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Items: 15

1.

Discovery and Optimization of Quinolinone Derivatives as Potent, Selective, and Orally Bioavailable Mutant Isocitrate Dehydrogenase 1 (mIDH1) Inhibitors.

Lin J, Lu W, Caravella JA, Campbell AM, Diebold RB, Ericsson A, Fritzen E, Gustafson GR, Lancia DR Jr, Shelekhin T, Wang Z, Castro J, Clarke A, Gotur D, Josephine HR, Katz M, Diep H, Kershaw M, Yao L, Kauffman G, Hubbs SE, Luke GP, Toms AV, Wang L, Bair KW, Barr KJ, Dinsmore C, Walker D, Ashwell S.

J Med Chem. 2019 Jul 8. doi: 10.1021/acs.jmedchem.9b00362. [Epub ahead of print]

PMID:
31199148
2.

Distinct USP25 and USP28 Oligomerization States Regulate Deubiquitinating Activity.

Gersch M, Wagstaff JL, Toms AV, Graves B, Freund SMV, Komander D.

Mol Cell. 2019 May 2;74(3):436-451.e7. doi: 10.1016/j.molcel.2019.02.030. Epub 2019 Mar 26.

3.

Discovery and optimization of novel piperazines as potent inhibitors of fatty acid synthase (FASN).

Martin MW, Lancia DR Jr, Li H, Schiller SER, Toms AV, Wang Z, Bair KW, Castro J, Fessler S, Gotur D, Hubbs SE, Kauffman GS, Kershaw M, Luke GP, McKinnon C, Yao L, Lu W, Millan DS.

Bioorg Med Chem Lett. 2019 Apr 15;29(8):1001-1006. doi: 10.1016/j.bmcl.2019.02.012. Epub 2019 Feb 11.

PMID:
30803804
4.

Molecular basis of USP7 inhibition by selective small-molecule inhibitors.

Turnbull AP, Ioannidis S, Krajewski WW, Pinto-Fernandez A, Heride C, Martin ACL, Tonkin LM, Townsend EC, Buker SM, Lancia DR, Caravella JA, Toms AV, Charlton TM, Lahdenranta J, Wilker E, Follows BC, Evans NJ, Stead L, Alli C, Zarayskiy VV, Talbot AC, Buckmelter AJ, Wang M, McKinnon CL, Saab F, McGouran JF, Century H, Gersch M, Pittman MS, Marshall CG, Raynham TM, Simcox M, Stewart LMD, McLoughlin SB, Escobedo JA, Bair KW, Dinsmore CJ, Hammonds TR, Kim S, Urbé S, Clague MJ, Kessler BM, Komander D.

Nature. 2017 Oct 26;550(7677):481-486. doi: 10.1038/nature24451. Epub 2017 Oct 18.

5.

Crystal Structure of the FERM-SH2 Module of Human Jak2.

McNally R, Toms AV, Eck MJ.

PLoS One. 2016 May 26;11(5):e0156218. doi: 10.1371/journal.pone.0156218. eCollection 2016.

6.

Structure of a pseudokinase-domain switch that controls oncogenic activation of Jak kinases.

Toms AV, Deshpande A, McNally R, Jeong Y, Rogers JM, Kim CU, Gruner SM, Ficarro SB, Marto JA, Sattler M, Griffin JD, Eck MJ.

Nat Struct Mol Biol. 2013 Oct;20(10):1221-3. doi: 10.1038/nsmb.2673. Epub 2013 Sep 8.

7.

Structure and ubiquitination-dependent activation of TANK-binding kinase 1.

Tu D, Zhu Z, Zhou AY, Yun CH, Lee KE, Toms AV, Li Y, Dunn GP, Chan E, Thai T, Yang S, Ficarro SB, Marto JA, Jeon H, Hahn WC, Barbie DA, Eck MJ.

Cell Rep. 2013 Mar 28;3(3):747-58. doi: 10.1016/j.celrep.2013.01.033. Epub 2013 Feb 28.

8.

Genetic resistance to JAK2 enzymatic inhibitors is overcome by HSP90 inhibition.

Weigert O, Lane AA, Bird L, Kopp N, Chapuy B, van Bodegom D, Toms AV, Marubayashi S, Christie AL, McKeown M, Paranal RM, Bradner JE, Yoda A, Gaul C, Vangrevelinghe E, Romanet V, Murakami M, Tiedt R, Ebel N, Evrot E, De Pover A, Régnier CH, Erdmann D, Hofmann F, Eck MJ, Sallan SE, Levine RL, Kung AL, Baffert F, Radimerski T, Weinstock DM.

J Exp Med. 2012 Feb 13;209(2):259-73. doi: 10.1084/jem.20111694. Epub 2012 Jan 23.

9.

Structure and function of the interacting domains of Spire and Fmn-family formins.

Vizcarra CL, Kreutz B, Rodal AA, Toms AV, Lu J, Zheng W, Quinlan ME, Eck MJ.

Proc Natl Acad Sci U S A. 2011 Jul 19;108(29):11884-9. doi: 10.1073/pnas.1105703108. Epub 2011 Jul 5.

10.

Crystal structure of a coiled-coil domain from human ROCK I.

Tu D, Li Y, Song HK, Toms AV, Gould CJ, Ficarro SB, Marto JA, Goode BL, Eck MJ.

PLoS One. 2011 Mar 21;6(3):e18080. doi: 10.1371/journal.pone.0018080.

11.

Binucleine 2, an isoform-specific inhibitor of Drosophila Aurora B kinase, provides insights into the mechanism of cytokinesis.

Smurnyy Y, Toms AV, Hickson GR, Eck MJ, Eggert US.

ACS Chem Biol. 2010 Nov 19;5(11):1015-20. doi: 10.1021/cb1001685.

12.

The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP.

Yun CH, Mengwasser KE, Toms AV, Woo MS, Greulich H, Wong KK, Meyerson M, Eck MJ.

Proc Natl Acad Sci U S A. 2008 Feb 12;105(6):2070-5. doi: 10.1073/pnas.0709662105. Epub 2008 Jan 28.

13.

Novel multisubstrate inhibitors of mammalian purine nucleoside phosphorylase.

Toms AV, Wang W, Li Y, Ganem B, Ealick SE.

Acta Crystallogr D Biol Crystallogr. 2005 Nov;61(Pt 11):1449-58. Epub 2005 Oct 19.

PMID:
16239721
14.

Structural characterization of the regulatory proteins TenA and TenI from Bacillus subtilis and identification of TenA as a thiaminase II.

Toms AV, Haas AL, Park JH, Begley TP, Ealick SE.

Biochemistry. 2005 Feb 22;44(7):2319-29.

PMID:
15709744
15.

Evolutionary links as revealed by the structure of Thermotoga maritima S-adenosylmethionine decarboxylase.

Toms AV, Kinsland C, McCloskey DE, Pegg AE, Ealick SE.

J Biol Chem. 2004 Aug 6;279(32):33837-46. Epub 2004 May 18.

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