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Items: 1 to 50 of 251

1.

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

Zhao Y, Keshiya S, Atashrazm F, Gao J, Ittner LM, Alessi DR, Halliday GM, Fu Y, Dzamko N.

Neurobiol Dis. 2018 Sep 5;120:76-87. doi: 10.1016/j.nbd.2018.09.003. [Epub ahead of print]

2.

PP1 Phosphatase Complexes: Undruggable No Longer.

Vagnarelli P, Alessi DR.

Cell. 2018 Aug 23;174(5):1049-1051. doi: 10.1016/j.cell.2018.08.007.

PMID:
30142342
3.

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

Wang J, Erazo T, Ferguson FM, Buckley DL, Gomez N, Muñoz-Guardiola P, Diéguez-Martínez N, Deng X, Hao M, Massefski W, Fedorov O, Offei-Addo NK, Park PM, Dai L, DiBona A, Becht K, Kim ND, McKeown MR, Roberts JM, Zhang J, Sim T, Alessi DR, Bradner JE, Lizcano JM, Blacklow SC, Qi J, Xu X, Gray NS.

ACS Chem Biol. 2018 Sep 21;13(9):2438-2448. doi: 10.1021/acschembio.7b00638. Epub 2018 Aug 31.

PMID:
30102854
4.

LRRK2 activation in idiopathic Parkinson's disease.

Di Maio R, Hoffman EK, Rocha EM, Keeney MT, Sanders LH, De Miranda BR, Zharikov A, Van Laar A, Stepan AF, Lanz TA, Kofler JK, Burton EA, Alessi DR, Hastings TG, Greenamyre JT.

Sci Transl Med. 2018 Jul 25;10(451). pii: eaar5429. doi: 10.1126/scitranslmed.aar5429.

PMID:
30045977
5.

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 BD, Lee H, Flynn R, Cowley SA, Davies P, Lewis PA, Ganley IG, Martinez J, Alessi DR, Reith AD, Trost M, Gutierrez MG.

EMBO J. 2018 Jun 15;37(12). pii: e98694. doi: 10.15252/embj.201798694. Epub 2018 May 22.

6.

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 NK, Martinez TN, Chou MY, Howden AJM, König T, Hotzy C, Milenkovic I, Brücke T, Zimprich A, Sammler E, Alessi DR.

Biochem J. 2018 Jun 6;475(11):1861-1883. doi: 10.1042/BCJ20180248.

7.

LRRK2 kinase in Parkinson's disease.

Alessi DR, Sammler E.

Science. 2018 Apr 6;360(6384):36-37. doi: 10.1126/science.aar5683. No abstract available.

PMID:
29622645
8.

Rab29 activation of the Parkinson's disease-associated LRRK2 kinase.

Purlyte E, Dhekne HS, Sarhan AR, Gomez R, Lis P, Wightman M, Martinez TN, Tonelli F, Pfeffer SR, Alessi DR.

EMBO J. 2018 Jan 4;37(1):1-18. doi: 10.15252/embj.201798099. Epub 2017 Dec 6.

9.

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

Malik N, Macartney T, Hornberger A, Anderson KE, Tovell H, Prescott AR, Alessi DR.

Biochem J. 2018 Jan 2;475(1):117-135. doi: 10.1042/BCJ20170650.

10.

Development of phospho-specific Rab protein antibodies to monitor in vivo activity of the LRRK2 Parkinson's disease kinase.

Lis P, Burel S, Steger M, Mann M, Brown F, Diez F, Tonelli F, Holton JL, Ho PW, Ho SL, Chou MY, Polinski NK, Martinez TN, Davies P, Alessi DR.

Biochem J. 2018 Jan 2;475(1):1-22. doi: 10.1042/BCJ20170802.

11.

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

Fan Y, Howden AJM, Sarhan AR, Lis P, Ito G, Martinez TN, Brockmann K, Gasser T, Alessi DR, Sammler EM.

Biochem J. 2018 Jan 2;475(1):23-44. doi: 10.1042/BCJ20170803.

12.

Systematic proteomic analysis of LRRK2-mediated Rab GTPase phosphorylation establishes a connection to ciliogenesis.

Steger M, Diez F, Dhekne HS, Lis P, Nirujogi RS, Karayel O, Tonelli F, Martinez TN, Lorentzen E, Pfeffer SR, Alessi DR, Mann M.

Elife. 2017 Nov 10;6. pii: e31012. doi: 10.7554/eLife.31012.

13.

USP7 small-molecule inhibitors interfere with ubiquitin binding.

Kategaya L, Di Lello P, Rougé L, Pastor R, Clark KR, Drummond J, Kleinheinz T, Lin E, Upton JP, Prakash S, Heideker J, McCleland M, Ritorto MS, Alessi DR, Trost M, Bainbridge TW, Kwok MCM, Ma TP, Stiffler Z, Brasher B, Tang Y, Jaishankar P, Hearn BR, Renslo AR, Arkin MR, Cohen F, Yu K, Peale F, Gnad F, Chang MT, Klijn C, Blackwood E, Martin SE, Forrest WF, Ernst JA, Ndubaku C, Wang X, Beresini MH, Tsui V, Schwerdtfeger C, Blake RA, Murray J, Maurer T, Wertz IE.

Nature. 2017 Oct 26;550(7677):534-538. doi: 10.1038/nature24006. Epub 2017 Oct 18.

PMID:
29045385
14.

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

Maniaci C, Hughes SJ, Testa A, Chen W, Lamont DJ, Rocha S, Alessi DR, Romeo R, Ciulli A.

Nat Commun. 2017 Oct 10;8(1):830. doi: 10.1038/s41467-017-00954-1.

15.

Disruption of the with no lysine kinase-STE20-proline alanine-rich kinase pathway reduces the hypertension induced by angiotensin II.

Cervantes-Perez LG, Castaneda-Bueno M, Jimenez JV, Vazquez N, Rojas-Vega L, Alessi DR, Bobadilla NA, Gamba G.

J Hypertens. 2018 Feb;36(2):361-367. doi: 10.1097/HJH.0000000000001554.

16.

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

Gilbert AS, Seoane PI, Sephton-Clark P, Bojarczuk A, Hotham R, Giurisato E, Sarhan AR, Hillen A, Velde GV, Gray NS, Alessi DR, Cunningham DL, Tournier C, Johnston SA, May RC.

Sci Adv. 2017 Aug 16;3(8):e1700898. doi: 10.1126/sciadv.1700898. eCollection 2017 Aug.

17.

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

Wang L, Fan J, Francis JM, Georghiou G, Hergert S, Li S, Gambe R, Zhou CW, Yang C, Xiao S, Cin PD, Bowden M, Kotliar D, Shukla SA, Brown JR, Neuberg D, Alessi DR, Zhang CZ, Kharchenko PV, Livak KJ, Wu CJ.

Genome Res. 2017 Aug;27(8):1300-1311. doi: 10.1101/gr.217331.116. Epub 2017 Jul 5.

18.

Small-Molecule Inhibitors of LRRK2.

Hatcher JM, Choi HG, Alessi DR, Gray NS.

Adv Neurobiol. 2017;14:241-264. doi: 10.1007/978-3-319-49969-7_13.

PMID:
28353288
19.

Regulation of membrane ruffling by polarized STIM1 and ORAI1 in cortactin-rich domains.

Lopez-Guerrero AM, Tomas-Martin P, Pascual-Caro C, Macartney T, Rojas-Fernandez A, Ball G, Alessi DR, Pozo-Guisado E, Martin-Romero FJ.

Sci Rep. 2017 Mar 24;7(1):383. doi: 10.1038/s41598-017-00331-4.

20.

B-cell-intrinsic function of TAPP adaptors in controlling germinal center responses and autoantibody production in mice.

Jayachandran N, Landego I, Hou S, Alessi DR, Marshall AJ.

Eur J Immunol. 2017 Feb;47(2):280-290. doi: 10.1002/eji.201646596. Epub 2016 Dec 21.

21.

The hVps34-SGK3 pathway alleviates sustained PI3K/Akt inhibition by stimulating mTORC1 and tumour growth.

Bago R, Sommer E, Castel P, Crafter C, Bailey FP, Shpiro N, Baselga J, Cross D, Eyers PA, Alessi DR.

EMBO J. 2016 Oct 17;35(20):2263. No abstract available.

22.

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 AR, Shmukler BE, Daubner GM, de Los Heros P, Davies P, Varghese J, Bhuiyan MI, Duan J, Zhang J, Duran D, Alper SL, Sun D, Elledge SJ, Alessi DR, Kahle KT.

Sci Rep. 2016 Oct 26;6:35986. doi: 10.1038/srep35986.

23.

The hVps34-SGK3 pathway alleviates sustained PI3K/Akt inhibition by stimulating mTORC1 and tumour growth.

Bago R, Sommer E, Castel P, Crafter C, Bailey FP, Shpiro N, Baselga J, Cross D, Eyers PA, Alessi DR.

EMBO J. 2016 Sep 1;35(17):1902-22. doi: 10.15252/embj.201693929. Epub 2016 Aug 1. Erratum in: EMBO J. 2016 Oct 17;35(20):2263.

24.

Phos-tag analysis of Rab10 phosphorylation by LRRK2: a powerful assay for assessing kinase function and inhibitors.

Ito G, Katsemonova K, Tonelli F, Lis P, Baptista MA, Shpiro N, Duddy G, Wilson S, Ho PW, Ho SL, Reith AD, Alessi DR.

Biochem J. 2016 Sep 1;473(17):2671-85. doi: 10.1042/BCJ20160557. Epub 2016 Jul 29.

25.

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 FJ, Kannan S, Verma CS, Dickler M, Chandarlapaty S, Brogi E, Alessi DR, Baselga J, Scaltriti M.

Cancer Cell. 2016 Aug 8;30(2):229-242. doi: 10.1016/j.ccell.2016.06.004. Epub 2016 Jul 21.

26.

Phosphoproteomics reveals that Parkinson's disease kinase LRRK2 regulates a subset of Rab GTPases.

Steger M, Tonelli F, Ito G, Davies P, Trost M, Vetter M, Wachter S, Lorentzen E, Duddy G, Wilson S, Baptista MA, Fiske BK, Fell MJ, Morrow JA, Reith AD, Alessi DR, Mann M.

Elife. 2016 Jan 29;5. pii: e12813. doi: 10.7554/eLife.12813.

27.

Binding to serine 65-phosphorylated ubiquitin primes Parkin for optimal PINK1-dependent phosphorylation and activation.

Kazlauskaite A, Martínez-Torres RJ, Wilkie S, Kumar A, Peltier J, Gonzalez A, Johnson C, Zhang J, Hope AG, Peggie M, Trost M, van Aalten DM, Alessi DR, Prescott AR, Knebel A, Walden H, Muqit MM.

EMBO Rep. 2015 Aug;16(8):939-54. doi: 10.15252/embr.201540352. Epub 2015 Jun 25.

28.

Discovery of a Pyrrolopyrimidine (JH-II-127), a Highly Potent, Selective, and Brain Penetrant LRRK2 Inhibitor.

Hatcher JM, Zhang J, Choi HG, Ito G, Alessi DR, Gray NS.

ACS Med Chem Lett. 2015 Apr 7;6(5):584-9. doi: 10.1021/acsmedchemlett.5b00064. eCollection 2015 May 14.

29.

Critical role of the SPAK protein kinase CCT domain in controlling blood pressure.

Zhang J, Siew K, Macartney T, O'Shaughnessy KM, Alessi DR.

Hum Mol Genet. 2015 Aug 15;24(16):4545-58. doi: 10.1093/hmg/ddv185. Epub 2015 May 20.

30.

Structural Characterization of LRRK2 Inhibitors.

Gilsbach BK, Messias AC, Ito G, Sattler M, Alessi DR, Wittinghofer A, Kortholt A.

J Med Chem. 2015 May 14;58(9):3751-6. doi: 10.1021/jm5018779. Epub 2015 May 1.

PMID:
25897865
31.

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

Zhang N, Gordon SL, Fritsch MJ, Esoof N, Campbell DG, Gourlay R, Velupillai S, Macartney T, Peggie M, van Aalten DM, Cousin MA, Alessi DR.

J Neurosci. 2015 Feb 11;35(6):2492-507. doi: 10.1523/JNEUROSCI.4248-14.2015.

32.

USP45 deubiquitylase controls ERCC1-XPF endonuclease-mediated DNA damage responses.

Perez-Oliva AB, Lachaud C, Szyniarowski P, Muñoz I, Macartney T, Hickson I, Rouse J, Alessi DR.

EMBO J. 2015 Feb 3;34(3):326-43. doi: 10.15252/embj.201489184. Epub 2014 Dec 23.

33.

A next-generation dual-recombinase system for time- and host-specific targeting of pancreatic cancer.

Schönhuber N, Seidler B, Schuck K, Veltkamp C, Schachtler C, Zukowska M, Eser S, Feyerabend TB, Paul MC, Eser P, Klein S, Lowy AM, Banerjee R, Yang F, Lee CL, Moding EJ, Kirsch DG, Scheideler A, Alessi DR, Varela I, Bradley A, Kind A, Schnieke AE, Rodewald HR, Rad R, Schmid RM, Schneider G, Saur D.

Nat Med. 2014 Nov;20(11):1340-1347. doi: 10.1038/nm.3646. Epub 2014 Oct 19. Erratum in: Nat Med. 2015 Apr;21(4):414.

34.

Characterization of VPS34-IN1, a selective inhibitor of Vps34, reveals that the phosphatidylinositol 3-phosphate-binding SGK3 protein kinase is a downstream target of class III phosphoinositide 3-kinase.

Bago R, Malik N, Munson MJ, Prescott AR, Davies P, Sommer E, Shpiro N, Ward R, Cross D, Ganley IG, Alessi DR.

Biochem J. 2014 Nov 1;463(3):413-27. doi: 10.1042/BJ20140889.

35.

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

Ritorto MS, Ewan R, Perez-Oliva AB, Knebel A, Buhrlage SJ, Wightman M, Kelly SM, Wood NT, Virdee S, Gray NS, Morrice NA, Alessi DR, Trost M.

Nat Commun. 2014 Aug 27;5:4763. doi: 10.1038/ncomms5763.

36.

The WNK-SPAK/OSR1 pathway: master regulator of cation-chloride cotransporters.

Alessi DR, Zhang J, Khanna A, Hochdörfer T, Shang Y, Kahle KT.

Sci Signal. 2014 Jul 15;7(334):re3. doi: 10.1126/scisignal.2005365. Review.

PMID:
25028718
37.

Interplay between Polo kinase, LKB1-activated NUAK1 kinase, PP1βMYPT1 phosphatase complex and the SCFβTrCP E3 ubiquitin ligase.

Banerjee S, Zagórska A, Deak M, Campbell DG, Prescott AR, Alessi DR.

Biochem J. 2014 Jul 15;461(2):233-45. doi: 10.1042/BJ20140408.

38.

Parkin is activated by PINK1-dependent phosphorylation of ubiquitin at Ser65.

Kazlauskaite A, Kondapalli C, Gourlay R, Campbell DG, Ritorto MS, Hofmann K, Alessi DR, Knebel A, Trost M, Muqit MM.

Biochem J. 2014 May 15;460(1):127-39. doi: 10.1042/BJ20140334.

39.

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

van der Wijst J, Blanchard MG, Woodroof HI, Macartney TJ, Gourlay R, Hoenderop JG, Bindels RJ, Alessi DR.

Biochem J. 2014 Jun 1;460(2):165-75. doi: 10.1042/BJ20131639.

40.

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 CJ, Peggie M, Macartney T, Woodroof HI, Alessi DR, Pedrioli PG, Muqit MM.

Open Biol. 2014 Mar 19;4:130213. doi: 10.1098/rsob.130213.

41.

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

Schumacher FR, Sorrell FJ, Alessi DR, Bullock AN, Kurz T.

Biochem J. 2014 Jun 1;460(2):237-46. doi: 10.1042/BJ20140153.

42.

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

de Los Heros P, Alessi DR, Gourlay R, Campbell DG, Deak M, Macartney TJ, Kahle KT, Zhang J.

Biochem J. 2014 Mar 15;458(3):559-73. doi: 10.1042/BJ20131478.

43.

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

Houde VP, Ritorto MS, Gourlay R, Varghese J, Davies P, Shpiro N, Sakamoto K, Alessi DR.

Biochem J. 2014 Feb 15;458(1):41-56. doi: 10.1042/BJ20131324.

44.

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 JM, Zhang J, Yang Q, Erazo T, Gomez N, Choi HG, Wang J, Dzamko N, Lee JD, Sim T, Kim N, Alessi DR, Lizcano JM, Knapp S, Gray NS.

Eur J Med Chem. 2013;70:758-67. doi: 10.1016/j.ejmech.2013.10.052. Epub 2013 Oct 29.

45.

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

Banerjee S, Buhrlage SJ, Huang HT, Deng X, Zhou W, Wang J, Traynor R, Prescott AR, Alessi DR, Gray NS.

Biochem J. 2014 Jan 1;457(1):215-25. doi: 10.1042/BJ20131152.

46.

N-terminal serine dephosphorylation is required for KCC3 cotransporter full activation by cell swelling.

Melo Z, de los Heros P, Cruz-Rangel S, Vázquez N, Bobadilla NA, Pasantes-Morales H, Alessi DR, Mercado A, Gamba G.

J Biol Chem. 2013 Nov 1;288(44):31468-76. doi: 10.1074/jbc.M113.475574. Epub 2013 Sep 16.

47.

Structural biology: Security measures of a master regulator.

Alessi DR, Kulathu Y.

Nature. 2013 May 9;497(7448):193-4. doi: 10.1038/nature12101. Epub 2013 May 1. No abstract available.

PMID:
23636322
48.

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

Hardie DG, Alessi DR.

BMC Biol. 2013 Apr 15;11:36. doi: 10.1186/1741-7007-11-36. Review.

49.

Elevated SGK1 predicts resistance of breast cancer cells to Akt inhibitors.

Sommer EM, Dry H, Cross D, Guichard S, Davies BR, Alessi DR.

Biochem J. 2013 Jun 15;452(3):499-508. doi: 10.1042/BJ20130342.

50.

Comprehensive characterization and optimization of anti-LRRK2 (leucine-rich repeat kinase 2) monoclonal antibodies.

Davies P, Hinkle KM, Sukar NN, Sepulveda B, Mesias R, Serrano G, Alessi DR, Beach TG, Benson DL, White CL, Cowell RM, Das SS, West AB, Melrose HL.

Biochem J. 2013 Jul 1;453(1):101-13. doi: 10.1042/BJ20121742.

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