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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.


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.


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.


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.


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.


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.


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):1340-7. doi: 10.1038/nm.3646. Epub 2014 Oct 19. Erratum in: Nat Med. 2015 Apr;21(4):414.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.

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