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Displaying 1 - 50 of 1099

2016

Corrigendum: Structural biology: HDAC6 finally crystal clear.
Liu Y, Li L, Min J
Nat. Chem. Biol.. 20.09.2016 12(10):885. doi: 10.1038/nchembio1016-885
PMID: 27649056

Hemi-methylated DNA regulates DNA methylation inheritance through allosteric activation of H3 ubiquitylation by UHRF1.
Harrison JS, Cornett EM, Goldfarb D, DaRosa PA, Li ZM, Yan F, Dickson BM, Guo AH, Cantu DV, Kaustov L, Brown PJ, Arrowsmith CH, Erie DA, Major MB, Klevit RE, Krajewski K, Kuhlman B, Strahl BD, Rothbart SB
Elife. 07.09.2016 5:. doi: 10.7554/eLife.17101
PMID: 27595565

Discovery of a Potent, Selective and Cell-active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6.
Shen Y, Szewczyk MM, Eram MS, Smil D, Kaniskan HÜ, de Freitas RF, Senisterra G, Li F, Schapira M, Brown PJ, Arrowsmith CH, Barsyte-Lovejoy D, Liu J, Vedadi M, Jin J
J. Med. Chem.. 01.09.2016 . doi: 10.1021/acs.jmedchem.6b01033
PMID: 27584694

Discovery of a Potent, Selective and Cell-active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6
Shen Y, Szewczyk MM, Eram MS, Smil D, Kaniskan HÜ, de Freitas RF, Senisterra G, Li F, Schapira M, Brown PJ, Arrowsmith CH, Barsyte-Lovejoy D, Liu J, Vedadi M, Jin J
J. Med. Chem.. 2016-9-1 . doi:
PMID: 27584694

A Suite of Biochemical Assays for Screening RNA Methyltransferase BCDIN3D.
Blazer LL, Li F, Kennedy S, Zheng YG, Arrowsmith CH, Vedadi M
J Biomol Screen. 31.08.2016 . doi: 10.1177/1087057116666276
PMID: 27581605

A Suite of Biochemical Assays for Screening RNA Methyltransferase BCDIN3D
Blazer LL, Li F, Kennedy S, Zheng YG, Arrowsmith CH, Vedadi M
J Biomol Screen. 2016-8-31 . doi:
PMID: 27581605

Chemical Inhibition of Protein Methyltransferases
Schapira M
Cell Chem Biol. 2016-8-24 . doi:
PMID: 27569753

Structural Basis of Intracellular TGF-β Signaling: Receptors and Smads.
Chaikuad, A; Bullock, AN;
Cold Spring Harbor perspectives in biology. 22.8.2016 :-. doi: 10.1101/cshperspect.a022111
PMID: 27549117

Structural biology: HDAC6 finally crystal clear.
Liu Y, Li L, Min J
Nat. Chem. Biol.. 18.08.2016 12(9):660-1. doi: 10.1038/nchembio.2158
PMID: 27538024

Salt-Inducible Kinase 2 Couples Ovarian Cancer Cell Metabolism with Survival at the Adipocyte-Rich Metastatic Niche.
Miranda, F; Mannion, D; Liu, S; Zheng, Y; Mangala, LS; Redondo, C; Herrero-Gonzalez, S; Xu, R; Taylor, C; Chedom, DF; Karaminejadranjbar, M; Albukhari, A; Jiang, D; Pradeep, S; Rodriguez-Aguayo, C; Lopez-Berestein, G; Salah, E; Abdul Azeez, KR; Elkins, JM; Campo, L; Myers, KA; Klotz, D; Bivona, S; Dhar, S; Bast, RC; Saya, H; Choi, HG; Gray, NS; Fischer, R; Kessler, BM; Yau, C; Sood, AK; Motohara, T; Knapp, S; Ahmed, AA;
Cancer Cell. 01.8.2016 30:273-289. doi:
PMID: 27478041

Structural basis of arginine asymmetrical dimethylation by PRMT6.
Wu H, Zheng W, Eram MS, Vhuiyan M, Dong A, Zeng H, He H, Brown P, Frankel A, Vedadi M, Luo M, Min J
Biochem. J.. 01.08.2016 . doi: 10.1042/BCJ20160537
PMID: 27480107

Structure-Activity Relationship Studies for Enhancer of Zeste Homologue 2 (EZH2) and Enhancer of Zeste Homologue 1 (EZH1) Inhibitors.
Yang X, Li F, Konze KD, Meslamani J, Ma A, Brown PJ, Zhou MM, Arrowsmith CH, Kaniskan HÜ, Vedadi M, Jin J
J. Med. Chem.. 28.07.2016 . doi: 10.1021/acs.jmedchem.6b00855
PMID: 27468126

New small molecule inhibitors of histone methyl transferase DOT1L with a nitrile as a non-traditional replacement for heavy halogen atoms.
Spurr SS, Bayle ED, Yu W, Li F, Tempel W, Vedadi M, Schapira M, Fish PV
Bioorg. Med. Chem. Lett.. 21.07.2016 . doi: 10.1016/j.bmcl.2016.07.041
PMID: 27485386

High resolution crystal structure of DPF3b in complex with an acetylated histone peptide.
Li W, Zhao A, Tempel W, Loppnau P, Liu Y
J. Struct. Biol.. 08.07.2016 . doi: 10.1016/j.jsb.2016.07.001
PMID: 27402533

Discovery of a Potent and Selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) Inhibitor by Virtual Screening.
Ferreira de Freitas R, Eram MS, Smil D, Szewczyk MM, Kennedy S, Brown PJ, Santhakumar V, Barsyte-Lovejoy D, Arrowsmith CH, Vedadi M, Schapira M
J. Med. Chem.. 08.07.2016 . doi: 10.1021/acs.jmedchem.6b00668
PMID: 27390919

Mapping the chemical chromatin reactivation landscape identifies BRD4-TAF1 cross-talk.
Sdelci, S; Lardeau, CH; Tallant, C; Klepsch, F; Klaiber, B; Bennett, J; Rathert, P; Schuster, M; Penz, T; Fedorov, O; Superti-Furga, G; Bock, C; Zuber, J; Huber, KV; Knapp, S; Müller, S; Kubicek, S;
Nature Chemical Biology. 01.7.2016 12:504-510. doi:
PMID: 27159579

Cardiac myosin light chain is phosphorylated by Ca2+/calmodulin-dependent and -independent kinase activities.
Chang, AN; Mahajan, P; Knapp, S; Barton, H; Sweeney, HL; Kamm, KE; Stull, JT;
Proceedings of the National Academy of Sciences of USA. 01.7.2016 113:E3824-E3833. doi:
PMID: 27325775

Advances and challenges in understanding histone demethylase biology.
Nowak, RP; Tumber, A; Johansson, C; Che, KH; Brennan, P; Owen, D; Oppermann, U;
Current Opinion in Chemical Biology. 29.6.2016 33:151-159. doi:
PMID: 27371875

Methyltransferase inhibitors for modulation of the epigenome and beyond.
Schapira M, Arrowsmith CH
Curr Opin Chem Biol. 16.06.2016 33:81-87. doi: 10.1016/j.cbpa.2016.05.030
PMID: 27318562

Structure and function of histone methylation-binding proteins in plants.
Liu Y, Min J
Biochem. J.. 15.06.2016 473(12):1663-80. doi: 10.1042/BCJ20160123
PMID: 27288029

Mammalian Glucose Transporter Activity Is Dependent upon Anionic and Conical Phospholipids.
Hresko, RC; Kraft, TE; Quigley, A; Carpenter, EP; Hruz, PW;
Journal of Biological Chemistry. 01.8.2016 291:17271-17282. doi:
PMID: 27302065

The BET inhibitor JQ1 selectively impairs tumour response to hypoxia and downregulates CA9 and angiogenesis in triple negative breast cancer.
da Motta, LL; Ledaki, I; Purshouse, K; Haider, S; De Bastiani, MA; Baban, D; Morotti, M; Steers, G; Wigfield, S; Bridges, E; Li, JL; Knapp, S; Ebner, D; Klamt, F; Harris, AL; McIntyre, A;
Oncogene. 13.6.2016 :-. doi:
PMID: 27292261

Functional interdependence of BRD4 and DOT1L in MLL leukemia.
Gilan O, Lam EY, Becher I, Lugo D, Cannizzaro E, Joberty G, Ward A, Wiese M, Fong CY, Ftouni S, Tyler D, Stanley K, MacPherson L, Weng CF, Chan YC, Ghisi M, Smil D, Carpenter C, Brown P, Garton N, Blewitt ME, Bannister AJ, Kouzarides T, Huntly BJ, Johnstone RW, Drewes G, Dawson SJ, Arrowsmith CH, Grandi P, Prinjha RK, Dawson MA
Nat. Struct. Mol. Biol.. 13.06.2016 . doi: 10.1038/nsmb.3249
PMID: 27294782

SET9-Mediated Regulation of TGF-β Signaling Links Protein Methylation to Pulmonary Fibrosis.
Elkouris M, Kontaki H, Stavropoulos A, Antonoglou A, Nikolaou KC, Samiotaki M, Szantai E, Saviolaki D, Brown PJ, Sideras P, Panayotou G, Talianidis I
Cell Rep. 08.06.2016 . doi: 10.1016/j.celrep.2016.05.051
PMID: 27292644

Structure-Based Design of Tetrahydroisoquinoline-7-carboxamides as Selective Discoidin Domain Receptor 1 (DDR1) Inhibitors.
Wang, Z; Bian, H; Bartual, SG; Du, W; Luo, J; Zhao, H; Zhang, S; Mo, C; Zhou, Y; Xu, Y; Tu, Z; Ren, X; Lu, X; Brekken, RA; Yao, L; Bullock, AN; Su, J; Ding, K;
Journal of Medicinal Chemistry. 01.6.2016 59:5911-5916. doi:
PMID: 27219676

Structural Basis of the Recruitment of Ubiquitin-Specific Protease USP15 by Spliceosome Recycling Factor SART3.
Zhang Q, Harding R, Hou F, Dong A, Walker JR, Bteich J, Tong Y
J. Biol. Chem.. 02.06.2016 . doi: 10.1074/jbc.M116.740787
PMID: 27255711

Polymodal activation of the TREK-2 K2P channel produces structurally distinct open states.
McClenaghan, C; Schewe, M; Aryal, P; Carpenter, EP; Baukrowitz, T; Tucker, SJ;
Journal of General Physiology. 01.6.2016 147:497-505. doi:
PMID: 27241700

BET inhibition as a new strategy for the treatment of gastric cancer.
Montenegro, RC; Clark, PG; Howarth, A; Wan, X; Ceroni, A; Siejka, P; Nunez-Alonso, GA; Monteiro, O; Rogers, C; Gamble, V; Burbano, R; Brennan, PE; Tallant, C; Ebner, D; Fedorov, O; O'Neill, E; Knapp, S; Dixon, D; Müller, S;
Oncotarget. 01.6.2016 :-. doi:
PMID: 27259267

From structural biology to designing therapy for inborn errors of metabolism.
Yue WW
Journal of Inherited Metabolic Disease. 01.7.2016 39:489-498. doi:
PMID: 27240455

PHF13 is a molecular reader and transcriptional co-regulator of H3K4me2/3.
Chung HR, Xu C, Fuchs A, Mund A, Lange M, Staege H, Schubert T, Bian C, Dunkel I, Eberharter A, Regnard C, Klinker H, Meierhofer D, Cozzuto L, Winterpacht A, DiCroce L, Min J, Will H, Kinkley S
Elife. 25.05.2016 5:. doi: 10.7554/eLife.10607
PMID: 27223324

Protein-Protein Interaction Inhibition (2P2I)-Oriented Chemical Library Accelerates Hit Discovery.
Milhas, S; Raux, B; Betzi, S; Derviaux, C; Roche, P; Restouin, A; Basse, MJ; Rebuffet, E; Lugari, A; Badol, M; Kashyap, R; Lissitzky, JC; Eydoux, C; Hamon, V; Gourdel, ME; Combes, S; Zimmermann, P; Aurrand-Lions, M; Roux, T; Rogers, C; Müller, S; Knapp, S; Trinquet, E; Collette, Y; Guillemot, JC; Morelli, X;
ACS Chemical Biology. 01.8.2016 11:2140-2148. doi:
PMID: 27219844

CIS is a potent checkpoint in NK cell-mediated tumor immunity.
Delconte, RB; Kolesnik, TB; Dagley, LF; Rautela, J; Shi, W; Putz, EM; Stannard, K; Zhang, JG; Teh, C; Firth, M; Ushiki, T; Andoniou, CE; Degli-Esposti, MA; Sharp, PP; Sanvitale, CE; Infusini, G; Liau, NP; Linossi, EM; Burns, CJ; Carotta, S; Gray, DH; Seillet, C; Hutchinson, DS; Belz, GT; Webb, AI; Alexander, WS; Li, SS; Bullock, AN; Babon, JJ; Smyth, MJ; Nicholson, SE; Huntington, ND;
Nature Immunology. 01.7.2016 17:816-824. doi:
PMID: 27213690

Structural analysis of human KDM5B guides histone demethylase inhibitor development.
Johansson, C; Velupillai, S; Tumber, A; Szykowska, A; Hookway, ES; Nowak, RP; Strain-Damerell, C; Gileadi, C; Philpott, M; Burgess-Brown, N; Wu, N; Kopec, J; Nuzzi, A; Steuber, H; Egner, U; Badock, V; Munro, S; LaThangue, NB; Westaway, S; Brown, J; Athanasou, N; Prinjha, R; Brennan, PE; Oppermann, U;
Nature Chemical Biology. 01.7.2016 12:539-545. doi:
PMID: 27214403

An Integrative Proteomic Approach Identifies Novel Cellular SMYD2 Substrates.
Ahmed H, Duan S, Arrowsmith CH, Barsyte-Lovejoy D, Schapira M
J. Proteome Res.. 10.05.2016 . doi: 10.1021/acs.jproteome.6b00220
PMID: 27163177

Global Profiling of Acetyltransferase Feedback Regulation.
Montgomery DC, Garlick J, Kulkarni RA, Kennedy S, Allali-Hassani A, Kuo YM, Andrews AJ, Wu H, Vedadi M, Meier JL
J. Am. Chem. Soc.. 05.05.2016 . doi: 10.1021/jacs.6b03036
PMID: 27149119

Regulatory barriers to the advancement of precision medicine
Pettitt, D; Smith, J; Meadows, N; Arshad, Z; Schuh, A; DiGiusto, D; Bountra, C; Holländer, G; Barker, R; Brindley, D;
. 3.5.2016 1:319-329. doi: 10.1080/23808993.2016.1176526
PMID:

Co-crystal structures of the protein kinase haspin with bisubstrate inhibitors.
Lavogina, D; Kestav, K; Chaikuad, A; Heroven, C; Knapp, S; Uri, A;
Acta Crystallographica Section F: Structural Biology Communications. 01.5.2016 72:339-345. doi:
PMID: 27139824

PR Domain-Containing Protein 7 (PRDM7) is a Histone 3 Lysine 4 Trimethyltransferase.
Blazer LL, Lima-Fernandes E, Gibson E, Eram MS, Loppnau P, Arrowsmith CH, Schapira M, Vedadi M
J. Biol. Chem.. 29.04.2016 . doi: 10.1074/jbc.M116.721472
PMID: 27129774

Using a Genetically Encoded Sensor to Identify Inhibitors of Toxoplasma gondii Ca2+ Signalling.
Sidik SM, Hortua Triana MA, Paul AS, El Bakkouri M, Hackett CG, Tran F, Westwood NJ, Hui R, Zuercher WJ, Duraisingh MT, Moreno SN, Lourido S
J. Biol. Chem.. 29.04.2016 . doi: 10.1074/jbc.M115.703546
PMID: 26933036

Identification and Development of 2,3-Dihydropyrrolo[1,2-a]quinazolin-5(1H)-one Inhibitors Targeting Bromodomains within the Switch/Sucrose Nonfermenting Complex.
Sutherell, CL; Tallant, C; Monteiro, OP; Yapp, C; Fuchs, JE; Fedorov, O; Siejka, P; Müller, S; Knapp, S; Brenton, JD; Brennan, PE; Ley, SV;
Journal of Medicinal Chemistry. 01.5.2016 59:5095-5101. doi:
PMID: 27119626

Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit.
Gerstenberger, BS; Trzupek, JD; Tallant, C; Fedorov, O; Filippakopoulos, P; Brennan, PE; Fedele, V; Martin, S; Picaud, S; Rogers, C; Parikh, M; Taylor, A; Samas, B; O'Mahony, A; Berg, E; Pallares, G; Torrey, AD; Treiber, DK; Samardjiev, IJ; Nasipak, BT; Padilla-Benavides, T; Wu, Q; Imbalzano, AN; Nickerson, JA; Bunnage, ME; Müller, S; Knapp, S; Owen, DR;
Journal of Medicinal Chemistry. 01.5.2016 59:4800-4811. doi:
PMID: 27115555

Discovery and Characterization of a Highly Potent and Selective Aminopyrazoline-Based in vivo Probe (BAY-598) for the Protein Lysine Methyltransferase SMYD2.
Eggert E, Hillig RC, Köhr S, Stöckigt D, Weiske J, Barak N, Mowat J, Brumby T, Christ CD, Ter Laak A, Lang T, Fernández-Montalván AE, Badock V, Weinmann H, Hartung IV, Barsyte-Lovejoy D, Szewczyk M, Kennedy S, Li F, Vedadi M, Brown PJ, Santhakumar V, Arrowsmith CH, Stellfeld T, Stresemann C
J. Med. Chem.. 13.04.2016 . doi: 10.1021/acs.jmedchem.5b01890
PMID: 27075367

Structural basis for ligand-dependent dimerization of phenylalanine hydroxylase regulatory domain.
Patel, D; Kopec, J; Fitzpatrick, F; McCorvie, TJ; Yue, WW;
Scientific Reports. 01.1.2016 6:23748-. doi:
PMID: 27049649

Outcome of the First wwPDB/CCDC/D3R Ligand Validation Workshop.
Adams PD, Aertgeerts K, Bauer C, Bell JA, Berman HM, Bhat TN, Blaney JM, Bolton E, Bricogne G, Brown D, Burley SK, Case DA, Clark KL, Darden T, Emsley P, Feher VA, Feng Z, Groom CR, Harris SF, Hendle J, Holder T, Joachimiak A, Kleywegt GJ, Krojer T, Marcotrigiano J, Mark AE, Markley JL, Miller M, Minor W, Montelione GT, Murshudov G, Nakagawa A, Nakamura H, Nicholls A, Nicklaus M, Nolte RT, Padyana AK, Peishoff CE, Pieniazek S, Read RJ, Shao C, Sheriff S, Smart O, Soisson S, Spurlino J, Stouch T, Svobodova R, Tempel W, Terwilliger TC, Tronrud D, Velankar S, Ward SC, Warren GL, Westbrook JD, Williams P, Yang H, Young J
Structure. 05.04.2016 24(4):502-8. doi: 10.1016/j.str.2016.02.017
PMID: 27050687

Discovery of pyrido[3,4-g]quinazoline derivatives as CMGC family protein kinase inhibitors: Design, synthesis, inhibitory potency and X-ray co-crystal structure.
Esvan, YJ; Zeinyeh, W; Boibessot, T; Nauton, L; Théry, V; Knapp, S; Chaikuad, A; Loaëc, N; Meijer, L; Anizon, F; Giraud, F; Moreau, P;
European Journal of Medicinal Chemistry. 5.4.2016 118:170-177. doi:
PMID: 27128181

SETD7 Controls Intestinal Regeneration and Tumorigenesis by Regulating Wnt/β-Catenin and Hippo/YAP Signaling.
Oudhoff MJ, Braam MJ, Freeman SA, Wong D, Rattray DG, Wang J, Antignano F, Snyder K, Refaeli I, Hughes MR, McNagny KM, Gold MR, Arrowsmith CH, Sato T, Rossi FM, Tatlock JH, Owen DR, Brown PJ, Zaph C
Dev. Cell. 04.04.2016 37(1):47-57. doi: 10.1016/j.devcel.2016.03.002
PMID: 27046831

The first international workshop on the epigenetics of osteoarthritis.
Meulenbelt, IM; Bhutani, N; den Hollander, W; Gay, S; Oppermann, U; Reynard, LN; Skelton, AJ; Young, DA; Beier, F; Loughlin, J;
Connective Tissue Research. 30.3.2016 :-. doi:
PMID: 27028588

Quality control in oocytes by p63 is based on a spring-loaded activation mechanism on the molecular and cellular level.
Coutandin, D; Osterburg, C; Srivastav, RK; Sumyk, M; Kehrloesser, S; Gebel, J; Tuppi, M; Hannewald, J; Schäfer, B; Salah, E; Mathea, S; Müller-Kuller, U; Doutch, J; Grez, M; Knapp, S; Dötsch, V;
eLife. 01.1.2016 5:-. doi:
PMID: 27021569

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