Publications | Structural Genomics Consortium

Classification of the short-chain dehydrogenase/reductase superfamily using hidden Markov models.

Kallberg Y, Oppermann U, Persson B

FEBS J.. 277(10):2375-86. doi: 10.1111/j.1742-4658.2010.07656.x

Publication date: April 29, 2010

PMID: 20423462

New potent dual inhibitors of CK2 and Pim kinases: discovery and structural insights.

López-Ramos M, Prudent R, Moucadel V, Sautel CF, Barette C, Lafanechère L, Mouawad L, Grierson D, Schmidt F, Florent JC, Filippakopoulos P, Bullock AN, Knapp S, Reiser JB, Cochet C

FASEB J.. 24(9):3171-85. doi: 10.1096/fj.09-143743

Publication date: April 16, 2010

PMID: 20400536

Finding Inspiration in the Protein Data Bank to Chemically Antagonize Readers of the Histone Code.

Campagna-Slater V, Schapira M

Mol Inform. 29(4):322-31. doi: 10.1002/minf.201000018

Publication date: April 12, 2010

PMID: 27463059

Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function.

Kwiatkowski N, Jelluma N, Filippakopoulos P, Soundararajan M, Manak MS, Kwon M, Choi HG, Sim T, Deveraux QL, Rottmann S, Pellman D, Shah JV, Kops GJ, Knapp S, Gray NS

Nat. Chem. Biol.. 6(5):359-68. doi: 10.1038/nchembio.345

Publication date: April 11, 2010

PMID: 20383151

Structural basis of human CYP51 inhibition by antifungal azoles.

Strushkevich N, Usanov SA, Park HW

J. Mol. Biol.. 397(4):1067-78. doi: 10.1016/j.jmb.2010.01.075

Publication date: April 9, 2010

PMID: 20149798

Structure and function of a G-actin sequestering protein with a vital role in malaria oocyst development inside the mosquito vector.

Hliscs M, Sattler JM, Tempel W, Artz JD, Dong A, Hui R, Matuschewski K, Schüler H

J. Biol. Chem.. 285(15):11572-83. doi: 10.1074/jbc.M109.054916

Publication date: April 9, 2010

PMID: 20083609

N-myristoyltransferase inhibitors as new leads to treat sleeping sickness.

Frearson JA, Brand S, McElroy SP, Cleghorn LA, Smid O, Stojanovski L, Price HP, Guther ML, Torrie LS, Robinson DA, Hallyburton I, Mpamhanga CP, Brannigan JA, Wilkinson AJ, Hodgkinson M, Hui R, Qiu W, Raimi OG, van Aalten DM, Brenk R, Gilbert IH, Read KD, Fairlamb AH, Ferguson MA, Smith DF, Wyatt PG

Nature. 464(7289):728-32. doi: 10.1038/nature08893

Publication date: April 1, 2010

PMID: 20360736

Tamoxifen enhances the Hsp90 molecular chaperone ATPase activity.

Zhao R, Leung E, Grüner S, Schapira M, Houry WA

PLoS ONE. 5(4):e9934. doi: 10.1371/journal.pone.0009934

Publication date: April 1, 2010

PMID: 20376192

Toward a unified nomenclature for mammalian ADP-ribosyltransferases.

Hottiger MO, Hassa PO, Lüscher B, Schüler H, Koch-Nolte F

Trends Biochem. Sci.. 35(4):208-19. doi: 10.1016/j.tibs.2009.12.003

Publication date: April 1, 2010

PMID: 20106667

Pharmacophore screening of the protein data bank for specific binding site chemistry.

Campagna-Slater V, Arrowsmith AG, Zhao Y, Schapira M

J Chem Inf Model. 50(3):358-67. doi: 10.1021/ci900427b

Publication date: March 22, 2010

PMID: 20112952

Probing the structural basis of RecQ helicase function.

Vindigni A, Marino F, Gileadi O

Biophys. Chem.. 149(3):67-77. doi: 10.1016/j.bpc.2010.03.012

Publication date: March 20, 2010

PMID: 20392558

The ubiquitin-activating enzyme E1 as a therapeutic target for the treatment of leukemia and multiple myeloma.

Xu GW, Ali M, Wood TE, Wong D, Maclean N, Wang X, Gronda M, Skrtic M, Li X, Hurren R, Mao X, Venkatesan M, Beheshti Zavareh R, Ketela T, Reed JC, Rose D, Moffat J, Batey RA, Dhe-Paganon S, Schimmer AD

Blood. 115(11):2251-9. doi: 10.1182/blood-2009-07-231191

Publication date: March 18, 2010

PMID: 20075161

PARP-3 is a mono-ADP-ribosylase that activates PARP-1 in the absence of DNA.

Loseva O, Jemth AS, Bryant HE, Schüler H, Lehtiö L, Karlberg T, Helleday T

J. Biol. Chem.. 285(11):8054-60. doi: 10.1074/jbc.M109.077834

Publication date: March 12, 2010

PMID: 20064938

Open-access public-private partnerships to enable drug discovery--new approaches.

Müller S, Weigelt J

IDrugs. 13(3):175-80.

Publication date: March 2, 2010

PMID: 20191434

Selective inhibitors of the JMJD2 histone demethylases: combined nondenaturing mass spectrometric screening and crystallographic approaches.

Rose NR, Woon EC, Kingham GL, King ON, Mecinović J, Clifton IJ, Ng SS, Talib-Hardy J, Oppermann U, McDonough MA, Schofield CJ

J. Med. Chem.. 53(4):1810-8. doi: 10.1021/jm901680b

Publication date: February 25, 2010

PMID: 20088513

Crystal structure of the PHF8 Jumonji domain, an Nepsilon-methyl lysine demethylase.

Yue WW, Hozjan V, Ge W, Loenarz C, Cooper CD, Schofield CJ, Kavanagh KL, Oppermann U, McDonough MA

FEBS Lett.. 584(4):825-30. doi: 10.1016/j.febslet.2009.12.055

Publication date: February 19, 2010

PMID: 20067792

Generating a panel of highly specific antibodies to 20 human SH2 domains by phage display.

Pershad K, Pavlovic JD, Gräslund S, Nilsson P, Colwill K, Karatt-Vellatt A, Schofield DJ, Dyson MR, Pawson T, Kay BK, McCafferty J

Protein Eng. Des. Sel.. 23(4):279-88. doi: 10.1093/protein/gzq003

Publication date: February 17, 2010

PMID: 20164216

Crystal structure of the catalytic domain of human PARP2 in complex with PARP inhibitor ABT-888.

Karlberg T, Hammarström M, Schütz P, Svensson L, Schüler H

Biochemistry. 49(6):1056-8. doi: 10.1021/bi902079y

Publication date: February 16, 2010

PMID: 20092359

The (un)targeted cancer kinome.

Fedorov O, Müller S, Knapp S

Nat. Chem. Biol.. 6(3):166-169. doi: 10.1038/nchembio.297

Publication date: February 16, 2010

PMID: 20154661

Assessing the stability of membrane proteins to detect ligand binding using differential static light scattering.

Senisterra GA, Ghanei H, Khutoreskaya G, Dobrovetsky E, Edwards AM, Privé GG, Vedadi M

J Biomol Screen. 15(3):314-20. doi: 10.1177/1087057109357117

Publication date: February 11, 2010

PMID: 20150591

Evaluation of substituted N,N'-diarylsulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase.

Boxer MB, Jiang JK, Vander Heiden MG, Shen M, Skoumbourdis AP, Southall N, Veith H, Leister W, Austin CP, Park HW, Inglese J, Cantley LC, Auld DS, Thomas CJ

J. Med. Chem.. 53(3):1048-55. doi: 10.1021/jm901577g

Publication date: February 11, 2010

PMID: 20017496

PIM serine/threonine kinases in the pathogenesis and therapy of hematologic malignancies and solid cancers.

Brault L, Gasser C, Bracher F, Huber K, Knapp S, Schwaller J

Haematologica. 95(6):1004-15. doi: 10.3324/haematol.2009.017079

Publication date: February 9, 2010

PMID: 20145274

A conserved mechanism of autoinhibition for the AMPK kinase domain: ATP-binding site and catalytic loop refolding as a means of regulation.

Littler DR, Walker JR, Davis T, Wybenga-Groot LE, Finerty PJ, Newman E, Mackenzie F, Dhe-Paganon S

Acta Crystallogr. Sect. F Struct. Biol. Cryst. Commun.. 66(Pt 2):143-51. doi: 10.1107/S1744309109052543

Publication date: February 1, 2010

PMID: 20124709

A miniaturized screen for inhibitors of Jumonji histone demethylases.

Sakurai M, Rose NR, Schultz L, Quinn AM, Jadhav A, Ng SS, Oppermann U, Schofield CJ, Simeonov A

Mol Biosyst. 6(2):357-64. doi: 10.1039/b912993f

Publication date: January 21, 2010

PMID: 20094655

A non-enzymatic function of 17beta-hydroxysteroid dehydrogenase type 10 is required for mitochondrial integrity and cell survival.

Rauschenberger K, Schöler K, Sass JO, Sauer S, Djuric Z, Rumig C, Wolf NI, Okun JG, Kölker S, Schwarz H, Fischer C, Grziwa B, Runz H, Nümann A, Shafqat N, Kavanagh KL, Hämmerling G, Wanders RJ, Shield JP, Wendel U, Stern D, Nawroth P, Hoffmann GF, Bartram CR, Arnold B, Bierhaus A, Oppermann U, Steinbeisser H, Zschocke J

EMBO Mol Med. 2(2):51-62. doi: 10.1002/emmm.200900055

Publication date: January 16, 2010

PMID: 20077426

UHRF1 Links the Histone code and DNA Methylation to ensure Faithful Epigenetic Memory Inheritance.

Bronner C, Fuhrmann G, Chédin FL, Macaluso M, Dhe-Paganon S

Genet Epigenet. 2009(2):29-36.

Publication date: January 14, 2010

PMID: 21643543

Crystal structures of the ATPase domains of four human Hsp70 isoforms: HSPA1L/Hsp70-hom, HSPA2/Hsp70-2, HSPA6/Hsp70B', and HSPA5/BiP/GRP78.

Wisniewska M, Karlberg T, Lehtiö L, Johansson I, Kotenyova T, Moche M, Schüler H

PLoS ONE. 5(1):e8625. doi: 10.1371/journal.pone.0008625

Publication date: January 11, 2010

PMID: 20072699

Structural biology of human H3K9 methyltransferases.

Wu H, Min J, Lunin VV, Antoshenko T, Dombrovski L, Zeng H, Allali-Hassani A, Campagna-Slater V, Vedadi M, Arrowsmith CH, Plotnikov AN, Schapira M

PLoS ONE. 5(1):e8570. doi: 10.1371/journal.pone.0008570

Publication date: January 11, 2010

PMID: 20084102

Structure and function of the PLAA/Ufd3-p97/Cdc48 complex.

Qiu L, Pashkova N, Walker JR, Winistorfer S, Allali-Hassani A, Akutsu M, Piper R, Dhe-Paganon S

J. Biol. Chem.. 285(1):365-72. doi: 10.1074/jbc.M109.044685

Publication date: January 1, 2010

PMID: 19887378

Discovery of a 2,4-diamino-7-aminoalkoxyquinazoline as a potent and selective inhibitor of histone lysine methyltransferase G9a.

Liu F, Chen X, Allali-Hassani A, Quinn AM, Wasney GA, Dong A, Barsyte D, Kozieradzki I, Senisterra G, Chau I, Siarheyeva A, Kireev DB, Jadhav A, Herold JM, Frye SV, Arrowsmith CH, Brown PJ, Simeonov A, Vedadi M, Jin J

J. Med. Chem.. 52(24):7950-3. doi: 10.1021/jm901543m

Publication date: December 24, 2009

PMID: 19891491

Structure and function of the intracellular region of the plexin-b1 transmembrane receptor.

Tong Y, Hota PK, Penachioni JY, Hamaneh MB, Kim S, Alviani RS, Shen L, He H, Tempel W, Tamagnone L, Park HW, Buck M

J. Biol. Chem.. 284(51):35962-72. doi: 10.1074/jbc.M109.056275

Publication date: December 18, 2009

PMID: 19843518

Screening for inhibitors of low-affinity epigenetic peptide-protein interactions: an AlphaScreen-based assay for antagonists of methyl-lysine binding proteins.

Wigle TJ, Herold JM, Senisterra GA, Vedadi M, Kireev DB, Arrowsmith CH, Frye SV, Janzen WP

J Biomol Screen. 15(1):62-71. doi: 10.1177/1087057109352902

Publication date: December 11, 2009

PMID: 20008125

Mouse Piwi interactome identifies binding mechanism of Tdrkh Tudor domain to arginine methylated Miwi.

Chen C, Jin J, James DA, Adams-Cioaba MA, Park JG, Guo Y, Tenaglia E, Xu C, Gish G, Min J, Pawson T

Proc. Natl. Acad. Sci. U.S.A.. 106(48):20336-41. doi: 10.1073/pnas.0911640106

Publication date: December 1, 2009

PMID: 19918066

Structure and functional characterization of the atypical human kinase haspin.

Eswaran J, Patnaik D, Filippakopoulos P, Wang F, Stein RL, Murray JW, Higgins JM, Knapp S

Proc. Natl. Acad. Sci. U.S.A.. 106(48):20198-203. doi: 10.1073/pnas.0901989106

Publication date: December 1, 2009

PMID: 19918057

Vital role for the Plasmodium actin capping protein (CP) beta-subunit in motility of malaria sporozoites.

Ganter M, Schüler H, Matuschewski K

Mol. Microbiol.. 74(6):1356-67. doi: 10.1111/j.1365-2958.2009.06828.x

Publication date: December 1, 2009

PMID: 19682250

SH2 domains: modulators of nonreceptor tyrosine kinase activity.

Filippakopoulos P, Müller S, Knapp S

Curr. Opin. Struct. Biol.. 19(6):643-9. doi: 10.1016/j.sbi.2009.10.001

Publication date: November 18, 2009

PMID: 19926274

A survey of proteins encoded by non-synonymous single nucleotide polymorphisms reveals a significant fraction with altered stability and activity.

Allali-Hassani A, Wasney GA, Chau I, Hong BS, Senisterra G, Loppnau P, Shi Z, Moult J, Edwards AM, Arrowsmith CH, Park HW, Schapira M, Vedadi M

Biochem. J.. 424(1):15-26. doi: 10.1042/BJ20090723

Publication date: November 15, 2009

PMID: 19702579

Ring1B contains a ubiquitin-like docking module for interaction with Cbx proteins.

Bezsonova I, Walker JR, Bacik JP, Duan S, Dhe-Paganon S, Arrowsmith CH

Biochemistry. 48(44):10542-8. doi: 10.1021/bi901131u

Publication date: November 10, 2009

PMID: 19791798

A homogeneous method for investigation of methylation-dependent protein-protein interactions in epigenetics.

Quinn AM, Bedford MT, Espejo A, Spannhoff A, Austin CP, Oppermann U, Simeonov A

Nucleic Acids Res.. 38(2):e11. doi: 10.1093/nar/gkp899

Publication date: November 6, 2009

PMID: 19897549

Investigating the genetic association between ERAP1 and ankylosing spondylitis.

Harvey D, Pointon JJ, Evans DM, Karaderi T, Farrar C, Appleton LH, Sturrock RD, Stone MA, Oppermann U, Brown MA, Wordsworth BP

Hum. Mol. Genet.. 18(21):4204-12. doi: 10.1093/hmg/ddp371

Publication date: November 1, 2009

PMID: 19692350

Insights into protein kinase regulation and inhibition by large scale structural comparison.

Eswaran J, Knapp S

Biochim. Biophys. Acta. 1804(3):429-32. doi: 10.1016/j.bbapap.2009.10.013

Publication date: October 22, 2009

PMID: 19854302

Synthesis, kinase inhibitory potencies, and in vitro antiproliferative evaluation of new Pim kinase inhibitors.

Akué-Gédu R, Rossignol E, Azzaro S, Knapp S, Filippakopoulos P, Bullock AN, Bain J, Cohen P, Prudhomme M, Anizon F, Moreau P

J. Med. Chem.. 52(20):6369-81. doi: 10.1021/jm901018f

Publication date: October 22, 2009

PMID: 19788246