Publications

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

2016

Development of chemical probes for the bromodomains of BRD7 and BRD9.

Clark PG, Dixon DJ, Brennan PE

Drug Discov Today Technol. 19:73-80. doi: 10.1016/j.ddtec.2016.05.002

Publication date: October 23, 2016

PMID: 27769361

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

An Unusual Binding Model of the Methyl 9-Anilinothiazolo[5,4-f] quinazoline-2-carbimidates (EHT 1610 and EHT 5372) Confers High Selectivity for Dual-specificity Tyrosine Phosphorylation-Regulated Kinases.

Chaikuad A, Diharce J, Schröder M, Foucourt A, Leblond B, Casagrande AS, Desire L, Bonnet P, Knapp S, Besson T

J. Med. Chem.. doi: 10.1021/acs.jmedchem.6b01083

Publication date: October 21, 2016

PMID: 27766861

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

Sci Adv. 2(10):e1600760. doi: 10.1126/sciadv.1600760

Publication date: October 21, 2016

PMID: 27757418

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 Differ.. doi: 10.1038/cdd.2016.83

Publication date: October 7, 2016

PMID: 27716744

Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors.

Popp TA, Tallant C, Rogers C, Fedorov O, Brennan PE, Müller S, Knapp S, Bracher F

J. Med. Chem.. doi: 10.1021/acs.jmedchem.6b00774

Publication date: September 27, 2016

PMID: 27673482

The oncometabolite 2-hydroxyglutarate activates the mTOR signalling pathway.

Carbonneau M, M Gagné L, Lalonde ME, Germain MA, Motorina A, Guiot MC, Secco B, Vincent EE, Tumber A, Hulea L, Bergeman J, Oppermann U, Jones RG, Laplante M, Topisirovic I, Petrecca K, Huot MÉ, Mallette FA

Nat Commun. 7:12700. doi: 10.1038/ncomms12700

Publication date: September 15, 2016

PMID: 27624942

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

J. Med. Chem.. doi: 10.1021/acs.jmedchem.6b00355

Publication date: September 12, 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

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. doi: 10.1093/brain/aww221

Publication date: September 6, 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

Generation and analyses of human synthetic antibody libraries and their application for protein microarrays.

Säll A, Walle M, Wingren C, Müller S, Nyman T, Vala A, Ohlin M, Borrebaeck CA, Persson H

Protein Eng. Des. Sel.. doi: 10.1093/protein/gzw042

Publication date: September 1, 2016

PMID: 27590051

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

Targeting the Bromome: are we there yet?

Müller S

Future Med Chem. doi: 10.4155/fmc-2016-0136

Publication date: August 31, 2016

PMID: 27578167

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

Nat. Chem. Biol.. doi: 10.1038/nchembio.2166

Publication date: August 29, 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 Harb Perspect Biol. doi: 10.1101/cshperspect.a022111

Publication date: August 22, 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

A germline mutation of CDKN2A and a novel RPLP1-C19MC fusion detected in a rare melanotic neuroectodermal tumor of infancy: a case report.

Barnes DJ, Hookway E, Athanasou N, Kashima T, Oppermann U, Hughes S, Swan D, Lueerssen D, Anson J, Hassan AB

BMC Cancer. 16(1):629. doi: 10.1186/s12885-016-2669-3

Publication date: August 12, 2016

PMID: 27519597

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

Biochem. Pharmacol.. doi: 10.1016/j.bcp.2016.08.009

Publication date: August 9, 2016

PMID: 27520485

Accelerating target discovery using pre-competitive open science-patients need faster innovation more than anyone else.

Low E, Bountra C, Lee WH

Ecancermedicalscience. 10:ed57. doi: 10.3332/ecancer.2016.ed57

Publication date: August 3, 2016

PMID: 27594912

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

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

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. doi: 10.1016/j.ccell.2016.06.020

Publication date: July 27, 2016

PMID: 27478041

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

Effect of BET Missense Mutations on Bromodomain Function, Inhibitor Binding and Stability.

Lori L, Pasquo A, Lori C, Petrosino M, Chiaraluce R, Tallant C, Knapp S, Consalvi V

PLoS ONE. 11(7):e0159180. doi: 10.1371/journal.pone.0159180

Publication date: July 12, 2016

PMID: 27403962

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.. doi: 10.1021/acs.jmedchem.6b00668

Publication date: July 8, 2016

PMID: 27390919

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.. doi: 10.1016/j.jsb.2016.07.001

Publication date: July 8, 2016

PMID: 27402533

H3K27me3 demethylases regulate in vitro chondrogenesis and chondrocyte activity in osteoarthritis.

Yapp C, Carr AJ, Price A, Oppermann U, Snelling SJ

Arthritis Res. Ther.. 18(1):158. doi: 10.1186/s13075-016-1053-7

Publication date: July 7, 2016

PMID: 27388528

Exploring the role of water in molecular recognition: predicting protein ligandability using a combinatorial search of surface hydration sites.

Vukovic S, Brennan PE, Huggins DJ

J Phys Condens Matter. 28(34):344007. doi: 10.1088/0953-8984/28/34/344007

Publication date: July 1, 2016

PMID: 27367338

Advances and challenges in understanding histone demethylase biology.

Nowak RP, Tumber A, Johansson C, Che KH, Brennan P, Owen D, Oppermann U

Curr Opin Chem Biol. 33:151-159. doi: 10.1016/j.cbpa.2016.06.021

Publication date: June 29, 2016

PMID: 27371875

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

Proc. Natl. Acad. Sci. U.S.A.. doi: 10.1073/pnas.1600633113

Publication date: June 20, 2016

PMID: 27325775

Methyltransferase inhibitors for modulation of the epigenome and beyond.

Schapira M, Arrowsmith CH

Curr Opin Chem Biol. 33:81-87. doi: 10.1016/j.cbpa.2016.05.030

Publication date: June 16, 2016

PMID: 27318562

Structure and function of histone methylation-binding proteins in plants.

Liu Y, Min J

Biochem. J.. 473(12):1663-80. doi: 10.1042/BCJ20160123

Publication date: June 15, 2016

PMID: 27288029

Mammalian Glucose Transporter Activity is Dependent upon Anionic and Conical Phospholipids.

Hresko RC, Kraft TE, Quigley A, Carpenter EP, Hruz PW

J. Biol. Chem.. doi: 10.1074/jbc.M116.730168

Publication date: June 14, 2016

PMID: 27302065

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.. doi: 10.1038/nsmb.3249

Publication date: June 13, 2016

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. doi: 10.1016/j.celrep.2016.05.051

Publication date: June 8, 2016

PMID: 27292644

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.. doi: 10.1074/jbc.M116.740787

Publication date: June 2, 2016

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. doi: 10.18632/oncotarget.9766

Publication date: June 1, 2016

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

J. Gen. Physiol.. 147(6):497-505. doi: 10.1085/jgp.201611601

Publication date: June 1, 2016

PMID: 27241700

From structural biology to designing therapy for inborn errors of metabolism.

Yue WW

J. Inherit. Metab. Dis.. doi: 10.1007/s10545-016-9923-3

Publication date: May 30, 2016

PMID: 27240455

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. 5:. doi: 10.7554/eLife.10607

Publication date: May 25, 2016

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 Chem. Biol.. doi: 10.1021/acschembio.6b00286

Publication date: May 24, 2016

PMID: 27219844

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

J. Med. Chem.. doi: 10.1021/acs.jmedchem.6b00140

Publication date: May 24, 2016

PMID: 27219676

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

Nat. Immunol.. doi: 10.1038/ni.3470

Publication date: May 23, 2016

PMID: 27213690

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

Nat. Chem. Biol.. doi: 10.1038/nchembio.2087

Publication date: May 23, 2016

PMID: 27214403

Perspective: Science is still too closed.

Edwards A

Nature. 533:S70. doi: 10.1038/533S70a

Publication date: May 12, 2016

PMID: 27167397

Displaying 1001 - 1050 of 1839
Download XLS