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Displaying 1 - 50 of 1161

2017

Functions of bromodomain-containing proteins and their roles in homeostasis and cancer
Filippakopoulos, P; Fujisawa, T;
Nature Reviews: Molecular Cell Biology. 5.1.2017 :-. doi: 10.1038/nrm.2016.143
PMID:

Combinatorial Drug Screening Identifies Ewing Sarcoma-specific Sensitivities.
Radic-Sarikas, B; Tsafou, KP; Emdal, KB; Papamarkou, T; Huber, KV; Mutz, C; Toretsky, JA; Bennett, KL; Olsen, JV; Brunak, S; Kovar, H; Superti-Furga, G;
Molecular Cancer Therapeutics. 01.1.2017 16:88-101. doi: 10.1158/1535-7163.MCT-16-0235
PMID: 28062706

2016

Early-life antibiotic treatment enhances the pathogenicity of CD4+ T cells during intestinal inflammation.
Scheer S, Medina TS, Murison A, Taves MD, Antignano F, Chenery A, Soma KK, Perona-Wright G, Lupien M, Arrowsmith CH, De Carvalho DD, Zaph C
J. Leukoc. Biol.. 29.12.2016 . doi: 10.1189/jlb.3MA0716-334RR
PMID: 28034915

Structure of the polycystic kidney disease TRP channel Polycystin-2 (PC2).
Grieben, M; Pike, AC; Shintre, CA; Venturi, E; El-Ajouz, S; Tessitore, A; Shrestha, L; Mukhopadhyay, S; Mahajan, P; Chalk, R; Burgess-Brown, NA; Sitsapesan, R; Huiskonen, JT; Carpenter, EP;
Nature Structural and Molecular Biology. 19.12.2016 :-. doi: 10.1038/nsmb.3343
PMID: 27991905

Discovery of a PCAF Bromodomain Chemical Probe.
Moustakim, M; Clark, PG; Trulli, L; Fuentes de Arriba, AL; Ehebauer, MT; Chaikuad, A; Murphy, EJ; Mendez-Johnson, J; Daniels, D; Hou, CD; Lin, YH; Walker, JR; Hui, R; Yang, H; Dorrell, L; Rogers, CM; Monteiro, OP; Fedorov, O; Huber, KV; Knapp, S; Heer, J; Dixon, DJ; Brennan, PE;
Angewandte Chemie International Edition. 14.12.2016 :-. doi: 10.1002/anie.201610816
PMID: 27966810

CBP/p300 Bromodomains Regulate Amyloid-like Protein Aggregation upon Aberrant Lysine Acetylation.
Olzscha, H; Fedorov, O; Kessler, BM; Knapp, S; La Thangue, NB;
Cell chemical biology. 10.12.2016 :-. doi: 10.1016/j.chembiol.2016.11.009
PMID: 27989401

Turning a Substrate Peptide into a Potent Inhibitor for the Histone Methyltransferase SETD8.
Judge RA, Zhu H, Upadhyay AK, Bodelle PM, Hutchins CW, Torrent M, Marin VL, Yu W, Vedadi M, Li F, Brown PJ, Pappano WN, Sun C, Petros AM
ACS Med Chem Lett. 08.12.2016 7(12):1102-1106. doi: 10.1021/acsmedchemlett.6b00303
PMID: 27994746

Multivalent Histone and DNA Engagement by a PHD/BRD/PWWP Triple Reader Cassette Recruits ZMYND8 to K14ac-Rich Chromatin.
Savitsky, P; Krojer, T; Fujisawa, T; Lambert, JP; Picaud, S; Wang, CY; Shanle, EK; Krajewski, K; Friedrichsen, H; Kanapin, A; Goding, C; Schapira, M; Samsonova, A; Strahl, BD; Gingras, AC; Filippakopoulos, P;
Cell Reports. 6.12.2016 17:2724-2737. doi: 10.1016/j.celrep.2016.11.014
PMID: 27926874

Multivalent Histone and DNA Engagement by a PHD/BRD/PWWP Triple Reader Cassette Recruits ZMYND8 to K14ac-Rich Chromatin.
Savitsky P, Krojer T, Fujisawa T, Lambert JP, Picaud S, Wang CY, Shanle EK, Krajewski K, Friedrichsen H, Kanapin A, Goding C, Schapira M, Samsonova A, Strahl BD, Gingras AC, Filippakopoulos P
Cell Rep. 06.12.2016 17(10):2724-2737. doi: 10.1016/j.celrep.2016.11.014
PMID: 27926874

Heme drives hemolysis-induced susceptibility to infection via disruption of phagocyte functions.
Martins, R; Maier, J; Gorki, AD; Huber, KV; Sharif, O; Starkl, P; Saluzzo, S; Quattrone, F; Gawish, R; Lakovits, K; Aichinger, MC; Radic-Sarikas, B; Lardeau, CH; Hladik, A; Korosec, A; Brown, M; Vaahtomeri, K; Duggan, M; Kerjaschki, D; Esterbauer, H; Colinge, J; Eisenbarth, SC; Decker, T; Bennett, KL; Kubicek, S; Sixt, M; Superti-Furga, G; Knapp, S;
Nature Immunology. 01.12.2016 17:1361-1372. doi: 10.1038/ni.3590
PMID: 27798618

Mass spectrometry captures off-target drug binding and provides mechanistic insights into the human metalloprotease ZMPSTE24.
Mehmood, S; Marcoux, J; Gault, J; Quigley, A; Michaelis, S; Young, SG; Carpenter, EP; Robinson, CV;
Nature Chemistry. 01.12.2016 8:1152-1158. doi: 10.1038/nchem.2591
PMID: 27874871

Artemisinins Target GABAA Receptor Signaling and Impair α Cell Identity.
Li, J; Casteels, T; Frogne, T; Ingvorsen, C; Honoré, C; Courtney, M; Huber, KV; Schmitner, N; Kimmel, RA; Romanov, RA; Sturtzel, C; Lardeau, CH; Klughammer, J; Farlik, M; Sdelci, S; Vieira, A; Avolio, F; Briand, F; Baburin, I; Májek, P; Pauler, FM; Penz, T; Stukalov, A; Gridling, M; Parapatics, K; Barbieux, C; Berishvili, E; Spittler, A; Colinge, J; Bennett, KL; Hering, S; Sulpice, T; Bock, C; Distel, M; Harkany, T; Meyer, D; Superti-Furga, G; Collombat, P; Hecksher-Sørensen, J; Kubicek, S;
Cell. 30.11.2016 :-. doi: 10.1016/j.cell.2016.11.010
PMID: 27916275

Metalloprotease SPRTN/DVC1 Orchestrates Replication-Coupled DNA-Protein Crosslink Repair.
Vaz, B; Popovic, M; Newman, JA; Fielden, J; Aitkenhead, H; Halder, S; Singh, AN; Vendrell, I; Fischer, R; Torrecilla, I; Drobnitzky, N; Freire, R; Amor, DJ; Lockhart, PJ; Kessler, BM; McKenna, GW; Gileadi, O; Ramadan, K;
Molecular Cell. 17.11.2016 64:704-719. doi: 10.1016/j.molcel.2016.09.032
PMID: 27871366

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

Mechanism of TAp73 inhibition by ΔNp63 and structural basis of p63/p73 hetero-tetramerization.
Gebel, J; Luh, LM; Coutandin, D; Osterburg, C; Löhr, F; Schäfer, B; Frombach, AS; Sumyk, M; Buchner, L; Krojer, T; Salah, E; Mathea, S; Güntert, P; Knapp, S; Dötsch, V;
Cell Death and Differentiation. 01.12.2016 23:1930-1940. doi: 10.1038/cdd.2016.83
PMID: 27716744

Epigenetic blockade of neoplastic transformation by bromodomain and extra-terminal (BET) domain protein inhibitor JQ-1.
Zhang, C; Su, ZY; Wang, L; Shu, L; Yang, Y; Guo, Y; Pung, D; Bountra, C; Kong, AN;
Biochemical Pharmacology. 01.10.2016 117:35-45. doi:
PMID: 27520485

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

The MAPK pathway regulates intrinsic resistance to BET inhibitors in colorectal cancer.
Ma, Y; Wang, L; Neitzel, LR; Loganathan, S; Tang, N; Qin, L; Emily, CE; Guo, Y; Knapp, S; Beauchamp, RD; Lee, E; Wang, J;
Clinical Cancer Research. 27.9.2016 :-. doi:
PMID: 27678457

BRD4 localization to lineage-specific enhancers is associated with a distinct transcription factor repertoire.
Najafova, Z; Tirado-Magallanes, R; Subramaniam, M; Hossan, T; Schmidt, G; Nagarajan, S; Baumgart, SJ; Mishra, VK; Bedi, U; Hesse, E; Knapp, S; Hawse, JR; Johnsen, SA;
Nucleic Acids Research. 19.9.2016 :-. doi: 10.1093/nar/gkw826
PMID: 27651452

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

Chemical probes and inhibitors of bromodomains outside the BET family
Moustakim, M; Clark, PGK; Hay, DA; Dixon, DJ; Brennan, PE;
MedChemComm. 7.9.2016 :-. doi: 10.1039/C6MD00373G
PMID:

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

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