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Items: 16

1.

Irreversible inhibition of cytosolic thioredoxin reductase 1 as a mechanistic basis for anticancer therapy.

Stafford WC, Peng X, Olofsson MH, Zhang X, Luci DK, Lu L, Cheng Q, Trésaugues L, Dexheimer TS, Coussens NP, Augsten M, Ahlzén HM, Orwar O, Östman A, Stone-Elander S, Maloney DJ, Jadhav A, Simeonov A, Linder S, Arnér ESJ.

Sci Transl Med. 2018 Feb 14;10(428). pii: eaaf7444. doi: 10.1126/scitranslmed.aaf7444.

PMID:
29444979
2.

Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH).

Rai G, Brimacombe KR, Mott BT, Urban DJ, Hu X, Yang SM, Lee TD, Cheff DM, Kouznetsova J, Benavides GA, Pohida K, Kuenstner EJ, Luci DK, Lukacs CM, Davies DR, Dranow DM, Zhu H, Sulikowski G, Moore WJ, Stott GM, Flint AJ, Hall MD, Darley-Usmar VM, Neckers LM, Dang CV, Waterson AG, Simeonov A, Jadhav A, Maloney DJ.

J Med Chem. 2017 Nov 22;60(22):9184-9204. doi: 10.1021/acs.jmedchem.7b00941. Epub 2017 Nov 9.

3.

First Selective 12-LOX Inhibitor, ML355, Impairs Thrombus Formation and Vessel Occlusion In Vivo With Minimal Effects on Hemostasis.

Adili R, Tourdot BE, Mast K, Yeung J, Freedman JC, Green A, Luci DK, Jadhav A, Simeonov A, Maloney DJ, Holman TR, Holinstat M.

Arterioscler Thromb Vasc Biol. 2017 Oct;37(10):1828-1839. doi: 10.1161/ATVBAHA.117.309868. Epub 2017 Aug 3.

4.

12-Lipoxygenase Inhibitor Improves Functions of Cytokine-Treated Human Islets and Type 2 Diabetic Islets.

Ma K, Xiao A, Park SH, Glenn L, Jackson L, Barot T, Weaver JR, Taylor-Fishwick DA, Luci DK, Maloney DJ, Mirmira RG, Imai Y, Nadler JL.

J Clin Endocrinol Metab. 2017 Aug 1;102(8):2789-2797. doi: 10.1210/jc.2017-00267.

5.

Correction: A High-Throughput Screen Identifies 2,9-Diazaspiro[5.5]Undecanes as Inducers of the Endoplasmic Reticulum Stress Response with Cytotoxic Activity in 3D Glioma Cell Models.

Martinez NJ, Rai G, Yasgar A, Lea WA, Sun H, Wang Y, Luci DK, Yang SM, Nishihara K, Takeda S, Mohiuddin, Earnshaw I, Okada T, Mori K, Wilson K, Riggins GJ, Xia M, Grimaldi M, Jadhav A, Maloney DJ, Simeonov A.

PLoS One. 2016 Nov 8;11(11):e0166506. doi: 10.1371/journal.pone.0166506. eCollection 2016.

6.

A High-Throughput Screen Identifies 2,9-Diazaspiro[5.5]Undecanes as Inducers of the Endoplasmic Reticulum Stress Response with Cytotoxic Activity in 3D Glioma Cell Models.

Martinez NJ, Rai G, Yasgar A, Lea WA, Sun H, Wang Y, Luci DK, Yang SM, Nishihara K, Takeda S, Sagor M, Earnshaw I, Okada T, Mori K, Wilson K, Riggins GJ, Xia M, Grimaldi M, Jadhav A, Maloney DJ, Simeonov A.

PLoS One. 2016 Aug 29;11(8):e0161486. doi: 10.1371/journal.pone.0161486. eCollection 2016. Erratum in: PLoS One. 2016 Nov 8;11(11):e0166506.

7.

Synthesis and structure-activity relationship studies of N-benzyl-2-phenylpyrimidin-4-amine derivatives as potent USP1/UAF1 deubiquitinase inhibitors with anticancer activity against nonsmall cell lung cancer.

Dexheimer TS, Rosenthal AS, Luci DK, Liang Q, Villamil MA, Chen J, Sun H, Kerns EH, Simeonov A, Jadhav A, Zhuang Z, Maloney DJ.

J Med Chem. 2014 Oct 9;57(19):8099-110. doi: 10.1021/jm5010495. Epub 2014 Sep 17.

8.

Platelet 12-LOX is essential for FcγRIIa-mediated platelet activation.

Yeung J, Tourdot BE, Fernandez-Perez P, Vesci J, Ren J, Smyrniotis CJ, Luci DK, Jadhav A, Simeonov A, Maloney DJ, Holman TR, McKenzie SE, Holinstat M.

Blood. 2014 Oct 2;124(14):2271-9. doi: 10.1182/blood-2014-05-575878. Epub 2014 Aug 6.

9.

A selective USP1-UAF1 inhibitor links deubiquitination to DNA damage responses.

Liang Q, Dexheimer TS, Zhang P, Rosenthal AS, Villamil MA, You C, Zhang Q, Chen J, Ott CA, Sun H, Luci DK, Yuan B, Simeonov A, Jadhav A, Xiao H, Wang Y, Maloney DJ, Zhuang Z.

Nat Chem Biol. 2014 Apr;10(4):298-304. doi: 10.1038/nchembio.1455. Epub 2014 Feb 16.

10.

Synthesis and structure-activity relationship studies of 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide derivatives as potent and selective inhibitors of 12-lipoxygenase.

Luci DK, Jameson JB 2nd, Yasgar A, Diaz G, Joshi N, Kantz A, Markham K, Perry S, Kuhn N, Yeung J, Kerns EH, Schultz L, Holinstat M, Nadler JL, Taylor-Fishwick DA, Jadhav A, Simeonov A, Holman TR, Maloney DJ.

J Med Chem. 2014 Jan 23;57(2):495-506. doi: 10.1021/jm4016476. Epub 2014 Jan 6.

11.

Disrupting malaria parasite AMA1-RON2 interaction with a small molecule prevents erythrocyte invasion.

Srinivasan P, Yasgar A, Luci DK, Beatty WL, Hu X, Andersen J, Narum DL, Moch JK, Sun H, Haynes JD, Maloney DJ, Jadhav A, Simeonov A, Miller LH.

Nat Commun. 2013;4:2261. doi: 10.1038/ncomms3261.

12.

Pyrimidinopyrimidine inhibitors of ketohexokinase: exploring the ring C2 group that interacts with Asp-27B in the ligand binding pocket.

Maryanoff BE, O'Neill JC, McComsey DF, Yabut SC, Luci DK, Gibbs AC, Connelly MA.

Bioorg Med Chem Lett. 2012 Aug 15;22(16):5326-9. doi: 10.1016/j.bmcl.2012.06.008. Epub 2012 Jun 17.

PMID:
22795331
13.

Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site.

Maryanoff BE, O'Neill JC, McComsey DF, Yabut SC, Luci DK, Jordan AD Jr, Masucci JA, Jones WJ, Abad MC, Gibbs AC, Petrounia I.

ACS Med Chem Lett. 2011 Apr 18;2(7):538-43. doi: 10.1021/ml200070g. eCollection 2011 Jul 14. Erratum in: ACS Med Chem Lett. 2012 Mar 8;3(3):263.

14.

Nonpeptide urotensin-II receptor antagonists: a new ligand class based on piperazino-phthalimide and piperazino-isoindolinone subunits.

Lawson EC, Luci DK, Ghosh S, Kinney WA, Reynolds CH, Qi J, Smith CE, Wang Y, Minor LK, Haertlein BJ, Parry TJ, Damiano BP, Maryanoff BE.

J Med Chem. 2009 Dec 10;52(23):7432-45. doi: 10.1021/jm900683d.

PMID:
19731961
15.

Phenylpiperidine-benzoxazinones as urotensin-II receptor antagonists: synthesis, SAR, and in vivo assessment.

Luci DK, Ghosh S, Smith CE, Qi J, Wang Y, Haertlein B, Parry TJ, Li J, Almond HR Jr, Minor LK, Damiano BP, Kinney WA, Maryanoff BE, Lawson EC.

Bioorg Med Chem Lett. 2007 Dec 1;17(23):6489-92. Epub 2007 Oct 1.

PMID:
17933531
16.

Synthesis and biological evaluation of a targeted library of protein phosphatase inhibitors.

Wipf P, Aslan DC, Luci DK, Southwick EC, Lazo JS.

Biotechnol Bioeng. 2000 Winter;71(1):58-70.

PMID:
10629537

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