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  • Dario Alessi
2012

Interaction of TAPP adapter proteins with phosphatidylinositol (3,4)-bisphosphate regulates B cell activation and autoantibody production

Jayachandran, N., Landego, I., Gibson, I., Miller, A., Wullschleger, S., Alessi, D. & Marshall, A., 1 May 2012, In : Journal of Immunology. 188, Suppl.1, 159.5.

Research output: Contribution to journalMeeting abstract

23 Citations (Scopus)

The IkappaB kinase family phosphorylates the Parkinson's disease kinase LRRK2 at Ser935 and Ser910 during Toll-Like Receptor signaling

Dzamko, N., Inesta-Vaquera, F., Zhang, J., Arthur, S., Cohen, P., Clark, K., Alessi, D. R., Xie, C., Cai, H., Tan, L., Choi, H., Gray, N. & Pedrioli, P., 2012, In : PLoS ONE. 7, 6, e39132.

Research output: Contribution to journalArticle

119 Citations (Scopus)
2011

Regulation of the NKCC2 ion cotransporter by SPAK-OSR1-dependent and -independent pathways

Richardson, C., Sakamoto, K., de los Heros, P., Deak, M., Campbell, D. G., Prescott, A. R. & Alessi, D. R., 1 Mar 2011, In : Journal of Cell Science. 124, 5, p. 789-800 12 p.

Research output: Contribution to journalArticle

117 Citations (Scopus)
2016

Functional kinomics establishes a critical node of volume-sensitive cation-Cl- cotransporter regulation in the mammalian brain

Zhang, J., Gao, G., Begum, G., Wang, J., Khanna, A. R., Shmukler, B. E., Daubner, G. M., De Los Heros, P., Davies, P., Varghese, J., Bhuiyan, M. I. H., Duan, J., Zhang, J., Duran, D., Alper, S. L., Sun, D., Elledge, S. J., Alessi, D. R. & Kahle, K. T., 26 Oct 2016, In : Scientific Reports. 6, p. 1-19 19 p., 35986.

Research output: Contribution to journalArticle

Open Access
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14 Citations (Scopus)
147 Downloads (Pure)
2013

Development of an enzyme-linked immunosorbent assay for detection of cellular and in vivo LRRK2 S935 phosphorylation

Delbroek, L., Van Kolen, K., Steegmans, L., da Cunha, R., Mandemakers, W., Daneels, G., De Bock, P-J., Zhang, J., Gevaert, K., De Strooper, B., Alessi, D. R., Verstreken, P. & Moechars, D. W., 25 Mar 2013, In : Journal of Pharmaceutical and Biomedical Analysis. 76, p. 49-58 10 p.

Research output: Contribution to journalArticle

16 Citations (Scopus)
2011

Characterization of GSK2334470, a novel and highly specific inhibitor of PDK1

Najafov, A., Sommer, E. M., Axten, J. M., DeYoung, M. P. & Alessi, D. R., 15 Jan 2011, In : Biochemical Journal. 433, p. 357-369 13 p.

Research output: Contribution to journalArticle

93 Citations (Scopus)
2012

Characterization of TAE684 as a potent LRRK2 kinase inhibitor

Zhang, J., Deng, X., Choi, H. G., Alessi, D. R. & Gray, N. S., 1 Mar 2012, In : Bioorganic & Medicinal Chemistry Letters. 22, 5, p. 1864-1869 6 p.

Research output: Contribution to journalArticle

56 Citations (Scopus)
2015

Phosphorylation of synaptic vesicle protein 2A at Thr84 by casein kinase 1 family kinases controls the specific retrieval of synaptotagmin-1

Zhang, N., Gordon, S. L., Fritsch, M. J., Esoof, N., Campbell, D. G., Gourlay, R., Srikannathasan, V., Macartney, T., Peggie, M., van Aalten, D. M. F., Cousin, M. A. & Alessi, D. R., 11 Feb 2015, In : Journal of Neuroscience. 35, 6, p. 2492-2507 16 p.

Research output: Contribution to journalArticle

Open Access
35 Citations (Scopus)
2012

GSK2578215A: a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor

Reith, A. D., Bamborough, P., Jandu, K., Andreotti, D., Mensah, L., Dossang, P., Choi, H. G., Deng, X., Zhang, J., Alessi, D. R. & Gray, N. S., 2012, In : Bioorganic & Medicinal Chemistry Letters. 22, 17, p. 5625-5629 5 p.

Research output: Contribution to journalArticle

96 Citations (Scopus)
2017

Regulation of membrane ruffling by polarized STIM1 and ORAI1in cortactin-rich domains

M. López-Guerrero, A., Tomas-Martin, P., Pascual-Caro, C., Macartney, T., Rojas-Fernandez, A., Ball, G., Alessi, D. R., Pozo-Guisado, E. & Martin-Romero, F. J., 24 Mar 2017, In : Scientific Reports. 7, 15 p., 383.

Research output: Contribution to journalArticle

Open Access
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8 Citations (Scopus)
125 Downloads (Pure)

Integrated single-cell genetic and transcriptional analysis suggests novel drivers of chronic lymphocytic leukemia

Wang, L., Fan, J., Francis, J. M., Georghiou, G., Hergert, S., Li, S., Gambe, R., Zhou, C. W., Yang, C., Xiao, S., Cin, P. D., Bowden, M., Kotliar, D., Shukla, S. A., Brown, J. R., Neuberg, D., Alessi, D. R., Zhang, C-Z., Kharchenko, P. V., Livak, K. J. & 1 others, Wu, C. J., 5 Jul 2017, In : Genome Research. 27, p. 1300-1311 11 p.

Research output: Contribution to journalArticle

Open Access
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25 Citations (Scopus)
163 Downloads (Pure)
2014
Open Access
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10 Citations (Scopus)
146 Downloads (Pure)

Kinase and channel activity of TRPM6 are co-ordinated by a dimerization motif and pocket interaction

van der Wijst, J., Blanchard, M. G., Woodroof, H. I., Macartney, T. J., Gourlay, R., Hoenderop, J. G., Bindels, R. J. & Alessi, D. R., 1 Jun 2014, In : Biochemical Journal. 460, 2, p. 165-175 11 p.

Research output: Contribution to journalArticle

Open Access
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9 Citations (Scopus)
139 Downloads (Pure)
2017

Vomocytosis of live pathogens from macrophages is regulated by the atypical MAP kinase ERK5

Gilbert, A. S., Seoane, P. I., Sephton-Clark, P., Bojarczuk, A., Hotham, R., Giurisato, E., Sarhan, A. R., Hillen, A., Velde, G. V., Gray, N. S., Alessi, D. R., Cunningham, D. L., Tournier, C., Johnston, S. A. & May, R. C., 16 Aug 2017, In : Science Advances. 3, 8, p. 1-9 9 p., e1700898.

Research output: Contribution to journalArticle

Open Access
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22 Citations (Scopus)
153 Downloads (Pure)
2018

A pathway for Parkinson's Disease LRRK2 kinase to block primary cilia and Sonic hedgehog signaling in the brain

Dhekne, H. S., Yanatori, I., Gomez, R. C., Tonelli, F., Diez, F., Schüle, B., Steger, M., Alessi, D. R. & Pfeffer, S. R., 6 Nov 2018, In : eLife. 7, p. 1-26 26 p., e40202.

Research output: Contribution to journalArticle

Open Access
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29 Citations (Scopus)
145 Downloads (Pure)

Structural and Atropisomeric Factors Governing the Selectivity of Pyrimido-benzodiazipinones as Inhibitors of Kinases and Bromodomains

Wang, J., Erazo, T., Ferguson, F. M., Buckley, D. L., Gomez, N., Muñoz-Guardiola, P., Diéguez-Martínez, N., Deng, X., Hao, M., Massefski, W., Fedorov, O., Offei-Addo, N. K., Park, P. M., Dai, L., DiBona, A., Becht, K., Kim, N. D., McKeown, M. R., Roberts, J. M., Zhang, J. & 8 others, Sim, T., Alessi, D. R., Bradner, J. E., Lizcano, J. M., Blacklow, S. C., Qi, J., Xu, X. & Gray, N. S., 21 Sep 2018, In : ACS Chemical Biology. 13, 9, p. 2438-2448 11 p.

Research output: Contribution to journalArticle

Open Access
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9 Citations (Scopus)
173 Downloads (Pure)
2014

Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases

Banerjee, S., Buhrlage, S. J., Huang, H-T., Deng, X., Zhou, W., Wang, J., Traynor, R., Prescott, A. R., Alessi, D. R. & Gray, N. S., 1 Jan 2014, In : Biochemical Journal. 457, 1, p. 215-225 11 p.

Research output: Contribution to journalArticle

27 Citations (Scopus)
2011

Protor-1 is required for efficient mTORC2-mediated activation of SGK1 in the kidney

Pearce, L. R., Sommer, E. M., Sakamoto, K., Wullschleger, S. & Alessi, D. R., 15 May 2011, In : Biochemical Journal. 436, p. 169-179 11 p.

Research output: Contribution to journalArticle

112 Citations (Scopus)
2018

Mechanism of activation of SGK3 by growth factors-via the Class 1 and Class 3 PI3Ks

Malik, N., Macartney, T., Hornberger, A., Anderson, K., Tovell, H., Prescott, A. R. & Alessi, D. R., 2 Jan 2018, In : Biochemical Journal. 475, 1, p. 117-135 19 p.

Research output: Contribution to journalArticle

Open Access
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10 Citations (Scopus)
249 Downloads (Pure)

The Parkinson's disease VPS35[D620N] mutation enhances LRRK2 mediated Rab protein phosphorylation in mouse and human

Mir, R., Tonelli, F., Lis, P., Macartney, T., Polinski, N. K., Martinez, T. N., Chou, M-Y., Howden, A., König, T., Hotzy, C., Milenkovic, I., Brücke, T., Zimprich, A., Sammler, E. & Alessi, D., 6 Jun 2018, In : Biochemical Journal. 475, 11, p. 1861-1883 19 p.

Research output: Contribution to journalArticle

Open Access
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41 Citations (Scopus)
176 Downloads (Pure)
2016

PDK1-SGK1 signaling sustains AKT-independent mTORC1 activation and confers resistance to PI3Kα inhibition

Castel, P., Ellis, H., Bago, R., Toska, E., Razavi, P., Carmona, F. J., kannan, S., Verma, C. S., Dickler, M., Chandarlapaty, S., Brogi, E., Alessi, D., Baselga, J. & Scaltriti, M., 8 Aug 2016, In : Cancer Cell. 30, 2, p. 229-242 14 p.

Research output: Contribution to journalArticle

Open Access
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72 Citations (Scopus)
315 Downloads (Pure)
2014

Screening of DUB activity and specificity by MALDI-TOF mass spectrometry

Ritorto, M. S., Ewan, R., Perez-Oliva, A. B., Knebel, A., Buhrlage, S. J., Wightman, M., Kelly, S. M., Wood, N. T., Virdee, S., Gray, N. S., Morrice, N. A., Alessi, D. R. & Trost, M., 27 Aug 2014, In : Nature Communications. 5, 11 p., 4763.

Research output: Contribution to journalArticle

Open Access
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133 Citations (Scopus)
201 Downloads (Pure)
2017

Homo-PROTACs: bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation

Maniaci, C., Hughes, S. J., Testa, A., Chen, W., Lamont, D. J., Rocha, S., Alessi, D. R., Romeo, R. & Ciulli, A., 10 Oct 2017, In : Nature Communications. 8, p. 1-14 14 p., 830.

Research output: Contribution to journalArticle

Open Access
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59 Citations (Scopus)
186 Downloads (Pure)
2019

PPM1H phosphatase counteracts LRRK2 signaling by selectively dephosphorylating Rab proteins

Berndsen, K., Lis, P., Yeshaw, W. M., Wawro, P. S., Nirujogi, R., Wightman, M., Macartney, T., Dorward, M., Knebel, A., Tonelli, F., Pfeffer, S. R. & Alessi, D., 30 Oct 2019, In : eLife. 8, p. 1-37 37 p., e50416.

Research output: Contribution to journalArticle

Open Access
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6 Citations (Scopus)
57 Downloads (Pure)
2014

Structural and biochemical characterization of the KLHL3-WNK kinase interaction important in blood pressure regulation

Schumacher, F-R., Sorrell, F. J., Alessi, D. R., Bullock, A. N. & Kurz, T., 1 Jun 2014, In : Biochemical Journal. 460, 2, p. 237-246 10 p.

Research output: Contribution to journalArticle

Open Access
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32 Citations (Scopus)
165 Downloads (Pure)
2020

Structural Basis for Rab8a Recruitment of RILPL2 via LRRK2 Phosphorylation of Switch 2

Waschbüsch, D., Purlyte, E., Pal, P., McGrath, E., Alessi, D. R. & Khan, A. R., 7 Apr 2020, In : Structure. 28, 4, p. 406-417.e6 19 p.

Research output: Contribution to journalArticle

Open Access
File
1 Citation (Scopus)
43 Downloads (Pure)
2018

LRRK2 is a negative regulator of Mycobacterium tuberculosis phagosome maturation in macrophages

Härtlova, A., Herbst, S., Peltier, J., Rodgers, A., Bilkei-Gorzo, O., Fearns, A., Dill, B. D., Lee, H., Flynn, R., Cowley, S. A., Davies, P., Lewis, P. A., Ganley, I. G., Martinez, J., Alessi, D. R., Reith, A. D., Trost, M. & Gutierrez, M. G., 15 Jun 2018, In : The EMBO Journal. 37, 12, p. 1-17 17 p., e98694.

Research output: Contribution to journalArticle

Open Access
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45 Citations (Scopus)
184 Downloads (Pure)
2011

MO25 is a master regulator of SPAK/OSR1 and MST3/MST4/YSK1 protein kinases

Filippi, B. M., de los Heros, P., Mehellou, Y., Navratilova, I., Gourlay, R., Deak, M., Plater, L., Toth, R., Zeqiraj, E. & Alessi, D. R., 4 May 2011, In : EMBO Journal. 30, 9, p. 1730-1741 12 p.

Research output: Contribution to journalArticle

84 Citations (Scopus)
2012

Discovery of potent and selective covalent inhibitors of JNK

Zhang, T., Inesta-Vaquera, F., Niepel, M., Zhang, J., Ficarro, S. B., Machleidt, T., Xie, T., Marto, J. A., Kim, N., Sim, T., Laughlin, J. D., Park, H., LoGrasso, P. V., Patricelli, M., Nomanbhoy, T. K., Sorger, P. K., Alessi, D. R. & Gray, N. S., 27 Jan 2012, In : Chemistry & Biology. 19, 1, p. 140-154 15 p.

Research output: Contribution to journalArticle

177 Citations (Scopus)

Effect of heterozygous deletion of WNK1 on the WNK-OSR1/SPAK-NCC/NKCC1/NKCC2 signal cascade in the kidney and blood vessels

Susa, K., Kita, S., Iwamoto, T., Yang, S-S., Lin, S-H., Ohta, A., Sohara, E., Rai, T., Sasaki, S., Alessi, D. R. & Uchida, S., Aug 2012, In : Clinical and Experimental Nephrology. 16, 4, p. 530-538 9 p.

Research output: Contribution to journalArticle

40 Citations (Scopus)
2018

PP1 Phosphatase complexes: Undruggable No Longer

Vagnarelli, P. & Alessi, D. R., 23 Aug 2018, In : Cell. 174, 5, p. 1049-1051 3 p.

Research output: Contribution to journalArticle

Open Access
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3 Citations (Scopus)
90 Downloads (Pure)

Nigrostriatal pathology with reduced astrocytes in LRRK2 S910/S935 phosphorylation deficient knockin mice

Zhao, Y., Keshiya, S., Atashrazm, F., Gao, J., Ittner, L. M., Alessi, D. R., Halliday, G. M., Fu, Y. & Dzamko, N., 1 Dec 2018, In : Neurobiology of Disease. 120, p. 76-87 12 p.

Research output: Contribution to journalArticle

Open Access
File
5 Citations (Scopus)
167 Downloads (Pure)

LRRK2 activation in idiopathic Parkinson's disease

Di Maio, R., Hoffman, E. K., Rocha, E. M., Keeney, M. T., Sanders, L. H., De Miranda, B. R., Zharikov, A., Van Laar, A., Stepan, A. F., Lanz, T. A., Kofler, J. K., Burton, E. A., Alessi, D. R., Hastings, T. G. & Timothy Greenamyre, J., 25 Jul 2018, In : Science Translational Medicine. 10, 451, p. 1-12 12 p., eaar5429.

Research output: Contribution to journalArticle

Open Access
File
72 Citations (Scopus)
90 Downloads (Pure)
2014

The WNK-regulated SPAK/OSR1 kinases directly phosphorylate and inhibit the K+-Cl- co-transporters

De Los Heros, P., Alessi, D. R., Gourlay, R., Campbell, D. G., Deak, M., Macartney, T. J., Kahle, K. T. & Zhang, J., 15 Mar 2014, In : Biochemical Journal. 458, 3, p. 559-573 15 p.

Research output: Contribution to journalArticle

Open Access
File
93 Citations (Scopus)
172 Downloads (Pure)
2019

Crystal structure of the WD40 domain dimer of LRRK2

Zhang, P., Fan, Y., Ru, H., Wang, L., Magupalli, V. G., Taylor, S. S., Alessi, D. R. & Wu, H., 29 Jan 2019, In : Proceedings of the National Academy of Sciences of the United States of America. 116, 5, p. 1579-1584 6 p.

Research output: Contribution to journalArticle

Open Access
File
6 Citations (Scopus)
137 Downloads (Pure)
2013

LKB1 and AMPK and the cancer-metabolism link - ten years after

Hardie, D. G. & Alessi, D. R., 15 Apr 2013, In : BMC Biology. 11, p. 1-11 11 p., 36.

Research output: Contribution to journalArticle

Open Access
File
194 Citations (Scopus)
132 Downloads (Pure)
2014

Investigation of LKB1 Ser431 phosphorylation and Cys433 farnesylation using mouse knockin analysis reveals an unexpected role of prenylation in regulating AMPK activity

Houde, V. P., Ritorto, M. S., Gourlay, R., Davies, P., Shpiro, N., Sakamoto, K. & Alessi, D. R., 15 Feb 2014, In : Biochemical Journal. 458, 1, p. 41-56 16 p.

Research output: Contribution to journalArticle

Open Access
File
30 Citations (Scopus)
156 Downloads (Pure)
2012

Phenformin as prophylaxis and therapy in breast cancer xenografts

Appleyard, M. V. C. L., Murray, K. E., Coates, P. J., Wullschleger, S., Bray, S. E., Kernohan, N. M., Fleming, S., Alessi, D. R. & Thompson, A. M., 13 Mar 2012, In : British Journal of Cancer. 106, 6, p. 1117-1122 6 p.

Research output: Contribution to journalArticle

68 Citations (Scopus)

PINK1 is activated by mitochondrial membrane potential depolarization and stimulates Parkin E3 ligase activity by phosphorylating Serine 65

Kondapalli, C., Kazlauskaite, A., Zhang, N., Woodroof, H. I., Campbell, D. G., Gourlay, R., Burchell, L., Walden, H., MacArtney, T. J., Deak, M., Knebel, A., Alessi, D. R. & Muqit, M. M. K., 2012, In : Open Biology. 2, 120080.

Research output: Contribution to journalArticle

336 Citations (Scopus)
2013

Kinase inhibitors arrest neurodegeneration in cell and C. elegans models of LRRK2 toxicity

Yao, C., Johnson, W. M., Gao, Y., Wang, W., Zhang, J., Deak, M., Alessi, D. R., Zhu, X., Mieyal, J. J., Roder, H., Wilson-Delfosse, A. L. & Chen, S. G., 15 Jan 2013, In : Human Molecular Genetics. 22, 2, p. 328-344 17 p.

Research output: Contribution to journalArticle

51 Citations (Scopus)

Structural biology: Security measures of a master regulator

Alessi, D. R. & Kulathu, Y., 1 May 2013, In : Nature.

Research output: Contribution to journalArticle

2 Citations (Scopus)
2019

Discovery of potent and selective 5-azaindazole inhibitors of leucine-rich repeat kinase 2 (LRRK2) - Part 1

Osborne, J., Birchall, K., Tsagris, D. J., Lewis, S. J., Smiljanic-Hurley, E., Taylor, D. L., Levy, A., Alessi, D. & McIver, E. G., 15 Feb 2019, In : Bioorganic & Medicinal Chemistry Letters. 29, 4, p. 668-673 6 p.

Research output: Contribution to journalArticle

Open Access
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61 Downloads (Pure)
2020

Human Peripheral Blood Neutrophil Isolation for Interrogating the Parkinson’s Associated LRRK2 Kinase Pathway by Assessing Rab10 Phosphorylation

Fan, Y., Tonelli, F., Padmanabhan, S., Baptista, M., Riley, L., Smith, D., Marras, C., Howden, A., Alessi, D. & Sammler, E., 22 Mar 2020, In : JoVE: Journal of Visualized Experiments. 157, e58956.

Research output: Contribution to journalArticle

2011

Role of TAPP1 and TAPP2 adaptor binding to PtdIns(3,4)P-2 in regulating insulin sensitivity defined by knock-in analysis

Wullschleger, S., Wasserman, D. H., Gray, A., Sakamoto, K. & Alessi, D. R., 1 Mar 2011, In : Biochemical Journal. 434, p. 265-274 10 p.

Research output: Contribution to journalArticle

34 Citations (Scopus)
2012

SPAK/OSR1 regulate NKCC1 and WNK activity: analysis of WNK isoform interactions and activation by T-loop trans-autophosphorylation

Thastrup, J. O., Rafiqi, F. H., Vitari, A. C., Pozo-Guisado, E., Deak, M., Mehellou, Y. & Alessi, D. R., 1 Jan 2012, In : Biochemical Journal. 441, p. 325-337 13 p.

Research output: Contribution to journalArticle

65 Citations (Scopus)
2018

Interrogating Parkinson's disease LRRK2 kinase pathway activity by assessing Rab10 phosphorylation in human neutrophils

Fan, Y., Howden, A. J. M., Sarhan, A. R., Lis, P., Ito, G., Martinez, T. N., Brockmann, K., Gasser, T., Alessi, D. R. & Sammler, E., 2 Jan 2018, In : Biochemical Journal. 475, 1, p. 23-44 22 p.

Research output: Contribution to journalArticle

Open Access
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37 Citations (Scopus)
189 Downloads (Pure)
2015

Discovery of a pyrrolopyrimidine (JH-II-127), a highly potent, selective, and brain penetrant LRRK2 inhibitor

Hatcher, J. M., Zhang, J., Choi, H. G., Ito, G., Alessi, D. R. & Gray, N. S., 14 May 2015, In : ACS Medicinal Chemistry Letters. 6, 5, p. 584-589 6 p.

Research output: Contribution to journalArticle

26 Citations (Scopus)
2013

Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones

Deng, X., Elkins, J. M., Zhang, J., Yang, Q., Erazo, T., Gomez, N., Choi, H. G., Wang, J., Dzamko, N., Lee, J-D., Sim, T., Kim, N., Alessi, D. R., Lizcano, J. M., Knapp, S. & Gray, N. S., Dec 2013, In : European Journal of Medicinal Chemistry. 70, p. 758-767 10 p.

Research output: Contribution to journalArticle

25 Citations (Scopus)
2014

Phosphorylation of Parkin at Serine65 is essential for activation: elaboration of a Miro1 substrate-based assay of Parkin E3 ligase activity

Kazlauskaite, A., Kelly, V., Johnson, C., Baillie, C., Hastie, C. J., Peggie, M., Macartney, T., Woodroof, H. I., Alessi, D. R., Pedrioli, P. G. A. & Muqit, M. M. K., 19 Mar 2014, In : Open Biology. 4, 14 p., 130213.

Research output: Contribution to journalArticle

62 Citations (Scopus)
2011

TTBK2 kinase substrate specificity and the impact of spinocerebellar-ataxia-causing mutations on expression, activity, localization and development

Bouskila, M., Esoof, N., Gay, L., Fang, E. H., Deak, M., Begley, M. J., Cantley, L. C., Prescott, A., Storey, K. G. & Alessi, D. R., 2011, In : Biochemical Journal. 437, p. 157-167 11 p.

Research output: Contribution to journalArticle

23 Citations (Scopus)