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Items: 1 to 50 of 89

1.

Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders.

Rageot D, Bohnacker T, Melone A, Langlois JB, Borsari C, Hillmann P, Sele AM, Beaufils F, Zvelebil M, Hebeisen P, Loescher W, Burke JE, Fabbro D, Wymann MP.

J Med Chem. 2018 Oct 25. doi: 10.1021/acs.jmedchem.8b01262. [Epub ahead of print]

PMID:
30359003
2.

Erratum for Brunschwig et al., "UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria".

Brunschwig C, Lawrence N, Taylor D, Abay E, Njoroge M, Basarab GS, Le Manach C, Paquet T, Gonzàlez Cabrera D, Nchinda AT, de Kock C, Wiesner L, Denti P, Waterson D, Blasco B, Leroy D, Witty MJ, Donini C, Duffy J, Wittlin S, White KL, Charman SA, Jiménez-Díaz MB, Angulo-Barturen I, Herreros E, Gamo FJ, Rochford R, Mancama D, Coetzer TL, van der Watt ME, Reader J, Birkholtz LM, Marsh KC, Solapure SM, Burke JE, McPhail JA, Vanaerschot M, Fidock DA, Fish PV, Siegl P, Smith DA, Wirjanata G, Noviyanti R, Price RN, Marfurt J, Silue KD, Street LJ, Chibale K.

Antimicrob Agents Chemother. 2018 Oct 24;62(11). pii: e01941-18. doi: 10.1128/AAC.01941-18. Print 2018 Nov. No abstract available.

PMID:
30355750
3.

Structural and mechanistic insights into the function of the unconventional class XIV myosin MyoA from Toxoplasma gondii.

Powell CJ, Ramaswamy R, Kelsen A, Hamelin DJ, Warshaw DM, Bosch J, Burke JE, Ward GE, Boulanger MJ.

Proc Natl Acad Sci U S A. 2018 Nov 6;115(45):E10548-E10555. doi: 10.1073/pnas.1811167115. Epub 2018 Oct 22.

PMID:
30348763
4.

Endo-fucoidan hydrolases from glycoside hydrolase family 107 (GH107) display structural and mechanistic similarities to α-L-fucosidases from GH29.

Vickers C, Liu F, Abe K, Salama-Alber O, Jenkins ML, Springate CM, Burke JE, Withers SG, Boraston AB.

J Biol Chem. 2018 Oct 3. pii: jbc.RA118.005134. doi: 10.1074/jbc.RA118.005134. [Epub ahead of print]

5.

Structural determinants of Rab11 activation by the guanine nucleotide exchange factor SH3BP5.

Jenkins ML, Margaria JP, Stariha JTB, Hoffmann RM, McPhail JA, Hamelin DJ, Boulanger MJ, Hirsch E, Burke JE.

Nat Commun. 2018 Sep 14;9(1):3772. doi: 10.1038/s41467-018-06196-z.

6.

Structural Basis for Regulation of Phosphoinositide Kinases and Their Involvement in Human Disease.

Burke JE.

Mol Cell. 2018 Sep 6;71(5):653-673. doi: 10.1016/j.molcel.2018.08.005. Review.

PMID:
30193094
7.

Pathogenic TFG Mutations Underlying Hereditary Spastic Paraplegia Impair Secretory Protein Trafficking and Axon Fasciculation.

Slosarek EL, Schuh AL, Pustova I, Johnson A, Bird J, Johnson M, Frankel EB, Bhattacharya N, Hanna MG, Burke JE, Ruhl DA, Quinney K, Block S, Peotter JL, Chapman ER, Sheets MD, Butcher SE, Stagg SM, Audhya A.

Cell Rep. 2018 Aug 28;24(9):2248-2260. doi: 10.1016/j.celrep.2018.07.081.

8.

Brr6 plays a role in gene recruitment and transcriptional regulation at the nuclear envelope.

Kops AB, Burke JE, Guthrie C.

Mol Biol Cell. 2018 Oct 15;29(21):2578-2590. doi: 10.1091/mbc.E18-04-0258. Epub 2018 Aug 22.

PMID:
30133335
9.

Probing the Architecture, Dynamics, and Inhibition of the PI4KIIIα/TTC7/FAM126 Complex.

Dornan GL, Dalwadi U, Hamelin DJ, Hoffmann RM, Yip CK, Burke JE.

J Mol Biol. 2018 Sep 14;430(18 Pt B):3129-3142. doi: 10.1016/j.jmb.2018.07.020. Epub 2018 Jul 18.

PMID:
30031006
10.

UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria.

Brunschwig C, Lawrence N, Taylor D, Abay E, Njoroge M, Basarab GS, Le Manach C, Paquet T, Cabrera DG, Nchinda AT, de Kock C, Wiesner L, Denti P, Waterson D, Blasco B, Leroy D, Witty MJ, Donini C, Duffy J, Wittlin S, White KL, Charman SA, Jiménez-Díaz MB, Angulo-Barturen I, Herreros E, Gamo FJ, Rochford R, Mancama D, Coetzer TL, van der Watt ME, Reader J, Birkholtz LM, Marsh KC, Solapure SM, Burke JE, McPhail JA, Vanaerschot M, Fidock DA, Fish PV, Siegl P, Smith DA, Wirjanata G, Noviyanti R, Price RN, Marfurt J, Silue KD, Street LJ, Chibale K.

Antimicrob Agents Chemother. 2018 Aug 27;62(9). pii: e00012-18. doi: 10.1128/AAC.00012-18. Print 2018 Sep. Erratum in: Antimicrob Agents Chemother. 2018 Oct 24;62(11):.

PMID:
29941635
11.

Spliceosome Profiling Visualizes Operations of a Dynamic RNP at Nucleotide Resolution.

Burke JE, Longhurst AD, Merkurjev D, Sales-Lee J, Rao B, Moresco JJ, Yates JR 3rd, Li JJ, Madhani HD.

Cell. 2018 May 3;173(4):1014-1030.e17. doi: 10.1016/j.cell.2018.03.020.

PMID:
29727661
12.

Conformational sampling of membranes by Akt controls its activation and inactivation.

Lučić I, Rathinaswamy MK, Truebestein L, Hamelin DJ, Burke JE, Leonard TA.

Proc Natl Acad Sci U S A. 2018 Apr 24;115(17):E3940-E3949. doi: 10.1073/pnas.1716109115. Epub 2018 Apr 9.

13.

Molecular Mechanisms of Human Disease Mediated by Oncogenic and Primary Immunodeficiency Mutations in Class IA Phosphoinositide 3-Kinases.

Dornan GL, Burke JE.

Front Immunol. 2018 Mar 19;9:575. doi: 10.3389/fimmu.2018.00575. eCollection 2018. Review.

14.

An intrinsic lipid-binding interface controls sphingosine kinase 1 function.

Pulkoski-Gross MJ, Jenkins ML, Truman JP, Salama MF, Clarke CJ, Burke JE, Hannun YA, Obeid LM.

J Lipid Res. 2018 Mar;59(3):462-474. doi: 10.1194/jlr.M081307. Epub 2018 Jan 11.

PMID:
29326159
15.

Novel K-Ras G12C Switch-II Covalent Binders Destabilize Ras and Accelerate Nucleotide Exchange.

Nnadi CI, Jenkins ML, Gentile DR, Bateman LA, Zaidman D, Balius TE, Nomura DK, Burke JE, Shokat KM, London N.

J Chem Inf Model. 2018 Feb 26;58(2):464-471. doi: 10.1021/acs.jcim.7b00399. Epub 2018 Jan 31.

16.

Ras Binder Induces a Modified Switch-II Pocket in GTP and GDP States.

Gentile DR, Rathinaswamy MK, Jenkins ML, Moss SM, Siempelkamp BD, Renslo AR, Burke JE, Shokat KM.

Cell Chem Biol. 2017 Dec 21;24(12):1455-1466.e14. doi: 10.1016/j.chembiol.2017.08.025. Epub 2017 Oct 12.

PMID:
29033317
17.

Dissecting the molecular assembly of the Toxoplasma gondii MyoA motility complex.

Powell CJ, Jenkins ML, Parker ML, Ramaswamy R, Kelsen A, Warshaw DM, Ward GE, Burke JE, Boulanger MJ.

J Biol Chem. 2017 Nov 24;292(47):19469-19477. doi: 10.1074/jbc.M117.809632. Epub 2017 Sep 25.

PMID:
28972141
18.

An overview of hydrogen deuterium exchange mass spectrometry (HDX-MS) in drug discovery.

Masson GR, Jenkins ML, Burke JE.

Expert Opin Drug Discov. 2017 Oct;12(10):981-994. doi: 10.1080/17460441.2017.1363734. Epub 2017 Aug 17. Review.

PMID:
28770632
19.

Expanding the Scope of Electrophiles Capable of Targeting K-Ras Oncogenes.

McGregor LM, Jenkins ML, Kerwin C, Burke JE, Shokat KM.

Biochemistry. 2017 Jun 27;56(25):3178-3183. doi: 10.1021/acs.biochem.7b00271. Epub 2017 Jun 16.

20.

Molecular mechanism of activation of class IA phosphoinositide 3-kinases (PI3Ks) by membrane-localized HRas.

Siempelkamp BD, Rathinaswamy MK, Jenkins ML, Burke JE.

J Biol Chem. 2017 Jul 21;292(29):12256-12266. doi: 10.1074/jbc.M117.789263. Epub 2017 May 17.

21.

Novel PIK3CD mutations affecting N-terminal residues of p110δ cause activated PI3Kδ syndrome (APDS) in humans.

Takeda AJ, Zhang Y, Dornan GL, Siempelkamp BD, Jenkins ML, Matthews HF, McElwee JJ, Bi W, Seeborg FO, Su HC, Burke JE, Lucas CL.

J Allergy Clin Immunol. 2017 Oct;140(4):1152-1156.e10. doi: 10.1016/j.jaci.2017.03.026. Epub 2017 Apr 13. No abstract available.

22.

Deconvolution of Buparlisib's mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention.

Bohnacker T, Prota AE, Beaufils F, Burke JE, Melone A, Inglis AJ, Rageot D, Sele AM, Cmiljanovic V, Cmiljanovic N, Bargsten K, Aher A, Akhmanova A, Díaz JF, Fabbro D, Zvelebil M, Williams RL, Steinmetz MO, Wymann MP.

Nat Commun. 2017 Mar 9;8:14683. doi: 10.1038/ncomms14683.

23.

Conformational disruption of PI3Kδ regulation by immunodeficiency mutations in PIK3CD and PIK3R1.

Dornan GL, Siempelkamp BD, Jenkins ML, Vadas O, Lucas CL, Burke JE.

Proc Natl Acad Sci U S A. 2017 Feb 21;114(8):1982-1987. doi: 10.1073/pnas.1617244114. Epub 2017 Feb 6.

24.

Recognition of protein-linked glycans as a determinant of peptidase activity.

Noach I, Ficko-Blean E, Pluvinage B, Stuart C, Jenkins ML, Brochu D, Buenbrazo N, Wakarchuk W, Burke JE, Gilbert M, Boraston AB.

Proc Natl Acad Sci U S A. 2017 Jan 31;114(5):E679-E688. doi: 10.1073/pnas.1615141114. Epub 2017 Jan 17.

25.

Using Hydrogen-Deuterium Exchange Mass Spectrometry to Examine Protein-Membrane Interactions.

Vadas O, Jenkins ML, Dornan GL, Burke JE.

Methods Enzymol. 2017;583:143-172. doi: 10.1016/bs.mie.2016.09.008. Epub 2016 Oct 18. Review.

PMID:
28063489
26.

The Molecular Basis of Aichi Virus 3A Protein Activation of Phosphatidylinositol 4 Kinase IIIβ, PI4KB, through ACBD3.

McPhail JA, Ottosen EH, Jenkins ML, Burke JE.

Structure. 2017 Jan 3;25(1):121-131. doi: 10.1016/j.str.2016.11.016. Epub 2016 Dec 15.

27.

Regulation of a Coupled MARCKS-PI3K Lipid Kinase Circuit by Calmodulin: Single-Molecule Analysis of a Membrane-Bound Signaling Module.

Ziemba BP, Swisher GH, Masson G, Burke JE, Williams RL, Falke JJ.

Biochemistry. 2016 Nov 22;55(46):6395-6405. Epub 2016 Nov 10.

28.

Characterization of Atg38 and NRBF2, a fifth subunit of the autophagic Vps34/PIK3C3 complex.

Ohashi Y, Soler N, García Ortegón M, Zhang L, Kirsten ML, Perisic O, Masson GR, Burke JE, Jakobi AJ, Apostolakis AA, Johnson CM, Ohashi M, Ktistakis NT, Sachse C, Williams RL.

Autophagy. 2016 Nov;12(11):2129-2144. Epub 2016 Sep 14.

29.

Molecular basis of Lys11-polyubiquitin specificity in the deubiquitinase Cezanne.

Mevissen TET, Kulathu Y, Mulder MPC, Geurink PP, Maslen SL, Gersch M, Elliott PR, Burke JE, van Tol BDM, Akutsu M, Oualid FE, Kawasaki M, Freund SMV, Ovaa H, Komander D.

Nature. 2016 Oct 20;538(7625):402-405. doi: 10.1038/nature19836. Epub 2016 Oct 12.

30.

Diversity-oriented synthesis yields novel multistage antimalarial inhibitors.

Kato N, Comer E, Sakata-Kato T, Sharma A, Sharma M, Maetani M, Bastien J, Brancucci NM, Bittker JA, Corey V, Clarke D, Derbyshire ER, Dornan GL, Duffy S, Eckley S, Itoe MA, Koolen KM, Lewis TA, Lui PS, Lukens AK, Lund E, March S, Meibalan E, Meier BC, McPhail JA, Mitasev B, Moss EL, Sayes M, Van Gessel Y, Wawer MJ, Yoshinaga T, Zeeman AM, Avery VM, Bhatia SN, Burke JE, Catteruccia F, Clardy JC, Clemons PA, Dechering KJ, Duvall JR, Foley MA, Gusovsky F, Kocken CH, Marti M, Morningstar ML, Munoz B, Neafsey DE, Sharma A, Winzeler EA, Wirth DF, Scherer CA, Schreiber SL.

Nature. 2016 Oct 20;538(7625):344-349. doi: 10.1038/nature19804. Epub 2016 Sep 7.

31.

Molecular Basis for Recognition of the Cancer Glycobiomarker, LacdiNAc (GalNAc[β1→4]GlcNAc), by Wisteria floribunda Agglutinin.

Haji-Ghassemi O, Gilbert M, Spence J, Schur MJ, Parker MJ, Jenkins ML, Burke JE, van Faassen H, Young NM, Evans SV.

J Biol Chem. 2016 Nov 11;291(46):24085-24095. Epub 2016 Sep 6.

32.

Regulation of PI3K by PKC and MARCKS: Single-Molecule Analysis of a Reconstituted Signaling Pathway.

Ziemba BP, Burke JE, Masson G, Williams RL, Falke JJ.

Biophys J. 2016 Apr 26;110(8):1811-1825. doi: 10.1016/j.bpj.2016.03.001.

33.

Methods in the Study of PTEN Structure: X-Ray Crystallography and Hydrogen Deuterium Exchange Mass Spectrometry.

Masson GR, Burke JE, Williams RL.

Methods Mol Biol. 2016;1388:215-30. doi: 10.1007/978-1-4939-3299-3_14.

PMID:
27033079
34.

Design and Structural Characterization of Potent and Selective Inhibitors of Phosphatidylinositol 4 Kinase IIIβ.

Rutaganira FU, Fowler ML, McPhail JA, Gelman MA, Nguyen K, Xiong A, Dornan GL, Tavshanjian B, Glenn JS, Shokat KM, Burke JE.

J Med Chem. 2016 Mar 10;59(5):1830-9. doi: 10.1021/acs.jmedchem.5b01311. Epub 2016 Feb 26.

35.

Type III phosphatidylinositol 4 kinases: structure, function, regulation, signalling and involvement in disease.

Dornan GL, McPhail JA, Burke JE.

Biochem Soc Trans. 2016 Feb;44(1):260-6. doi: 10.1042/BST20150219. Review.

PMID:
26862213
36.

Using hydrogen deuterium exchange mass spectrometry to engineer optimized constructs for crystallization of protein complexes: Case study of PI4KIIIβ with Rab11.

Fowler ML, McPhail JA, Jenkins ML, Masson GR, Rutaganira FU, Shokat KM, Williams RL, Burke JE.

Protein Sci. 2016 Apr;25(4):826-39. doi: 10.1002/pro.2879. Epub 2016 Feb 1.

37.

Structural Analysis of Multi-Helical RNAs by NMR-SAXS/WAXS: Application to the U4/U6 di-snRNA.

Cornilescu G, Didychuk AL, Rodgers ML, Michael LA, Burke JE, Montemayor EJ, Hoskins AA, Butcher SE.

J Mol Biol. 2016 Feb 27;428(5 Pt A):777-789. doi: 10.1016/j.jmb.2015.11.026. Epub 2015 Dec 2.

38.

Global shape mimicry of tRNA within a viral internal ribosome entry site mediates translational reading frame selection.

Au HH, Cornilescu G, Mouzakis KD, Ren Q, Burke JE, Lee S, Butcher SE, Jan E.

Proc Natl Acad Sci U S A. 2015 Nov 24;112(47):E6446-55. doi: 10.1073/pnas.1512088112. Epub 2015 Nov 9.

39.

The intrinsically disordered tails of PTEN and PTEN-L have distinct roles in regulating substrate specificity and membrane activity.

Masson GR, Perisic O, Burke JE, Williams RL.

Biochem J. 2016 Jan 15;473(2):135-44. doi: 10.1042/BJ20150931. Epub 2015 Nov 2.

40.

Probing the dynamic regulation of peripheral membrane proteins using hydrogen deuterium exchange-MS (HDX-MS).

Vadas O, Burke JE.

Biochem Soc Trans. 2015 Oct;43(5):773-86. doi: 10.1042/BST20150065. Review.

PMID:
26517882
41.

Structure and flexibility of the endosomal Vps34 complex reveals the basis of its function on membranes.

Rostislavleva K, Soler N, Ohashi Y, Zhang L, Pardon E, Burke JE, Masson GR, Johnson C, Steyaert J, Ktistakis NT, Williams RL.

Science. 2015 Oct 9;350(6257):aac7365. doi: 10.1126/science.aac7365.

42.

Structural mechanisms of DNA binding and unwinding in bacterial RecQ helicases.

Manthei KA, Hill MC, Burke JE, Butcher SE, Keck JL.

Proc Natl Acad Sci U S A. 2015 Apr 7;112(14):4292-7. doi: 10.1073/pnas.1416746112. Epub 2015 Mar 23.

43.

Spliceosome assembly in the absence of stable U4/U6 RNA pairing.

Burke JE, Butcher SE, Brow DA.

RNA. 2015 May;21(5):923-34. doi: 10.1261/rna.048421.114. Epub 2015 Mar 11.

44.

Synergy in activating class I PI3Ks.

Burke JE, Williams RL.

Trends Biochem Sci. 2015 Feb;40(2):88-100. doi: 10.1016/j.tibs.2014.12.003. Epub 2015 Jan 5. Review.

PMID:
25573003
45.

The function of phosphatidylinositol 5-phosphate 4-kinase γ (PI5P4Kγ) explored using a specific inhibitor that targets the PI5P-binding site.

Clarke JH, Giudici ML, Burke JE, Williams RL, Maloney DJ, Marugan J, Irvine RF.

Biochem J. 2015 Mar 1;466(2):359-67. doi: 10.1042/BJ20141333.

46.

Structures of PI4KIIIβ complexes show simultaneous recruitment of Rab11 and its effectors.

Burke JE, Inglis AJ, Perisic O, Masson GR, McLaughlin SH, Rutaganira F, Shokat KM, Williams RL.

Science. 2014 May 30;344(6187):1035-8. doi: 10.1126/science.1253397.

47.

Molecular determinants of PI3Kγ-mediated activation downstream of G-protein-coupled receptors (GPCRs).

Vadas O, Dbouk HA, Shymanets A, Perisic O, Burke JE, Abi Saab WF, Khalil BD, Harteneck C, Bresnick AR, Nürnberg B, Backer JM, Williams RL.

Proc Natl Acad Sci U S A. 2013 Nov 19;110(47):18862-7. doi: 10.1073/pnas.1304801110. Epub 2013 Nov 4.

48.

Vesicular and non-vesicular transport feed distinct glycosylation pathways in the Golgi.

D'Angelo G, Uemura T, Chuang CC, Polishchuk E, Santoro M, Ohvo-Rekilä H, Sato T, Di Tullio G, Varriale A, D'Auria S, Daniele T, Capuani F, Johannes L, Mattjus P, Monti M, Pucci P, Williams RL, Burke JE, Platt FM, Harada A, De Matteis MA.

Nature. 2013 Sep 5;501(7465):116-20. doi: 10.1038/nature12423. Epub 2013 Aug 4.

PMID:
23913272
49.

PKCβ phosphorylates PI3Kγ to activate it and release it from GPCR control.

Walser R, Burke JE, Gogvadze E, Bohnacker T, Zhang X, Hess D, Küenzi P, Leitges M, Hirsch E, Williams RL, Laffargue M, Wymann MP.

PLoS Biol. 2013;11(6):e1001587. doi: 10.1371/journal.pbio.1001587. Epub 2013 Jun 25.

50.

Connecting with an old partner in a new way.

Burke JE, Williams RL.

Cancer Cell. 2013 May 13;23(5):559-61. doi: 10.1016/j.ccr.2013.04.023.

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