메뉴 건너뛰기




Volumn 133, Issue 3, 2015, Pages 440-451

A novel DYRK1A (Dual specificity tyrosine phosphorylation-regulated kinase 1A) inhibitor for the treatment of Alzheimer's disease: Effect on Tau and amyloid pathologies in vitro

Author keywords

Alzheimer's disease; amyloid precursor, protein; DYRK1A; EHT 5372; kinase; Tau

Indexed keywords

AMYLOID BETA PROTEIN; METHYL 9 (2,4 DICHLOROPHENYLAMINO) THIAZOLO[5,4 F]QUINAZOLINE 2 CARBIMIDATE; PHOSPHOTRANSFERASE INHIBITOR; TAU PROTEIN; UNCLASSIFIED DRUG; DYRK KINASE; PROTEIN KINASE INHIBITOR; PROTEIN SERINE THREONINE KINASE; PROTEIN TYROSINE KINASE;

EID: 84927129691     PISSN: 00223042     EISSN: 14714159     Source Type: Journal    
DOI: 10.1111/jnc.13018     Document Type: Article
Times cited : (96)

References (46)
  • 1
    • 0036937699 scopus 로고    scopus 로고
    • Specific tau phosphorylation sites correlate with severity of neuronal cytopathology in Alzheimer's disease
    • Augustinack J. C., Schneider A., Mandelkow E. M., and, Hyman B. T., (2002) Specific tau phosphorylation sites correlate with severity of neuronal cytopathology in Alzheimer's disease. Acta Neuropathol. 103, 26-35.
    • (2002) Acta Neuropathol. , vol.103 , pp. 26-35
    • Augustinack, J.C.1    Schneider, A.2    Mandelkow, E.M.3    Hyman, B.T.4
  • 2
    • 76749101192 scopus 로고    scopus 로고
    • High-content siRNA screening of the kinome identifies kinases involved in Alzheimer's disease-related tau hyperphosphorylation
    • Azorsa D. O., Robeson R. H., Frost D., et al,. (2010) High-content siRNA screening of the kinome identifies kinases involved in Alzheimer's disease-related tau hyperphosphorylation. BMC Genom. 12, 11-25.
    • (2010) BMC Genom , vol.12 , pp. 11-25
    • Azorsa, D.O.1    Robeson, R.H.2    Frost, D.3
  • 3
    • 34548036227 scopus 로고    scopus 로고
    • Tau-mediated neurodegeneration in Alzheimer's disease and related disorders
    • Ballatore C., Lee V. M., and, Trojanowski J. Q., (2007) Tau-mediated neurodegeneration in Alzheimer's disease and related disorders. Nat. Rev. Neurosci. 8, 663-672.
    • (2007) Nat. Rev. Neurosci. , vol.8 , pp. 663-672
    • Ballatore, C.1    Lee, V.M.2    Trojanowski, J.Q.3
  • 4
    • 0032475973 scopus 로고    scopus 로고
    • Sequence characteristics, subcellular localization, and substrate specificity of DYRK-related kinases, a novel family of dual specificity protein kinases
    • Becker W., Weber Y., Wetzel K., Eirmbter K., Tejedor F. J., and, Joost H. G., (1998) Sequence characteristics, subcellular localization, and substrate specificity of DYRK-related kinases, a novel family of dual specificity protein kinases. J. Biol. Chem. 273, 25893-25902.
    • (1998) J. Biol. Chem. , vol.273 , pp. 25893-25902
    • Becker, W.1    Weber, Y.2    Wetzel, K.3    Eirmbter, K.4    Tejedor, F.J.5    Joost, H.G.6
  • 5
    • 84896716499 scopus 로고    scopus 로고
    • DYRK1A: A potential drug target for multiple down syndrome neuropathologies
    • Becker W., Soppa U., and, Tejedor F. J., (2014) DYRK1A: a potential drug target for multiple down syndrome neuropathologies. CNS Neurol. Disord. Drug Targets. 13, 26-33.
    • (2014) CNS Neurol. Disord. Drug Targets. , vol.13 , pp. 26-33
    • Becker, W.1    Soppa, U.2    Tejedor, F.J.3
  • 6
    • 0025863618 scopus 로고
    • Neuropathological stageing of Alzheimer-related changes
    • Braak H., and, Braak E., (1991) Neuropathological stageing of Alzheimer-related changes. Acta Neuropathol. 82, 239-259.
    • (1991) Acta Neuropathol. , vol.82 , pp. 239-259
    • Braak, H.1    Braak, E.2
  • 7
    • 84861914969 scopus 로고    scopus 로고
    • Neurotoxicity and memory deficits induced by soluble low-molecular-weight amyloid-β1-42 oligomers are revealed in vivo by using a novel animal model
    • Brouillette J., Caillierez R., Zommer N., Alves-Pires C., Benilova I., Blum D., De Strooper B., and, Buée L., (2012) Neurotoxicity and memory deficits induced by soluble low-molecular-weight amyloid-β1-42 oligomers are revealed in vivo by using a novel animal model. J. Neurosci. 32, 7852-7861.
    • (2012) J. Neurosci. , vol.32 , pp. 7852-7861
    • Brouillette, J.1    Caillierez, R.2    Zommer, N.3    Alves-Pires, C.4    Benilova, I.5    Blum, D.6    De Strooper, B.7    Buée, L.8
  • 8
    • 84893373889 scopus 로고    scopus 로고
    • Epigallocatechin-3-gallate, a DYRK1A inhibitor, rescues cognitive deficits in Down syndrome mouse models and in humans
    • De la Torre R., De Sola S., Pons M., et al,. (2014) Epigallocatechin-3-gallate, a DYRK1A inhibitor, rescues cognitive deficits in Down syndrome mouse models and in humans. Mol. Nutr. Food Res. 58, 278-288.
    • (2014) Mol. Nutr. Food Res. , vol.58 , pp. 278-288
    • De La Torre, R.1    De Sola, S.2    Pons, M.3
  • 9
    • 79959406830 scopus 로고    scopus 로고
    • Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B. Modulation of alternative pre-RNA splicing
    • Debdab M., Carreaux F., Renault S., et al,. (2011) Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B. Modulation of alternative pre-RNA splicing. J. Med. Chem. 54, 4172-4186.
    • (2011) J. Med. Chem. , vol.54 , pp. 4172-4186
    • Debdab, M.1    Carreaux, F.2    Renault, S.3
  • 10
    • 26944433068 scopus 로고    scopus 로고
    • Constitutive Dyrk1A is abnormally expressed in Alzheimer disease, Down syndrome, Pick disease, and related transgenic models
    • Ferrer I., Barrachina M., Puig B., Martínez de Lagrán M., Martí E., Avila J., and, Dierssen M., (2005) Constitutive Dyrk1A is abnormally expressed in Alzheimer disease, Down syndrome, Pick disease, and related transgenic models. Neurobiol. Dis. 20, 392-400.
    • (2005) Neurobiol. Dis. , vol.20 , pp. 392-400
    • Ferrer, I.1    Barrachina, M.2    Puig, B.3    Martínez De Lagrán, M.4    Martí, E.5    Avila, J.6    Dierssen, M.7
  • 11
    • 34948848556 scopus 로고    scopus 로고
    • Mirk/Dyrk1B in cancer
    • Friedman E., (2007) Mirk/Dyrk1B in cancer. J. Cell. Biochem. 102, 274-279.
    • (2007) J. Cell. Biochem. , vol.102 , pp. 274-279
    • Friedman, E.1
  • 12
    • 79955827792 scopus 로고    scopus 로고
    • β-carboline compounds, including harmine, inhibit DYRK1A and tau phosphorylation at multiple Alzheimer's disease-related sites
    • Frost D., Meechoovet B., Wang T., Gately S., Giorgetti M., Shcherbakova I., and, Dunckley T., (2011) β-carboline compounds, including harmine, inhibit DYRK1A and tau phosphorylation at multiple Alzheimer's disease-related sites. PLoS ONE 6, e19264.
    • (2011) PLoS ONE , vol.6 , pp. e19264
    • Frost, D.1    Meechoovet, B.2    Wang, T.3    Gately, S.4    Giorgetti, M.5    Shcherbakova, I.6    Dunckley, T.7
  • 13
    • 70349947061 scopus 로고    scopus 로고
    • Harmine specifically inhibits protein kinase DYRK1A and interferes with neurite formation
    • Göckler N., Jofre G., Papadopoulos C., Soppa U., Tejedor F. J., and, Becker W., (2009) Harmine specifically inhibits protein kinase DYRK1A and interferes with neurite formation. FEBS J. 276, 6324-6337.
    • (2009) FEBS J. , vol.276 , pp. 6324-6337
    • Göckler, N.1    Jofre, G.2    Papadopoulos, C.3    Soppa, U.4    Tejedor, F.J.5    Becker, W.6
  • 14
    • 0022744803 scopus 로고
    • Abnormal phosphorylation of the microtubule-associated protein tau (tau) in Alzheimer cytoskeletal pathology
    • Grundke-Iqbal I., Iqbal K., Tung Y.C., Quinlan M., Wisniewski H.M., and, Binder L.I., (1986) Abnormal phosphorylation of the microtubule-associated protein tau (tau) in Alzheimer cytoskeletal pathology. Proc. Natl Acad. Sci. USA 83, 4913-4917.
    • (1986) Proc. Natl Acad. Sci. USA , vol.83 , pp. 4913-4917
    • Grundke-Iqbal, I.1    Iqbal, K.2    Tung, Y.C.3    Quinlan, M.4    Wisniewski, H.M.5    Binder, L.I.6
  • 15
    • 84864280635 scopus 로고    scopus 로고
    • Green tea polyphenols rescue of brain defects induced by overexpression of DYRK1A
    • Guedj F., Sébrié C., Rivals I., et al,. (2009) Green tea polyphenols rescue of brain defects induced by overexpression of DYRK1A. PLoS ONE 4, e4606.
    • (2009) PLoS ONE , vol.4 , pp. e4606
    • Guedj, F.1    Sébrié, C.2    Rivals, I.3
  • 16
    • 77955322042 scopus 로고    scopus 로고
    • Dendritic function of tau mediates amyloid-beta toxicity in Alzheimer's disease mouse models
    • Ittner L. M., Ke Y. D., Delerue F., et al,. (2010) Dendritic function of tau mediates amyloid-beta toxicity in Alzheimer's disease mouse models. Cell 142, 387-397.
    • (2010) Cell , vol.142 , pp. 387-397
    • Ittner, L.M.1    Ke, Y.D.2    Delerue, F.3
  • 17
    • 33846533244 scopus 로고    scopus 로고
    • The DYRK1A gene, encoded in chromosome 21 Down syndrome critical region, bridges between beta-amyloid production and tau phosphorylation in Alzheimer disease
    • Kimura R., Kamino K., Yamamoto M., et al,. (2007) The DYRK1A gene, encoded in chromosome 21 Down syndrome critical region, bridges between beta-amyloid production and tau phosphorylation in Alzheimer disease. Hum. Mol. Genet. 16, 15-23.
    • (2007) Hum. Mol. Genet. , vol.16 , pp. 15-23
    • Kimura, R.1    Kamino, K.2    Yamamoto, M.3
  • 22
    • 0021338217 scopus 로고    scopus 로고
    • Phosphorylation affects the ability of tau protein to promote microtubule assembly
    • Lindwall G., and, Cole R. D., (1999) Phosphorylation affects the ability of tau protein to promote microtubule assembly. J. Biol. Chem. 259, 5301-5305.
    • (1999) J. Biol. Chem. , vol.259 , pp. 5301-5305
    • Lindwall, G.1    Cole, R.D.2
  • 24
  • 28
    • 70350512022 scopus 로고    scopus 로고
    • Function and regulation of Dyrk1A: Towards understanding Down syndrome
    • Park J., Song W. J., and, Chung K. C., (2009) Function and regulation of Dyrk1A: towards understanding Down syndrome. Cell. Mol. Life Sci. 66, 3235-3240.
    • (2009) Cell. Mol. Life Sci. , vol.66 , pp. 3235-3240
    • Park, J.1    Song, W.J.2    Chung, K.C.3
  • 29
    • 64049093215 scopus 로고    scopus 로고
    • Molecular targets of (-)-epigallocatechin-3-gallate (EGCG): Specificity and interaction with membrane lipid rafts. J
    • Patra S. K., Rizzi F., Silva A., Rugina D. O., and, Bettuzzi S., (2008) Molecular targets of (-)-epigallocatechin-3-gallate (EGCG): specificity and interaction with membrane lipid rafts. J. Physiol. Pharmacol. 59, 217-235.
    • (2008) Physiol. Pharmacol. , vol.59 , pp. 217-235
    • Patra, S.K.1    Rizzi, F.2    Silva, A.3    Rugina, D.O.4    Bettuzzi, S.5
  • 32
  • 33
    • 36849075621 scopus 로고    scopus 로고
    • DYRK1A-mediated hyperphosphorylation of Tau. A functional link between Down syndrome and Alzheimer disease
    • Ryoo S. R., Jeong H. K., Radnaabazar C., et al,. (2007) DYRK1A-mediated hyperphosphorylation of Tau. A functional link between Down syndrome and Alzheimer disease. J. Biol. Chem. 282, 34850-34857.
    • (2007) J. Biol. Chem. , vol.282 , pp. 34850-34857
    • Ryoo, S.R.1    Jeong, H.K.2    Radnaabazar, C.3
  • 34
    • 39749196069 scopus 로고    scopus 로고
    • Dual-specificity tyrosine(Y)-phosphorylation regulated kinase 1A-mediated phosphorylation of amyloid precursor protein: Evidence for a functional link between Down syndrome and Alzheimer's disease
    • Ryoo S. R., Cho H. J., Lee H. W., et al,. (2008) Dual-specificity tyrosine(Y)-phosphorylation regulated kinase 1A-mediated phosphorylation of amyloid precursor protein: evidence for a functional link between Down syndrome and Alzheimer's disease. J. Neurochem. 104, 1333-1344.
    • (2008) J. Neurochem. , vol.104 , pp. 1333-1344
    • Ryoo, S.R.1    Cho, H.J.2    Lee, H.W.3
  • 35
  • 36
    • 43449128899 scopus 로고    scopus 로고
    • Biochemistry of Tau in Alzheimer's disease and related neurological disorders
    • Sergeant N., Bretteville A., Hamdane M., et al,. (2008) Biochemistry of Tau in Alzheimer's disease and related neurological disorders. Expert Rev. Proteomics 5, 207-224.
    • (2008) Expert Rev. Proteomics , vol.5 , pp. 207-224
    • Sergeant, N.1    Bretteville, A.2    Hamdane, M.3
  • 37
    • 57649134248 scopus 로고    scopus 로고
    • Increased dosage of Dyrk1A alters alternative splicing factor (ASF)-regulated alternative splicing of tau in Down syndrome
    • Shi J., Zhang T., Zhou C., et al,. (2008) Increased dosage of Dyrk1A alters alternative splicing factor (ASF)-regulated alternative splicing of tau in Down syndrome. J. Biol. Chem. 283, 28660-28669.
    • (2008) J. Biol. Chem. , vol.283 , pp. 28660-28669
    • Shi, J.1    Zhang, T.2    Zhou, C.3
  • 38
    • 84869782889 scopus 로고    scopus 로고
    • Recent advances in the design, synthesis, and biological evaluation of selective DYRK1A inhibitors: A new avenue for a disease modifying treatment of Alzheimer's? ACS Chem
    • Smith B., Medda F., Gokhale V., Dunckley T., and, Hulme C., (2012) Recent advances in the design, synthesis, and biological evaluation of selective DYRK1A inhibitors: a new avenue for a disease modifying treatment of Alzheimer's? ACS Chem. Neurosci. 3, 857-872.
    • (2012) Neurosci. , vol.3 , pp. 857-872
    • Smith, B.1    Medda, F.2    Gokhale, V.3    Dunckley, T.4    Hulme, C.5
  • 39
    • 84868530112 scopus 로고    scopus 로고
    • Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B
    • Tahtouh T., Elkins J. M., Filippakopoulos P., et al,. (2012a) Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. J. Med. Chem. 55, 9312-9330.
    • (2012) J. Med. Chem. , vol.55 , pp. 9312-9330
    • Tahtouh, T.1    Elkins, J.M.2    Filippakopoulos, P.3
  • 40
  • 41
    • 73249117681 scopus 로고    scopus 로고
    • DYRK1A genetic variants are not linked to Alzheimer's disease in a Spanish case-control cohort
    • Vázquez-Higuera J. L., Sánchez-Juan P., Rodríguez-Rodríguez E., et al,. (2009) DYRK1A genetic variants are not linked to Alzheimer's disease in a Spanish case-control cohort. BMC Med. Genet. 10, 129.
    • (2009) BMC Med. Genet. , vol.10 , pp. 129
    • Vázquez-Higuera, J.L.1    Sánchez-Juan, P.2    Rodríguez-Rodríguez, E.3
  • 42
    • 26944497892 scopus 로고    scopus 로고
    • Phosphorylation of amyloid precursor carboxy-terminal fragments enhances their processing by a gamma-secretase-dependent mechanism
    • Vingtdeux V., Hamdane M., Gompel M., et al,. (2005) Phosphorylation of amyloid precursor carboxy-terminal fragments enhances their processing by a gamma-secretase-dependent mechanism. Neurobiol. Dis. 20, 625-637.
    • (2005) Neurobiol. Dis. , vol.20 , pp. 625-637
    • Vingtdeux, V.1    Hamdane, M.2    Gompel, M.3
  • 43
    • 84872551783 scopus 로고    scopus 로고
    • Abnormal hyperphosphorylation of tau: Sites, regulation, and molecular mechanism of neurofibrillary degeneration
    • Wang J. Z., Xia Y. Y., Grundke-Iqbal I., and, Iqbal K., (2013) Abnormal hyperphosphorylation of tau: sites, regulation, and molecular mechanism of neurofibrillary degeneration. J. Alzheimers Dis. S1, S123-S139.
    • (2013) J. Alzheimers Dis. , vol.1 S , pp. S123-S139
    • Wang, J.Z.1    Xia, Y.Y.2    Grundke-Iqbal, I.3    Iqbal, K.4
  • 44
    • 51849158177 scopus 로고    scopus 로고
    • The role of overexpressed DYRK1A protein in the early onset of neurofibrillary degeneration in Down syndrome
    • Wegiel J., Dowjat K., Kaczmarski W., et al,. (2008) The role of overexpressed DYRK1A protein in the early onset of neurofibrillary degeneration in Down syndrome. Acta Neuropathol. 116, 391-394.
    • (2008) Acta Neuropathol. , vol.116 , pp. 391-394
    • Wegiel, J.1    Dowjat, K.2    Kaczmarski, W.3
  • 45
    • 78651061790 scopus 로고    scopus 로고
    • The role of DYRK1A in neurodegenerative diseases
    • Wegiel J., Gong C. X., and, Hwang Y. W., (2011) The role of DYRK1A in neurodegenerative diseases. FEBS J. 278, 236-245.
    • (2011) FEBS J. , vol.278 , pp. 236-245
    • Wegiel, J.1    Gong, C.X.2    Hwang, Y.W.3
  • 46
    • 0035340295 scopus 로고    scopus 로고
    • The kinase DYRK phosphorylates protein-synthesis initiation factor eIF2Bepsilon at Ser539 and the microtubule-associated protein tau at Thr212: Potential role for DYRK as a glycogen synthase kinase 3-priming kinase
    • Woods Y. L., Cohen P., Becker W., Jakes R., Goedert M., Wang X., and, Proud C. G., (2001) The kinase DYRK phosphorylates protein-synthesis initiation factor eIF2Bepsilon at Ser539 and the microtubule-associated protein tau at Thr212: potential role for DYRK as a glycogen synthase kinase 3-priming kinase. Biochem. J. 355, 609-615.
    • (2001) Biochem. J. , vol.355 , pp. 609-615
    • Woods, Y.L.1    Cohen, P.2    Becker, W.3    Jakes, R.4    Goedert, M.5    Wang, X.6    Proud, C.G.7


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.