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Displaying 1 - 50 of 1032

2016

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

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

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

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 extra-terminal 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. 16.3.2016 :-. 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: 10.1111/cge.12776
PMID: 26970254

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. 25.2.2016 :-. 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

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.. 01.03.2016 . doi: 10.1074/jbc.M115.703546
PMID: 26933036

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: 10.1107/s2059798316000401
PMID: 26960118

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

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

Citrullination-acetylation interplay guides E2F-1 activity during the inflammatory response.
Ghari, F; Quirke, AM; Munro, S; Kawalkowska, J; Picaud, S; McGouran, J; Subramanian, V; Muth, A; Williams, R; Kessler, B; Thompson, PR; Fillipakopoulos, P; Knapp, S; Venables, PJ; La Thangue, NB;
Science Advances. 5.2.2016 2:e1501257-. doi: 10.1126/sciadv.1501257
PMID: 26989780

Recent Progress in Histone Demethylase Inhibitors.
McAllister, TE; England, KS; Hopkinson, RJ; Brennan, PE; Kawamura, A; Schofield, CJ;
Journal of Medicinal Chemistry. 01.2.2016 59:1308-1329. doi: 10.1021/acs.jmedchem.5b01758
PMID: 26710088

Discovery of a Potent Class I Protein Arginine Methyltransferase Fragment Inhibitor.
Ferreira de Freitas R, Eram MS, Szewczyk MM, Steuber H, Smil D, Wu H, Li F, Senisterra G, Dong A, Brown PJ, Hitchcock M, Moosmayer D, Stegmann CM, Egner U, Arrowsmith C, Barsyte-Lovejoy D, Vedadi M, Schapira M
J. Med. Chem.. 29.01.2016 . doi: 10.1021/acs.jmedchem.5b01772
PMID: 26824386

Family-wide Structural Analysis of Human Numb-Associated Protein Kinases.
Sorrell, FJ; Szklarz, M; Abdul Azeez, KR; Elkins, JM; Knapp, S;
Structure. 01.3.2016 24:401-411. doi: 10.1016/j.str.2015.12.015
PMID: 26853940

Identification of LACTB2, a metallo-β-lactamase protein, as a human mitochondrial endoribonuclease.
Levy, S; Allerston, CK; Liveanu, V; Habib, MR; Gileadi, O; Schuster, G;
Nucleic Acids Research. 01.2.2016 44:1813-1832. doi: 10.1093/nar/gkw050
PMID: 26826708

A cellular chemical probe targeting the chromodomains of Polycomb repressive complex 1.
Stuckey JI, Dickson BM, Cheng N, Liu Y, Norris JL, Cholensky SH, Tempel W, Qin S, Huber KG, Sagum C, Black K, Li F, Huang XP, Roth BL, Baughman BM, Senisterra G, Pattenden SG, Vedadi M, Brown PJ, Bedford MT, Min J, Arrowsmith CH, James LI, Frye SV
Nat. Chem. Biol.. 25.01.2016 . doi: 10.1038/nchembio.2007
PMID: 26807715

Epigenomic regulation of oncogenesis by chromatin remodeling.
Kumar, R; Li, DQ; Müller, S; Knapp, S;
Oncogene. 25.1.2016 :-. doi: 10.1038/onc.2015.513
PMID: 26804164

EXD2 promotes homologous recombination by facilitating DNA end resection.
Broderick, R; Nieminuszczy, J; Baddock, HT; Deshpande, RA; Gileadi, O; Paull, TT; McHugh, PJ; Niedzwiedz, W;
Nature Cell Biology. 01.3.2016 18:271-280. doi: 10.1038/ncb3303
PMID: 26807646

Open Access Could Transform Drug Discovery: A Case Study of JQ1.
Arshad, Z; Smith, J; Roberts, M; Lee, WH; Davies, B; Bure, K; Hollander, GA; Dopson, S; Bountra, C; Brindley, D;
Expert Opinion on Drug Discovery. 01.3.2016 11:321-332. doi: 10.1517/17460441.2016.1144587
PMID: 26791045

Structure-Based Identification of Inhibitory Fragments Targeting the p300/CBP-Associated Factor Bromodomain.
Chaikuad, A; Lang, S; Brennan, PE; Temperini, C; Fedorov, O; Hollander, J; Nachane, R; Abell, C; Müller, S; Siegal, G; Knapp, S;
Journal of Medicinal Chemistry. 01.2.2016 59:1648-1653. doi: 10.1021/acs.jmedchem.5b01719
PMID: 26731131

Genome-wide profiling of histone H3 lysine 27 and lysine 4 trimethylation in multiple myeloma reveals the importance of Polycomb gene targeting and highlights EZH2 as a potential therapeutic target.
Agarwal P, Alzrigat M, Párraga AA, Enroth S, Singh U, Ungerstedt J, Österborg A, Brown PJ, Ma A, Jin J, Nilsson K, Öberg F, Kalushkova A, Jernberg-Wiklund H
Oncotarget. 07.01.2016 . doi: 10.18632/oncotarget.6843
PMID: 26755663

8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors.
Bavetsias, V; Lanigan, RM; Ruda, GF; Atrash, B; McLaughlin, MG; Tumber, A; Mok, NY; Le Bihan, YV; Dempster, S; Boxall, KJ; Jeganathan, F; Hatch, SB; Savitsky, P; Velupillai, S; Krojer, T; England, KS; Sejberg, J; Thai, C; Donovan, A; Pal, A; Scozzafava, G; Bennett, JM; Kawamura, A; Johansson, C; Szykowska, A; Gileadi, C; Burgess-Brown, NA; von Delft, F; Oppermann, U; Walters, Z; Shipley, J; Raynaud, FI; Westaway, SM; Prinjha, RK; Fedorov, O; Burke, R; Schofield, CJ; Westwood, IM; Bountra, C; Müller, S; van Montfort, RL; Brennan, PE; Blagg, J;
Journal of Medicinal Chemistry. 01.2.2016 59:1388-1409. doi: 10.1021/acs.jmedchem.5b01635
PMID: 26741168

Exploring Selective Inhibition of the First Bromodomain of the Human Bromodomain and Extra-terminal Domain (BET) Proteins.
Raux, B; Voitovich, Y; Derviaux, C; Lugari, A; Rebuffet, E; Milhas, S; Priet, S; Roux, T; Trinquet, E; Guillemot, JC; Knapp, S; Brunel, JM; Fedorov, AY; Collette, Y; Roche, P; Betzi, S; Combes, S; Morelli, X;
Journal of Medicinal Chemistry. 01.2.2016 59:1634-1641. doi: 10.1021/acs.jmedchem.5b01708
PMID: 26735842

Profiling of Small Molecules by Chemical Proteomics.
Huber, KV; Superti-Furga, G;
Methods in Molecular Biology. 01.1.2016 1394:211-218. doi: 10.1007/978-1-4939-3341-9_15
PMID: 26700051

Comprehensive characterization of the Published Kinase Inhibitor Set.
Elkins, JM; Fedele, V; Szklarz, M; Abdul Azeez, KR; Salah, E; Mikolajczyk, J; Romanov, S; Sepetov, N; Huang, XP; Roth, BL; Al Haj Zen, A; Fourches, D; Muratov, E; Tropsha, A; Morris, J; Teicher, BA; Kunkel, M; Polley, E; Lackey, KE; Atkinson, FL; Overington, JP; Bamborough, P; Müller, S; Price, DJ; Willson, TM; Drewry, DH; Knapp, S; Zuercher, WJ;
Nature Biotechnology. 01.1.2016 34:95-103. doi: 10.1038/nbt.3374
PMID: 26501955

Deciphering the true antiproliferative target of an MK2 activation inhibitor in glioblastoma.
B, P; r, E; e, ; n, ; n, ; a, ; n, ;
Cell Death and Disease. 28.1.2016 7:e2069-. doi: 10.1038/cddis.2015.384
PMID: 26821065

Structures of Two Melanoma-Associated Antigens Suggest Allosteric Regulation of Effector Binding.
Newman, JA; Cooper, CD; Roos, AK; Aitkenhead, H; Oppermann, UC; Cho, HJ; Osman, R; Gileadi, O;
PLoS One. 01.1.2016 11:e0148762-. doi: 10.1371/journal.pone.0148762
PMID: 26910052

Use of Methylmalonyl-CoA Epimerase in Enhancing Crotonase Stereoselectivity.
Hamed, RB; Gomez-Castellanos, JR; Sean Froese, D; Krysztofinska, E; Yue, WW; Schofield, CJ;
ChemBioChem: a European journal of chemical biology. 01.3.2016 17:471-473. doi: 10.1002/cbic.201500644
PMID: 26716911

Role of reverse phenotyping in interpretation of next generation sequencing data and a review of INPP5E related disorders.
de Goede, C; Yue, WW; Yan, G; Ariyaratnam, S; Chandler, KE; Downes, L; Khan, N; Mohan, M; Lowe, M; Banka, S;
European Journal of Paediatric Neurology. 01.3.2016 20:286-295. doi: 10.1016/j.ejpn.2015.11.012
PMID: 26748598

2015

A Radioactivity-Based Assay for Screening Human m6A-RNA Methyltransferase, METTL3-METTL14 Complex, and Demethylase ALKBH5.
Li F, Kennedy S, Hajian T, Gibson E, Seitova A, Xu C, Arrowsmith CH, Vedadi M
J Biomol Screen. 23.12.2015 . doi: 10.1177/1087057115623264
PMID: 26701100

SMN and symmetric arginine dimethylation of RNA polymerase II C-terminal domain control termination.
Yanling Zhao D, Gish G, Braunschweig U, Li Y, Ni Z, Schmitges FW, Zhong G, Liu K, Li W, Moffat J, Vedadi M, Min J, Pawson TJ, Blencowe BJ, Greenblatt JF
Nature. 23.12.2015 . doi: 10.1038/nature16469
PMID: 26700805

Human ISPD Is a Cytidyltransferase Required for Dystroglycan O-Mannosylation
Riemersma, M; Froese, DS; Van Tol, W; Engelke, UF; Kopec, J; Van Scherpenzeel, M; Ashikov, A; Krojer, T; Von Delft, F; Tessari, M; Buczkowska, A; Swiezewska, E; Jae, LT; Brummelkamp, TR; Manya, H; Endo, T; Van Bokhoven, H; Yue, WW; Lefeber, DJ;
Chemistry and Biology. 17.12.2015 22:1643-1652. doi: 10.1016/j.chembiol.2015.10.014
PMID:

Structural Insights into the MMACHC-MMADHC Protein Complex Involved in Vitamin B12 Trafficking.
Froese, DS; Kopec, J; Fitzpatrick, F; Schuller, M; McCorvie, TJ; Chalk, R; Plessl, T; Fettelschoss, V; Fowler, B; Baumgartner, MR; Yue, WW;
Journal of Biological Chemistry. 01.12.2015 290:29167-29177. doi: 10.1074/jbc.m115.683268
PMID: 26483544

Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy.
Picaud, S; Fedorov, O; Thanasopoulou, A; Leonards, K; Jones, K; Meier, J; Olzscha, H; Monteiro, O; Martin, S; Philpott, M; Tumber, A; Filippakopoulos, P; Yapp, C; Wells, C; Che, KH; Bannister, A; Robson, S; Kumar, U; Parr, N; Lee, K; Lugo, D; Jeffrey, P; Taylor, S; Vecellio, ML; Bountra, C; Brennan, PE; O'Mahony, A; Velichko, S; Müller, S; Hay, D; Daniels, DL; Urh, M; La Thangue, NB; Kouzarides, T; Prinjha, R; Schwaller, J; Knapp, S;
Cancer Research. 01.12.2015 75:5106-5119. doi: 10.1158/0008-5472.can-15-0236
PMID: 26552700

MLL5 Orchestrates a Cancer Self-Renewal State by Repressing the Histone Variant H3.3 and Globally Reorganizing Chromatin.
Gallo M, Coutinho FJ, Vanner RJ, Gayden T, Mack SC, Murison A, Remke M, Li R, Takayama N, Desai K, Lee L, Lan X, Park NI, Barsyte-Lovejoy D, Smil D, Sturm D, Kushida MM, Head R, Cusimano MD, Bernstein M, Clarke ID, Dick JE, Pfister SM, Rich JN, Arrowsmith CH, Taylor MD, Jabado N, Bazett-Jones DP, Lupien M, Dirks PB
Cancer Cell. 25.11.2015 . doi: 10.1016/j.ccell.2015.10.005
PMID: 26626085

A Potent, Selective and Cell-active Inhibitor of Human Type I Protein Arginine Methyltransferases.
Eram MS, Shen Y, Szewczyk M, Wu H, Senisterra G, Li F, Butler KV, Kaniskan HÜ, Speed BA, Dela Seña C, Dong A, Zeng H, Schapira M, Brown PJ, Arrowsmith CH, Barsyte-Lovejoy D, Liu J, Vedadi M, Jin J
ACS Chem. Biol.. 24.11.2015 . doi: 10.1021/acschembio.5b00839
PMID: 26598975

Structures of the CDK12/CycK complex with AMP-PNP reveal a flexible C-terminal kinase extension important for ATP binding.
Dixon-Clarke, SE; Elkins, JM; Cheng, SW; Morin, GB; Bullock, AN;
Scientific Reports. 01.1.2015 5:17122-. doi: 10.1038/srep17122
PMID: 26597175

Chemical basis for the recognition of trimethyllysine by epigenetic reader proteins.
Kamps JJ, Huang J, Poater J, Xu C, Pieters BJ, Dong A, Min J, Sherman W, Beuming T, Matthias Bickelhaupt F, Li H, Mecinović J
Nat Commun. 19.11.2015 6:8911. doi: 10.1038/ncomms9911
PMID: 26578293

The structures of the SNM1A and SNM1B/Apollo nuclease domains reveal a potential basis for their distinct DNA processing activities.
Allerston, CK; Lee, SY; Newman, JA; Schofield, CJ; McHugh, PJ; Gileadi, O;
Nucleic Acids Research. 01.12.2015 43:11047-11060. doi: 10.1093/nar/gkv1256
PMID: 26582912

Regulation of signaling interactomes in cancer
Lambert, J-P; Zhou, Y; Couzens, A; Tsou, C-C; Picaud, S; Ivosev, G; Tate, S; Nesvizhskii, A; Filippakopoulos, P; Gingras, A-C;
Cancer Research. 15.11.2015 75:-. doi: 10.1158/1538-7445.COMPSYSBIO-IA19
PMID:

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