Search Results - "Luci, Diane K."

A selective USP1–UAF1 inhibitor links deubiquitination to DNA damage responses by Liang, Qin, Dexheimer, Thomas S, Zhang, Ping, Rosenthal, Andrew S, Villamil, Mark A, You, Changjun, Zhang, Qiuting, Chen, Junjun, Ott, Christine A, Sun, Hongmao, Luci, Diane K, Yuan, Bifeng, Simeonov, Anton, Jadhav, Ajit, Xiao, Hui, Wang, Yinsheng, Maloney, David J, Zhuang, Zhihao

“…Deubiquitinases (DUBs) are peptidases that remove ubiquitin from post-translationally modified proteins. The identification of a selective small-molecule…”
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Nonpeptide Urotensin-II Receptor Antagonists: A New Ligand Class Based on Piperazino-Phthalimide and Piperazino-Isoindolinone Subunits by Lawson, Edward C, Luci, Diane K, Ghosh, Shyamali, Kinney, William A, Reynolds, Charles H, Qi, Jenson, Smith, Charles E, Wang, Yuanping, Minor, Lisa K, Haertlein, Barbara J, Parry, Tom J, Damiano, Bruce P, Maryanoff, Bruce E

“…We have discovered two related chemical series of nonpeptide urotensin-II (U-II) receptor antagonists based on piperazino-phthalimide (5 and 6) and…”
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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 by Martinez, Natalia J, Rai, Ganesha, Yasgar, Adam, Lea, Wendy A, Sun, Hongmao, Wang, Yuhong, Luci, Diane K, Yang, Shyh-Ming, Nishihara, Kana, Takeda, Shunichi, Sagor, Mohiuddin, Earnshaw, Irina, Okada, Tetsuya, Mori, Kazutoshi, Wilson, Kelli, Riggins, Gregory J, Xia, Menghang, Grimaldi, Maurizio, Jadhav, Ajit, Maloney, David J, Simeonov, Anton

“…The endoplasmic reticulum (ER) is involved in Ca2+ signaling and protein folding. ER Ca2+ depletion and accumulation of unfolded proteins activate the…”
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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 by Martinez, Natalia J, Rai, Ganesha, Yasgar, Adam, Lea, Wendy A, Sun, Hongmao, Wang, Yuhong, Luci, Diane K, Yang, Shyh-Ming, Nishihara, Kana, Takeda, Shunichi, Mohiuddin, Earnshaw, Irina, Okada, Tetsuya, Mori, Kazutoshi, Wilson, Kelli, Riggins, Gregory J, Xia, Menghang, Grimaldi, Maurizio, Jadhav, Ajit, Maloney, David J, Simeonov, Anton

“…[This corrects the article DOI: 10.1371/journal.pone.0161486.]…”
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First Selective 12-LOX Inhibitor, ML355, Impairs Thrombus Formation and Vessel Occlusion In Vivo With Minimal Effects on Hemostasis by Adili, Reheman, Tourdot, Benjamin E, Mast, Katherine, Yeung, Jennifer, Freedman, John C, Green, Abigail, Luci, Diane K, Jadhav, Ajit, Simeonov, Anton, Maloney, David J, Holman, Theodore R, Holinstat, Michael

“…Adequate platelet reactivity is required for maintaining hemostasis. However, excessive platelet reactivity can also lead to the formation of occlusive…”
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Irreversible inhibition of cytosolic thioredoxin reductase 1 as a mechanistic basis for anticancer therapy by Stafford, William C, Peng, Xiaoxiao, Olofsson, Maria Hägg, Zhang, Xiaonan, Luci, Diane K, Lu, Li, Cheng, Qing, Trésaugues, Lionel, Dexheimer, Thomas S, Coussens, Nathan P, Augsten, Martin, Ahlzén, Hanna-Stina Martinsson, Orwar, Owe, Östman, Arne, Stone-Elander, Sharon, Maloney, David J, Jadhav, Ajit, Simeonov, Anton, Linder, Stig, Arnér, Elias S J

“…Cancer cells adapt to their inherently increased oxidative stress through activation of the glutathione (GSH) and thioredoxin (TXN) systems. Inhibition of both…”
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Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH) by Rai, Ganesha, Brimacombe, Kyle R, Mott, Bryan T, Urban, Daniel J, Hu, Xin, Yang, Shyh-Ming, Lee, Tobie D, Cheff, Dorian M, Kouznetsova, Jennifer, Benavides, Gloria A, Pohida, Katie, Kuenstner, Eric J, Luci, Diane K, Lukacs, Christine M, Davies, Douglas R, Dranow, David M, Zhu, Hu, Sulikowski, Gary, Moore, William J, Stott, Gordon M, Flint, Andrew J, Hall, Matthew D, Darley-Usmar, Victor M, Neckers, Leonard M, Dang, Chi V, Waterson, Alex G, Simeonov, Anton, Jadhav, Ajit, Maloney, David J

“…We report the discovery and medicinal chemistry optimization of a novel series of pyrazole-based inhibitors of human lactate dehydrogenase (LDH). Utilization…”
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Discovering selective antiferroptotic inhibitors of the 15LOX/PEBP1 complex noninterfering with biosynthesis of lipid mediators by Dar, Haider H, Mikulska-Ruminska, Karolina, Tyurina, Yulia Y, Luci, Diane K, Yasgar, Adam, Samovich, Svetlana N, Kapralov, Alexander A, Souryavong, Austin B, Tyurin, Vladimir A, Amoscato, Andrew A, Epperly, Michael W, Shurin, Galina V, Standley, Melissa, Holman, Theodore R, St Croix, Claudette M, Watkins, Simon C, VanDemark, Andrew P, Rana, Sandeep, Zakharov, Alexey V, Simeonov, Anton, Marugan, Juan, Mallampalli, Rama K, Wenzel, Sally E, Greenberger, Joel S, Rai, Ganesha, Bayir, Hülya, Bahar, Ivet, Kagan, Valerian E

“…Programmed ferroptotic death eliminates cells in all major organs and tissues with imbalanced redox metabolism due to overwhelming iron-catalyzed lipid…”
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Platelet 12-LOX is essential for FcγRIIa-mediated platelet activation by Yeung, Jennifer, Tourdot, Benjamin E., Fernandez-Perez, Pilar, Vesci, Joanne, Ren, Jin, Smyrniotis, Christopher J., Luci, Diane K., Jadhav, Ajit, Simeonov, Anton, Maloney, David J., Holman, Theodore R., McKenzie, Steven E., Holinstat, Michael

“…Platelets are essential in maintaining hemostasis following inflammation or injury to the vasculature. Dysregulated platelet activity often results in…”
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Disrupting malaria parasite AMA1–RON2 interaction with a small molecule prevents erythrocyte invasion by Srinivasan, Prakash, Yasgar, Adam, Luci, Diane K., Beatty, Wandy L., Hu, Xin, Andersen, John, Narum, David L., Moch, J. Kathleen, Sun, Hongmao, Haynes, J. David, Maloney, David J., Jadhav, Ajit, Simeonov, Anton, Miller, Louis H.

“…Plasmodium falciparum resistance to artemisinin derivatives, the first-line antimalarial drug, drives the search for new classes of chemotherapeutic agents…”
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Synthesis and Structure–Activity Relationship Studies of 4‑((2-Hydroxy-3-methoxybenzyl)amino)benzenesulfonamide Derivatives as Potent and Selective Inhibitors of 12-Lipoxygenase by Luci, Diane K., Jameson, J. Brian, Yasgar, Adam, Diaz, Giovanni, Joshi, Netra, Kantz, Auric, Markham, Kate, Perry, Steve, Kuhn, Norine, Yeung, Jennifer, Kerns, Edward H., Schultz, Lena, Holinstat, Michael, Nadler, Jerry L., Taylor-Fishwick, David A., Jadhav, Ajit, Simeonov, Anton, Holman, Theodore R., Maloney, David J.

“…Human lipoxygenases (LOXs) are a family of iron-containing enzymes which catalyze the oxidation of polyunsaturated fatty acids to provide the corresponding…”
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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 by Dexheimer, Thomas S, Rosenthal, Andrew S, Luci, Diane K, Liang, Qin, Villamil, Mark A, Chen, Junjun, Sun, Hongmao, Kerns, Edward H, Simeonov, Anton, Jadhav, Ajit, Zhuang, Zhihao, Maloney, David J

“…Deregulation of ubiquitin conjugation or deconjugation has been implicated in the pathogenesis of many human diseases including cancer. The deubiquitinating…”
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12-Lipoxygenase Inhibitor Improves Functions of Cytokine-Treated Human Islets and Type 2 Diabetic Islets by Ma, Kaiwen, Xiao, An, Park, So Hyun, Glenn, Lindsey, Jackson, Laura, Barot, Tatvam, Weaver, Jessica R, Taylor-Fishwick, David A, Luci, Diane K, Maloney, David J, Mirmira, Raghavendra G, Imai, Yumi, Nadler, Jerry L

“…Abstract Context The 12-lipoxygenase (12-LO) pathway produces proinflammatory metabolites, and its activation is implicated in islet inflammation associated…”
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Generation of novel, potent urotensin-II receptor antagonists by alkylation–cyclization of isoindolinone C3-carbanions by Luci, Diane K., Lawson, Edward C., Ghosh, Shyamali, Kinney, William A., Smith, Charles E., Qi, Jenson, Wang, Yuanping, Minor, Lisa K., Maryanoff, Bruce E.

“…We report a facile alkylation–cyclization reaction involving the isoindolinone C3 position, which resulted in tricyclic derivatives 2 and 10 in 48% and 32%…”
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Pyrimidinopyrimidine inhibitors of ketohexokinase: Exploring the ring C2 group that interacts with Asp-27B in the ligand binding pocket by Maryanoff, Bruce E., O’Neill, John C., McComsey, David F., Yabut, Stephen C., Luci, Diane K., Gibbs, Alan C., Connelly, Margery A.

“…Inhibitors of ketohexokinase (KHK) have potential for the treatment of diabetes and obesity. We have continued studies on a pyrimidinopyrimidine series of…”
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Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site by Maryanoff, Bruce E, O'Neill, John C, McComsey, David F, Yabut, Stephen C, Luci, Diane K, Jordan, Alfonzo D, Masucci, John A, Jones, William J, Abad, Marta C, Gibbs, Alan C, Petrounia, Ioanna

“…Attenuation of fructose metabolism by the inhibition of ketohexokinase (KHK; fructokinase) should reduce body weight, free fatty acids, and triglycerides,…”
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Phenylpiperidine-benzoxazinones as urotensin-II receptor antagonists: Synthesis, SAR, and in vivo assessment by Luci, Diane K., Ghosh, Shyamali, Smith, Charles E., Qi, Jenson, Wang, Yuanping, Haertlein, Barbara, Parry, Tom J., Li, Jian, Almond, Harold R., Minor, Lisa K., Damiano, Bruce P., Kinney, William A., Maryanoff, Bruce E., Lawson, Edward C.

“…Various 4-phenylpiperidine-benzoxazin-3-ones were synthesized and biologically evaluated as urotensin-II (U-II) receptor antagonists. Compound 12i was…”
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Correction to Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site by Maryanoff, Bruce E, O'Neill, John C, McComsey, David F, Yabut, Stephen C, Luci, Diane K, Jordan, Alfonzo D, Masucci, John A, Jones, William J, Abad, Marta C, Gibbs, Alan C, Petrounia, Ioanna

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The Heck reaction with unprotected allylic amidines and guanidines by Lawson, Edward C, Kinney, William A, Luci, Diane K, Yabut, Stephen C, Wisnoski, David, Maryanoff, Bruce E

“…The applicability of Heck methodology to the introduction of unprotected amidines and guanidines was investigated. Unprotected guanidine-substituted olefins…”
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Synthesis and biological evaluation of a targeted library of protein phosphatase inhibitors by Wipf, Peter, Aslan, Diana C., Luci, Diane K., Southwick, Eileen C., Lazo, John S.

“…Phosphorylation of serine, threonine, and tyrosine controls fundamental mammalian cell events and is achieved by kinases which, in turn, are in dynamic…”
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