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Displaying 1 - 50 of 1138

2016

Structure-Based Design of a Covalent Inhibitor of the SET Domain-Containing Protein 8 (SETD8) Lysine Methyltransferase.
Butler KV, Ma A, Yu W, Li F, Tempel W, Babault N, Pittella-Silva F, Shao J, Wang J, Luo M, Vedadi M, Brown PJ, Arrowsmith CH, Jin J
J. Med. Chem.. 02.11.2016 . doi: 10.1021/acs.jmedchem.6b01244
PMID: 27804297

Structural insights into Gemin5-guided selection of pre-snRNAs for snRNP assembly.
Xu C, Ishikawa H, Izumikawa K, Li L, He H, Nobe Y, Yamauchi Y, Shahjee HM, Wu XH, Yu YT, Isobe T, Takahashi N, Min J
Genes Dev.. 01.11.2016 30(21):2376-2390. doi: 10.1101/gad.288340.116
PMID: 27881600

Biochemical and Structural Characterization of Selective Allosteric Inhibitors of the Plasmodium falciparum Drug Target, Prolyl-tRNA-synthetase.
Nakazawa Hewitt S, Dranow DM, Horst BG, Abendroth JA, Forte B, Hallyburton I, Jansen C, Baragana B, Choi R, Rivas KL, Hulverson MA, Dumais M, Edwards TE, Lorimer DD, Fairlamb AH, Gray DW, Read KD, Lehane AM, Kirk K, Myler PJ, Wernimont A, Walpole CS, Stacy R, Barrett LK, Gilbert IH, Van Voorhis WC
ACS Infect Dis. 31.10.2016 . doi: 10.1021/acsinfecdis.6b00078
PMID: 27798837

Characterizing Plexin GTPase Interactions Using Gel Filtration, Surface Plasmon Resonance Spectrometry, and Isothermal Titration Calorimetry.
Muller-Greven J, Kim S, Hota PK, Tong Y, Borthakur S, Buck M
Methods Mol. Biol.. 28.10.2016 1493:89-105. doi: 10.1007/978-1-4939-6448-2_6
PMID: 27787844

Solution NMR structure of the HLTF HIRAN domain: a conserved module in SWI2/SNF2 DNA damage tolerance proteins.
Korzhnev DM, Neculai D, Dhe-Paganon S, Arrowsmith CH, Bezsonova I
J. Biomol. NMR. 22.10.2016 . doi: 10.1007/s10858-016-0070-9
PMID: 27771863

The substrate binding domains of human SIAH E3 ubiquitin ligases are now crystal clear.
Zhang Q, Wang Z, Hou F, Harding R, Huang X, Dong A, Walker JR, Tong Y
Biochim. Biophys. Acta. 21.10.2016 . doi: 10.1016/j.bbagen.2016.10.019
PMID: 27776223

Promiscuous targeting of bromodomains by bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia.
Picaud, S; Leonards, K; Lambert, JP; Dovey, O; Wells, C; Fedorov, O; Monteiro, O; Fujisawa, T; Wang, CY; Lingard, H; Tallant, C; Nikbin, N; Guetzoyan, L; Ingham, R; Ley, SV; Brennan, P; Muller, S; Samsonova, A; Gingras, AC; Schwaller, J; Vassiliou, G; Knapp, S; Filippakopoulos, P;
Science Advances. 01.10.2016 2:e1600760-. doi: 10.1126/sciadv.1600760
PMID: 27757418

Patient-derived Mammosphere and Xenograft Tumour Initiation Correlates with Progression to Metastasis.
Eyre, R; Alférez, DG; Spence, K; Kamal, M; Shaw, FL; Simões, BM; Santiago-Gómez, A; Sarmiento-Castro, A; Bramley, M; Absar, M; Saad, Z; Chatterjee, S; Kirwan, C; Gandhi, A; Armstrong, AC; Wardley, AM; O'Brien, CS; Farnie, G; Howell, SJ; Clarke, RB;
Journal of Mammary Gland Biology and Neoplasia. 28.9.2016 :-. doi:
PMID: 27680982

Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors.
Popp, TA; Tallant, C; Rogers, C; Fedorov, O; Brennan, PE; Müller, S; Knapp, S; Bracher, F;
Journal of Medicinal Chemistry. 27.9.2016 :-. doi:
PMID: 27673482

Discovery and optimization of a selective ligand for the Switch/Sucrose Non-Fermenting-related bromodomains of Polybromo protein-1 by the use of virtual screening and hydration analysis.
Myrianthopoulos, V; Gaboriaud-Kolar, N; Tallant, C; Hall, ML; Grigoriou, S; Brownlee, PM; Fedorov, O; Rogers, C; Heidenreich, D; Wanior, M; Drosos, N; Mexia, N; Savitsky, P; Bagratuni, T; Kastritis, E; Terpos, E; Filippakopoulos, P; Müller, S; Skaltsounis, AL; Downs, JA; Knapp, S; Mikros, E;
Journal of Medicinal Chemistry. 12.9.2016 :-. doi:
PMID: 27617704

Discovery of Potent Pantothenamide Inhibitors of Staphylococcus aureus Pantothenate Kinase through a Minimal SAR Study: Inhibition Is Due to Trapping of the Product.
Hughes SJ, Barnard L, Mottaghi K, Tempel W, Antoshchenko T, Hong BS, Allali-Hassani A, Smil D, Vedadi M, Strauss E, Park HW
ACS Infect Dis. 09.09.2016 2(9):627-641. doi: 10.1021/acsinfecdis.6b00090
PMID: 27759386

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

Advantages and pitfalls of an extended gene panel for investigating complex neurometabolic phenotypes.
Reid, ES; Papandreou, A; Drury, S; Boustred, C; Yue, WW; Wedatilake, Y; Beesley, C; Jacques, TS; Anderson, G; Abulhoul, L; Broomfield, A; Cleary, M; Grunewald, S; Varadkar, SM; Lench, N; Rahman, S; Gissen, P; Clayton, PT; Mills, PB;
Brain: a journal of neurology. 6.9.2016 :-. doi:
PMID: 27604308

A proposal for validation of antibodies.
Uhlen M, Bandrowski A, Carr S, Edwards A, Ellenberg J, Lundberg E, Rimm DL, Rodriguez H, Hiltke T, Snyder M, Yamamoto T
Nat. Methods. 05.09.2016 . doi: 10.1038/nmeth.3995
PMID: 27595404

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

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

Covalent targeting of remote cysteine residues to develop CDK12 and CDK13 inhibitors.
Zhang, T; Kwiatkowski, N; Olson, CM; Dixon-Clarke, SE; Abraham, BJ; Greifenberg, AK; Ficarro, SB; Elkins, JM; Liang, Y; Hannett, NM; Manz, T; Hao, M; Bartkowiak, B; Greenleaf, AL; Marto, JA; Geyer, M; Bullock, AN; Young, RA; Gray, NS;
Nature Chemical Biology. 01.10.2016 12:876-884. doi:
PMID: 27571479

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

3D modelling identifies novel genetic dependencies associated with breast cancer progression in the isogenic MCF10 model.
Maguire, SL; Peck, B; Wai, PT; Campbell, J; Barker, H; Gulati, A; Daley, F; Vyse, S; Huang, P; Lord, CJ; Farnie, G; Brennan, K; Natrajan, R;
Journal of Pathology. 11.8.2016 :-. doi:
PMID: 27512948

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. 01.8.2016 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

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

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

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, W;
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

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

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

Perspective: Science is still too closed.
Edwards A
Nature. 12.05.2016 533:S70. doi: 10.1038/533S70a
PMID: 27167397

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:

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