 1057-1065
    • Bellon, S.1    Fitzgibbon, M.J.2    Fox, T.3    Hsiao, H.M.4    Wilson, K.P.5
  • 45
  • 47
    • 0034703030 scopus 로고    scopus 로고
    • The replacement of ATP by the competitive inhibitor emodin induces conformational modifications in the catalytic site of protein kinase CK2
    • Battistutta, R., Sarno, S., De Moliner, E., Papinutto, E., Zanotti, G. and Pinna, L. A. (2000) The replacement of ATP by the competitive inhibitor emodin induces conformational modifications in the catalytic site of protein kinase CK2. J. Biol. Chem. 275, 29618-29622
    • (2000) J. Biol. Chem. , vol.275 , pp. 29618-29622
    • Battistutta, R.1    Sarno, S.2    De Moliner, E.3    Papinutto, E.4    Zanotti, G.5    Pinna, L.A.6
  • 48
    • 0028978004 scopus 로고
    • Casein kinase i-gamma subfamily - Molecular-cloning, expression, and characterization of 3 mammalian isoforms and complementation of defects in the Saccharomyces cerevisiae yck genes
    • Zhai, L. M., Graves, P. R., Robinson, L. C., Italiano, M., Culbertson, M. R., Rowles, J., Cobb, M. H., Depaoliroach, A. A. and Roach, P. J. (1995) Casein kinase i-gamma subfamily - molecular-cloning, expression, and characterization of 3 mammalian isoforms and complementation of defects in the Saccharomyces cerevisiae yck genes. J. Biol. Chem. 270, 12717-12724
    • (1995) J. Biol. Chem. , vol.270 , pp. 12717-12724
    • Zhai, L.M.1    Graves, P.R.2    Robinson, L.C.3    Italiano, M.4    Culbertson, M.R.5    Rowles, J.6    Cobb, M.H.7    Depaoliroach, A.A.8    Roach, P.J.9
  • 49
    • 0023552288 scopus 로고
    • UCN-01, a selective inhibitor of protein-kinase-C from Streptomyces
    • Takahashi, I., Kobayashi, E., Asano, K., Yoshida, M. and Nakano, H. (1987) UCN-01, a selective inhibitor of protein-kinase-C from Streptomyces. J. Antibiot. 40, 1782-1784
    • (1987) J. Antibiot. , vol.40 , pp. 1782-1784
    • Takahashi, I.1    Kobayashi, E.2    Asano, K.3    Yoshida, M.4    Nakano, H.5


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.