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Results: 1 to 20 of 251

1.

(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells.

Barsyte-Lovejoy D, Li F, Oudhoff MJ, Tatlock JH, Dong A, Zeng H, Wu H, Freeman SA, Schapira M, Senisterra GA, Kuznetsova E, Marcellus R, Allali-Hassani A, Kennedy S, Lambert JP, Couzens AL, Aman A, Gingras AC, Al-Awar R, Fish PV, Gerstenberger BS, Roberts L, Benn CL, Grimley RL, Braam MJ, Rossi FM, Sudol M, Brown PJ, Bunnage ME, Owen DR, Zaph C, Vedadi M, Arrowsmith CH.

Proc Natl Acad Sci U S A. 2014 Sep 2;111(35):12853-8. doi: 10.1073/pnas.1407358111. Epub 2014 Aug 18.

PMID:
25136132
[PubMed - in process]
2.

Discovery of a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8.

Ma A, Yu W, Li F, Bleich RM, Herold JM, Butler KV, Norris JL, Korboukh V, Tripathy A, Janzen WP, Arrowsmith CH, Frye SV, Vedadi M, Brown PJ, Jin J.

J Med Chem. 2014 Aug 14;57(15):6822-33. doi: 10.1021/jm500871s. Epub 2014 Jul 25.

PMID:
25032507
[PubMed - in process]
3.

Structural and functional characterization of DUF1471 domains of Salmonella proteins SrfN, YdgH/SssB, and YahO.

Eletsky A, Michalska K, Houliston S, Zhang Q, Daily MD, Xu X, Cui H, Yee A, Lemak A, Wu B, Garcia M, Burnet MC, Meyer KM, Aryal UK, Sanchez O, Ansong C, Xiao R, Acton TB, Adkins JN, Montelione GT, Joachimiak A, Arrowsmith CH, Savchenko A, Szyperski T, Cort JR.

PLoS One. 2014 Jul 10;9(7):e101787. doi: 10.1371/journal.pone.0101787. eCollection 2014.

PMID:
25010333
[PubMed - in process]
Free PMC Article
4.

RPRD1A and RPRD1B are human RNA polymerase II C-terminal domain scaffolds for Ser5 dephosphorylation.

Ni Z, Xu C, Guo X, Hunter GO, Kuznetsova OV, Tempel W, Marcon E, Zhong G, Guo H, Kuo WH, Li J, Young P, Olsen JB, Wan C, Loppnau P, El Bakkouri M, Senisterra GA, He H, Huang H, Sidhu SS, Emili A, Murphy S, Mosley AL, Arrowsmith CH, Min J, Greenblatt JF.

Nat Struct Mol Biol. 2014 Aug;21(8):686-95. doi: 10.1038/nsmb.2853. Epub 2014 Jul 6.

PMID:
24997600
[PubMed - indexed for MEDLINE]
5.

Accessibility of different histone H3-binding domains of UHRF1 is allosterically regulated by phosphatidylinositol 5-phosphate.

Gelato KA, Tauber M, Ong MS, Winter S, Hiragami-Hamada K, Sindlinger J, Lemak A, Bultsma Y, Houliston S, Schwarzer D, Divecha N, Arrowsmith CH, Fischle W.

Mol Cell. 2014 Jun 19;54(6):905-19. doi: 10.1016/j.molcel.2014.04.004. Epub 2014 May 8.

PMID:
24813945
[PubMed - indexed for MEDLINE]
6.

Methyltransferase G9A regulates T cell differentiation during murine intestinal inflammation.

Antignano F, Burrows K, Hughes MR, Han JM, Kron KJ, Penrod NM, Oudhoff MJ, Wang SK, Min PH, Gold MJ, Chenery AL, Braam MJ, Fung TC, Rossi FM, McNagny KM, Arrowsmith CH, Lupien M, Levings MK, Zaph C.

J Clin Invest. 2014 May 1;124(5):1945-55. doi: 10.1172/JCI69592. Epub 2014 Mar 25.

PMID:
24667637
[PubMed - indexed for MEDLINE]
Free PMC Article
7.

Basic Tilted Helix Bundle - a new protein fold in human FKBP25/FKBP3 and HectD1.

Helander S, Montecchio M, Lemak A, Farès C, Almlöf J, Li Y, Yee A, Arrowsmith CH, Dhe-Paganon S, Sunnerhagen M.

Biochem Biophys Res Commun. 2014 Apr 25;447(1):26-31. doi: 10.1016/j.bbrc.2014.03.068. Epub 2014 Mar 22.

PMID:
24667607
[PubMed - indexed for MEDLINE]
8.

Trimethylation of histone H3 lysine 36 by human methyltransferase PRDM9 protein.

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. 2014 Apr 25;289(17):12177-88. doi: 10.1074/jbc.M113.523183. Epub 2014 Mar 14.

PMID:
24634223
[PubMed - indexed for MEDLINE]
Free PMC Article
9.

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. 2014 Mar 4;19(6):928-935. [Epub ahead of print]

PMID:
24595546
[PubMed - as supplied by publisher]
10.

Screening proteins for NMR suitability.

Yee AA, Semesi A, Garcia M, Arrowsmith CH.

Methods Mol Biol. 2014;1140:169-78. doi: 10.1007/978-1-4939-0354-2_13.

PMID:
24590717
[PubMed - indexed for MEDLINE]
11.

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. 2013 Nov;4(11):1501-1507.

PMID:
24466405
[PubMed]
12.

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. 2013 Dec 19;8(12):e83737. doi: 10.1371/journal.pone.0083737. eCollection 2013.

PMID:
24367611
[PubMed - indexed for MEDLINE]
Free PMC Article
13.

An unusual mode of galactose recognition by a family 32 carbohydrate-binding module.

Grondin JM, Chitayat S, Ficko-Blean E, Houliston S, Arrowsmith CH, Boraston AB, Smith SP.

J Mol Biol. 2014 Feb 20;426(4):869-80. doi: 10.1016/j.jmb.2013.11.029. Epub 2013 Dec 8.

PMID:
24326248
[PubMed - indexed for MEDLINE]
14.

Self-renewal as a therapeutic target in human colorectal cancer.

Kreso A, van Galen P, Pedley NM, Lima-Fernandes E, Frelin C, Davis T, Cao L, Baiazitov R, Du W, Sydorenko N, Moon YC, Gibson L, Wang Y, Leung C, Iscove NN, Arrowsmith CH, Szentgyorgyi E, Gallinger S, Dick JE, O'Brien CA.

Nat Med. 2014 Jan;20(1):29-36. doi: 10.1038/nm.3418. Epub 2013 Dec 1.

PMID:
24292392
[PubMed - indexed for MEDLINE]
15.

Solution NMR structure and histone binding of the PHD domain of human MLL5.

Lemak A, Yee A, Wu H, Yap D, Zeng H, Dombrovski L, Houliston S, Aparicio S, Arrowsmith CH.

PLoS One. 2013 Oct 9;8(10):e77020. doi: 10.1371/journal.pone.0077020. eCollection 2013.

PMID:
24130829
[PubMed - indexed for MEDLINE]
Free PMC Article
16.

Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP.

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

J Med Chem. 2013 Nov 14;56(21):8931-42. doi: 10.1021/jm401480r. Epub 2013 Oct 31.

PMID:
24102134
[PubMed - indexed for MEDLINE]
17.

Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3.

James LI, Korboukh VK, Krichevsky L, Baughman BM, Herold JM, Norris JL, Jin J, Kireev DB, Janzen WP, Arrowsmith CH, Frye SV.

J Med Chem. 2013 Sep 26;56(18):7358-71. doi: 10.1021/jm400919p. Epub 2013 Sep 16.

PMID:
24040942
[PubMed - indexed for MEDLINE]
Free PMC Article
18.

The ZIP5 ectodomain co-localizes with PrP and may acquire a PrP-like fold that assembles into a dimer.

Pocanschi CL, Ehsani S, Mehrabian M, Wille H, Reginold W, Trimble WS, Wang H, Yee A, Arrowsmith CH, Bozóky Z, Kay LE, Forman-Kay JD, Rini JM, Schmitt-Ulms G.

PLoS One. 2013 Sep 6;8(9):e72446. doi: 10.1371/journal.pone.0072446. eCollection 2013.

PMID:
24039764
[PubMed - indexed for MEDLINE]
Free PMC Article
19.

The study of epigenetic mechanisms based on the analysis of histone modification patterns by flow cytometry.

Watson M, Chow S, Barsyte D, Arrowsmith C, Shankey TV, Minden M, Hedley D.

Cytometry A. 2014 Jan;85(1):78-87. doi: 10.1002/cyto.a.22344. Epub 2013 Aug 26.

PMID:
24038859
[PubMed - indexed for MEDLINE]
20.

Control of the hippo pathway by Set7-dependent methylation of Yap.

Oudhoff MJ, Freeman SA, Couzens AL, Antignano F, Kuznetsova E, Min PH, Northrop JP, Lehnertz B, Barsyte-Lovejoy D, Vedadi M, Arrowsmith CH, Nishina H, Gold MR, Rossi FM, Gingras AC, Zaph C.

Dev Cell. 2013 Jul 29;26(2):188-94. doi: 10.1016/j.devcel.2013.05.025. Epub 2013 Jul 11.

PMID:
23850191
[PubMed - indexed for MEDLINE]
Free Article

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