Publications

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Displaying 1 - 50 of 1278

2017

July 2017

Global analysis of protein folding using massively parallel design, synthesis, and testing.
Rocklin GJ, Chidyausiku TM, Goreshnik I, Ford A, Houliston S, Lemak A, Carter L, Ravichandran R, Mulligan VK, Chevalier A, Arrowsmith CH, Baker D
Science 357(6347):168-175 . doi: 10.1126/science.aan0693
Publication date: July 14, 2017
PMID: 28706065
ASCL1 Reorganizes Chromatin to Direct Neuronal Fate and Suppress Tumorigenicity of Glioblastoma Stem Cells.
Park NI, Guilhamon P, Desai K, McAdam RF, Langille E, O'Connor M, Lan X, Whetstone H, Coutinho FJ, Vanner RJ, Ling E, Prinos P, Lee L, Selvadurai H, Atwal G, Kushida M, Clarke ID, Voisin V, Cusimano MD, Bernstein M, Das S, Bader G, Arrowsmith CH, Angers S, Huang X, Lupien M, Dirks PB
Cell Stem Cell . doi: 10.1016/j.stem.2017.06.004
Publication date: July 11, 2017
PMID: 28712938

June 2017

Structure-activity relationship studies of G9a-like protein (GLP) inhibitors.
Xiong Y, Li F, Babault N, Wu H, Dong A, Zeng H, Chen X, Arrowsmith CH, Brown PJ, Liu J, Vedadi M, Jin J
Bioorg. Med. Chem. . doi: 10.1016/j.bmc.2017.06.021
Publication date: June 19, 2017
PMID: 28662962
Readers, writers and erasers of N(6)-methylated adenosine modification.
Wu B, Li L, Huang Y, Ma J, Min J
Curr. Opin. Struct. Biol. 47:67-76 . doi: 10.1016/j.sbi.2017.05.011
Publication date: June 15, 2017
PMID: 28624569
Lapatinib potentiates cytotoxicity of  YM155 in neuroblastoma via inhibition of the ABCB1 efflux transporter.
Radic-Sarikas, B; Halasz, M; Huber, KVM; Winter, GE; Tsafou, KP; Papamarkou, T; Brunak, S; Kolch, W; Superti-Furga, G;
Scientific Reports 7:3091- . doi: 10.1038/s41598-017-03129-6
Publication date: June 7, 2017
PMID: 28596528
Generation and validation of intracellular ubiquitin variant inhibitors for USP7 and USP10.
Zhang W, Sartori MA, Makhnevych T, Federowicz KE, Dong X, Liu L, Nim S, Dong A, Yang J, Li Y, Haddad D, Ernst A, Heerding D, Tong Y, Moffat J, Sidhu SS
J. Mol. Biol. . doi: 10.1016/j.jmb.2017.05.025
Publication date: June 3, 2017
PMID: 28587923

May 2017

A trust approach for sharing research reagents.
Edwards A, Morgan M, Al Chawaf A, Andrusiak K, Charney R, Cynader Z, ElDessouki A, Lee Y, Moeser A, Stern S, Zuercher WJ
Sci Transl Med 9(392): . doi: 10.1126/scitranslmed.aai9055
Publication date: May 31, 2017
PMID: 28566431
The origin and evolution of human glutaminases and their atypical C-terminal ankyrin repeats.
Pascoal, CC; Islam, Z; Adamoski, D; Ferreira, IM; Righetto, RD; Bettini, J; Portugal, RV; Yue, WW; Gonzalez, A; Dias, SMG; Ambrosio, ALB;
Journal of Biological Chemistry :- . doi: 10.1074/jbc.M117.787291
Publication date: May 18, 2017
PMID: 28526749
Epigenetic pathway inhibitors represent potential drugs for treating pancreatic and bronchial neuroendocrine tumors.
Lines, KE; Stevenson, M; Filippakopoulos, P; Müller, S; Lockstone, HE; Wright, B; Grozinsky-Glasberg, S; Grossman, AB; Knapp, S; Buck, D; Bountra, C; Thakker, RV;
Oncogenesis 6:e332- . doi: 10.1038/oncsis.2017.30
Publication date: May 14, 2017
PMID: 28504695
Protein destabilization and loss of protein-protein interaction are fundamental mechanisms in cblA-type methylmalonic aciduria.
Plessl, T; Bürer, C; Lutz, S; Yue, WW; Baumgartner, MR; Froese, DS;
Human Mutation :- . doi: 10.1002/humu.23251
Publication date: May 11, 2017
PMID: 28497574
Structure-Based Design of Highly Selective Inhibitors of the CREB Binding Protein Bromodomain.
Denny, RA; Flick, AC; Coe, J; Langille, J; Basak, A; Liu, S; Stock, I; Sahasrabudhe, P; Bonin, P; Hay, DA; Brennan, PE; Pletcher, M; Jones, LH; Chekler, ELP;
Journal of Medicinal Chemistry :- . doi: 10.1021/acs.jmedchem.6b01839
Publication date: May 11, 2017
PMID: 28375629

April 2017

A multi-crystal method for extracting obscured crystallographic states from conventionally uninterpretable electron density.
Pearce, NM; Krojer, T; Bradley, AR; Collins, P; Nowak, RP; Talon, R; Marsden, BD; Kelm, S; Shi, J; Deane, CM; von Delft, F;
Nature Communications 8:15123- . doi: 10.1038/ncomms15123
Publication date: April 23, 2017
PMID: 28436492
Global survey of the immunomodulatory potential of common drugs.
Vladimer, GI; Snijder, B; Krall, N; Bigenzahn, JW; Huber, KVM; Lardeau, CH; Sanjiv, K; Ringler, A; Berglund, UW; Sabler, M; de la Fuente, OL; Knöbl, P; Kubicek, S; Helleday, T; Jäger, U; Superti-Furga, G;
Nature Chemical Biology 13:681-690 . doi: 10.1038/nchembio.2360
Publication date: April 23, 2017
PMID: 28437395
The RNF168 paralog RNF169 defines a new class of ubiquitylated-histone reader involved in the response to DNA damage.
Kitevski-LeBlanc J, Fradet-Turcotte A, Kukic P, Wilson MD, Portella G, Yuwen T, Panier S, Duan S, Canny MD, van Ingen H, Arrowsmith CH, Rubinstein JL, Vendruscolo M, Durocher D, Kay LE
Elife 6: . doi: 10.7554/eLife.23872
Publication date: April 13, 2017
PMID: 28406400
Benzoisoquinolinediones as Potent and Selective Inhibitors of BRPF2 and TAF1/TAF1L Bromodomains.
Bouché, L; Christ, CD; Siegel, S; Fernández-Montalván, AE; Holton, SJ; Fedorov, O; Ter Laak, A; Sugawara, T; Stöckigt, D; Tallant, C; Bennett, J; Monteiro, O; Díaz-Sáez, L; Siejka, P; Meier, J; Pütter, V; Weiske, J; Müller, S; Huber, KVM; Hartung, IV; Haendler, B;
Journal of Medicinal Chemistry 60:4002-4022 . doi: 10.1021/acs.jmedchem.7b00306
Publication date: April 11, 2017
PMID: 28402630
Highly selective inhibition of histone demethylases by de novo macrocyclic peptides.
Kawamura, A; Münzel, M; Kojima, T; Yapp, C; Bhushan, B; Goto, Y; Tumber, A; Katoh, T; King, ON; Passioura, T; Walport, LJ; Hatch, SB; Madden, S; Müller, S; Brennan, PE; Chowdhury, R; Hopkinson, RJ; Suga, H; Schofield, CJ;
Nature Communications 8:14773- . doi: 10.1038/ncomms14773
Publication date: April 5, 2017
PMID: 28382930
Molecular basis for the methylation specificity of ATXR5 for histone H3.
Bergamin E, Sarvan S, Malette J, Eram MS, Yeung S, Mongeon V, Joshi M, Brunzelle JS, Michaels SD, Blais A, Vedadi M, Couture JF
Nucleic Acids Res. . doi: 10.1093/nar/gkx224
Publication date: April 5, 2017
PMID: 28383693
MOB1 Mediated Phospho-recognition in the Core Mammalian Hippo Pathway.
Couzens, AL; Xiong, S; Knight, JDR; Mao, DY; Guettler, S; Picaud, S; Kurinov, I; Filippakopoulos, P; Sicheri, F; Gingras, AC;
Molecular and Cellular Proteomics 16:1098-1110 . doi: 10.1074/mcp.M116.065490
Publication date: April 2, 2017
PMID: 28373298

March 2017

Partial-occupancy binders identified by the Pan-Dataset Density Analysis method offer new chemical opportunities and reveal cryptic binding sites.
Pearce, NM; Bradley, AR; Krojer, T; Marsden, BD; Deane, CM; von Delft, F;
Structural Dynamics 4:032104- . doi: 10.1063/1.4974176
Publication date: March 30, 2017
PMID: 28345007
Bilayer-Mediated Structural Transitions Control Mechanosensitivity of the TREK-2 K2P Channel.
Aryal, P; Jarerattanachat, V; Clausen, MV; Schewe, M; McClenaghan, C; Argent, L; Conrad, LJ; Dong, YY; Pike, ACW; Carpenter, EP; Baukrowitz, T; Sansom, MSP; Tucker, SJ;
Structure 25:708-718.e2 . doi: 10.1016/j.str.2017.03.006
Publication date: March 24, 2017
PMID: 28392258
Human apo-SRP72 and SRP68/72 complex structures reveal the molecular basis of protein translocation.
Gao Y, Zhang Q, Lang Y, Liu Y, Dong X, Chen Z, Tian W, Tang J, Wu W, Tong Y, Chen Z
J Mol Cell Biol . doi: 10.1093/jmcb/mjx010
Publication date: March 20, 2017
PMID: 28369529
Development of a monoclonal anti-ADAMTS-5 antibody that specifically blocks the interaction with LRP1.
Santamaria, S; Fedorov, O; McCafferty, J; Murphy, G; Dudhia, J; Nagase, H; Yamamoto, K;
mAbs :0-0 . doi: 10.1080/19420862.2017.1304341
Publication date: March 17, 2017
PMID: 28306378
Tetrahydroisoquinoline-7-carboxamide Derivatives as New Selective Discoidin Domain Receptor 1 (DDR1) Inhibitors.
Wang, Z; Zhang, Y; Bartual, SG; Luo, J; Xu, T; Du, W; Xun, Q; Tu, Z; Brekken, RA; Ren, X; Bullock, AN; Liang, G; Lu, X; Ding, K;
ACS Medicinal Chemistry Letters 8:327-332 . doi: 10.1021/acsmedchemlett.6b00497
Publication date: March 9, 2017
PMID: 28337325
Oxalyl Boronates Enable Modular Synthesis of Bioactive Imidazoles.
Lee, CF; Holownia, A; Bennett, JM; Elkins, JM; St Denis, JD; Adachi, S; Yudin, AK;
Angewandte Chemie International Edition 56:6264-6267 . doi: 10.1002/anie.201611006
Publication date: March 7, 2017
PMID: 28267269
Antibody Validation by Immunoprecipitation Followed by Mass Spectrometry Analysis.
Persson H, Preger C, Marcon E, Lengqvist J, Gräslund S
Methods Mol. Biol. 1575:175-187 . doi: 10.1007/978-1-4939-6857-2_10
Publication date: March 4, 2017
PMID: 28255880
Potent and Selective KDM5 Inhibitor Stops Cellular Demethylation of H3K4me3 at Transcription Start Sites and Proliferation of MM1S Myeloma Cells.
Tumber, A; Nuzzi, A; Hookway, ES; Hatch, SB; Velupillai, S; Johansson, C; Kawamura, A; Savitsky, P; Yapp, C; Szykowska, A; Wu, N; Bountra, C; Strain-Damerell, C; Burgess-Brown, NA; Ruda, GF; Fedorov, O; Munro, S; England, KS; Nowak, RP; Schofield, CJ; La Thangue, NB; Pawlyn, C; Davies, F; Morgan, G; Athanasou, N; Müller, S; Oppermann, U; Brennan, PE;
Cell Chemical Biology 24:371-380 . doi: 10.1016/j.chembiol.2017.02.006
Publication date: March 2, 2017
PMID: 28262558
WONKA and OOMMPPAA: analysis of protein-ligand interaction data to direct structure-based drug design.
Deane, CM; Wall, ID; Green, DV; Marsden, BD; Bradley, AR;
Acta Crystallographica. Section d, Structural Biology 73:279-285 . doi: 10.1107/S2059798316009529
Publication date: March 1, 2017
PMID: 28291763
Assessing histone demethylase inhibitors in cells: lessons learned.
Hatch, SB; Yapp, C; Montenegro, RC; Savitsky, P; Gamble, V; Tumber, A; Ruda, GF; Bavetsias, V; Fedorov, O; Atrash, B; Raynaud, F; Lanigan, R; Carmichael, L; Tomlin, K; Burke, R; Westaway, SM; Brown, JA; Prinjha, RK; Martinez, ED; Oppermann, U; Schofield, CJ; Bountra, C; Kawamura, A; Blagg, J; Brennan, PE; Rossanese, O; Müller, S;
Epigenetics and Chromatin 10:9- . doi: 10.1186/s13072-017-0116-6
Publication date: March 1, 2017
PMID: 28265301
The XChemExplorer graphical workflow tool for routine or large-scale protein-ligand structure determination.
Krojer, T; Talon, R; Pearce, N; Collins, P; Douangamath, A; Brandao-Neto, J; Dias, A; Marsden, B; von Delft, F;
Acta Crystallographica. Section d, Structural Biology 73:267-278 . doi: 10.1107/S2059798316020234
Publication date: March 1, 2017
PMID: 28291762

February 2017

Thiazolidine derivatives as potent and selective inhibitors of the PIM kinase family.
Bataille, CJ; Brennan, MB; Byrne, S; Davies, SG; Durbin, M; Fedorov, O; Huber, KV; Jones, AM; Knapp, S; Liu, G; Nadali, A; Quevedo, CE; Russell, AJ; Walker, RG; Westwood, R; Wynne, GM;
Bioorganic and Medicinal Chemistry 25:2657-2665 . doi: 10.1016/j.bmc.2017.02.056
Publication date: February 28, 2017
PMID: 28341403
Peptide recognition by HP1 chromoshadow domains revisited: plasticity in the pseudosymmetric histone binding site of human HP1.
Liu Y, Qin S, Lei M, Tempel W, Zhang Y, Loppnau P, Li Y, Min J
J. Biol. Chem. . doi: 10.1074/jbc.M116.768374
Publication date: February 21, 2017
PMID: 28223359
Discovery of Peptidomimetic Ligands of EED as Allosteric Inhibitors of PRC2.
Barnash KD, The J, Norris-Drouin JL, Cholensky SH, Worley BM, Li F, Stuckey JI, Brown PJ, Vedadi M, Arrowsmith CH, Frye SV, James LI
ACS Comb Sci . doi: 10.1021/acscombsci.6b00174
Publication date: February 6, 2017
PMID: 28165227
Targeting human SET1/MLL family of proteins.
Vedadi M, Blazer L, Eram MS, Barsyte-Lovejoy D, Arrowsmith CH, Hajian T
Protein Sci. . doi: 10.1002/pro.3129
Publication date: February 4, 2017
PMID: 28160335
Establishing a reliable framework for harnessing the creative power of the scientific crowd.
Carter, AJ; Donner, A; Lee, WH; Bountra, C;
PLoS Biology 15:e2001387- . doi: 10.1371/journal.pbio.2001387
Publication date: February 1, 2017
PMID: 28199324

January 2017

The EED protein-protein interaction inhibitor A-395 inactivates the PRC2 complex.
He Y, Selvaraju S, Curtin ML, Jakob CG, Zhu H, Comess KM, Shaw B, The J, Lima-Fernandes E, Szewczyk MM, Cheng D, Klinge KL, Li HQ, Pliushchev M, Algire MA, Maag D, Guo J, Dietrich J, Panchal SC, Petros AM, Sweis RF, Torrent M, Bigelow LJ, Senisterra G, Li F, Kennedy S, Wu Q, Osterling DJ, Lindley DJ, Gao W, Galasinski S, Barsyte-Lovejoy D, Vedadi M, Buchanan FG, Arrowsmith CH, Chiang GG, Sun C, Pappano WN
Nat. Chem. Biol. . doi: 10.1038/nchembio.2306
Publication date: January 30, 2017
PMID: 28135237
Discovery of Potent and Selective Inhibitors for G9a-Like Protein (GLP) Lysine Methyltransferase.
Xiong Y, Li F, Babault N, Dong A, Zeng H, Wu H, Chen X, Arrowsmith CH, Brown PJ, Liu J, Vedadi M, Jin J
J. Med. Chem. . doi: 10.1021/acs.jmedchem.6b01645
Publication date: January 30, 2017
PMID: 28135087
Explicit treatment of active-site waters enhances quantum mechanical/implicit solvent scoring: Inhibition of CDK2 by new pyrazolo[1,5-a]pyrimidines.
Hylsová, M; Carbain, B; Fanfrlík, J; Musilová, L; Haldar, S; Köprülüoğlu, C; Ajani, H; Brahmkshatriya, PS; Jorda, R; Kryštof, V; Hobza, P; Echalier, A; Paruch, K; Lepšík, M;
European Journal of Medicinal Chemistry 126:1118-1128 . doi: 10.1016/j.ejmech.2016.12.023
Publication date: January 27, 2017
PMID: 28039837
Discovery and structure activity relationship of the first potent cryptosporidium FIKK kinase inhibitor.
Osman KT, Ye J, Shi Z, Toker C, Lovato D, Jumani RS, Zuercher W, Huston CD, Edwards AM, Lautens M, Santhakumar V, Hui R
Bioorg. Med. Chem. . doi: 10.1016/j.bmc.2017.01.036
Publication date: January 24, 2017
PMID: 28162900
The SUV4-20 inhibitor A-196 verifies a role for epigenetics in genomic integrity.
Bromberg KD, Mitchell TR, Upadhyay AK, Jakob CG, Jhala MA, Comess KM, Lasko LM, Li C, Tuzon CT, Dai Y, Li F, Eram MS, Nuber A, Soni NB, Manaves V, Algire MA, Sweis RF, Torrent M, Schotta G, Sun C, Michaelides MR, Shoemaker AR, Arrowsmith CH, Brown PJ, Santhakumar V, Martin A, Rice JC, Chiang GG, Vedadi M, Barsyte-Lovejoy D, Pappano WN
Nat. Chem. Biol. . doi: 10.1038/nchembio.2282
Publication date: January 23, 2017
PMID: 28114273
Target engagement: Shining a light.
H, K; u, V; b, ; e, ; r, ;
Nature Chemical Biology 13:133-134 . doi: 10.1038/nchembio.2295
Publication date: January 19, 2017
PMID: 28103226
Insights into the RecQ helicase mechanism revealed by the structure of the helicase domain of human RECQL5.
Newman, JA; Aitkenhead, H; Savitsky, P; Gileadi, O;
Nucleic Acids Research 45:4231-4243 . doi: 10.1093/nar/gkw1362
Publication date: January 18, 2017
PMID: 28100692
Molecular insights into lipid-assisted Ca(2+) regulation of the TRP channel Polycystin-2.
Wilkes, M; Madej, MG; Kreuter, L; Rhinow, D; Heinz, V; De Sanctis, S; Ruppel, S; Richter, RM; Joos, F; Grieben, M; Pike, AC; Huiskonen, JT; Carpenter, EP; Kühlbrandt, W; Witzgall, R; Ziegler, C;
Nature Structural and Molecular Biology 24:123-130 . doi: 10.1038/nsmb.3357
Publication date: January 16, 2017
PMID: 28092368
Chemical Probes Targeting Epigenetic Proteins: Applications Beyond Oncology.
Ackloo S, Brown PJ, Müller S
Epigenetics 0 . doi: 10.1080/15592294.2017.1279371
Publication date: January 12, 2017
PMID: 28080202
Design of a Biased Potent Small Molecule Inhibitor of the Bromodomain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo Studies.
Igoe, N; Bayle, ED; Fedorov, O; Tallant, C; Savitsky, P; Rogers, C; Owen, DR; Deb, G; Somervaille, TC; Andrews, DM; Jones, N; Cheasty, A; Ryder, H; Brennan, PE; Müller, S; Knapp, S; Fish, PV;
Journal of Medicinal Chemistry 60:668-680 . doi: 10.1021/acs.jmedchem.6b01583
Publication date: January 9, 2017
PMID: 28068087
Epigenetic siRNA and Chemical Screens Identify SETD8 Inhibition as a Therapeutic Strategy for p53 Activation in High-Risk Neuroblastoma.
Veschi V, Liu Z, Voss TC, Ozbun L, Gryder B, Yan C, Hu Y, Ma A, Jin J, Mazur SJ, Lam N, Souza BK, Giannini G, Hager GL, Arrowsmith CH, Khan J, Appella E, Thiele CJ
Cancer Cell 31(1):50-63 . doi: 10.1016/j.ccell.2016.12.002
Publication date: January 9, 2017
PMID: 28073004
Functions of bromodomain-containing proteins and their roles in homeostasis and cancer.
Fujisawa, T; Filippakopoulos, P;
Nature Reviews: Molecular Cell Biology 18:246-262 . doi: 10.1038/nrm.2016.143
Publication date: January 5, 2017
PMID: 28053347
Structure and inhibitor specificity of the PCTAIRE-family kinase CDK16.
Dixon-Clarke, SE; Shehata, SN; Krojer, T; Sharpe, TD; von Delft, F; Sakamoto, K; Bullock, AN;
Biochemical Journal 474:699-713 . doi: 10.1042/BCJ20160941
Publication date: January 5, 2017
PMID: 28057719
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 16:88-101 . doi: 10.1158/1535-7163.MCT-16-0235
Publication date: January 1, 2017
PMID: 28062706
2016

December 2016

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 24:114-122 . doi: 10.1038/nsmb.3343
Publication date: December 19, 2016
PMID: 27991905
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 24:9-23 . doi: 10.1016/j.chembiol.2016.11.009
Publication date: December 10, 2016
PMID: 27989401

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