Publications | Structural Genomics Consortium

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