Publications

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Displaying 1 - 50 of 1168

2017

February 2017

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

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
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
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
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
Filippakopoulos, P; Fujisawa, T;
Nature Reviews: Molecular Cell Biology :- . doi: 10.1038/nrm.2016.143
Publication date: January 5, 2017
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 16:88-101 . doi: 10.1158/1535-7163.MCT-16-0235
Publication date: January 1, 2017
PMID: 28062706
2016

December 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. . doi: 10.1189/jlb.3MA0716-334RR
Publication date: December 29, 2016
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 :- . doi: 10.1038/nsmb.3343
Publication date: December 19, 2016
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
Angew. Chem. Int. Ed. Engl. . doi: 10.1002/anie.201610816
Publication date: December 14, 2016
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 :- . doi: 10.1016/j.chembiol.2016.11.009
Publication date: December 10, 2016
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 7(12):1102-1106 . doi: 10.1021/acsmedchemlett.6b00303
Publication date: December 8, 2016
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 Rep 17(10):2724-2737 . doi: 10.1016/j.celrep.2016.11.014
Publication date: December 6, 2016
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 17:1361-1372 . doi: 10.1038/ni.3590
Publication date: December 1, 2016
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 8:1152-1158 . doi: 10.1038/nchem.2591
Publication date: December 1, 2016
PMID: 27874871

November 2016

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 :- . doi: 10.1016/j.cell.2016.11.010
Publication date: November 30, 2016
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 64:704-719 . doi: 10.1016/j.molcel.2016.09.032
Publication date: November 17, 2016
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. . doi: 10.1021/acs.jmedchem.6b01244
Publication date: November 2, 2016
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. 30(21):2376-2390 . doi: 10.1101/gad.288340.116
Publication date: November 1, 2016
PMID: 27881600

October 2016

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 . doi: 10.1021/acsinfecdis.6b00078
Publication date: October 31, 2016
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. 1493:89-105 . doi: 10.1007/978-1-4939-6448-2_6
Publication date: October 28, 2016
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 . doi: 10.1007/s10858-016-0070-9
Publication date: October 22, 2016
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 . doi: 10.1016/j.bbagen.2016.10.019
Publication date: October 21, 2016
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 23:1930-1940 . doi: 10.1038/cdd.2016.83
Publication date: October 6, 2016
PMID: 27716744

September 2016

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 2:e1600760- . doi: 10.1126/sciadv.1600760
Publication date: September 30, 2016
PMID: 27757418
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 117:35-45 . doi:
Publication date: September 30, 2016
PMID: 27520485
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 :- . doi:
Publication date: September 27, 2016
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 :- . doi:
Publication date: September 26, 2016
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 :- . doi:
Publication date: September 26, 2016
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 :- . doi: 10.1093/nar/gkw826
Publication date: September 18, 2016
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 :- . doi:
Publication date: September 11, 2016
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 2(9):627-641 . doi: 10.1021/acsinfecdis.6b00090
Publication date: September 9, 2016
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 5: . doi: 10.7554/eLife.17101
Publication date: September 7, 2016
PMID: 27595565
Chemical probes and inhibitors of bromodomains outside the BET family
Moustakim, M; Clark, PGK; Hay, DA; Dixon, DJ; Brennan, PE;
MedChemComm :- . doi: 10.1039/C6MD00373G
Publication date: September 6, 2016
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 :- . doi:
Publication date: September 5, 2016
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 . doi: 10.1038/nmeth.3995
Publication date: September 5, 2016
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. . doi: 10.1021/acs.jmedchem.6b01033
Publication date: September 1, 2016
PMID: 27584694

August 2016

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 . doi: 10.1177/1087057116666276
Publication date: August 31, 2016
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 12:876-884 . doi:
Publication date: August 28, 2016
PMID: 27571479
Chemical Inhibition of Protein Methyltransferases.
Schapira M
Cell Chem Biol . doi: 10.1016/j.chembiol.2016.07.014
Publication date: August 24, 2016
PMID: 27569753
Structural Basis of Intracellular TGF-β Signaling: Receptors and Smads.
Chaikuad, A; Bullock, AN;
Cold Spring Harbor perspectives in biology :- . doi:
Publication date: August 21, 2016
PMID: 27549117
Structural biology: HDAC6 finally crystal clear.
Liu Y, Li L, Min J
Nat. Chem. Biol. 12(9):660-1 . doi: 10.1038/nchembio.2158
Publication date: August 18, 2016
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 :- . doi:
Publication date: August 10, 2016
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 30:273-289 . doi:
Publication date: August 4, 2016
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. . doi: 10.1042/BCJ20160537
Publication date: August 1, 2016
PMID: 27480107

July 2016

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. . doi: 10.1021/acs.jmedchem.6b00855
Publication date: July 28, 2016
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. . doi: 10.1016/j.bmcl.2016.07.041
Publication date: July 21, 2016
PMID: 27485386

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