Publications | Structural Genomics Consortium

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

The Structural Basis of PI3K Cancer Mutations: From Mechanism to Therapy.

Liu S, Knapp S, Ahmed AA

Cancer Res.. doi: 10.1158/0008-5472.CAN-13-2319

Publication date: January 23, 2014

PMID: 24459181

A Chemical Tool for In Vitro and In Vivo Precipitation of Lysine Methyltransferase G9a.

Konze KD, Pattenden SG, Liu F, Barsyte-Lovejoy D, Li F, Simon JM, Davis IJ, Vedadi M, Jin J

ChemMedChem. doi: 10.1002/cmdc.201300450

Publication date: January 17, 2014

PMID: 24443078

Leri's pleonosteosis, a congenital rheumatic disease, results from microduplication at 8q22.1 encompassing GDF6 and SDC2 and provides insight into systemic sclerosis pathogenesis.

Banka S, Cain SA, Carim S, Daly SB, Urquhart JE, Erdem G, Harris J, Bottomley M, Donnai D, Kerr B, Kingston H, Superti-Furga A, Unger S, Ennis H, Worthington J, Herrick AL, Merry CL, Yue WW, Kielty CM, Newman WG

Ann. Rheum. Dis.. doi: 10.1136/annrheumdis-2013-204309

Publication date: January 17, 2014

PMID: 24442880

Structure of Cyclin G associated kinase (GAK) Trapped in different Conformations using Nanobodies.

Chaikuad A, Keates T, Vincke C, Kaufholz M, Zenn M, Zimmermann B, Gutiérrez C, Zhang RG, Hatzos-Skintges C, Joachimiak A, Muyldermans S, Herberg FW, Knapp S, Müller S

Biochem. J.. doi: 10.1042/BJ20131399

Publication date: January 17, 2014

PMID: 24438162

Identification of a Major Determinant for Serine-Threonine Kinase Phosphoacceptor Specificity.

Chen C, Ha BH, Thévenin AF, Lou HJ, Zhang R, Yip KY, Peterson JR, Gerstein M, Kim PM, Filippakopoulos P, Knapp S, Boggon TJ, Turk BE

Mol. Cell. doi: 10.1016/j.molcel.2013.11.013

Publication date: December 24, 2013

PMID: 24374310

Stimulation of Hepatic Apolipoprotein A-I Production by Novel Thieno-Triazolodiazepines: Roles of the Classical Benzodiazepine Receptor, PAF Receptor, and Bromodomain Binding.

Kempen HJ, Bellus D, Fedorov O, Nicklisch S, Filippakopoulos P, Picaud S, Knapp S

Lipid Insights. 6:47-54. doi: 10.4137/Lpi.s13258

Publication date: December 22, 2013

PMID: 25278768

Diverse Levels of Sequence Selectivity and Catalytic Efficiency of Protein-Tyrosine Phosphatases.

Selner NG, Luechapanichkul R, Chen X, Neel BG, Zhang ZY, Knapp S, Bell CE, Pei D

Biochemistry. doi: 10.1021/bi401223r

Publication date: December 20, 2013

PMID: 24359314

Structure of the Catalytic Domain of EZH2 Reveals Conformational Plasticity in Cofactor and Substrate Binding Sites and Explains Oncogenic Mutations.

Wu H, Zeng H, Dong A, Li F, He H, Senisterra G, Seitova A, Duan S, Brown PJ, Vedadi M, Arrowsmith CH, Schapira M

PLoS ONE. 8(12):e83737. doi: 10.1371/journal.pone.0083737

Publication date: December 19, 2013

PMID: 24367611

[1,2,4]Triazolo[4,3-a]phthalazines: inhibitors of diverse bromodomains.

Fedorov O, Lingard H, Wells C, Monteiro OP, Picaud S, Keates T, Yapp C, Philpott M, Martin SJ, Felletar I, Marsden B, Filippakopoulos P, Muller-Knapp S, Knapp S, Brennan PE

J. Med. Chem.. doi: 10.1021/jm401568s

Publication date: December 8, 2013

PMID: 24313754

ChromoHub V2: Cancer Genomics.

Shah MA, Denton EL, Liu L, Schapira M

Bioinformatics. doi: 10.1093/bioinformatics/btt710

Publication date: December 6, 2013

PMID: 24319001

Neculai D, Schwake M, Ravichandran M, Zunke F, Collins RF, Peters J, Neculai M, Plumb J, Loppnau P, Pizarro JC, Seitova A, Trimble WS, Saftig P, Grinstein S, Dhe-Paganon S.

Structure of LIMP-2 provides functional insights with implications for SR-BI and CD36.

Nature. 504(7478):172-176. doi: 10.1038/nature12684

Publication date: December 5, 2013

PMID: 24162852

Targeting low-druggability bromodomains: Fragment based screening and inhibitor design against the BAZ2B bromodomain.

Ferguson FM, Fedorov O, Chaikuad A, Philpott M, Muniz J, Felletar I, von Delft F, Heightman TD, Knapp S, Abell C, Ciulli A

J. Med. Chem.. doi: 10.1021/jm401582c

Publication date: December 4, 2013

PMID: 24304323

A versatile spectrophotometric protein tyrosine phosphatase assay based on 3-nitrophosphotyrosine containing substrates.

Ameijde JV, Overvoorde J, Knapp S, Hertog JD, Ruijtenbeek R, Liskamp RM

Anal. Biochem.. doi: 10.1016/j.ab.2013.11.023

Publication date: December 2, 2013

PMID: 24309020

Crystal structures of the human histone H4K20 methyltransferases SUV420H1 and SUV420H2.

Wu H, Siarheyeva A, Zeng H, Lam R, Dong A, Wu XH, Li Y, Schapira M, Vedadi M, Min J

FEBS Lett.. 587(23):3859-68. doi: 10.1016/j.febslet.2013.10.020

Publication date: November 29, 2013

PMID: 24396869

Mutant prolactin receptor and familial hyperprolactinemia.

Newey PJ, Gorvin CM, Cleland SJ, Willberg CB, Bridge M, Azharuddin M, Drummond RS, van der Merwe PA, Klenerman P, Bountra C, Thakker RV

N. Engl. J. Med.. 369(21):2012-20. doi: 10.1056/NEJMoa1307557

Publication date: November 21, 2013

PMID: 24195502

Stochastic detection of Pim protein kinases reveals electrostatically enhanced association of a peptide substrate.

Harrington L, Cheley S, Alexander LT, Knapp S, Bayley H

Proc. Natl. Acad. Sci. U.S.A.. 110(47):E4417-26. doi: 10.1073/pnas.1312739110

Publication date: November 19, 2013

PMID: 24194548

RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain.

Picaud S, Wells C, Felletar I, Brotherton D, Martin S, Savitsky P, Diez-Dacal B, Philpott M, Bountra C, Lingard H, Fedorov O, Müller S, Brennan PE, Knapp S, Filippakopoulos P

Proc. Natl. Acad. Sci. U.S.A.. doi: 10.1073/pnas.1310658110

Publication date: November 18, 2013

PMID: 24248379

Medium-throughput production of recombinant human proteins: ligation-independent cloning.

Strain-Damerell C, Mahajan P, Gileadi O, Burgess-Brown NA

Methods Mol. Biol.. 1091:55-72. doi: 10.1007/978-1-62703-691-7_4

Publication date: November 10, 2013

PMID: 24203324

Medium-Throughput Production of Recombinant Human Proteins: Protein Production in E. coli.

Burgess-Brown NA, Mahajan P, Strain-Damerell C, Gileadi O, Gräslund S

Methods Mol. Biol.. 1091:73-94. doi: 10.1007/978-1-62703-691-7_5

Publication date: November 10, 2013

PMID: 24203325

Medium-throughput production of recombinant human proteins: protein production in insect cells.

Mahajan P, Strain-Damerell C, Gileadi O, Burgess-Brown NA

Methods Mol. Biol.. 1091:95-121. doi: 10.1007/978-1-62703-691-7_6

Publication date: November 10, 2013

PMID: 24203326

Maintenance of muscle myosin levels in adult C. elegans requires both the double bromodomain protein BET-1 and sumoylation.

Fisher K, Gee F, Wang S, Xue F, Knapp S, Philpott M, Wells C, Rodriguez M, Snoek LB, Kammenga J, Poulin GB

Biol Open. doi: 10.1242/bio.20136007

Publication date: November 8, 2013

PMID: 24285704

Real-Time Monitoring of the Dephosphorylating Activity of Protein Tyrosine Phosphatases Using Microarrays with 3-Nitrophosphotyrosine Substrates.

van Ameijde J, Overvoorde J, Knapp S, den Hertog J, Ruijtenbeek R, Liskamp RMJ

Chempluschem. 78(11):1349-1357. doi: 10.1002/cplu.201300299

Publication date: November 1, 2013

PMID: 31986648

Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones.

Deng X, Elkins JM, Zhang J, Yang Q, Erazo T, Gomez N, Choi HG, Wang J, Dzamko N, Lee JD, Sim T, Kim N, Alessi DR, Lizcano JM, Knapp S, Gray NS

Eur J Med Chem. 70C:758-767. doi: 10.1016/j.ejmech.2013.10.052

Publication date: October 29, 2013

PMID: 24239623

Biochemical and Structural Studies of Conserved Maf Proteins Revealed Nucleotide Pyrophosphatases with a Preference for Modified Nucleotides.

Tchigvintsev A, Tchigvintsev D, Flick R, Popovic A, Dong A, Xu X, Brown G, Lu W, Wu H, Cui H, Dombrowski L, Joo JC, Beloglazova N, Min J, Savchenko A, Caudy AA, Rabinowitz JD, Murzin AG, Yakunin AF

Chem. Biol.. doi: 10.1016/j.chembiol.2013.09.011

Publication date: October 22, 2013

PMID: 24210219

Exploring the Trypanosoma brucei Hsp83 Potential as a Target for Structure Guided Drug Design.

Pizarro JC, Hills T, Senisterra G, Wernimont AK, Mackenzie C, Norcross NR, Ferguson MA, Wyatt PG, Gilbert IH, Hui R

PLoS Negl Trop Dis. 7(10):e2492. doi: 10.1371/journal.pntd.0002492

Publication date: October 17, 2013

PMID: 24147171

Small-Molecule Modulators for Epigenetics Targets.

Knapp S, Weinmann H

ChemMedChem. doi: 10.1002/cmdc.201300344

Publication date: October 14, 2013

PMID: 24127276

Identification of Novel Functionally Selective Kappa Opioid Receptor Scaffolds.

White KL, Scopton AP, Rives ML, Bikbulatov RV, Polepally PR, Brown PJ, Kenakin T, Javitch JA, Zjawiony JK, Roth BL

Mol. Pharmacol.. doi: 10.1124/mol.113.089649

Publication date: October 10, 2013

PMID: 24113749

Discovery of an in vivo Chemical Probe of the Lysine Methyltransferases G9a and GLP.

Liu F, Barsyte-Lovejoy D, Li F, Xiong Y, Korboukh VK, Huang X, Allali-Hassani A, Janzen WP, Roth BL, Frye SV, Arrowsmith CH, Brown PJ, Vedadi M, Jin J

J. Med. Chem.. doi: 10.1021/jm401480r

Publication date: October 8, 2013

PMID: 24102134

Structural insights into functional overlapping and differentiation among myosin V motors.

Nascimento AF, Trindade DM, Tonoli CC, de Giuseppe PO, Assis LH, Honorato RV, de Oliveira PS, Mahajan P, Burgess-Brown NA, von Delft F, Larson RE, Murakami MT

J. Biol. Chem.. doi: 10.1074/jbc.M113.507202

Publication date: October 4, 2013

PMID: 24097982

Discovery of Novel Small-Molecule Inhibitors of BRD4 Using Structure-Based Virtual Screening.

Vidler LR, Filippakopoulos P, Fedorov O, Picaud S, Martin S, Tomsett M, Woodward H, Brown N, Knapp S, Hoelder S

J. Med. Chem.. doi: 10.1021/jm4011302

Publication date: October 3, 2013

PMID: 24090311

Molecular Basis for the Regulation of the H3K4 Methyltransferase Activity of PRDM9.

Wu H, Mathioudakis N, Diagouraga B, Dong A, Dombrovski L, Baudat F, Cusack S, de Massy B, Kadlec J

Cell Rep. doi: 10.1016/j.celrep.2013.08.035

Publication date: October 2, 2013

PMID: 24095733

Defining efficient enzyme-cofactor pairs for bioorthogonal profiling of protein methylation.

Islam K, Chen Y, Wu H, Bothwell IR, Blum GJ, Zeng H, Dong A, Zheng W, Min J, Deng H, Luo M

Proc. Natl. Acad. Sci. U.S.A.. doi: 10.1073/pnas.1216365110

Publication date: September 30, 2013

PMID: 24082136

Structural basis for Cul3 protein assembly with the BTB-Kelch family of E3 ubiquitin ligases.

Canning P, Cooper CD, Krojer T, Murray JW, Pike AC, Chaikuad A, Keates T, Thangaratnarajah C, Hojzan V, Ayinampudi V, Marsden BD, Gileadi O, Knapp S, von Delft F, Bullock AN

J. Biol. Chem.. 288(39):28304.

Publication date: September 27, 2013

PMID: 24078033

Highly Functionalized Terpyridines as Competitive Inhibitors of AKAP-PKA Interactions.

Schäfer G, Milić J, Eldahshan A, Götz F, Zühlke K, Schillinger C, Kreuchwig A, Elkins JM, Abdul Azeez KR, Oder A, Moutty MC, Masada N, Beerbaum M, Schlegel B, Niquet S, Schmieder P, Krause G, von Kries JP, Cooper DM, Knapp S, Rademann J, Rosenthal W, Klussmann E

Angew. Chem. Int. Ed. Engl.. doi: 10.1002/anie.201304686

Publication date: September 23, 2013

PMID: 24115519