Publications

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2014

Corrigendum: Dual kinase-bromodomain inhibitors for rationally designed polypharmacology.

Ciceri P, Müller S, O'Mahony A, Fedorov O, Filippakopoulos P, Hunt JP, Lasater EA, Pallares G, Picaud S, Wells C, Martin S, Wodicka LM, Shah NP, Treiber DK, Knapp S

Nat. Chem. Biol.. 10(8):692.

Publication date: July 18, 2014

PMID: 25036311

Discovery of a Selective, Substrate-competitive Inhibitor of the Lysine Methyltransferase SETD8.

Ma A, Yu W, Li F, Bleich RM, Herold JM, Butler KV, Norris JL, Korboukh V, Tripathy A, Janzen WP, Arrowsmith CH, Frye SV, Vedadi M, Brown PJ, Jin J

J. Med. Chem.. doi: 10.1021/jm500871s

Publication date: July 17, 2014

PMID: 25032507

A Methylation-Phosphorylation Switch Determines Sox2 Stability and Function in ESC Maintenance or Differentiation.

Fang L, Zhang L, Wei W, Jin X, Wang P, Tong Y, Li J, Du JX, Wong J

Mol. Cell. doi: 10.1016/j.molcel.2014.06.018

Publication date: July 16, 2014

PMID: 25042802

Assessing cellular efficacy of bromodomain inhibitors using fluorescence recovery after photobleaching.

Philpott M, Rogers CM, Yapp C, Wells C, Lambert JP, Strain-Damerell C, Burgess-Brown NA, Gingras AC, Knapp S, Müller S

Epigenetics Chromatin. 7:14. doi: 10.1186/1756-8935-7-14

Publication date: July 13, 2014

PMID: 25097667

Human-chromatin-related protein interactions identify a demethylase complex required for chromosome segregation.

Marcon E, Ni Z, Pu S, Turinsky AL, Trimble SS, Olsen JB, Silverman-Gavrila R, Silverman-Gavrila L, Phanse S, Guo H, Zhong G, Guo X, Young P, Bailey S, Roudeva D, Zhao D, Hewel J, Li J, Gräslund S, Paduch M, Kossiakoff AA, Lupien M, Emili A, Wodak SJ, Greenblatt J

Cell Rep. 8(1):297-310. doi: 10.1016/j.celrep.2014.05.050

Publication date: July 10, 2014

PMID: 24981860

Bromodomain Protein BRD4 Is Required for Estrogen Receptor-Dependent Enhancer Activation and Gene Transcription.

Nagarajan S, Hossan T, Alawi M, Najafova Z, Indenbirken D, Bedi U, Taipaleenmäki H, Ben-Batalla I, Scheller M, Loges S, Knapp S, Hesse E, Chiang CM, Grundhoff A, Johnsen SA

Cell Rep. doi: 10.1016/j.celrep.2014.06.016

Publication date: July 9, 2014

PMID: 25017071

A scintillation proximity assay for histone demethylases.

Yu W, Eram MS, Hajian T, Szykowska A, Burgess-Brown N, Vedadi M, Brown PJ

Anal. Biochem.. doi: 10.1016/j.ab.2014.06.023

Publication date: July 8, 2014

PMID: 25010373

RPRD1A and RPRD1B are human RNA polymerase II C-terminal domain scaffolds for Ser5 dephosphorylation.

Ni Z, Xu C, Guo X, Hunter GO, Kuznetsova OV, Tempel W, Marcon E, Zhong G, Guo H, Kuo WH, Li J, Young P, Olsen JB, Wan C, Loppnau P, El Bakkouri M, Senisterra GA, He H, Huang H, Sidhu SS, Emili A, Murphy S, Mosley AL, Arrowsmith CH, Min J, Greenblatt JF

Nat. Struct. Mol. Biol.. doi: 10.1038/nsmb.2853

Publication date: July 6, 2014

PMID: 24997600

Discovery and Optimization of Small-Molecule Ligands for the CBP/p300 Bromodomains.

Hay DA, Fedorov O, Martin S, Singleton DC, Tallant C, Wells C, Picaud S, Philpott M, Monteiro OP, Rogers CM, Conway SJ, Rooney TP, Tumber A, Yapp C, Filippakopoulos P, Bunnage ME, Müller S, Knapp S, Schofield CJ, Brennan PE

J. Am. Chem. Soc.. 136(26):9308-19. doi: 10.1021/ja412434f

Publication date: July 2, 2014

PMID: 24946055

Multiparameter Optimization in CNS Drug Discovery: Design of Pyrimido[4,5-d]azepines as Potent 5-Hydroxytryptamine 2C (5-HT2C) Receptor Agonists with Exquisite Functional Selectivity over 5-HT2A and 5-HT2B Receptors.

Storer RI, Brennan PE, Brown AD, Bungay PJ, Conlon KM, Corbett MS, DePianta RP, Fish PV, Heifetz A, Ho DK, Jessiman AS, McMurray G, de Oliveira CA, Roberts LR, Root JA, Shanmugasundaram V, Shapiro MJ, Skerten M, Westbrook D, Wheeler S, Whitlock GA, Wright J

J. Med. Chem.. 57(12):5258-69. doi: 10.1021/jm5003292

Publication date: June 26, 2014

PMID: 24878222

Linking genotypes database with locus-specific database and genotype-phenotype correlation in phenylketonuria.

Wettstein S, Underhaug J, Perez B, Marsden BD, Yue WW, Martinez A, Blau N

Eur. J. Hum. Genet.. doi: 10.1038/ejhg.2014.114

Publication date: June 18, 2014

PMID: 24939588

STRUCTURAL CHARACTERIZATION OF HUMAN CHOLESTEROL 7α-HYDROXYLASE.

Tempel W, Grabovec I, MacKenzie F, Dichenko YV, Usanov SA, Gilep AA, Park HW, Strushkevich N

J. Lipid Res.. doi: 10.1194/jlr.M050765

Publication date: June 13, 2014

PMID: 24927729

A comparison of protein kinases inhibitor screening methods using both enzymatic activity and binding affinity determination.

Rudolf AF, Skovgaard T, Knapp S, Jensen LJ, Berthelsen J

PLoS ONE. 9(6):e98800. doi: 10.1371/journal.pone.0098800

Publication date: June 10, 2014

PMID: 24915177

Structural basis for histone mimicry and hijacking of host proteins by influenza virus protein NS1.

Qin S, Liu Y, Tempel W, Eram MS, Bian C, Liu K, Senisterra G, Crombet L, Vedadi M, Min J

Nat Commun. 5:3952. doi: 10.1038/ncomms4952

Publication date: May 24, 2014

PMID: 24853335

A Series of Potent CREBBP Bromodomain Ligands Reveals an Induced-Fit Pocket Stabilized by a Cation-π Interaction.

Rooney TP, Filippakopoulos P, Fedorov O, Picaud S, Cortopassi WA, Hay DA, Martin S, Tumber A, Rogers CM, Philpott M, Wang M, Thompson AL, Heightman TD, Pryde DC, Cook A, Paton RS, Müller S, Knapp S, Brennan PE, Conway SJ

Angew. Chem. Int. Ed. Engl.. doi: 10.1002/anie.201402750

Publication date: May 12, 2014

PMID: 24821300

Ribosomal oxygenases are structurally conserved from prokaryotes to humans.

Chowdhury R, Sekirnik R, Brissett NC, Krojer T, Ho CH, Ng SS, Clifton IJ, Ge W, Kershaw NJ, Fox GC, Muniz JR, Vollmar M, Phillips C, Pilka ES, Kavanagh KL, von Delft F, Oppermann U, McDonough MA, Doherty AJ, Schofield CJ

Nature. doi: 10.1038/nature13263

Publication date: May 11, 2014

PMID: 24814345

A Chromatin-Dependent Role of the Fragile X Mental Retardation Protein FMRP in the DNA Damage Response.

Alpatov R, Lesch BJ, Nakamoto-Kinoshita M, Blanco A, Chen S, Stützer A, Armache KJ, Simon MD, Xu C, Ali M, Murn J, Prisic S, Kutateladze TG, Vakoc CR, Min J, Kingston RE, Fischle W, Warren ST, Page DC, Shi Y

Cell. 157(4):869-81. doi: 10.1016/j.cell.2014.03.040

Publication date: May 8, 2014

PMID: 24813610

Structural basis for phosphoinositide substrate recognition, catalysis, and membrane interactions in human inositol polyphosphate 5-phosphatases.

Trésaugues L, Silvander C, Flodin S, Welin M, Nyman T, Gräslund S, Hammarström M, Berglund H, Nordlund P

Structure. 22(5):744-55. doi: 10.1016/j.str.2014.01.013

Publication date: May 6, 2014

PMID: 24704254

Human UTY(KDM6C) is a Male-Specific N{epsilon}-Methyl Lysyl-Demethylase.

Walport LJ, Hopkinson RJ, Vollmar M, Madden SK, Gileadi C, Oppermann U, Schofield CJ, Johansson C

J. Biol. Chem.. doi: 10.1074/jbc.M114.555052

Publication date: May 5, 2014

PMID: 24798337

Enzymatic and Structural Characterization of rTSγ Provides Insights into the Function of rTSβ.

Wichelecki DJ, Froese DS, Kopec J, Muniz JR, Yue WW, Gerlt JA

Biochemistry. 53(16):2732-8. doi: 10.1021/bi500349e

Publication date: April 29, 2014

PMID: 24697329

Exploration of Type II Binding Mode: A Privileged Approach for Kinase Inhibitor Focused Drug Discovery?

Zhao Z, Wu H, Wang L, Liu Y, Knapp S, Liu Q, Gray NS

ACS Chem. Biol.. doi: 10.1021/cb500129t

Publication date: April 29, 2014

PMID: 24730530

Structures of human ALKBH5 demethylase reveal a unique binding mode for specific single stranded m6A RNA demethylation.

Xu C, Liu K, Tempel W, Demetriades M, Aik W, Schofield CJ, Min J

J. Biol. Chem.. doi: 10.1074/jbc.M114.550350

Publication date: April 28, 2014

PMID: 24778178

Structural Mechanisms Determining Inhibition of the Collagen Receptor DDR1 by Selective and Multi-Targeted Type II Kinase Inhibitors.

Canning P, Tan L, Chu K, Lee SW, Gray NS, Bullock AN

J. Mol. Biol.. doi: 10.1016/j.jmb.2014.04.014

Publication date: April 23, 2014

PMID: 24768818

Targeting bromodomains: epigenetic readers of lysine acetylation.

Filippakopoulos P, Knapp S

Nat Rev Drug Discov. 13(5):337-56. doi: 10.1038/nrd4286

Publication date: April 22, 2014

PMID: 24751816

Modulation of the chromatin phosphoproteome by the Haspin protein kinase.

Maiolica A, De Medina Redondo M, Schoof EM, Chaikuad A, Villa F, Gatti M, Jeganatgan S, Lou HJ, Novy K, Hauri S, Toprak UH, Herzog F, Meraldi P, Penengo L, Turk BE, Knapp S, Linding R, Aebersold R

Mol. Cell Proteomics. doi: 10.1074/mcp.M113.034819

Publication date: April 14, 2014

PMID: 24732914

Stereospecific targeting of MTH1 by (S)-crizotinib as an anticancer strategy.

Huber KV, Salah E, Radic B, Gridling M, Elkins JM, Stukalov A, Jemth AS, Göktürk C, Sanjiv K, Strömberg K, Pham T, Berglund UW, Colinge J, Bennett KL, Loizou JI, Helleday T, Knapp S, Superti-Furga G

Nature. 508(7495):222-7. doi: 10.1038/nature13194

Publication date: April 10, 2014

PMID: 24695225

Copper is required for oncogenic BRAF signalling and tumorigenesis.

Brady DC, Crowe MS, Turski ML, Hobbs GA, Yao X, Chaikuad A, Knapp S, Xiao K, Campbell SL, Thiele DJ, Counter CM

Nature. doi: 10.1038/nature13180

Publication date: April 9, 2014

PMID: 24717435

Recurrent activating ACVR1 mutations in diffuse intrinsic pontine glioma.

Taylor KR, Mackay A, Truffaux N, Butterfield YS, Morozova O, Philippe C, Castel D, Grasso CS, Vinci M, Carvalho D, Carcaboso AM, de Torres C, Cruz O, Mora J, Entz-Werle N, Ingram WJ, Monje M, Hargrave D, Bullock AN, Puget S, Yip S, Jones C, Grill J

Nat. Genet.. 46(5):457-61. doi: 10.1038/ng.2925

Publication date: April 6, 2014

PMID: 24705252

Epigenetic targets and drug discovery: Part 1: Histone methylation.

Liu Y, Liu K, Qin S, Xu C, Min J

Pharmacol. Ther.. doi: 10.1016/j.pharmthera.2014.03.007

Publication date: April 2, 2014

PMID: 24704322

Novel approaches for targeting kinases: allosteric inhibition, allosteric activation and pseudokinases.

Cowan-Jacob SW, Jahnke W, Knapp S

Future Med Chem. 6(5):541-61. doi: 10.4155/fmc.13.216

Publication date: March 22, 2014

PMID: 24649957

Correction to Discovery of a Potent and Selective DDR1 Receptor Tyrosine Kinase Inhibitor.

Kim HG, Tan L, Weisberg EL, Liu F, Canning P, Choi HG, Ezell S, Zhao Z, Wu H, Wang J, Mandinova A, Bullock AN, Liu Q, Lee SW, Gray NS

ACS Chem. Biol.. 9(3):840.

Publication date: March 21, 2014

PMID: 24527812

Benzoselenadiazole-based responsive long-lifetime photoluminescent probes for protein kinases.

Ekambaram R, Enkvist E, Manoharan GB, Ugandi M, Kasari M, Viht K, Knapp S, Issinger OG, Uri A

Chem. Commun. (Camb.). 50(31):4096-8. doi: 10.1039/c3cc49198f

Publication date: March 20, 2014

PMID: 24619026

Protein ISGylation delays but does not overcome coronavirus proliferation in a model of fulminant hepatitis.

Ma XZ, Bartczak A, Zhang J, He W, Shalev I, Smil D, Chen L, Phillips J, Feld JJ, Selzner N, Levy G, McGilvray I

J. Virol.. doi: 10.1128/JVI.03801-13

Publication date: March 19, 2014

PMID: 24648452

Structural and biochemical characterisation of the KLHL3-WNK kinase interaction important in blood pressure regulation.

Schumacher FR, Sorrell FJ, Alessi DR, Bullock AN, Kurz T

Biochem. J.. doi: 10.1042/BJ20140153

Publication date: March 18, 2014

PMID: 24641320

Trimethylation of Histone H3 Lysine 36 by Human Methyltransferase PRDM9.

Eram MS, Bustos SP, Lima-Fernandes E, Siarheyeva A, Senisterra G, Hajian T, Chau I, Duan S, Wu H, Dombrovski L, Schapira M, Arrowsmith CH, Vedadi M

J. Biol. Chem.. doi: 10.1074/jbc.M113.523183

Publication date: March 14, 2014

PMID: 24634223

Crystal Structures of Human RNA Demethylase Alkbh5 Reveal Basis for Substrate Recognition.

Feng C, Liu Y, Wang G, Deng Z, Zhang Q, Wu W, Tong Y, Cheng C, Chen Z

J. Biol. Chem.. doi: 10.1074/jbc.M113.546168

Publication date: March 10, 2014

PMID: 24616105

Case study--structural genomics and human protein kinases.

Elkins JM

Methods Mol. Biol.. 1140:325-36. doi: 10.1007/978-1-4939-0354-2_24

Publication date: March 5, 2014

PMID: 24590728

Salvage or recovery of failed targets by in situ proteolysis.

Tong Y, Dong A, Xu X, Wernimont A

Methods Mol. Biol.. 1140:179-88. doi: 10.1007/978-1-4939-0354-2_14

Publication date: March 5, 2014

PMID: 24590718

Structural genomics of human proteins.

Osman KT, Edwards A

Methods Mol. Biol.. 1140:27-34. doi: 10.1007/978-1-4939-0354-2_2

Publication date: March 5, 2014

PMID: 24590706

A Basic Post-SET Extension of NSDs Is Essential for Nucleosome Binding In Vitro.

Allali-Hassani A, Kuznetsova E, Hajian T, Wu H, Dombrovski L, Li Y, Gräslund S, Arrowsmith CH, Schapira M, Vedadi M

J Biomol Screen. doi: 10.1177/1087057114525854

Publication date: March 4, 2014

PMID: 24595546

The roles of Jumonji-type oxygenases in human disease.

Johansson C, Tumber A, Che K, Cain P, Nowak R, Gileadi C, Oppermann U

Epigenomics. 6(1):89-120. doi: 10.2217/epi.13.79

Publication date: March 4, 2014

PMID: 24579949

Dual kinase-bromodomain inhibitors for rationally designed polypharmacology.

Ciceri P, Müller S, O'Mahony A, Fedorov O, Filippakopoulos P, Hunt JP, Lasater EA, Pallares G, Picaud S, Wells C, Martin S, Wodicka LM, Shah NP, Treiber DK, Knapp S

Nat. Chem. Biol.. 10(4):305-12. doi: 10.1038/nchembio.1471

Publication date: March 2, 2014

PMID: 24584101

Mutation or knock-down of 17β-hydroxysteroid dehydrogenase type 10 cause loss of MRPP1 and impaired processing of mitochondrial heavy strand transcripts.

Deutschmann AJ, Amberger A, Zavadil C, Steinbeisser H, Mayr JA, Feichtinger RG, Oerum S, Yue WW, Zschocke J

Hum. Mol. Genet.. doi: 10.1093/hmg/ddu072

Publication date: February 26, 2014

PMID: 24549042

Discovery and development of potent and selective inhibitors of histone methyltransferase g9a.

Sweis RF, Pliushchev M, Brown PJ, Guo J, Li F, Maag D, Petros AM, Soni NB, Tse C, Vedadi M, Michaelides MR, Chiang GG, Pappano WN

ACS Med Chem Lett. 5(2):205-9. doi: 10.1021/ml400496h

Publication date: February 13, 2014

PMID: 24900801

EMA401, an orally administered highly selective angiotensin II type 2 receptor antagonist, as a novel treatment for postherpetic neuralgia: a randomised, double-blind, placebo-controlled phase 2 clinical trial.

Rice AS, Dworkin RH, McCarthy TD, Anand P, Bountra C, McCloud PI, Hill J, Cutter G, Kitson G, Desem N, Raff M

Lancet. doi: 10.1016/S0140-6736(13)62337-5

Publication date: February 4, 2014

PMID: 24507377

New strategies to inhibit KEAP1 and the Cul3-based E3 ubiquitin ligases.

Canning P, Bullock AN

Biochem. Soc. Trans.. 42(1):103-7. doi: 10.1042/BST20130215

Publication date: February 1, 2014

PMID: 24450635

Recent advances in the structural molecular biology of Ets transcription factors: interactions, interfaces and inhibition.

Cooper CD, Newman JA, Gileadi O

Biochem. Soc. Trans.. 42(1):130-8. doi: 10.1042/BST20130227

Publication date: February 1, 2014

PMID: 24450640

Structures of soluble guanylate cyclase: implications for regulatory mechanisms and drug development.

Gileadi O

Biochem. Soc. Trans.. 42(1):108-13. doi: 10.1042/BST20130228

Publication date: February 1, 2014

PMID: 24450636

Structural characterization of a new N-substituted pantothenamide bound to pantothenate kinases from Klebsiella pneumonia and Staphylococcus aureus.

Hughes SJ, Antoshchenko T, Kim KP, Smil D, Park HW

Proteins. doi: 10.1002/prot.24524

Publication date: January 28, 2014

PMID: 24470271

The structure-activity relationships of L3MBTL3 inhibitors: flexibility of the dimer interface.

Camerino MA, Zhong N, Dong A, Dickson BM, James LI, Baughman BM, Norris JL, Kireev DB, Janzen WP, Arrowsmith CH, Frye SV

Medchemcomm. 4(11):1501-1507. doi: 10.1039/C3MD00197K

Publication date: January 28, 2014

PMID: 24466405

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