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Items: 1 to 50 of 136

1.

Selective, Small-Molecule Co-Factor Binding Site Inhibition of a Su(var)3-9, Enhancer of Zeste, Trithorax Domain Containing Lysine Methyltransferase.

Taylor AP, Swewczyk M, Kennedy S, Trush VV, Wu H, Zeng H, Dong A, Ferreira de Freitas R, Tatlock J, Kumpf RA, Wythes M, Casimiro-Garcia A, Denny RA, Parikh MD, Li F, Barsyte-Lovejoy D, Schapira M, Vedadi M, Brown PJ, Arrowsmith CH, Owen DR.

J Med Chem. 2019 Sep 12;62(17):7669-7683. doi: 10.1021/acs.jmedchem.9b00112. Epub 2019 Sep 3.

PMID:
31415173
2.

The MLL1 trimeric catalytic complex is a dynamic conformational ensemble stabilized by multiple weak interactions.

Kaustov L, Lemak A, Wu H, Faini M, Fan L, Fang X, Zeng H, Duan S, Allali-Hassani A, Li F, Wei Y, Vedadi M, Aebersold R, Wang Y, Houliston S, Arrowsmith CH.

Nucleic Acids Res. 2019 Aug 10. pii: gkz697. doi: 10.1093/nar/gkz697. [Epub ahead of print]

PMID:
31400120
3.

Identification and characterization of the first fragment hits for SETDB1 Tudor domain.

Mader P, Mendoza-Sanchez R, Iqbal A, Dong A, Dobrovetsky E, Corless VB, Liew SK, Houliston SR, De Freitas RF, Smil D, Sena CCD, Kennedy S, Diaz DB, Wu H, Dombrovski L, Allali-Hassani A, Min J, Schapira M, Vedadi M, Brown PJ, Santhakumar V, Yudin AK, Arrowsmith CH.

Bioorg Med Chem. 2019 Sep 1;27(17):3866-3878. doi: 10.1016/j.bmc.2019.07.020. Epub 2019 Jul 12.

PMID:
31327677
4.

Fragment-based discovery of a chemical probe for the PWWP1 domain of NSD3.

Böttcher J, Dilworth D, Reiser U, Neumüller RA, Schleicher M, Petronczki M, Zeeb M, Mischerikow N, Allali-Hassani A, Szewczyk MM, Li F, Kennedy S, Vedadi M, Barsyte-Lovejoy D, Brown PJ, Huber KVM, Rogers CM, Wells CI, Fedorov O, Rumpel K, Zoephel A, Mayer M, Wunberg T, Böse D, Zahn S, Arnhof H, Berger H, Reiser C, Hörmann A, Krammer T, Corcokovic M, Sharps B, Winkler S, Häring D, Cockcroft XL, Fuchs JE, Müllauer B, Weiss-Puxbaum A, Gerstberger T, Boehmelt G, Vakoc CR, Arrowsmith CH, Pearson M, McConnell DB.

Nat Chem Biol. 2019 Aug;15(8):822-829. doi: 10.1038/s41589-019-0310-x. Epub 2019 Jul 8.

PMID:
31285596
5.

Discovery of a Potent and Selective Fragment-like Inhibitor of Methyllysine Reader Protein Spindlin 1 (SPIN1).

Xiong Y, Greschik H, Johansson C, Seifert L, Bacher J, Park KS, Babault N, Martini M, Fagan V, Li F, Chau I, Christott T, Dilworth D, Barsyte-Lovejoy D, Vedadi M, Arrowsmith CH, Brennan P, Fedorov O, Jung M, Farnie G, Liu J, Oppermann U, Schüle R, Jin J.

J Med Chem. 2019 Jul 24. doi: 10.1021/acs.jmedchem.9b00522. [Epub ahead of print]

PMID:
31260300
6.

Discovery of selective activators of PRC2 mutant EED-I363M.

Suh JL, Barnash KD, Abramyan TM, Li F, The J, Engelberg IA, Vedadi M, Brown PJ, Kireev DB, Arrowsmith CH, James LI, Frye SV.

Sci Rep. 2019 Apr 25;9(1):6524. doi: 10.1038/s41598-019-43005-z.

7.

A chemical toolbox for the study of bromodomains and epigenetic signaling.

Wu Q, Heidenreich D, Zhou S, Ackloo S, Krämer A, Nakka K, Lima-Fernandes E, Deblois G, Duan S, Vellanki RN, Li F, Vedadi M, Dilworth J, Lupien M, Brennan PE, Arrowsmith CH, Müller S, Fedorov O, Filippakopoulos P, Knapp S.

Nat Commun. 2019 Apr 23;10(1):1915. doi: 10.1038/s41467-019-09672-2.

8.

Crystal structure and activity-based labeling reveal the mechanisms for linkage-specific substrate recognition by deubiquitinase USP9X.

Paudel P, Zhang Q, Leung C, Greenberg HC, Guo Y, Chern YH, Dong A, Li Y, Vedadi M, Zhuang Z, Tong Y.

Proc Natl Acad Sci U S A. 2019 Apr 9;116(15):7288-7297. doi: 10.1073/pnas.1815027116. Epub 2019 Mar 26.

9.

Addendum: A cellular chemical probe targeting the chromodomains of Polycomb repressive complex 1.

Stuckey JI, Dickson BM, Cheng N, Liu Y, Norris JL, Cholensky SH, Tempel W, Qin S, Huber KG, Sagum C, Black K, Li F, Huang XP, Roth BL, Baughman BM, Senisterra G, Pattenden SG, Vedadi M, Brown PJ, TBedford M, Min J, Arrowsmith CH, James LI, Frye SV.

Nat Chem Biol. 2019 Aug;15(8):846. doi: 10.1038/s41589-019-0242-5. No abstract available.

PMID:
30842648
10.

A chemical biology toolbox to study protein methyltransferases and epigenetic signaling.

Scheer S, Ackloo S, Medina TS, Schapira M, Li F, Ward JA, Lewis AM, Northrop JP, Richardson PL, Kaniskan HÜ, Shen Y, Liu J, Smil D, McLeod D, Zepeda-Velazquez CA, Luo M, Jin J, Barsyte-Lovejoy D, Huber KVM, De Carvalho DD, Vedadi M, Zaph C, Brown PJ, Arrowsmith CH.

Nat Commun. 2019 Jan 3;10(1):19. doi: 10.1038/s41467-018-07905-4.

11.

LLY-283, a Potent and Selective Inhibitor of Arginine Methyltransferase 5, PRMT5, with Antitumor Activity.

Bonday ZQ, Cortez GS, Grogan MJ, Antonysamy S, Weichert K, Bocchinfuso WP, Li F, Kennedy S, Li B, Mader MM, Arrowsmith CH, Brown PJ, Eram MS, Szewczyk MM, Barsyte-Lovejoy D, Vedadi M, Guccione E, Campbell RM.

ACS Med Chem Lett. 2018 Apr 23;9(7):612-617. doi: 10.1021/acsmedchemlett.8b00014. eCollection 2018 Jul 12.

12.

Correction to Discovery of Bisubstrate Inhibitors of Nicotinamide N-Methyltransferase (NNMT).

Babault N, Allali-Hassani A, Li F, Fan J, Yue A, Ju K, Liu F, Vedadi M, Liu J, Jin J.

J Med Chem. 2018 Jul 12;61(13):5771-5772. doi: 10.1021/acs.jmedchem.8b00849. Epub 2018 Jun 27. No abstract available.

PMID:
29947518
13.

TP-064, a potent and selective small molecule inhibitor of PRMT4 for multiple myeloma.

Nakayama K, Szewczyk MM, Dela Sena C, Wu H, Dong A, Zeng H, Li F, de Freitas RF, Eram MS, Schapira M, Baba Y, Kunitomo M, Cary DR, Tawada M, Ohashi A, Imaeda Y, Saikatendu KS, Grimshaw CE, Vedadi M, Arrowsmith CH, Barsyte-Lovejoy D, Kiba A, Tomita D, Brown PJ.

Oncotarget. 2018 Apr 6;9(26):18480-18493. doi: 10.18632/oncotarget.24883. eCollection 2018 Apr 6.

14.

Discovery of Small-Molecule Antagonists of the H3K9me3 Binding to UHRF1 Tandem Tudor Domain.

Senisterra G, Zhu HY, Luo X, Zhang H, Xun G, Lu C, Xiao W, Hajian T, Loppnau P, Chau I, Li F, Allali-Hassani A, Atadja P, Oyang C, Li E, Brown PJ, Arrowsmith CH, Zhao K, Yu Z, Vedadi M.

SLAS Discov. 2018 Oct;23(9):930-940. doi: 10.1177/2472555218766278. Epub 2018 Mar 21.

PMID:
29562800
15.

Discovery of Bisubstrate Inhibitors of Nicotinamide N-Methyltransferase (NNMT).

Babault N, Allali-Hassani A, Li F, Fan J, Yue A, Ju K, Liu F, Vedadi M, Liu J, Jin J.

J Med Chem. 2018 Feb 22;61(4):1541-1551. doi: 10.1021/acs.jmedchem.7b01422. Epub 2018 Jan 31. Erratum in: J Med Chem. 2018 Jul 12;61(13):5771-5772.

16.

Histone lysine methyltransferase structure activity relationships that allow for segregation of G9a inhibition and anti-Plasmodium activity.

Sundriyal S, Chen PB, Lubin AS, Lueg GA, Li F, White AJP, Malmquist NA, Vedadi M, Scherf A, Fuchter MJ.

Medchemcomm. 2017 May 1;8(5):1069-1092. doi: 10.1039/c7md00052a. Epub 2017 Mar 15.

17.

Discovery of Potent and Selective Allosteric Inhibitors of Protein Arginine Methyltransferase 3 (PRMT3).

Kaniskan HÜ, Eram MS, Zhao K, Szewczyk MM, Yang X, Schmidt K, Luo X, Xiao S, Dai M, He F, Zang I, Lin Y, Li F, Dobrovetsky E, Smil D, Min SJ, Lin-Jones J, Schapira M, Atadja P, Li E, Barsyte-Lovejoy D, Arrowsmith CH, Brown PJ, Liu F, Yu Z, Vedadi M, Jin J.

J Med Chem. 2018 Feb 8;61(3):1204-1217. doi: 10.1021/acs.jmedchem.7b01674. Epub 2018 Jan 5.

18.

Discovery of a Highly Selective Cell-Active Inhibitor of the Histone Lysine Demethylases KDM2/7.

Gerken PA, Wolstenhulme JR, Tumber A, Hatch SB, Zhang Y, Müller S, Chandler SA, Mair B, Li F, Nijman SMB, Konietzny R, Szommer T, Yapp C, Fedorov O, Benesch JLP, Vedadi M, Kessler BM, Kawamura A, Brennan PE, Smith MD.

Angew Chem Int Ed Engl. 2017 Dec 4;56(49):15555-15559. doi: 10.1002/anie.201706788. Epub 2017 Nov 7.

19.

Erratum: The EED protein-protein interaction inhibitor A-395 inactivates the PRC2 complex.

He Y, Selvaraju S, Curtin ML, Jakob CG, Zhu H, Comess KM, Shaw B, The J, Lima-Fernandes E, Szewczyk MM, Cheng D, Klinge KL, Li HQ, Pliushchev M, Algire MA, Maag D, Guo J, Dietrich J, Panchal SC, Petros AM, Sweis RF, Torrent M, Bigelow LJ, Senisterra G, Li F, Kennedy S, Wu Q, Osterling DJ, Lindley DJ, Gao W, Galasinski S, Barsyte-Lovejoy D, Vedadi M, Buchanan FG, Arrowsmith CH, Chiang GG, Sun C, Pappano WN.

Nat Chem Biol. 2017 Jul 18;13(8):922. doi: 10.1038/nchembio0817-922b. No abstract available.

PMID:
28853738
20.

Structure-activity relationship studies of G9a-like protein (GLP) inhibitors.

Xiong Y, Li F, Babault N, Wu H, Dong A, Zeng H, Chen X, Arrowsmith CH, Brown PJ, Liu J, Vedadi M, Jin J.

Bioorg Med Chem. 2017 Aug 15;25(16):4414-4423. doi: 10.1016/j.bmc.2017.06.021. Epub 2017 Jun 19.

21.

Molecular basis for the methylation specificity of ATXR5 for histone H3.

Bergamin E, Sarvan S, Malette J, Eram MS, Yeung S, Mongeon V, Joshi M, Brunzelle JS, Michaels SD, Blais A, Vedadi M, Couture JF.

Nucleic Acids Res. 2017 Jun 20;45(11):6375-6387. doi: 10.1093/nar/gkx224.

22.

Discovery of Peptidomimetic Ligands of EED as Allosteric Inhibitors of PRC2.

Barnash KD, The J, Norris-Drouin JL, Cholensky SH, Worley BM, Li F, Stuckey JI, Brown PJ, Vedadi M, Arrowsmith CH, Frye SV, James LI.

ACS Comb Sci. 2017 Mar 13;19(3):161-172. doi: 10.1021/acscombsci.6b00174. Epub 2017 Feb 22.

23.

Targeting human SET1/MLL family of proteins.

Vedadi M, Blazer L, Eram MS, Barsyte-Lovejoy D, Arrowsmith CH, Hajian T.

Protein Sci. 2017 Apr;26(4):662-676. doi: 10.1002/pro.3129. Epub 2017 Mar 6. Review.

24.

The EED protein-protein interaction inhibitor A-395 inactivates the PRC2 complex.

He Y, Selvaraju S, Curtin ML, Jakob CG, Zhu H, Comess KM, Shaw B, The J, Lima-Fernandes E, Szewczyk MM, Cheng D, Klinge KL, Li HQ, Pliushchev M, Algire MA, Maag D, Guo J, Dietrich J, Panchal SC, Petros AM, Sweis RF, Torrent M, Bigelow LJ, Senisterra G, Li F, Kennedy S, Wu Q, Osterling DJ, Lindley DJ, Gao W, Galasinski S, Barsyte-Lovejoy D, Vedadi M, Buchanan FG, Arrowsmith CH, Chiang GG, Sun C, Pappano WN.

Nat Chem Biol. 2017 Apr;13(4):389-395. doi: 10.1038/nchembio.2306. Epub 2017 Jan 30. Erratum in: Nat Chem Biol. 2017 Jul 18;13(8):922.

PMID:
28135237
25.

Discovery of Potent and Selective Inhibitors for G9a-Like Protein (GLP) Lysine Methyltransferase.

Xiong Y, Li F, Babault N, Dong A, Zeng H, Wu H, Chen X, Arrowsmith CH, Brown PJ, Liu J, Vedadi M, Jin J.

J Med Chem. 2017 Mar 9;60(5):1876-1891. doi: 10.1021/acs.jmedchem.6b01645. Epub 2017 Feb 14.

26.

The SUV4-20 inhibitor A-196 verifies a role for epigenetics in genomic integrity.

Bromberg KD, Mitchell TR, Upadhyay AK, Jakob CG, Jhala MA, Comess KM, Lasko LM, Li C, Tuzon CT, Dai Y, Li F, Eram MS, Nuber A, Soni NB, Manaves V, Algire MA, Sweis RF, Torrent M, Schotta G, Sun C, Michaelides MR, Shoemaker AR, Arrowsmith CH, Brown PJ, Santhakumar V, Martin A, Rice JC, Chiang GG, Vedadi M, Barsyte-Lovejoy D, Pappano WN.

Nat Chem Biol. 2017 Mar;13(3):317-324. doi: 10.1038/nchembio.2282. Epub 2017 Jan 23.

PMID:
28114273
27.

Design and synthesis of selective, small molecule inhibitors of coactivator-associated arginine methyltransferase 1 (CARM1).

Kaniskan HÜ, Eram MS, Liu J, Smil D, Martini ML, Shen Y, Santhakumar V, Brown PJ, Arrowsmith C, Vedadi M, Jin J.

Medchemcomm. 2016 Sep 1;7(9):1793-1796. doi: 10.1039/C6MD00342G. Epub 2016 Jul 13.

28.

Turning a Substrate Peptide into a Potent Inhibitor for the Histone Methyltransferase SETD8.

Judge RA, Zhu H, Upadhyay AK, Bodelle PM, Hutchins CW, Torrent M, Marin VL, Yu W, Vedadi M, Li F, Brown PJ, Pappano WN, Sun C, Petros AM.

ACS Med Chem Lett. 2016 Oct 11;7(12):1102-1106. eCollection 2016 Dec 8.

29.

Structure-Based Design of a Covalent Inhibitor of the SET Domain-Containing Protein 8 (SETD8) Lysine Methyltransferase.

Butler KV, Ma A, Yu W, Li F, Tempel W, Babault N, Pittella-Silva F, Shao J, Wang J, Luo M, Vedadi M, Brown PJ, Arrowsmith CH, Jin J.

J Med Chem. 2016 Nov 10;59(21):9881-9889. Epub 2016 Nov 2.

30.

Discovery of Potent Pantothenamide Inhibitors of Staphylococcus aureus Pantothenate Kinase through a Minimal SAR Study: Inhibition Is Due to Trapping of the Product.

Hughes SJ, Barnard L, Mottaghi K, Tempel W, Antoshchenko T, Hong BS, Allali-Hassani A, Smil D, Vedadi M, Strauss E, Park HW.

ACS Infect Dis. 2016 Sep 9;2(9):627-641. Epub 2016 Aug 3.

PMID:
27759386
31.

Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6.

Shen Y, Szewczyk MM, Eram MS, Smil D, Kaniskan HÜ, de Freitas RF, Senisterra G, Li F, Schapira M, Brown PJ, Arrowsmith CH, Barsyte-Lovejoy D, Liu J, Vedadi M, Jin J.

J Med Chem. 2016 Oct 13;59(19):9124-9139. doi: 10.1021/acs.jmedchem.6b01033. Epub 2016 Sep 15.

32.

A Suite of Biochemical Assays for Screening RNA Methyltransferase BCDIN3D.

Blazer LL, Li F, Kennedy S, Zheng YG, Arrowsmith CH, Vedadi M.

SLAS Discov. 2017 Jan;22(1):32-39. doi: 10.1177/1087057116666276. Epub 2016 Sep 27.

PMID:
27581605
33.

Correction to Discovery of a Potent and Selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) Inhibitor by Virtual Screening.

Ferreira de Freitas R, Eram MS, Smil D, Szewczyk MM, Kennedy S, Brown PJ, Santhakumar V, Barsyte-Lovejoy D, Arrowsmith CH, Vedadi M, Schapira M.

J Med Chem. 2016 Aug 25;59(16):7698. doi: 10.1021/acs.jmedchem.6b01095. Epub 2016 Aug 3. No abstract available.

PMID:
27486787
34.

New small molecule inhibitors of histone methyl transferase DOT1L with a nitrile as a non-traditional replacement for heavy halogen atoms.

Spurr SS, Bayle ED, Yu W, Li F, Tempel W, Vedadi M, Schapira M, Fish PV.

Bioorg Med Chem Lett. 2016 Sep 15;26(18):4518-4522. doi: 10.1016/j.bmcl.2016.07.041. Epub 2016 Jul 21.

PMID:
27485386
35.

Structural basis of arginine asymmetrical dimethylation by PRMT6.

Wu H, Zheng W, Eram MS, Vhuiyan M, Dong A, Zeng H, He H, Brown P, Frankel A, Vedadi M, Luo M, Min J.

Biochem J. 2016 Oct 1;473(19):3049-63. doi: 10.1042/BCJ20160537. Epub 2016 Aug 1.

36.

Structure-Activity Relationship Studies for Enhancer of Zeste Homologue 2 (EZH2) and Enhancer of Zeste Homologue 1 (EZH1) Inhibitors.

Yang X, Li F, Konze KD, Meslamani J, Ma A, Brown PJ, Zhou MM, Arrowsmith CH, Kaniskan HÜ, Vedadi M, Jin J.

J Med Chem. 2016 Aug 25;59(16):7617-33. doi: 10.1021/acs.jmedchem.6b00855. Epub 2016 Aug 11.

37.

Discovery of a Potent and Selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) Inhibitor by Virtual Screening.

Ferreira de Freitas R, Eram MS, Smil D, Szewczyk MM, Kennedy S, Brown PJ, Santhakumar V, Barsyte-Lovejoy D, Arrowsmith CH, Vedadi M, Schapira M.

J Med Chem. 2016 Jul 28;59(14):6838-47. doi: 10.1021/acs.jmedchem.6b00668. Epub 2016 Jul 8. Erratum in: J Med Chem. 2016 Aug 25;59(16):7698.

PMID:
27390919
38.

Global Profiling of Acetyltransferase Feedback Regulation.

Montgomery DC, Garlick JM, Kulkarni RA, Kennedy S, Allali-Hassani A, Kuo YM, Andrews AJ, Wu H, Vedadi M, Meier JL.

J Am Chem Soc. 2016 May 25;138(20):6388-91. doi: 10.1021/jacs.6b03036. Epub 2016 May 17.

39.

PR Domain-containing Protein 7 (PRDM7) Is a Histone 3 Lysine 4 Trimethyltransferase.

Blazer LL, Lima-Fernandes E, Gibson E, Eram MS, Loppnau P, Arrowsmith CH, Schapira M, Vedadi M.

J Biol Chem. 2016 Jun 24;291(26):13509-19. doi: 10.1074/jbc.M116.721472. Epub 2016 Apr 29.

40.

Discovery and Characterization of a Highly Potent and Selective Aminopyrazoline-Based in Vivo Probe (BAY-598) for the Protein Lysine Methyltransferase SMYD2.

Eggert E, Hillig RC, Koehr S, Stöckigt D, Weiske J, Barak N, Mowat J, Brumby T, Christ CD, Ter Laak A, Lang T, Fernandez-Montalvan AE, Badock V, Weinmann H, Hartung IV, Barsyte-Lovejoy D, Szewczyk M, Kennedy S, Li F, Vedadi M, Brown PJ, Santhakumar V, Arrowsmith CH, Stellfeld T, Stresemann C.

J Med Chem. 2016 May 26;59(10):4578-600. doi: 10.1021/acs.jmedchem.5b01890. Epub 2016 May 3.

41.

Structure-Based Optimization of a Small Molecule Antagonist of the Interaction Between WD Repeat-Containing Protein 5 (WDR5) and Mixed-Lineage Leukemia 1 (MLL1).

Getlik M, Smil D, Zepeda-Velázquez C, Bolshan Y, Poda G, Wu H, Dong A, Kuznetsova E, Marcellus R, Senisterra G, Dombrovski L, Hajian T, Kiyota T, Schapira M, Arrowsmith CH, Brown PJ, Vedadi M, Al-Awar R.

J Med Chem. 2016 Mar 24;59(6):2478-96. doi: 10.1021/acs.jmedchem.5b01630. Epub 2016 Mar 9.

PMID:
26958703
42.

Discovery of a Potent Class I Protein Arginine Methyltransferase Fragment Inhibitor.

Ferreira de Freitas R, Eram MS, Szewczyk MM, Steuber H, Smil D, Wu H, Li F, Senisterra G, Dong A, Brown PJ, Hitchcock M, Moosmayer D, Stegmann CM, Egner U, Arrowsmith C, Barsyte-Lovejoy D, Vedadi M, Schapira M.

J Med Chem. 2016 Feb 11;59(3):1176-83. doi: 10.1021/acs.jmedchem.5b01772. Epub 2016 Jan 29.

PMID:
26824386
43.

A cellular chemical probe targeting the chromodomains of Polycomb repressive complex 1.

Stuckey JI, Dickson BM, Cheng N, Liu Y, Norris JL, Cholensky SH, Tempel W, Qin S, Huber KG, Sagum C, Black K, Li F, Huang XP, Roth BL, Baughman BM, Senisterra G, Pattenden SG, Vedadi M, Brown PJ, Bedford MT, Min J, Arrowsmith CH, James LI, Frye SV.

Nat Chem Biol. 2016 Mar;12(3):180-7. doi: 10.1038/nchembio.2007. Epub 2016 Jan 25.

44.

A Radioactivity-Based Assay for Screening Human m6A-RNA Methyltransferase, METTL3-METTL14 Complex, and Demethylase ALKBH5.

Li F, Kennedy S, Hajian T, Gibson E, Seitova A, Xu C, Arrowsmith CH, Vedadi M.

J Biomol Screen. 2016 Mar;21(3):290-7. doi: 10.1177/1087057115623264. Epub 2015 Dec 23.

PMID:
26701100
45.

SMN and symmetric arginine dimethylation of RNA polymerase II C-terminal domain control termination.

Zhao DY, Gish G, Braunschweig U, Li Y, Ni Z, Schmitges FW, Zhong G, Liu K, Li W, Moffat J, Vedadi M, Min J, Pawson TJ, Blencowe BJ, Greenblatt JF.

Nature. 2016 Jan 7;529(7584):48-53. doi: 10.1038/nature16469. Epub 2015 Dec 23.

PMID:
26700805
46.

A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases.

Eram MS, Shen Y, Szewczyk M, Wu H, Senisterra G, Li F, Butler KV, Kaniskan HÜ, Speed BA, Dela Seña C, Dong A, Zeng H, Schapira M, Brown PJ, Arrowsmith CH, Barsyte-Lovejoy D, Liu J, Vedadi M, Jin J.

ACS Chem Biol. 2016 Mar 18;11(3):772-781. doi: 10.1021/acschembio.5b00839. Epub 2015 Dec 8.

47.

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. 2016 Jan 14;14(2):631-638. doi: 10.1039/c5ob01794g.

48.

WDR5 Supports an N-Myc Transcriptional Complex That Drives a Protumorigenic Gene Expression Signature in Neuroblastoma.

Sun Y, Bell JL, Carter D, 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, Hüttelmaier S, Perini G, Marshall GM, Braithwaite A, Liu T.

Cancer Res. 2015 Dec 1;75(23):5143-54. doi: 10.1158/0008-5472.CAN-15-0423. Epub 2015 Oct 15.

49.

Erratum: 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. 2015 Oct;11(10):815. doi: 10.1038/nchembio1015-815b. No abstract available.

PMID:
26379026
50.

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. 2015 Sep 10;525(7568):206-11. doi: 10.1038/nature15251. Epub 2015 Sep 2.

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