Publications | Structural Genomics Consortium

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

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