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Volumn 19, Issue 7, 2014, Pages 1024-1034

Enzymatic characterization of ER stress-dependent kinase, PERK, and development of a high-throughput assay for identification of PERK inhibitors

Author keywords

HTS; PERK; small molecule inhibitors

Indexed keywords

ADENOSINE TRIPHOSPHATE; IMATINIB; INITIATION FACTOR 2ALPHA; LDN 0020506; LDN 0070977; PERK KINASE; PROTEIN SERINE THREONINE KINASE; PROTEIN SERINE THREONINE KINASE INHIBITOR; SARCOPLASMIC RETICULUM CALCIUM TRANSPORTING ADENOSINE TRIPHOSPHATASE; UNCLASSIFIED DRUG; EIF2AK3 PROTEIN, HUMAN; ENZYME INHIBITOR; INITIATION FACTOR 2; PROTEIN KINASE R;

EID: 84904639817     PISSN: 10870571     EISSN: 1552454X     Source Type: Journal    
DOI: 10.1177/1087057114525853     Document Type: Article
Times cited : (23)

References (35)
  • 1
    • 0031755020 scopus 로고    scopus 로고
    • Identification and Characterization of Pancreatic Eukaryotic Initiation Factor 2 Alpha-Subunit Kinase, PEK, Involved in Translational Control
    • Shi Y., Vattem K. M., Sood R., et al. Identification and Characterization of Pancreatic Eukaryotic Initiation Factor 2 Alpha-Subunit Kinase, PEK, Involved in Translational Control. Mol. Cell Biol. 1998 ; 18: 7499-7509
    • (1998) Mol. Cell Biol , vol.18 , pp. 7499-7509
    • Shi, Y.1    Vattem, K.M.2    Sood, R.3
  • 2
    • 0032190546 scopus 로고    scopus 로고
    • Cloning of Mammalian Ire1 Reveals Diversity in the ER Stress Responses
    • Wang X. Z., Harding H. P., Zhang Y., et al. Cloning of Mammalian Ire1 Reveals Diversity in the ER Stress Responses. Embo J. 1998 ; 17: 5708-5717
    • (1998) Embo J , vol.17 , pp. 5708-5717
    • Wang, X.Z.1    Harding, H.P.2    Zhang, Y.3
  • 3
    • 0032693671 scopus 로고    scopus 로고
    • Mammalian Transcription Factor ATF6 Is Synthesized as a Transmembrane Protein and Activated by Proteolysis in Response to Endoplasmic Reticulum Stress
    • Haze K., Yoshida H., Yanagi H., et al. Mammalian Transcription Factor ATF6 Is Synthesized as a Transmembrane Protein and Activated by Proteolysis in Response to Endoplasmic Reticulum Stress. Mol. Biol. Cell. 1999 ; 10: 3787-3799
    • (1999) Mol. Biol. Cell , vol.10 , pp. 3787-3799
    • Haze, K.1    Yoshida, H.2    Yanagi, H.3
  • 4
    • 34548172495 scopus 로고    scopus 로고
    • Transcriptional Induction of Mammalian ER Quality Control Proteins Is Mediated by Single or Combined Action of ATF6alpha and XBP1
    • Yamamoto K., Sato T., Matsui T., et al. Transcriptional Induction of Mammalian ER Quality Control Proteins Is Mediated by Single or Combined Action of ATF6alpha and XBP1. Dev. Cell. 2007 ; 13: 365-376
    • (2007) Dev. Cell , vol.13 , pp. 365-376
    • Yamamoto, K.1    Sato, T.2    Matsui, T.3
  • 5
    • 34548189283 scopus 로고    scopus 로고
    • ATF6alpha Optimizes Long-Term Endoplasmic Reticulum Function to Protect Cells from Chronic Stress
    • Wu J., Rutkowski D. T., Dubois M., et al. ATF6alpha Optimizes Long-Term Endoplasmic Reticulum Function to Protect Cells from Chronic Stress. Dev. Cell. 2007 ; 13: 351-364
    • (2007) Dev. Cell , vol.13 , pp. 351-364
    • Wu, J.1    Rutkowski, D.T.2    Dubois, M.3
  • 6
    • 60149106099 scopus 로고    scopus 로고
    • PERK-Dependent Regulation of IAP Translation during ER Stress
    • Hamanaka R. B., Bobrovnikova-Marjon E., Ji X., et al. PERK-Dependent Regulation of IAP Translation during ER Stress. Oncogene. 2009 ; 28: 910-920
    • (2009) Oncogene , vol.28 , pp. 910-920
    • Hamanaka, R.B.1    Bobrovnikova-Marjon, E.2    Ji, X.3
  • 7
    • 33751285479 scopus 로고    scopus 로고
    • The PERK/eIF2alpha/ATF4 Module of the UPR in Hypoxia Resistance and Tumor Growth
    • Fels D. R., Koumenis C.. The PERK/eIF2alpha/ATF4 Module of the UPR in Hypoxia Resistance and Tumor Growth. Cancer Biol. Ther. 2006 ; 5: 723-728
    • (2006) Cancer Biol. Ther , vol.5 , pp. 723-728
    • Fels, D.R.1    Koumenis, C.2
  • 8
    • 0141752795 scopus 로고    scopus 로고
    • Nrf2 Is a Direct PERK Substrate and Effector of PERK-Dependent Cell Survival
    • Cullinan S. B., Zhang D., Hannink M., et al. Nrf2 Is a Direct PERK Substrate and Effector of PERK-Dependent Cell Survival. Mol. Cell Biol. 2003 ; 23: 7198-7209
    • (2003) Mol. Cell Biol , vol.23 , pp. 7198-7209
    • Cullinan, S.B.1    Zhang, D.2    Hannink, M.3
  • 9
    • 33845958175 scopus 로고    scopus 로고
    • The Unfolded Protein Response
    • Schroder M.. The Unfolded Protein Response. Mol. Biotechnol. 2006 ; 34: 279-290
    • (2006) Mol. Biotechnol , vol.34 , pp. 279-290
    • Schroder, M.1
  • 10
    • 57049117856 scopus 로고    scopus 로고
    • Cell Death and Endoplasmic Reticulum Stress: Disease Relevance and Therapeutic Opportunities
    • Kim I., Xu W., Reed J. C.. Cell Death and Endoplasmic Reticulum Stress: Disease Relevance and Therapeutic Opportunities. Nat. Rev. Drug Discov. 2008 ; 7: 1013-1030
    • (2008) Nat. Rev. Drug Discov , vol.7 , pp. 1013-1030
    • Kim, I.1    Xu, W.2    Reed, J.C.3
  • 11
    • 55849112292 scopus 로고    scopus 로고
    • PERK-Dependent Regulation of Lipogenesis during Mouse Mammary Gland Development and Adipocyte Differentiation
    • Bobrovnikova-Marjon E., Hatzivassiliou G., Grigoriadou C., et al. PERK-Dependent Regulation of Lipogenesis during Mouse Mammary Gland Development and Adipocyte Differentiation. Proc. Natl. Acad. Sci. U. S. A. 2008 ; 105: 16314-16319
    • (2008) Proc. Natl. Acad. Sci. U. S. A , vol.105 , pp. 16314-16319
    • Bobrovnikova-Marjon, E.1    Hatzivassiliou, G.2    Grigoriadou, C.3
  • 12
    • 79955656979 scopus 로고    scopus 로고
    • The Structure of the PERK Kinase Domain Suggests the Mechanism for Its Activation
    • Cui W., Li J., Ron D., et al. The Structure of the PERK Kinase Domain Suggests the Mechanism for Its Activation. Acta Crystallogr. D Biol. Crystallogr. 2011 ; 67: 423-428
    • (2011) Acta Crystallogr. D Biol. Crystallogr , vol.67 , pp. 423-428
    • Cui, W.1    Li, J.2    Ron, D.3
  • 15
    • 77749255337 scopus 로고    scopus 로고
    • Kinetic Mechanistic Studies of Wild-Type Leucine-Rich Repeat Kinase 2: Characterization of the Kinase and GTPase Activities
    • Liu M., Dobson B., Glicksman M. A., et al. Kinetic Mechanistic Studies of Wild-Type Leucine-Rich Repeat Kinase 2: Characterization of the Kinase and GTPase Activities. Biochemistry. 2010 ; 49: 2008-2017
    • (2010) Biochemistry , vol.49 , pp. 2008-2017
    • Liu, M.1    Dobson, B.2    Glicksman, M.A.3
  • 16
    • 77954457246 scopus 로고    scopus 로고
    • Development of a Mechanism-Based High-Throughput Screen Assay for Leucine-Rich Repeat Kinase 2 - Discovery of LRRK2 Inhibitors
    • Liu M., Poulose S., Schuman E., et al. Development of a Mechanism-Based High-Throughput Screen Assay for Leucine-Rich Repeat Kinase 2 - Discovery of LRRK2 Inhibitors. Anal. Biochem. 2010 ; 404: 186-192
    • (2010) Anal. Biochem , vol.404 , pp. 186-192
    • Liu, M.1    Poulose, S.2    Schuman, E.3
  • 17
    • 80054979896 scopus 로고    scopus 로고
    • Kinetic, Mechanistic, and Structural Modeling Studies of Truncated Wild-Type Leucine-Rich Repeat Kinase 2 and the G2019S Mutant
    • Liu M., Kang S., Ray S., et al. Kinetic, Mechanistic, and Structural Modeling Studies of Truncated Wild-Type Leucine-Rich Repeat Kinase 2 and the G2019S Mutant. Biochemistry. 2011 ; 50: 9399-9408
    • (2011) Biochemistry , vol.50 , pp. 9399-9408
    • Liu, M.1    Kang, S.2    Ray, S.3
  • 18
    • 0033541662 scopus 로고    scopus 로고
    • Homogeneous Proximity Tyrosine Kinase Assays: Scintillation Proximity Assay versus Homogeneous Time-Resolved Fluorescence
    • Park Y. W., Cummings R. T., Wu L.. Homogeneous Proximity Tyrosine Kinase Assays: Scintillation Proximity Assay versus Homogeneous Time-Resolved Fluorescence. Anal. Biochem. 1999 ; 10: 94-104
    • (1999) Anal. Biochem , vol.10 , pp. 94-104
    • Park, Y.W.1    Cummings, R.T.2    Wu, L.3
  • 19
    • 49449101644 scopus 로고    scopus 로고
    • Kinetic Studies of Cdk5/p25 Kinase: Phosphorylation of Tau and Complex Inhibition by Two Prototype Inhibitors
    • Liu M., Choi S., Cuny G. D., et al. Kinetic Studies of Cdk5/p25 Kinase: Phosphorylation of Tau and Complex Inhibition by Two Prototype Inhibitors. Biochemistry. 2008 ; 47: 8367-8377
    • (2008) Biochemistry , vol.47 , pp. 8367-8377
    • Liu, M.1    Choi, S.2    Cuny, G.D.3
  • 20
    • 84871730931 scopus 로고    scopus 로고
    • Approaches to Discover Non-ATP Site Kinase Inhibitors
    • Gavrin L. K., Saiah E.. Approaches to Discover Non-ATP Site Kinase Inhibitors. Med. Chem. Commun. 2013 ; 4: 41-51
    • (2013) Med. Chem. Commun , vol.4 , pp. 41-51
    • Gavrin, L.K.1    Saiah, E.2
  • 21
    • 84970616541 scopus 로고
    • Alkaloids of the Australian Rutaceae: Pentaceras australis Hook. F. I. Isolation of the Alkaloids and Identification of Canthin-6-One
    • Haynes H. F., Nelson E. R., Price J. R.. Alkaloids of the Australian Rutaceae: Pentaceras australis Hook. F. I. Isolation of the Alkaloids and Identification of Canthin-6-One. Aust. J. Sci. Res. A Phys. Sci. 1952 ; 5: 387-400
    • (1952) Aust. J. Sci. Res. A Phys. Sci , vol.5 , pp. 387-400
    • Haynes, H.F.1    Nelson, E.R.2    Price, J.R.3
  • 22
    • 33847241204 scopus 로고    scopus 로고
    • Beta-Carboline Alkaloids: Biochemical and Pharmacological Functions
    • Cao R., Peng W., Wang Z., et al. Beta-Carboline Alkaloids: Biochemical and Pharmacological Functions. Curr. Med. Chem. 2007 ; 14: 479-500
    • (2007) Curr. Med. Chem , vol.14 , pp. 479-500
    • Cao, R.1    Peng, W.2    Wang, Z.3
  • 23
    • 79959469862 scopus 로고    scopus 로고
    • Synthesis and Cytotoxic Activity of New Beta-Carboline Derivatives
    • Peduto A., More V., de Caprariis P., et al. Synthesis and Cytotoxic Activity of New Beta-Carboline Derivatives. Mini Rev. Med. Chem. 2011 ; 11: 486-491
    • (2011) Mini Rev. Med. Chem , vol.11 , pp. 486-491
    • Peduto, A.1    More, V.2    De Caprariis, P.3
  • 24
    • 84863644419 scopus 로고    scopus 로고
    • Alkaloids from Rutaceae: Activities of Canthin-6-One Alkaloids and Synthetic Analogues on Glioblastoma Stem Cells
    • Cebrian-Torrejon G., Kahn S. A., Ferreira M. E., et al. Alkaloids from Rutaceae: Activities of Canthin-6-One Alkaloids and Synthetic Analogues on Glioblastoma Stem Cells. MedChemComm. 2012 ; 3: 771-774
    • (2012) MedChemComm , vol.3 , pp. 771-774
    • Cebrian-Torrejon, G.1    Kahn, S.A.2    Ferreira, M.E.3
  • 25
    • 33845894735 scopus 로고    scopus 로고
    • Effects of Canthin-6-One Alkaloids from Zanthoxylum chiloperone on Trypanosoma cruzi-Infected Mice
    • Ferreira M. E., Nakayama H., de Arias A. R., et al. Effects of Canthin-6-One Alkaloids from Zanthoxylum chiloperone on Trypanosoma cruzi-Infected Mice. J. Ethnopharmacol. 2007 ; 109: 258-263
    • (2007) J. Ethnopharmacol , vol.109 , pp. 258-263
    • Ferreira, M.E.1    Nakayama, H.2    De Arias, A.R.3
  • 26
    • 33646271827 scopus 로고    scopus 로고
    • 1-Methoxy-Canthin-6-One Induces c-Jun NH2-Terminal Kinase-Dependent Apoptosis and Synergizes with Tumor Necrosis Factor-Related Apoptosis-Inducing Ligand Activity in Human Neoplastic Cells of Hematopoietic or Endodermal Origin
    • Ammirante M., Di Giacomo R., De Martino L., et al. 1-Methoxy-Canthin-6- One Induces c-Jun NH2-Terminal Kinase-Dependent Apoptosis and Synergizes with Tumor Necrosis Factor-Related Apoptosis-Inducing Ligand Activity in Human Neoplastic Cells of Hematopoietic or Endodermal Origin. Cancer Res. 2006 ; 66: 4385-4393
    • (2006) Cancer Res , vol.66 , pp. 4385-4393
    • Ammirante, M.1    Di Giacomo, R.2    De Martino, L.3
  • 27
    • 84866905708 scopus 로고    scopus 로고
    • Discovery of 7-Methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3- dihydro-1H-indol-5-yl)-7H-p yrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a Potent and Selective First-in-Class Inhibitor of Protein Kinase R (PKR)-Like Endoplasmic Reticulum Kinase (PERK)
    • Axten J. M., Medina J. R., Feng Y., et al. Discovery of 7-Methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl) -7H-p yrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a Potent and Selective First-in-Class Inhibitor of Protein Kinase R (PKR)-Like Endoplasmic Reticulum Kinase (PERK). J. Med. Chem. 2012 ; 55: 7193-7207
    • (2012) J. Med. Chem , vol.55 , pp. 7193-7207
    • Axten, J.M.1    Medina, J.R.2    Feng, Y.3
  • 28
    • 84885447174 scopus 로고    scopus 로고
    • Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development
    • Axten J. M., Romeril S. P., Shu A., et al. Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development. ACS Med. Chem. Lett. 2013 ; 4: 964-968
    • (2013) ACS Med. Chem. Lett , vol.4 , pp. 964-968
    • Axten, J.M.1    Romeril, S.P.2    Shu, A.3
  • 29
    • 84875235453 scopus 로고    scopus 로고
    • Characterization of a Novel PERK Kinase Inhibitor with Antitumor and Antiangiogenic Activity
    • Atkins C., Liu Q., Minthorn E., et al. Characterization of a Novel PERK Kinase Inhibitor with Antitumor and Antiangiogenic Activity. Cancer Res. 2013 ; 15: 1993-2002
    • (2013) Cancer Res , vol.15 , pp. 1993-2002
    • Atkins, C.1    Liu, Q.2    Minthorn, E.3
  • 30
    • 77954535031 scopus 로고    scopus 로고
    • PERK Promotes Cancer Cell Proliferation and Tumor Growth by Limiting Oxidative DNA Damage
    • Bobrovnikova-Marjon E., Grigoriadou C., Pytel D., et al. PERK Promotes Cancer Cell Proliferation and Tumor Growth by Limiting Oxidative DNA Damage. Oncogene. 2010 ; 29: 3881-3895
    • (2010) Oncogene , vol.29 , pp. 3881-3895
    • Bobrovnikova-Marjon, E.1    Grigoriadou, C.2    Pytel, D.3
  • 31
    • 27144458505 scopus 로고    scopus 로고
    • ER Stress-Regulated Translation Increases Tolerance to Extreme Hypoxia and Promotes Tumor Growth
    • Bi M., Naczki C., Koritzinsky M., et al. ER Stress-Regulated Translation Increases Tolerance to Extreme Hypoxia and Promotes Tumor Growth. Embo J. 2005 ; 24: 3470-3481
    • (2005) Embo J , vol.24 , pp. 3470-3481
    • Bi, M.1    Naczki, C.2    Koritzinsky, M.3
  • 32
    • 84869391588 scopus 로고    scopus 로고
    • The PERK-eIF2alpha Phosphorylation Arm Is a Pro-Survival Pathway of BCR-ABL Signaling and Confers Resistance to Imatinib Treatment in Chronic Myeloid Leukemia Cells
    • Kusio-Kobialka M., Podszywalow-Bartnicka P., Peidis P., et al. The PERK-eIF2alpha Phosphorylation Arm Is a Pro-Survival Pathway of BCR-ABL Signaling and Confers Resistance to Imatinib Treatment in Chronic Myeloid Leukemia Cells. Cell Cycle. 2012 ; 11: 4069-4078
    • (2012) Cell Cycle , vol.11 , pp. 4069-4078
    • Kusio-Kobialka, M.1    Podszywalow-Bartnicka, P.2    Peidis, P.3
  • 33
    • 24344489466 scopus 로고    scopus 로고
    • The Unfolded Protein Response Is Activated in Alzheimer's Disease
    • Hoozemans J. J., Veerhuis R., Van Haastert E. S., et al. The Unfolded Protein Response Is Activated in Alzheimer's Disease. Acta Neuropathol. 2005 ; 110: 165-172
    • (2005) Acta Neuropathol , vol.110 , pp. 165-172
    • Hoozemans, J.J.1    Veerhuis, R.2    Van Haastert, E.S.3
  • 34
    • 0037147666 scopus 로고    scopus 로고
    • Phosphorylation of Eukaryotic Initiation Factor-2alpha (eIF2alpha) Is Associated with Neuronal Degeneration in Alzheimer's Disease
    • Chang R. C., Wong A. K., Ng H. K., et al. Phosphorylation of Eukaryotic Initiation Factor-2alpha (eIF2alpha) Is Associated with Neuronal Degeneration in Alzheimer's Disease. Neuroreport. 2002 ; 13: 2429-2432
    • (2002) Neuroreport , vol.13 , pp. 2429-2432
    • Chang, R.C.1    Wong, A.K.2    Ng, H.K.3
  • 35
    • 0033777547 scopus 로고    scopus 로고
    • Axonal and Neuronal Amyloid Precursor Protein Immunoreactivity in the Brains of Guinea Pigs Given Tunicamycin
    • Finnie J. W., Manavis J., Blumbergs P. C., et al. Axonal and Neuronal Amyloid Precursor Protein Immunoreactivity in the Brains of Guinea Pigs Given Tunicamycin. Vet. Pathol. 2000 ; 37: 677-680
    • (2000) Vet. Pathol , vol.37 , pp. 677-680
    • Finnie, J.W.1    Manavis, J.2    Blumbergs, P.C.3


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