Publications

Stay Updated
Subscribe to receive new SGC publications- email us at
publications[at]thesgc.org (Subject: Subscribe)

You can search the extensive SGC publications list with keywords from the title, authors or journal name.
Your search results can be exported to an Excel file by clicking the orange XLS button next to the search filters.

Displaying 1 - 50 of 1073

2016

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

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

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, ZC; Ren, X; Lu, X; Brekken, RA; Yao, L; Bullock, AN; Su, J; Ding, K;
Journal of Medicinal Chemistry. 24.5.2016 :-. 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

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

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

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. 24.5.2016 :-. 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. 23.5.2016 :-. 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. 23.5.2016 :-. doi:
PMID: 27213690

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

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. 9.5.2016 :-. doi:
PMID: 27159579

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

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

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

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

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;
. 29.4.2016 :1-11. doi: 10.1080/23808993.2016.1176526
PMID:

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

H3K27ME3 DEMETHYLASES REGULATE IN VITRO CHONDROGENESIS AND CHONDROCYTE ACTIVITY IN OSTEOARTHRITIS
Yapp, C; Carr, AJ; Price, AJ; Oppermann, U; Snelling, SJ;
Osteoarthritis and Cartilage. 01.4.2016 24:S181-S181. doi:
PMID:

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

Molecular basis of classic galactosemia from the structure of human galactose 1-phosphate uridylyltransferase.
McCorvie, TJ; Kopec, J; Pey, AL; Fitzpatrick, F; Patel, D; Chalk, R; Streetha, L; Yue, WW;
Human Molecular Genetics. 22.3.2016 :-. doi:
PMID: 27005423

Structure of the Human Protein Kinase ZAK in Complex with Vemurafenib.
Mathea, S; Abdul Azeez, KR; Salah, E; Tallant, C; Wolfreys, F; Konietzny, R; Fischer, R; Lou, HJ; Brennan, PE; Schnapp, G; Pautsch, A; Kessler, BM; Turk, BE; Knapp, S;
ACS Chemical Biology. 21.3.2016 :-. doi:
PMID: 26999302

Dual Targeting of Bromodomain and Extraterminal Domain Proteins, and WNT or MAPK Signaling, Inhibits c-MYC Expression and Proliferation of Colorectal Cancer Cells.
Tögel, L; Nightingale, R; Chueh, AC; Jayachandran, A; Tran, H; Phesse, T; Wu, R; Sieber, OM; Arango, D; Dhillon, AS; Dawson, MA; Diez-Dacal, B; Gahman, TC; Filippakopoulos, P; Shiau, AK; Mariadason, JM;
Molecular Cancer Therapeutics. 01.6.2016 15:1217-1226. doi:
PMID: 26983878

Expanding the Genotypic Spectrum of Perrault syndrome.
Demain, LA; Urquhart, JE; O'Sullivan, J; Williams, SG; Bhaskar, SS; Jenkinson, EM; Lourenco, CM; Heiberg, A; Pearce, SH; Shalev, SA; Yue, WW; Mackinnon, S; Munro, KJ; Newbury-Ecob, R; Becker, K; Kim, MJ; O' Keefe, RT; Newman, WG;
Clinical Genetics: an international journal of genetics and molecular medicine. 11.3.2016 :-. doi:
PMID: 26970254

Identification of small molecule inhibitors that block the Toxoplasma gondii rhoptry kinase ROP18.
Simpson C, Jones NG, Hull-Ryde EA, Kireev D, Stashko M, Tang K, Janetka J, Wildman SA, Zuercher WJ, Schapira M, Hui R, Janzen W, Sibley LD
ACS Infect Dis. 11.03.2016 2(3):194-206. doi: 10.1021/acsinfecdis.5b00102
PMID: 27379343

Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor.
Martin, LJ; Koegl, M; Bader, G; Cockcroft, XL; Fedorov, O; Fiegen, D; Gerstberger, T; Hofmann, MH; Hohmann, AF; Kessler, D; Knapp, S; Knesl, P; Kornigg, S; Müller, S; Nar, H; Rogers, C; Rumpel, K; Schaaf, O; Steurer, S; Tallant, C; Vakoc, CR; Zeeb, M; Zoephel, A; Pearson, M; Boehmelt, G; McConnell, D;
Journal of Medicinal Chemistry. 01.5.2016 59:4462-4475. doi:
PMID: 26914985

Structure-Based Optimization of a Small Molecule Antagonist of the Interaction Between WD Repeat-Containing Protein 5 (WDR5) and Mixed-Lineage Leukemia 1 (MLL1).
Getlik M, Smil D, Zepeda-Velázquez C, Bolshan Y, Poda G, Wu H, Dong A, Kuznetsova E, Marcellus R, Senisterra G, Dombrovski L, Hajian T, Kiyota T, Schapira M, Arrowsmith CH, Brown PJ, Vedadi M, Al-Awar R
J. Med. Chem.. 09.03.2016 . doi: 10.1021/acs.jmedchem.5b01630
PMID: 26958703

System-Wide Modulation of HECT E3 Ligases with Selective Ubiquitin Variant Probes.
Zhang W, Wu KP, Sartori MA, Kamadurai HB, Ordureau A, Jiang C, Mercredi PY, Murchie R, Hu J, Persaud A, Mukherjee M, Li N, Doye A, Walker JR, Sheng Y, Hao Z, Li Y, Brown KR, Lemichez E, Chen J, Tong Y, Harper JW, Moffat J, Rotin D, Schulman BA, Sidhu SS
Mol. Cell. 02.03.2016 . doi: 10.1016/j.molcel.2016.02.005
PMID: 26949039

Biochemical Screening of Five Protein Kinases from Plasmodium falciparum against 14,000 Cell-Active Compounds.
Crowther GJ, Hillesland HK, Keyloun KR, Reid MC, Lafuente-Monasterio MJ, Ghidelli-Disse S, Leonard SE, He P, Jones JC, Krahn MM, Mo JS, Dasari KS, Fox AM, Boesche M, El Bakkouri M, Rivas KL, Leroy D, Hui R, Drewes G, Maly DJ, Van Voorhis WC, Ojo KK
PLoS ONE. 02.03.2016 11(3):e0149996. doi: 10.1371/journal.pone.0149996
PMID: 26934697

Family-wide characterization of histone binding abilities of human CW domain containing proteins.
Liu Y, Tempel W, Zhang Q, Liang X, Loppnau P, Qin S, Min J
J. Biol. Chem.. 01.03.2016 . doi: 10.1074/jbc.M116.718973
PMID: 26933034

A poised fragment library enables rapid synthetic expansion yielding the first reported inhibitors of PHIP(2), an atypical bromodomain
Cox, OB; Krojer, T; Collins, P; Monteiro, O; Talon, R; Bradley, A; Fedorov, O; Amin, J; Marsden, BD; Spencer, J; von Delft, F; Brennan, PE;
Chemical Science. 01.01.2016 7:2322-2330. doi: 10.1039/c5sc03115j
PMID:

An overview of heavy-atom derivatization of protein crystals.
Pike, AC; Garman, EF; Krojer, T; von Delft, F; Carpenter, EP;
Acta crystallographica. Section D, Structural biology. 01.3.2016 72:303-318. doi:
PMID: 26960118

Characterization of NK Cells in Endometriosis Associated Pain.
Soderstrom, K; Southcombe, J; Malzahn, J; Putsep, L; Oppermann, U; Shang, C; Becker, C; Zondervan, K; Martin-Fischer, O; Zollner, TM; Granne, I; Sacher, F;
Reproductive Sciences. 01.3.2016 23:161A-161A. doi:
PMID:

Structural Basis for Substrate Preference of SMYD3, A SET Domain-containing Protein Lysine Methyltransferase.
Fu W, Liu N, Qiao Q, Wang M, Min J, Zhu B, Xu RM, Yang N
J. Biol. Chem.. 29.02.2016 . doi: 10.1074/jbc.M115.709832
PMID: 26929412

Structural basis for a novel interaction between TXNIP and Vav2.
Liu S, Wu X, Zong M, Tempel W, Loppnau P, Liu Y
FEBS Lett.. 25.02.2016 . doi: 10.1002/1873-3468.12110
PMID: 26919541

Sclerostin expression in bone tumours and tumour-like lesions.
Inagaki, Y; Hookway, ES; Kashima, TG; Munemoto, M; Tanaka, Y; Hassan, AB; Oppermann, U; Athanasou, NA;
Histopathology. 20.2.2016 :-. doi:
PMID: 26896083

Identification of a small-molecule ligand of the epigenetic reader protein Spindlin1 via a versatile screening platform.
Wagner, T; Greschik, H; Burgahn, T; Schmidtkunz, K; Schott, AK; McMillan, J; Baranauskienė, L; Xiong, Y; Fedorov, O; Jin, J; Oppermann, U; Matulis, D; Schüle, R; Jung, M;
Nucleic Acids Research. 01.5.2016 44:e88-. doi:
PMID: 26893353

Chemical Biology Approaches for Characterization of Epigenetic Regulators.
Barsyte-Lovejoy D, Szewczyk MM, Prinos P, Lima-Fernandes E, Ackloo S, Arrowsmith CH
Meth. Enzymol.. 16.02.2016 574:79-103. doi: 10.1016/bs.mie.2016.01.011
PMID: 27423858

Apollo-NADP(+): a spectrally tunable family of genetically encoded sensors for NADP(.)
Cameron WD, Bui CV, Hutchinson A, Loppnau P, Gräslund S, Rocheleau JV
Nat. Methods. 15.02.2016 . doi: 10.1038/nmeth.3764
PMID: 26878383

Pages

Download Publication List
glqxz9283 sfy39587stf02 mnesdcuix8
sfy39587stf03