Publications

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2015

Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance.

Fedorov O, Castex J, Tallant C, Owen DR, Martin S, Aldeghi M, Monteiro O, Filippakopoulos P, Picaud S, Trzupek JD, Gerstenberger BS, Bountra C, Willmann D, Wells C, Philpott M, Rogers C, Biggin PC, Brennan PE, Bunnage ME, Schüle R, Günther T, Knapp S, Müller S

Sci Adv. 1(10):e1500723. doi: 10.1126/sciadv.1500723

Publication date: November 13, 2015

PMID: 26702435

Structural Chemistry of Human RNA Methyltransferases.

Schapira M

ACS Chem. Biol.. doi: 10.1021/acschembio.5b00781

Publication date: November 13, 2015

PMID: 26566070

Emerging Target Families: Intractable Targets.

Knapp S

Handb Exp Pharmacol. doi: 10.1007/164_2015_28

Publication date: November 10, 2015

PMID: 26552403

Generation of a selective small molecule inhibitor of the CBP/p300 bromodomain for leukemia therapy.

Picaud S, Fedorov O, Thanasopoulou A, Leonards K, Jones K, Meier J, Olzscha H, Monteiro O, Martin S, Philpott M, Tumber A, Filippakopoulos P, Yapp C, Wells C, Hing Che K, Bannister A, Robson S, Kumar U, Parr N, Lee K, Lugo D, Jeffrey P, Taylor S, Vecellio ML, Bountra C, Brennan P, O'Mahony A, Velichko S, Muller S, Hay D, Daniels DL, Urh M, La Thangue NB, Kouzarides T, Prinjha R, Schwaller J, Knapp S

Cancer Res.. doi: 10.1158/0008-5472.CAN-15-0236

Publication date: November 9, 2015

PMID: 26552700

Design of a fluorescent ligand targeting the S-adenosylmethionine binding site of the histone methyltransferase MLL1.

Luan Y, Blazer LL, Hu H, Hajian T, Zhang J, Wu H, Houliston S, Arrowsmith CH, Vedadi M, Zheng YG

Org. Biomol. Chem.. doi: 10.1039/c5ob01794g

Publication date: November 6, 2015

PMID: 26541578

Structural basis for substrate recognition by the human N-terminal methyltransferase 1.

Dong C, Mao Y, Tempel W, Qin S, Li L, Loppnau P, Huang R, Min J

Genes Dev.. doi: 10.1101/gad.270611.115

Publication date: November 5, 2015

PMID: 26543161

Structural basis for the regulatory role of the PPxY motifs in the thioredoxin-interacting protein TXNIP.

Liu Y, Lau J, Li W, Tempel W, Li L, Dong A, Narula A, Qin S, Min J

Biochem. J.. doi: 10.1042/BJ20150830

Publication date: November 2, 2015

PMID: 26527736

Inflammation activation and resolution in human tendon disease.

Dakin SG, Martinez FO, Yapp C, Wells G, Oppermann U, Dean BJ, Smith RD, Wheway K, Watkins B, Roche L, Carr AJ

Sci Transl Med. 7(311):311ra173. doi: 10.1126/scitranslmed.aac4269

Publication date: October 28, 2015

PMID: 26511510

Comprehensive characterization of the Published Kinase Inhibitor Set.

Elkins JM, Fedele V, Szklarz M, Abdul Azeez KR, Salah E, Mikolajczyk J, Romanov S, Sepetov N, Huang XP, Roth BL, Al Haj Zen A, Fourches D, Muratov E, Tropsha A, Morris J, Teicher BA, Kunkel M, Polley E, Lackey KE, Atkinson FL, Overington JP, Bamborough P, Müller S, Price DJ, Willson TM, Drewry DH, Knapp S, Zuercher WJ

Nat. Biotechnol.. doi: 10.1038/nbt.3374

Publication date: October 26, 2015

PMID: 26501955

New Insights into the RNA-Binding and E3 Ubiquitin Ligase Activities of Roquins.

Zhang Q, Fan L, Hou F, Dong A, Wang YX, Tong Y

Sci Rep. 5:15660. doi: 10.1038/srep15660

Publication date: October 23, 2015

PMID: 26489670

The ins and outs of selective kinase inhibitor development.

Müller S, Chaikuad A, Gray NS, Knapp S

Nat. Chem. Biol.. 11(11):818-21. doi: 10.1038/nchembio.1938

Publication date: October 20, 2015

PMID: 26485069

Structural basis of metallo-β-lactamase inhibition by captopril stereoisomers.

Brem J, van Berkel SS, Zollman D, Lee SY, Gileadi O, McHugh PJ, Walsh TR, McDonough MA, Schofield CJ

Antimicrob. Agents Chemother.. doi: 10.1128/AAC.01335-15

Publication date: October 19, 2015

PMID: 26482303

Structural insights into the MMACHC-MMADHC protein complex involved in vitamin B12 trafficking.

Froese DS, Kopec J, Fitzpatrick F, Schuller M, McCorvie TJ, Chalk R, Plessl T, Fettelschoss V, Fowler B, Baumgartner MR, Yue WW

J. Biol. Chem.. doi: 10.1074/jbc.M115.683268

Publication date: October 19, 2015

PMID: 26483544

STRUCTURAL BIOLOGY. Chromatin complex, crystal clear.

Schapira M

Science. 350(6258):278-9. doi: 10.1126/science.aad5203

Publication date: October 16, 2015

PMID: 26472895

WDR5 supports an N-Myc transcriptional complex that drives a pro-tumorigenic gene expression signature in neuroblastoma.

Sun Y, Bell JL, Carter DR, Gherardi S, Poulos RC, Milazzo G, Wong JW, Al-Awar R, Tee AE, Liu PY, Liu B, Atmadibrata B, Wong M, Trahair T, Zhao Q, Shohet JM, Haupt Y, Schulte JH, Brown PJ, Arrowsmith CH, Vedadi M, MacKenzie KL, Huttelmaier S, Perini G, Marshall GM, Braithwaite A, Liu T

Cancer Res.. doi: 10.1158/0008-5472.CAN-15-0423

Publication date: October 15, 2015

PMID: 26471359

Targeting RIPK1,2,3 to combat inflammation.

Bullock AN, Degterev A

Oncotarget. doi: 10.18632/oncotarget.6106

Publication date: October 13, 2015

PMID: 26472031

Atad2 is a generalist facilitator of chromatin dynamics in embryonic stem cells.

Morozumi Y, Boussouar F, Tan M, Chaikuad A, Jamshidikia M, Colak G, He H, Nie L, Petosa C, de Dieuleveult M, Curtet S, Vitte AL, Rabatel C, Debernardi A, Cosset FL, Verhoeyen E, Emadali A, Schweifer N, Gianni D, Gut M, Guardiola P, Rousseaux S, Gérard M, Knapp S, Zhao Y, Khochbin S

J Mol Cell Biol. doi: 10.1093/jmcb/mjv060

Publication date: October 12, 2015

PMID: 26459632

Streamlining the Pipeline for Generation of Recombinant Affinity Reagents by Integrating the Affinity Maturation Step.

Huang R, Gorman KT, Vinci CR, Dobrovetsky E, Gräslund S, Kay BK

Int J Mol Sci. 16(10):23587-603. doi: 10.3390/ijms161023587

Publication date: October 6, 2015

PMID: 26437402

Optimizing Production of Antigens and Fabs in the Context of Generating Recombinant Antibodies to Human Proteins.

Zhong N, Loppnau P, Seitova A, Ravichandran M, Fenner M, Jain H, Bhattacharya A, Hutchinson A, Paduch M, Lu V, Olszewski M, Kossiakoff AA, Dowdell E, Koide A, Koide S, Huang H, Nadeem V, Sidhu SS, Greenblatt JF, Marcon E, Arrowsmith CH, Edwards AM, Gräslund S

PLoS ONE. 10(10):e0139695. doi: 10.1371/journal.pone.0139695

Publication date: October 5, 2015

PMID: 26437229

Towards an understanding of the role of DNA methylation in rheumatoid arthritis: therapeutic and diagnostic implications.

Cribbs A, Feldmann M, Oppermann U

Ther Adv Musculoskelet Dis. 7(5):206-19. doi: 10.1177/1759720X15598307

Publication date: October 2, 2015

PMID: 26425149

Structures and functions of mitochondrial ABC transporters.

Schaedler TA, Faust B, Shintre CA, Carpenter EP, Srinivasan V, van Veen HW, Balk J

Biochem. Soc. Trans.. 43(5):943-51. doi: 10.1042/BST20150118

Publication date: October 1, 2015

PMID: 26517908

Open access chemical probes for epigenetic targets.

Brown PJ, Müller S

Future Med Chem. doi: 10.4155/fmc.15.127

Publication date: September 23, 2015

PMID: 26397018

Crystal structure of human nuclear pore complex component NUP43.

Xu C, Li Z, He H, Wernimont A, Li Y, Loppnau P, Min J

FEBS Lett.. doi: 10.1016/j.febslet.2015.09.008

Publication date: September 19, 2015

PMID: 26391640

Gain-of-function p53 mutants co-opt chromatin pathways to drive cancer growth.

Zhu J, Sammons MA, Donahue G, Dou Z, Vedadi M, Getlik M, Barsyte-Lovejoy D, Al-awar R, Katona BW, Shilatifard A, Huang J, Hua X, Arrowsmith CH, Berger SL

Nature. 525(7568):206-11. doi: 10.1038/nature15251

Publication date: September 10, 2015

PMID: 26331536

Overcoming ABCG2-mediated drug resistance with imidazo-[1,2-b]-pyridazine-based Pim1 kinase inhibitors.

Darby RA, Unsworth A, Knapp S, Kerr ID, Callaghan R

Cancer Chemother. Pharmacol.. 76(4):853-64. doi: 10.1007/s00280-015-2858-9

Publication date: September 9, 2015

PMID: 26351135

Mutations in Known Monogenic High Bone Mass Loci Only Explain a Small Proportion of High Bone Mass cases.

Gregson CL, Wheeler L, Hardcastle SA, Appleton LH, Addison KA, Brugmans M, Clark GR, Ward K, Paggiosi M, Stone M, Thomas J, Agarwal R, Poole K, McCloskey E, Fraser WD, Williams E, Bullock AN, Smith GD, Brown MA, Tobias JH, Duncan EL

J. Bone Miner. Res.. doi: 10.1002/jbmr.2706

Publication date: September 8, 2015

PMID: 26348019

Proteomic and biochemical studies of lysine malonylation suggests its malonic aciduria-associated regulatory role in mitochondrial function and fatty acid oxidation.

Colak G, Pougovkina O, Dai L, Tan M, Te Brinke H, Huang H, Cheng Z, Park J, Wan X, Liu X, Yue WW, Wanders RJ, Locasale JW, Lombard DB, de Boer VC, Zhao Y

Mol. Cell Proteomics. doi: 10.1074/mcp.M115.048850

Publication date: August 28, 2015

PMID: 26320211

Structural basis for the discriminative recognition of N6-methyladenosine RNA by the human YT521-B homology domain family of proteins.

Xu C, Liu K, Ahmed H, Loppnau P, Schapira M, Min J

J. Biol. Chem.. doi: 10.1074/jbc.M115.680389

Publication date: August 28, 2015

PMID: 26318451

The inhibition of human farnesyl pyrophosphate synthase by nitrogen-containing bisphosphonates. Elucidating the role of active site threonine 201 and tyrosine 204 residues using enzyme mutants.

Tsoumpra MK, Muniz JR, Barnett BL, Kwaasi AA, Pilka ES, Kavanagh KL, Evdokimov A, Walter RL, Von Delft F, Ebetino FH, Oppermann U, Russell RG, Dunford JE

Bone. doi: 10.1016/j.bone.2015.08.020

Publication date: August 28, 2015

PMID: 26318908

Inflammatory Signaling by NOD-RIPK2 Is Inhibited by Clinically Relevant Type II Kinase Inhibitors.

Canning P, Ruan Q, Schwerd T, Hrdinka M, Maki JL, Saleh D, Suebsuwong C, Ray S, Brennan PE, Cuny GD, Uhlig HH, Gyrd-Hansen M, Degterev A, Bullock AN

Chem. Biol.. doi: 10.1016/j.chembiol.2015.07.017

Publication date: August 26, 2015

PMID: 26320862

21(st) Century Cures Act: An Act of Cure or Diagnosis?

Brindley DA, Arshad Z, Luo D, Dopson S, Hollander G, Frost S, Bountra C, Smith JA

Rejuvenation Res. 18(4):295-8. doi: 10.1089/rej.2015.1757

Publication date: August 21, 2015

PMID: 26291241

Dual EZH2 and EHMT2 histone methyltransferase inhibition increases biological efficacy in breast cancer cells.

Curry E, Green I, Chapman-Rothe N, Shamsaei E, Kandil S, Cherblanc FL, Payne L, Bell E, Ganesh T, Srimongkolpithak N, Caron J, Li F, Uren AG, Snyder JP, Vedadi M, Fuchter MJ, Brown R

Clin Epigenetics. 7(1):84. doi: 10.1186/s13148-015-0118-9

Publication date: August 21, 2015

PMID: 26300989

Differential recognition preferences of the three Src homology 3 (SH3) domains from the adaptor CD2-associated protein (CD2AP), and direct association with Ras and Rab interactor 3 (RIN3).

Rouka E, Simister PC, Janning M, Kumbrink J, Konstantinou T, Muniz JR, Joshi D, O'Reilly N, Volkmer R, Ritter B, Knapp S, von Delft F, Kirsch KH, Feller SM

J. Biol. Chem.. doi: 10.1074/jbc.M115.637207

Publication date: August 20, 2015

PMID: 26296892

A High Through-put Platform for Recombinant Antibodies to Folded Proteins.

Hornsby M, Paduch M, Miersch S, Sääf A, Matsuguchi T, Lee B, Wypisniak K, Doak A, King D, Usatyuk S, Perry K, Lu V, Thomas W, Luke J, Goodman J, Hoey RJ, Lai D, Griffin C, Li Z, Vizeacoumar FJ, Dong D, Campbell E, Anderson S, Zhong N, Gräslund S, Koide S, Moffat J, Sidhu S, Kossiakoff A, Wells J

Mol. Cell Proteomics. doi: 10.1074/mcp.O115.052209

Publication date: August 19, 2015

PMID: 26290498

CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses.

Hammitzsch A, Tallant C, Fedorov O, O'Mahony A, Brennan PE, Hay DA, Martinez FO, Al-Mossawi MH, de Wit J, Vecellio M, Wells C, Wordsworth P, Müller S, Knapp S, Bowness P

Proc. Natl. Acad. Sci. U.S.A.. doi: 10.1073/pnas.1501956112

Publication date: August 10, 2015

PMID: 26261308

Defined PEG smears as an alternative approach to enhance the search for crystallization conditions and crystal-quality improvement in reduced screens.

Chaikuad A, Knapp S, von Delft F

Acta Crystallogr. D Biol. Crystallogr.. 71(Pt 8):1627-39. doi: 10.1107/S1399004715007968

Publication date: August 1, 2015

PMID: 26249344

Structure of the human MLH1 N-terminus: implications for predisposition to Lynch syndrome.

Wu H, Zeng H, Lam R, Tempel W, Kerr ID, Min J

Acta Crystallogr F Struct Biol Commun. 71(Pt 8):981-5. doi: 10.1107/S2053230X15010183

Publication date: August 1, 2015

PMID: 26249686

A Call for Systematic Research on Solute Carriers.

César-Razquin A, Snijder B, Frappier-Brinton T, Isserlin R, Gyimesi G, Bai X, Reithmeier RA, Hepworth D, Hediger MA, Edwards AM, Superti-Furga G

Cell. 162(3):478-87. doi: 10.1016/j.cell.2015.07.022

Publication date: July 30, 2015

PMID: 26232220

BET inhibition upregulates SIRT1 and alleviates inflammatory responses.

Suuronen T, Pesonen M, Filippakopoulos P, Salminen A, Jarho EM, Lahtela-Kakkonen M, Kokkola T

Chembiochem. doi: 10.1002/cbic.201500272

Publication date: July 25, 2015

PMID: 26212199

Crystal structure of Porphyromonas gingivalis peptidylarginine deiminase: implications for autoimmunity in rheumatoid arthritis.

Montgomery AB, Kopec J, Shrestha L, Thezenas ML, Burgess-Brown NA, Fischer R, Yue WW, Venables PJ

Ann. Rheum. Dis.. doi: 10.1136/annrheumdis-2015-207656

Publication date: July 24, 2015

PMID: 26209657

Discovery of NCT-501, a Potent and Selective Theophylline-Based Inhibitor of Aldehyde Dehydrogenase 1A1 (ALDH1A1).

Yang SM, Yasgar A, Miller B, Lal-Nag M, Brimacombe K, Hu X, Sun H, Wang A, Xu X, Nguyen K, Oppermann U, Ferrer M, Vasiliou V, Simeonov A, Jadhav A, Maloney DJ

J. Med. Chem.. doi: 10.1021/acs.jmedchem.5b00577

Publication date: July 24, 2015

PMID: 26207746

A core of kinase-regulated interactomes defines the neoplastic MDSC lineage.

Gato-Cañas M, Martinez de Morentin X, Blanco-Luquin I, Fernandez-Irigoyen J, Zudaire I, Liechtenstein T, Arasanz H, Lozano T, Casares N, Chaikuad A, Knapp S, Guerrero-Setas D, Escors D, Kochan G, Santamaría E

Oncotarget.

Publication date: July 23, 2015

PMID: 26320174

Probing the epigenome.

Huston A, Arrowsmith CH, Knapp S, Schapira M

Nat. Chem. Biol.. 11(8):542-5. doi: 10.1038/nchembio.1871

Publication date: July 21, 2015

PMID: 26196765

Structural basis of glycogen branching enzyme deficiency and pharmacologic rescue by rational peptide design.

Froese DS, Michaeli A, McCorvie TJ, Krojer T, Sasi M, Melaev E, Goldblum A, Zatsepin M, Lossos A, Álvarez R, Escribá PV, Minaissan BA, von Delft F, Kakhlon O, Yue WW

Hum. Mol. Genet.. doi: 10.1093/hmg/ddv280

Publication date: July 21, 2015

PMID: 26199317

The promise and peril of chemical probes.

Arrowsmith CH, Audia JE, Austin C, Baell J, Bennett J, Blagg J, Bountra C, Brennan PE, Brown PJ, Bunnage ME, Buser-Doepner C, Campbell RM, Carter AJ, Cohen P, Copeland RA, Cravatt B, Dahlin JL, Dhanak D, Edwards AM, Frye SV, Gray N, Grimshaw CE, Hepworth D, Howe T, Huber KV, Jin J, Knapp S, Kotz JD, Kruger RG, Lowe D, Mader MM, Marsden B, Mueller-Fahrnow A, Müller S, O'Hagan RC, Overington JP, Owen DR, Rosenberg SH, Roth B, Ross R, Schapira M, Schreiber SL, Shoichet B, Sundström M, Superti-Furga G, Taunton J, Toledo-Sherman L, Walpole C, Walters MA, Willson TM, Workman P, Young RN, Zuercher WJ

Nat. Chem. Biol.. 11(8):536-41. doi: 10.1038/nchembio.1867

Publication date: July 21, 2015

PMID: 26196764

Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia.

Grebien F, Vedadi M, Getlik M, Giambruno R, Grover A, Avellino R, Skucha A, Vittori S, Kuznetsova E, Smil D, Barsyte-Lovejoy D, Li F, Poda G, Schapira M, Wu H, Dong A, Senisterra G, Stukalov A, Huber KV, Schönegger A, Marcellus R, Bilban M, Bock C, Brown PJ, Zuber J, Bennett KL, Al-Awar R, Delwel R, Nerlov C, Arrowsmith CH, Superti-Furga G

Nat. Chem. Biol.. doi: 10.1038/nchembio.1859

Publication date: July 13, 2015

PMID: 26167872

Type II inhibitors targeting CDK2.

Alexander LT, Moebitz H, Drueckes P, Savitsky P, Fedorov O, Elkins JM, Deane CM, Cowan-Jacob SW, Knapp S

ACS Chem. Biol.. doi: 10.1021/acschembio.5b00398

Publication date: July 9, 2015

PMID: 26158339

Designing selective inhibitors for calcium-dependent protein kinases in apicomplexans.

Hui R, El Bakkouri M, Sibley LD

Trends Pharmacol. Sci.. doi: 10.1016/j.tips.2015.04.011

Publication date: July 5, 2015

PMID: 26002073

Beating the odds: BETs in disease.

Wang CY, Filippakopoulos P

Trends Biochem. Sci.. doi: 10.1016/j.tibs.2015.06.002

Publication date: July 2, 2015

PMID: 26145250

Mutations in GMPPB cause congenital myasthenic syndrome and bridge myasthenic disorders with dystroglycanopathies.

Belaya K, Rodríguez Cruz PM, Liu WW, Maxwell S, McGowan S, Farrugia ME, Petty R, Walls TJ, Sedghi M, Basiri K, Yue WW, Sarkozy A, Bertoli M, Pitt M, Kennett R, Schaefer A, Bushby K, Parton M, Lochmüller H, Palace J, Muntoni F, Beeson D

Brain. doi: 10.1093/brain/awv185

Publication date: June 30, 2015

PMID: 26133662

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