메뉴 건너뛰기




Volumn 21, Issue 2, 2016, Pages 145-155

A High-Throughput Screen to Identify LRRK2 Kinase Inhibitors for the Treatment of Parkinson's Disease Using RapidFire Mass Spectrometry

Author keywords

LRRK2; LRRKtide; mass spectrometry; Parkinson's disease; RapidFire

Indexed keywords

ADENOSINE DIPHOSPHATE; ADENOSINE TRIPHOSPHATE; DIMETHYL SULFOXIDE; GUANOSINE TRIPHOSPHATASE; LEUCINE RICH REPEAT KINASE 2; LEUCINE RICH REPEAT KINASE 2 INHIBITOR; PROTEIN KINASE INHIBITOR; UNCLASSIFIED DRUG; COMPLEMENTARY DNA; LRRK2 PROTEIN, HUMAN; PROTEIN SERINE THREONINE KINASE;

EID: 84954506599     PISSN: 10870571     EISSN: 1552454X     Source Type: Journal    
DOI: 10.1177/1087057115606707     Document Type: Article
Times cited : (35)

References (38)
  • 1
    • 8844266996 scopus 로고    scopus 로고
    • Cloning of the Gene Containing Mutations That Cause PARK8-Linked Parkinson's Disease
    • Paisan-Ruiz C., Jain S., Whitney Evans E., et al. Cloning of the Gene Containing Mutations That Cause PARK8-Linked Parkinson's Disease. Neuron 2004, 44, 595-600.
    • (2004) Neuron , vol.44 , pp. 595-600
    • Paisan-Ruiz, C.1    Jain, S.2    Whitney Evans, E.3
  • 2
    • 33646538477 scopus 로고    scopus 로고
    • Leucine-Rich Repeat Kinase 2: Relevance to Parkinson's Disease
    • Guo L., Wang W., Chen S. G., Leucine-Rich Repeat Kinase 2: Relevance to Parkinson's Disease. Int. J. Biochem. Cell Biol. 2006, 38, 1469-1475.
    • (2006) Int. J. Biochem. Cell Biol , vol.38 , pp. 1469-1475
    • Guo, L.1    Wang, W.2    Chen, S.G.3
  • 4
    • 33646151866 scopus 로고    scopus 로고
    • LRRK2 in Parkinson's Disease: Protein Domains and Functional Insights
    • Mata I., Wedemeyer W., Farrer M., et al. LRRK2 in Parkinson's Disease: Protein Domains and Functional Insights. Trends Neurosci. 2006, 29, 286-293.
    • (2006) Trends Neurosci , vol.29 , pp. 286-293
    • Mata, I.1    Wedemeyer, W.2    Farrer, M.3
  • 5
    • 33748876153 scopus 로고    scopus 로고
    • The LRRK2-G2019S Mutation: Opening a Novel Era in Parkinson's Disease Genetics
    • Bonifati V., The LRRK2-G2019S Mutation: Opening a Novel Era in Parkinson's Disease Genetics. Eur. J. Hum. Genet. 2006, 14, 1061-1062.
    • (2006) Eur. J. Hum. Genet , vol.14 , pp. 1061-1062
    • Bonifati, V.1
  • 6
    • 84969416832 scopus 로고    scopus 로고
    • Clinicogenetics of Parkinson's Disease: A Drawing but Not Completed Picture
    • Wang C. D., Chan P., Clinicogenetics of Parkinson's Disease: A Drawing but Not Completed Picture. Neuroimmunol. Neuroinflammation 2014, 1, 115-126.
    • (2014) Neuroimmunol. Neuroinflammation , vol.1 , pp. 115-126
    • Wang, C.D.1    Chan, P.2
  • 7
    • 28044460070 scopus 로고    scopus 로고
    • Parkinson's Disease-Associated Mutations in Leucine-Rich Repeat Kinase 2 Augment Kinase Activity
    • West A., Moore D., Biskup S., et al. Parkinson's Disease-Associated Mutations in Leucine-Rich Repeat Kinase 2 Augment Kinase Activity. Proc. Natl. Acad. Sci. U. S. A. 2005, 102, 16842-16847.
    • (2005) Proc. Natl. Acad. Sci. U. S. A , vol.102 , pp. 16842-16847
    • West, A.1    Moore, D.2    Biskup, S.3
  • 8
    • 77956441086 scopus 로고    scopus 로고
    • Inhibitors of Leucine-Rich Repeat Kinase-2 Protect against Models of Parkinson's Disease
    • Lee B., Shin J. H., VanKampen J., et al. Inhibitors of Leucine-Rich Repeat Kinase-2 Protect against Models of Parkinson's Disease. Nat. Med 2010, 16, 998-1000.
    • (2010) Nat. Med , vol.16 , pp. 998-1000
    • Lee, B.1    Shin, J.H.2    VanKampen, J.3
  • 9
    • 84869830250 scopus 로고    scopus 로고
    • Leucine-Rich Repeat Kinase 2 Inhibitors: A Patent Review (2006-2011)
    • Deng X., Choi H., Buhrlage S., et al. Leucine-Rich Repeat Kinase 2 Inhibitors: A Patent Review (2006-2011). Expert Opin. Ther. Patents 2012, 22, 1415-1426.
    • (2012) Expert Opin. Ther. Patents , vol.22 , pp. 1415-1426
    • Deng, X.1    Choi, H.2    Buhrlage, S.3
  • 10
    • 84925854124 scopus 로고    scopus 로고
    • CNS Drug Design: Balancing Physicochemical Properties for Optimal Brain Exposure
    • Rankovic Z., CNS Drug Design: Balancing Physicochemical Properties for Optimal Brain Exposure. J. Med. Chem. 2015, 58, 2584-2608.
    • (2015) J. Med. Chem , vol.58 , pp. 2584-2608
    • Rankovic, Z.1
  • 11
    • 70350747591 scopus 로고    scopus 로고
    • Targeting Protein Kinases in Central Nervous System Disorders
    • Chico L. K., Van Eldik L. J., Watterson D. M., Targeting Protein Kinases in Central Nervous System Disorders. Nat. Rev. Drug. Discov. 2009, 8, 892-909.
    • (2009) Nat. Rev. Drug. Discov , vol.8 , pp. 892-909
    • Chico, L.K.1    Van Eldik, L.J.2    Watterson, D.M.3
  • 12
    • 34447118788 scopus 로고    scopus 로고
    • LRRK2 Phosphorylates Moesin at Threonine-558: Characterisation of How Parkinson's Disease Mutants Affect Kinase Activity
    • Jaleel M., Nichols J., Deak M., et al. LRRK2 Phosphorylates Moesin at Threonine-558: Characterisation of How Parkinson's Disease Mutants Affect Kinase Activity. Biochem. J. 2007, 405, 307-317.
    • (2007) Biochem. J , vol.405 , pp. 307-317
    • Jaleel, M.1    Nichols, J.2    Deak, M.3
  • 13
    • 70350653779 scopus 로고    scopus 로고
    • Substrate Specificity and Inhibitors of LRRK2, a Protein Kinase Mutated in Parkinson's Disease
    • Nichols J., Dzamko N., Hutti J., et al. Substrate Specificity and Inhibitors of LRRK2, a Protein Kinase Mutated in Parkinson's Disease. Biochem. J. 2009, 424, 47-60.
    • (2009) Biochem. J , vol.424 , pp. 47-60
    • Nichols, J.1    Dzamko, N.2    Hutti, J.3
  • 14
    • 77954088674 scopus 로고    scopus 로고
    • Development of a High-Throughput AlphaScreen Assay Measuring Full-Length LRRK2(G2019S) Kinase Activity Using Moesin Protein Substrate
    • Pedro L., Padrós J., Beaudet L., et al. Development of a High-Throughput AlphaScreen Assay Measuring Full-Length LRRK2(G2019S) Kinase Activity Using Moesin Protein Substrate. Anal. Biochem. 2010, 404, 45-51.
    • (2010) Anal. Biochem , vol.404 , pp. 45-51
    • Pedro, L.1    Padrós, J.2    Beaudet, L.3
  • 15
    • 84911363804 scopus 로고    scopus 로고
    • Unique Functional and Structural Properties of the LRRK2 Protein ATP-Binding Pocket
    • Liu Z., Galemmo R., Fraser K., et al. Unique Functional and Structural Properties of the LRRK2 Protein ATP-Binding Pocket. J. Biol. Chem. 2014, 289, 32937-32951.
    • (2014) J. Biol. Chem , vol.289 , pp. 32937-32951
    • Liu, Z.1    Galemmo, R.2    Fraser, K.3
  • 16
    • 84865515027 scopus 로고    scopus 로고
    • Screening for Novel LRRK2 Inhibitors Using a High-Throughput TR-FRET Cellular Assay for LRRK2 Ser935 Phosphorylation
    • Hermanson S., Carlson C., Riddle S., et al. Screening for Novel LRRK2 Inhibitors Using a High-Throughput TR-FRET Cellular Assay for LRRK2 Ser935 Phosphorylation. PLoS ONE 2012, 7, e43580.
    • (2012) PLoS ONE , vol.7 , pp. e43580
    • Hermanson, S.1    Carlson, C.2    Riddle, S.3
  • 17
    • 45949106612 scopus 로고    scopus 로고
    • The Challenge of Selecting Protein Kinase Assays for Lead Discovery Optimisation
    • Ma H., Deacon S., Horiuchi K., The Challenge of Selecting Protein Kinase Assays for Lead Discovery Optimisation. Expert Opin. Drug Discov. 2008, 3, 607-621.
    • (2008) Expert Opin. Drug Discov , vol.3 , pp. 607-621
    • Ma, H.1    Deacon, S.2    Horiuchi, K.3
  • 18
    • 72749105819 scopus 로고    scopus 로고
    • Identification of the Autophosphorylation Sites of LRRK2
    • Kamikawaji S., Ito G., Iwatsubo T., Identification of the Autophosphorylation Sites of LRRK2. Biochemistry 2009, 48, 10963-10975.
    • (2009) Biochemistry , vol.48 , pp. 10963-10975
    • Kamikawaji, S.1    Ito, G.2    Iwatsubo, T.3
  • 19
    • 77956655427 scopus 로고    scopus 로고
    • Inhibition of LRRK2 Kinase Activity Leads to Dephosphorylation of Ser910/Ser935, Disruption of 14-3-3 Binding and Altered Cytoplasmic Localization
    • Dzamko N., Deak M., Hentati F., et al. Inhibition of LRRK2 Kinase Activity Leads to Dephosphorylation of Ser910/Ser935, Disruption of 14-3-3 Binding and Altered Cytoplasmic Localization. Biochem. J. 2010, 430, 405-413.
    • (2010) Biochem. J , vol.430 , pp. 405-413
    • Dzamko, N.1    Deak, M.2    Hentati, F.3
  • 20
    • 79952302007 scopus 로고    scopus 로고
    • Phosphorylation-Dependent 14-3-3 Binding to LRRK2 Is Impaired by Common Mutations of Familial Parkinson's Disease
    • Li X., Wang Q. J., Pan N., et al. Phosphorylation-Dependent 14-3-3 Binding to LRRK2 Is Impaired by Common Mutations of Familial Parkinson's Disease. PLoS ONE 2011, 6, e17153.
    • (2011) PLoS ONE , vol.6 , pp. e17153
    • Li, X.1    Wang, Q.J.2    Pan, N.3
  • 21
    • 84900455031 scopus 로고    scopus 로고
    • Identification of Small-Molecule Frequent Hitters from AlphaScreen High-Throughput Screens
    • Schorpp K., Rothenaigner I., Salmina E., et al. Identification of Small-Molecule Frequent Hitters from AlphaScreen High-Throughput Screens. J. Biomol. Screen. 2014, 19, 715-726.
    • (2014) J. Biomol. Screen , vol.19 , pp. 715-726
    • Schorpp, K.1    Rothenaigner, I.2    Salmina, E.3
  • 22
    • 84899889585 scopus 로고    scopus 로고
    • Structural Biology of the LRRK2 GTPase and Kinase Domains: Implications for Regulation
    • Gilsbach B., Kortholt A., Structural Biology of the LRRK2 GTPase and Kinase Domains: Implications for Regulation. Front. Mol. Neurosci. 2014, 7, 32.
    • (2014) Front. Mol. Neurosci , vol.7 , pp. 32
    • Gilsbach, B.1    Kortholt, A.2
  • 23
    • 77954197844 scopus 로고    scopus 로고
    • Membrane Localisation of LRRK2 Is Associated with Increased Formation of the Highly Active LRRK2 Dimer and Changes in Its Phosphorylation
    • Berger Z., Smith K., LaVoie J., Membrane Localisation of LRRK2 Is Associated with Increased Formation of the Highly Active LRRK2 Dimer and Changes in Its Phosphorylation. Biochemistry 2010, 49, 5511-5523.
    • (2010) Biochemistry , vol.49 , pp. 5511-5523
    • Berger, Z.1    Smith, K.2    LaVoie, J.3
  • 24
    • 79951961104 scopus 로고    scopus 로고
    • High-Throughput Screening Assay for Sphingosine Kinase Inhibitors in Whole Blood Using RapidFire Mass Spectrometry
    • Highkin M., Yates M., Nemirovskiy O., et al. High-Throughput Screening Assay for Sphingosine Kinase Inhibitors in Whole Blood Using RapidFire Mass Spectrometry. J. Biomol. Screen. 2011, 16, 272-277.
    • (2011) J. Biomol. Screen , vol.16 , pp. 272-277
    • Highkin, M.1    Yates, M.2    Nemirovskiy, O.3
  • 25
    • 84861809953 scopus 로고    scopus 로고
    • Enabling Lead Discovery for Histone Lysine Demethylases by High-Throughput RapidFire Mass Spectrometry
    • Hutchinson S., Leveridge M., Heathcote M., et al. Enabling Lead Discovery for Histone Lysine Demethylases by High-Throughput RapidFire Mass Spectrometry. J. Biomol. Screen. 2012, 17, 39-48.
    • (2012) J. Biomol. Screen , vol.17 , pp. 39-48
    • Hutchinson, S.1    Leveridge, M.2    Heathcote, M.3
  • 26
    • 84856134589 scopus 로고    scopus 로고
    • Lead-Oriented Synthesis: A New Opportunity for Synthetic Chemistry
    • Nadin A., Hattotuwagama C., Churcher I., Lead-Oriented Synthesis: A New Opportunity for Synthetic Chemistry. Angew. Chem. Int. Ed. 2012, 51, 1114-1122.
    • (2012) Angew. Chem. Int. Ed , vol.51 , pp. 1114-1122
    • Nadin, A.1    Hattotuwagama, C.2    Churcher, I.3
  • 27
    • 71049126548 scopus 로고    scopus 로고
    • Escape from Flatland: Increasing Saturation as an Approach to Improving Clinical Success
    • Lovering F., Bikker J., Humblet C., Escape from Flatland: Increasing Saturation as an Approach to Improving Clinical Success. J. Med. Chem. 2009, 52, 6752-6756.
    • (2009) J. Med. Chem , vol.52 , pp. 6752-6756
    • Lovering, F.1    Bikker, J.2    Humblet, C.3
  • 28
    • 80052844344 scopus 로고    scopus 로고
    • Getting Physical in Drug Discovery II: The Impact of Chromatographic Hydrophobicity Measurements and Aromaticity
    • Young R. J., Green D. V. S., Luscombe C. N., et al. Getting Physical in Drug Discovery II: The Impact of Chromatographic Hydrophobicity Measurements and Aromaticity. Drug Discov. Today 2011, 16, 822-830.
    • (2011) Drug Discov. Today , vol.16 , pp. 822-830
    • Young, R.J.1    Green, D.V.S.2    Luscombe, C.N.3
  • 29
    • 84908530414 scopus 로고    scopus 로고
    • Chemical Con Artists Foil Drug Discovery
    • Baell J. B., Walters M. A., Chemical Con Artists Foil Drug Discovery. Nature 2014, 513, 481-483.
    • (2014) Nature , vol.513 , pp. 481-483
    • Baell, J.B.1    Walters, M.A.2
  • 30
    • 58149158022 scopus 로고    scopus 로고
    • Investigation of Leucine-Rich Repeat Kinase 2: Enzymological Properties and Novel Assays
    • Anand V. S., Reichling L. J., Lipinski K., et al. Investigation of Leucine-Rich Repeat Kinase 2: Enzymological Properties and Novel Assays. FEBS J. 2009, 276, 466-478.
    • (2009) FEBS J , vol.276 , pp. 466-478
    • Anand, V.S.1    Reichling, L.J.2    Lipinski, K.3
  • 31
    • 79952918505 scopus 로고    scopus 로고
    • Characterisation of a Selective Inhibitor of the Parkinson's Disease Kinase LRRK2
    • Deng X., Dzamko N., Prescott A., et al. Characterisation of a Selective Inhibitor of the Parkinson's Disease Kinase LRRK2. Nat. Chem. Biol. 201l, 7, 203-205.
    • (2011) Nat. Chem. Biol , vol.7 , pp. 203-205
    • Deng, X.1    Dzamko, N.2    Prescott, A.3
  • 36
    • 1942453243 scopus 로고    scopus 로고
    • Ligand Efficiency: A Useful Metric for Lead Selection
    • Hopkins A. L., Groom C. R., Alex A., Ligand Efficiency: A Useful Metric for Lead Selection. Drug Discov. Today 2004, 9, 430-431.
    • (2004) Drug Discov. Today , vol.9 , pp. 430-431
    • Hopkins, A.L.1    Groom, C.R.2    Alex, A.3
  • 37
    • 84892755133 scopus 로고    scopus 로고
    • Demonstrating Enhanced Throughput of RapidFire Mass Spectrometry through Multiplexing Using the JmjD2d Demethylase as a Model System
    • Leveridge M., Buxton R., Argyrou A., et al. Demonstrating Enhanced Throughput of RapidFire Mass Spectrometry through Multiplexing Using the JmjD2d Demethylase as a Model System. J. Biomol. Screen. 2014, 19, 278-286.
    • (2014) J. Biomol. Screen , vol.19 , pp. 278-286
    • Leveridge, M.1    Buxton, R.2    Argyrou, A.3
  • 38
    • 84928796998 scopus 로고    scopus 로고
    • A Novel GTP-Binding Inhibitor, FX2149, Attenuates LRRK2 Toxicity in Parkinson's Disease Models
    • Li T., He X., Thomas J. M., et al. A Novel GTP-Binding Inhibitor, FX2149, Attenuates LRRK2 Toxicity in Parkinson's Disease Models. PLoS One 2015, 10, e0122461.
    • (2015) PLoS One , vol.10 , pp. e0122461
    • Li, T.1    He, X.2    Thomas, J.M.3


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.