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Items: 1 to 50 of 70

1.

Drug repurposing: progress, challenges and recommendations.

Pushpakom S, Iorio F, Eyers PA, Escott KJ, Hopper S, Wells A, Doig A, Guilliams T, Latimer J, McNamee C, Norris A, Sanseau P, Cavalla D, Pirmohamed M.

Nat Rev Drug Discov. 2018 Oct 12. doi: 10.1038/nrd.2018.168. [Epub ahead of print] Review.

PMID:
30310233
2.

Covalent inhibitors of EGFR family protein kinases induce degradation of human Tribbles 2 (TRIB2) pseudokinase in cancer cells.

Foulkes DM, Byrne DP, Yeung W, Shrestha S, Bailey FP, Ferries S, Eyers CE, Keeshan K, Wells C, Drewry DH, Zuercher WJ, Kannan N, Eyers PA.

Sci Signal. 2018 Sep 25;11(549). pii: eaat7951. doi: 10.1126/scisignal.aat7951.

PMID:
30254057
3.

BH3-only proteins are dispensable for apoptosis induced by pharmacological inhibition of both MCL-1 and BCL-XL.

Greaves G, Milani M, Butterworth M, Carter RJ, Byrne DP, Eyers PA, Luo X, Cohen GM, Varadarajan S.

Cell Death Differ. 2018 Sep 5. doi: 10.1038/s41418-018-0183-7. [Epub ahead of print]

PMID:
30185825
4.

New tools for carbohydrate sulfation analysis: heparan sulfate 2-O-sulfotransferase (HS2ST) is a target for small-molecule protein kinase inhibitors.

Byrne DP, Li Y, Ramakrishnan K, Barsukov IL, Yates EA, Eyers CE, Papy-Garcia D, Chantepie S, Pagadala V, Liu J, Wells C, Drewry DH, Zuercher WJ, Berry NG, Fernig DG, Eyers PA.

Biochem J. 2018 Aug 14;475(15):2417-2433. doi: 10.1042/BCJ20180265.

5.

New tools for evaluating protein tyrosine sulfation: tyrosylprotein sulfotransferases (TPSTs) are novel targets for RAF protein kinase inhibitors.

Byrne DP, Li Y, Ngamlert P, Ramakrishnan K, Eyers CE, Wells C, Drewry DH, Zuercher WJ, Berry NG, Fernig DG, Eyers PA.

Biochem J. 2018 Aug 14;475(15):2435-2455. doi: 10.1042/BCJ20180266.

6.

DNA Binding and Phosphorylation Regulate the Core Structure of the NF-κB p50 Transcription Factor.

Vonderach M, Byrne DP, Barran PE, Eyers PA, Eyers CE.

J Am Soc Mass Spectrom. 2018 Jun 5. doi: 10.1007/s13361-018-1984-0. [Epub ahead of print]

PMID:
29873020
7.

Trib2 expression in granulocyte-monocyte progenitors drives a highly drug resistant acute myeloid leukaemia linked to elevated Bcl2.

O'Connor C, Yalla K, Salomé M, Moka HA, Castañeda EG, Eyers PA, Keeshan K.

Oncotarget. 2018 Feb 19;9(19):14977-14992. doi: 10.18632/oncotarget.24525. eCollection 2018 Mar 13.

8.

Mps1 Phosphorylates Its N-Terminal Extension to Relieve Autoinhibition and Activate the Spindle Assembly Checkpoint.

Combes G, Barysz H, Garand C, Gama Braga L, Alharbi I, Thebault P, Murakami L, Bryne DP, Stankovic S, Eyers PA, Bolanos-Garcia VM, Earnshaw WC, Maciejowski J, Jallepalli PV, Elowe S.

Curr Biol. 2018 Mar 19;28(6):872-883.e5. doi: 10.1016/j.cub.2018.02.002. Epub 2018 Mar 1.

9.

Autophosphorylation Is a Mechanism of Inhibition in Twitchin Kinase.

Williams RM, Franke B, Wilkinson M, Fleming JR, Rigden DJ, Benian GM, Eyers PA, Mayans O.

J Mol Biol. 2018 Mar 16;430(6):793-805. doi: 10.1016/j.jmb.2018.01.020. Epub 2018 Feb 3.

PMID:
29408381
10.

Understanding protein-drug interactions using ion mobility-mass spectrometry.

Eyers CE, Vonderach M, Ferries S, Jeacock K, Eyers PA.

Curr Opin Chem Biol. 2018 Feb;42:167-176. doi: 10.1016/j.cbpa.2017.12.013. Epub 2018 Jan 11. Review.

11.
12.

New Perspectives, Opportunities, and Challenges in Exploring the Human Protein Kinome.

Wilson LJ, Linley A, Hammond DE, Hood FE, Coulson JM, MacEwan DJ, Ross SJ, Slupsky JR, Smith PD, Eyers PA, Prior IA.

Cancer Res. 2018 Jan 1;78(1):15-29. doi: 10.1158/0008-5472.CAN-17-2291. Epub 2017 Dec 18. Review.

PMID:
29254998
13.

Kinome-wide transcriptional profiling of uveal melanoma reveals new vulnerabilities to targeted therapeutics.

Bailey FP, Clarke K, Kalirai H, Kenyani J, Shahidipour H, Falciani F, Coulson JM, Sacco JJ, Coupland SE, Eyers PA.

Pigment Cell Melanoma Res. 2018 Mar;31(2):253-266. doi: 10.1111/pcmr.12650. Epub 2017 Oct 15.

PMID:
28972303
14.

Plk4 and Aurora A cooperate in the initiation of acentriolar spindle assembly in mammalian oocytes.

Bury L, Coelho PA, Simeone A, Ferries S, Eyers CE, Eyers PA, Zernicka-Goetz M, Glover DM.

J Cell Biol. 2017 Nov 6;216(11):3571-3590. doi: 10.1083/jcb.201606077. Epub 2017 Sep 28.

15.

Live and let die: insights into pseudoenzyme mechanisms from structure.

Murphy JM, Mace PD, Eyers PA.

Curr Opin Struct Biol. 2017 Dec;47:95-104. doi: 10.1016/j.sbi.2017.07.004. Epub 2017 Aug 5. Review.

PMID:
28787627
16.

Evaluation of Parameters for Confident Phosphorylation Site Localization Using an Orbitrap Fusion Tribrid Mass Spectrometer.

Ferries S, Perkins S, Brownridge PJ, Campbell A, Eyers PA, Jones AR, Eyers CE.

J Proteome Res. 2017 Sep 1;16(9):3448-3459. doi: 10.1021/acs.jproteome.7b00337. Epub 2017 Aug 11.

17.

Local protein kinase A action proceeds through intact holoenzymes.

Smith FD, Esseltine JL, Nygren PJ, Veesler D, Byrne DP, Vonderach M, Strashnov I, Eyers CE, Eyers PA, Langeberg LK, Scott JD.

Science. 2017 Jun 23;356(6344):1288-1293. doi: 10.1126/science.aaj1669.

18.

Bio-Zombie: the rise of pseudoenzymes in biology.

Murphy JM, Farhan H, Eyers PA.

Biochem Soc Trans. 2017 Apr 15;45(2):537-544. doi: 10.1042/BST20160400. Review.

PMID:
28408493
19.

Pseudokinases: update on their functions and evaluation as new drug targets.

Byrne DP, Foulkes DM, Eyers PA.

Future Med Chem. 2017 Jan;9(2):245-265. doi: 10.4155/fmc-2016-0207. Epub 2017 Jan 18. Review.

20.

DRP-1 is required for BH3 mimetic-mediated mitochondrial fragmentation and apoptosis.

Milani M, Byrne DP, Greaves G, Butterworth M, Cohen GM, Eyers PA, Varadarajan S.

Cell Death Dis. 2017 Jan 12;8(1):e2552. doi: 10.1038/cddis.2016.485.

21.

Mitotic phosphotyrosine network analysis reveals that tyrosine phosphorylation regulates Polo-like kinase 1 (PLK1).

Caron D, Byrne DP, Thebault P, Soulet D, Landry CR, Eyers PA, Elowe S.

Sci Signal. 2016 Dec 13;9(458):rs14.

PMID:
27965426
22.

Tribbles in the 21st Century: The Evolving Roles of Tribbles Pseudokinases in Biology and Disease.

Eyers PA, Keeshan K, Kannan N.

Trends Cell Biol. 2017 Apr;27(4):284-298. doi: 10.1016/j.tcb.2016.11.002. Epub 2016 Nov 28. Review.

23.
24.

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.

25.

KinView: a visual comparative sequence analysis tool for integrated kinome research.

McSkimming DI, Dastgheib S, Baffi TR, Byrne DP, Ferries S, Scott ST, Newton AC, Eyers CE, Kochut KJ, Eyers PA, Kannan N.

Mol Biosyst. 2016 Nov 15;12(12):3651-3665.

26.
27.

Human TRIB2 Oscillates during the Cell Cycle and Promotes Ubiquitination and Degradation of CDC25C.

Liang KL, Paredes R, Carmody R, Eyers PA, Meyer S, McCarthy TV, Keeshan K.

Int J Mol Sci. 2016 Aug 23;17(9). pii: E1378. doi: 10.3390/ijms17091378.

28.

Correction: Hydrophobic Core Variations Provide a Structural Framework for Tyrosine Kinase Evolution and Functional Specialization.

Mohanty S, Oruganty K, Kwon A, Byrne DP, Ferries S, Ruan Z, Hanold LE, Katiyar S, Kennedy EJ, Eyers PA, Kannan N.

PLoS Genet. 2016 Aug 11;12(8):e1006265. doi: 10.1371/journal.pgen.1006265. eCollection 2016 Aug.

29.

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.

30.

cAMP-dependent protein kinase (PKA) complexes probed by complementary differential scanning fluorimetry and ion mobility-mass spectrometry.

Byrne DP, Vonderach M, Ferries S, Brownridge PJ, Eyers CE, Eyers PA.

Biochem J. 2016 Oct 1;473(19):3159-75. doi: 10.1042/BCJ20160648. Epub 2016 Jul 21.

31.

Human CDK18 promotes replication stress signaling and genome stability.

Barone G, Staples CJ, Ganesh A, Patterson KW, Bryne DP, Myers KN, Patil AA, Eyers CE, Maslen S, Skehel JM, Eyers PA, Collis SJ.

Nucleic Acids Res. 2016 Oct 14;44(18):8772-8785. Epub 2016 Jul 5.

32.

Hydrophobic Core Variations Provide a Structural Framework for Tyrosine Kinase Evolution and Functional Specialization.

Mohanty S, Oruganty K, Kwon A, Byrne DP, Ferries S, Ruan Z, Hanold LE, Katiyar S, Kennedy EJ, Eyers PA, Kannan N.

PLoS Genet. 2016 Feb 29;12(2):e1005885. doi: 10.1371/journal.pgen.1005885. eCollection 2016 Feb. Erratum in: PLoS Genet. 2016 Aug;12(8):e1006265.

33.

TRIBBLES: A Twist in the Pseudokinase Tail.

Eyers PA.

Structure. 2015 Nov 3;23(11):1974-6. doi: 10.1016/j.str.2015.10.003.

34.

Tribbles pseudokinases: novel targets for chemical biology and drug discovery?

Foulkes DM, Byrne DP, Bailey FP, Eyers PA.

Biochem Soc Trans. 2015 Oct;43(5):1095-103. doi: 10.1042/BST20150109. Review.

PMID:
26517930
35.

Centrin 3 is an inhibitor of centrosomal Mps1 and antagonizes centrin 2 function.

Sawant DB, Majumder S, Perkins JL, Yang CH, Eyers PA, Fisk HA.

Mol Biol Cell. 2015 Nov 1;26(21):3741-53. doi: 10.1091/mbc.E14-07-1248. Epub 2015 Sep 9.

36.

TD-60 links RalA GTPase function to the CPC in mitosis.

Papini D, Langemeyer L, Abad MA, Kerr A, Samejima I, Eyers PA, Jeyaprakash AA, Higgins JM, Barr FA, Earnshaw WC.

Nat Commun. 2015 Jul 9;6:7678. doi: 10.1038/ncomms8678.

37.

2) Going for broke: targeting the human cancer pseudokinome.

Bailey FP, Byrne DP, McSkimming D, Kannan N, Eyers PA.

Biochem J. 2015 Feb 15;466(1):201. No abstract available.

PMID:
25656056
38.

The Tribbles 2 (TRB2) pseudokinase binds to ATP and autophosphorylates in a metal-independent manner.

Bailey FP, Byrne DP, Oruganty K, Eyers CE, Novotny CJ, Shokat KM, Kannan N, Eyers PA.

Biochem J. 2015 Apr 1;467(1):47-62. doi: 10.1042/BJ20141441.

39.

Going for broke: targeting the human cancer pseudokinome.

Bailey FP, Byrne DP, McSkimming D, Kannan N, Eyers PA.

Biochem J. 2015 Jan 15;465(2):195-211. doi: 10.1042/BJ20141060. Review. Erratum in: Biochem J. 2015 Feb 15;466(1):201.

PMID:
25559089
40.

The resistance tetrad: amino acid hotspots for kinome-wide exploitation of drug-resistant protein kinase alleles.

Bailey FP, Andreev VI, Eyers PA.

Methods Enzymol. 2014;548:117-46. doi: 10.1016/B978-0-12-397918-6.00005-7. Review.

PMID:
25399644
41.

DNA replication stress in CHK1-depleted tumour cells triggers premature (S-phase) mitosis through inappropriate activation of Aurora kinase B.

Zuazua-Villar P, Rodriguez R, Gagou ME, Eyers PA, Meuth M.

Cell Death Dis. 2014 May 22;5:e1253. doi: 10.1038/cddis.2014.231.

42.

Day of the dead: pseudokinases and pseudophosphatases in physiology and disease.

Reiterer V, Eyers PA, Farhan H.

Trends Cell Biol. 2014 Sep;24(9):489-505. doi: 10.1016/j.tcb.2014.03.008. Epub 2014 May 10. Review.

PMID:
24818526
43.

A robust methodology to subclassify pseudokinases based on their nucleotide-binding properties.

Murphy JM, Zhang Q, Young SN, Reese ML, Bailey FP, Eyers PA, Ungureanu D, Hammaren H, Silvennoinen O, Varghese LN, Chen K, Tripaydonis A, Jura N, Fukuda K, Qin J, Nimchuk Z, Mudgett MB, Elowe S, Gee CL, Liu L, Daly RJ, Manning G, Babon JJ, Lucet IS.

Biochem J. 2014 Jan 15;457(2):323-34. doi: 10.1042/BJ20131174.

44.

Dawn of the dead: protein pseudokinases signal new adventures in cell biology.

Eyers PA, Murphy JM.

Biochem Soc Trans. 2013 Aug;41(4):969-74. doi: 10.1042/BST20130115. Review.

PMID:
23863165
45.

Rheostat-ing mitosis.

Eyers PA.

Chem Biol. 2013 Feb 21;20(2):142-3. doi: 10.1016/j.chembiol.2013.02.001.

46.

A framework for identification of actionable cancer genome dependencies in small cell lung cancer.

Sos ML, Dietlein F, Peifer M, Schöttle J, Balke-Want H, Müller C, Koker M, Richters A, Heynck S, Malchers F, Heuckmann JM, Seidel D, Eyers PA, Ullrich RT, Antonchick AP, Vintonyak VV, Schneider PM, Ninomiya T, Waldmann H, Büttner R, Rauh D, Heukamp LC, Thomas RK.

Proc Natl Acad Sci U S A. 2012 Oct 16;109(42):17034-9. doi: 10.1073/pnas.1207310109. Epub 2012 Oct 3.

47.

Aurora A and Aurora B jointly coordinate chromosome segregation and anaphase microtubule dynamics.

Hégarat N, Smith E, Nayak G, Takeda S, Eyers PA, Hochegger H.

J Cell Biol. 2011 Dec 26;195(7):1103-13. doi: 10.1083/jcb.201105058. Epub 2011 Dec 19.

48.

Protein kinase A is central for forward transport of two-pore domain potassium channels K2P3.1 and K2P9.1.

Mant A, Elliott D, Eyers PA, O'Kelly IM.

J Biol Chem. 2011 Apr 22;286(16):14110-9. doi: 10.1074/jbc.M110.190702. Epub 2011 Feb 28.

49.

Drug-resistant aurora A mutants for cellular target validation of the small molecule kinase inhibitors MLN8054 and MLN8237.

Sloane DA, Trikic MZ, Chu ML, Lamers MB, Mason CS, Mueller I, Savory WJ, Williams DH, Eyers PA.

ACS Chem Biol. 2010 Jun 18;5(6):563-76. doi: 10.1021/cb100053q.

PMID:
20426425
50.

Biophysical and X-ray crystallographic analysis of Mps1 kinase inhibitor complexes.

Chu ML, Lang Z, Chavas LM, Neres J, Fedorova OS, Tabernero L, Cherry M, Williams DH, Douglas KT, Eyers PA.

Biochemistry. 2010 Mar 2;49(8):1689-701. doi: 10.1021/bi901970c.

PMID:
20099905

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