Search Results - "Thomas, D.Y"

New p32/gC1qR Ligands for Targeted Tumor Drug Delivery by Paasonen, Lauri, Sharma, Shweta, Braun, Gary B., Kotamraju, Venkata Ramana, Chung, Thomas D. Y., She, Zhi-Gang, Sugahara, Kazuki N., Yliperttula, Marjo, Wu, Bainan, Pellecchia, Maurizio, Ruoslahti, Erkki, Teesalu, Tambet

“…Cell surface p32, the target of LyP‐1 homing peptide, is upregulated in tumors and atherosclerotic plaques and has been widely used as a receptor for systemic…”
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Discovery of 4-oxo-6-((pyrimidin-2-ylthio)methyl)-4H-pyran-3-yl 4-nitrobenzoate (ML221) as a functional antagonist of the apelin (APJ) receptor by Maloney, Patrick R., Khan, Pasha, Hedrick, Michael, Gosalia, Palak, Milewski, Monika, Li, Linda, Roth, Gregory P., Sergienko, Eduard, Suyama, Eigo, Sugarman, Eliot, Nguyen, Kevin, Mehta, Alka, Vasile, Stefan, Su, Ying, Stonich, Derek, Nguyen, Hung, Zeng, Fu-Yue, Novo, Arianna Mangravita, Vicchiarelli, Michael, Diwan, Jena, Chung, Thomas D.Y., Smith, Layton H., Pinkerton, Anthony B.

“…The recently discovered apelin/APJ system has emerged as a critical mediator of cardiovascular homeostasis and is associated with the pathogenesis of…”
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Dual-Specificity Phosphatase 3 Deficiency or Inhibition Limits Platelet Activation and Arterial Thrombosis by Musumeci, Lucia, Kuijpers, Marijke J, Gilio, Karen, Hego, Alexandre, Théâtre, Emilie, Maurissen, Lisbeth, Vandereyken, Maud, Diogo, Catia V, Lecut, Christelle, Guilmain, William, Bobkova, Ekaterina V, Eble, Johannes A, Dahl, Russell, Drion, Pierre, Rascon, Justin, Mostofi, Yalda, Yuan, Hongbin, Sergienko, Eduard, Chung, Thomas D.Y, Thiry, Marc, Senis, Yotis, Moutschen, Michel, Mustelin, Tomas, Lancellotti, Patrizio, Heemskerk, Johan W.M, Tautz, Lutz, Oury, Cécile, Rahmouni, Souad

“…BACKGROUND—A limitation of current antiplatelet therapies is their inability to separate thrombotic events from bleeding occurrences. A better understanding of…”
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Translation to Practice: Accelerating the Cycle of Innovation to Impact by Anderson, Jeff R., Chung, Thomas D.Y., Clark, Leon, Weis, Jennifer A., Danielsen, Andrew J., Khosla, Sundeep, Gores, Gregory J., Badley, Andrew D.

“…The Office of Translation to Practice (OTP) is housed in the Center for Clinical and Translational Sciences at Mayo Clinic. Established in 2015, the office was…”
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Collaborative pre-competitive preclinical drug discovery with academics and pharma/biotech partners at Sanford|Burnham: infrastructure, capabilities & operational models by Chung, Thomas D Y

“…There has been increased concern that the current "blockbuster" model of drug discovery and development practiced by "Big Pharma" are unsustainable in terms of…”
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Discovery of a Plasmodium falciparum Glucose-6-phosphate Dehydrogenase 6‑phosphogluconolactonase Inhibitor (R,Z)‑N‑((1-Ethylpyrrolidin-2-yl)methyl)-2-(2-fluorobenzylidene)-3-oxo-3,4-dihydro‑2H‑benzo[b][1,4]thiazine-6-carboxamide (ML276) That Reduces Parasite Growth in Vitro by Preuss, Janina, Maloney, Patrick, Peddibhotla, Satyamaheshwar, Hedrick, Michael P, Hershberger, Paul, Gosalia, Palak, Milewski, Monika, Li, Yujie Linda, Sugarman, Eliot, Hood, Becky, Suyama, Eigo, Nguyen, Kevin, Vasile, Stefan, Sergienko, Eduard, Mangravita-Novo, Arianna, Vicchiarelli, Michael, McAnally, Danielle, Smith, Layton H, Roth, Gregory P, Diwan, Jena, Chung, Thomas D.Y, Jortzik, Esther, Rahlfs, Stefan, Becker, Katja, Pinkerton, Anthony B, Bode, Lars

“…A high-throughput screen of the NIH’s MLSMR collection of ∼340000 compounds was undertaken to identify compounds that inhibit Plasmodium falciparum…”
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Assay format as a critical success factor for identification of novel inhibitor chemotypes of tissue-nonspecific alkaline phosphatase from high-throughput screening by Chung, Thomas D Y, Sergienko, Eduard, Millán, José Luis

“…The tissue-nonspecific alkaline phosphatase (TNAP) isozyme is centrally involved in the control of normal skeletal mineralization and pathophysiological…”
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Design of High-Throughput Screening Assays and Identification of a SUMO1-Specific Small Molecule Chemotype Targeting the SUMO-Interacting Motif-Binding Surface by Alontaga, Aileen Y, Li, Yifei, Chen, Chih-Hong, Ma, Chen-Ting, Malany, Siobhan, Key, Danielle E, Sergienko, Eduard, Sun, Qing, Whipple, David A, Matharu, Daljit S, Li, Baozong, Vega, Ramir, Li, Yi-Jia, Schoenen, Frank J, Blagg, Brian S. J, Chung, Thomas D.Y, Chen, Yuan

“…Protein–protein interactions are generally challenging to target by small molecules. To address the challenge, we have used a multidisciplinary approach to…”
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ML314: A Biased Neurotensin Receptor Ligand for Methamphetamine Abuse by Barak, Larry S, Bai, Yushi, Peterson, Sean, Evron, Tama, Urs, Nikhil M, Peddibhotla, Satyamaheshwar, Hedrick, Michael P, Hershberger, Paul, Maloney, Patrick R, Chung, Thomas D.Y, Rodriguiz, Ramona M, Wetsel, William C, Thomas, James B, Hanson, Glen R, Pinkerton, Anthony B, Caron, Marc G

“…Pharmacological treatment for methamphetamine addiction will provide important societal benefits. Neurotensin receptor NTR1 and dopamine receptor distributions…”
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High-throughput fluorescence polarization assay for chemical library screening against anti-apoptotic Bcl-2 family member Bfl-1 by Zhai, Dayong, Godoi, Paulo, Sergienko, Eduard, Dahl, Russell, Chan, Xochella, Brown, Brock, Rascon, Justin, Hurder, Andrew, Su, Ying, Chung, Thomas D Y, Jin, Chaofang, Diaz, Paul, Reed, John C

“…Overexpression of the anti-apoptotic Bcl-2 family proteins occurs commonly in human cancers. Bfl-1 is highly expressed in some types of malignant cells,…”
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Phosphorylation by CK2 and MAPK enhances calnexin association with ribosomes by Chevet, E., Wong, H.N., Gerber, D., Cochet, C., Fazel, A., Cameron, P.H., Gushue, J.N., Thomas, D.Y., Bergeron, J.J.M.

“…Calnexin was initially identified as an endoplasmic reticulum (ER) type I integral membrane protein, phosphorylated on its cytosolic domain by ER‐associated…”
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Improvement of "hit-to-lead" optimization by integration of in vitro HTS experimental models for early determination of pharmacokinetic properties by Kariv, Ilona, Rourick, Robyn A, Kassel, Daniel B, Chung, Thomas D Y

“…Development of predictive in vitro surrogate methods for traditional approaches assessing bioavailability and pharmacokinetics of lead compounds must be made…”
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Selective inhibition of bacterial dihydroorotate dehydrogenases by thiadiazolidinediones by Marcinkeviciene, Jovita, Rogers, M.John, Kopcho, Lisa, Jiang, Wenjun, Wang, Kathy, Murphy, Dennis J, Lippy, Jonathan, Link, Steven, Chung, Thomas D.Y, Hobbs, Frank, Haque, Tasir, Trainor, George L, Slee, Andrew, Stern, Andrew M, Copeland, Robert A

“…Dihydroorotate dehydrogenase is a critical enzyme of de novo pyrimidine biosynthesis in prokaryotic and eukaryotic cells. Differences in the primary structure…”
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SSR alpha and associated calnexin are major calcium binding proteins of the endoplasmic reticulum membrane by I Wada, D Rindress, P H Cameron, W J Ou, J J Doherty, 2nd, D Louvard, A W Bell, D Dignard, D Y Thomas, J J Bergeron

“…GTP phosphorylation of rough microsomes in vitro is limited to four integral membrane proteins. Two of these, a phosphoprotein (pp90) and a phosphoglycoprotein…”
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High-throughput screening of compounds targeting RNA editing in Trypanosoma brucei: Novel molecular scaffolds with broad trypanocidal effects by Rostamighadi, Mojtaba, Kamelshahroudi, Arezou, Mehta, Vaibhav, Zeng, Fu-Yue, Pass, Ian, Chung, Thomas D Y, Salavati, Reza

“…Mitochondrial uridine insertion/deletion RNA editing, catalyzed by a multiprotein complex (editosome), is essential for gene expression in trypanosomes and…”
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Use of moving optical gradient fields for analysis of apoptotic cellular responses in a chronic myeloid leukemia cell model by Forster, Anita H, Wang, Mark M, Butler, William F, Chachisvilis, Mirianas, Chung, Thomas D.Y, Esener, Sadik C, Hall, Jeffrey M, Kibar, Osman, Lykstad, Kristie, Marchand, Philippe J, Mercer, Elinore M, Pestana, Luis M, Sur, Sudipto, Tu, Eugene, Yang, Rong, Zhang, Haichuan, Kariv, Ilona

“…To facilitate quantitation of cellular apoptotic responses to various antineoplastic agents, a laser-based technology, Optophoresis, has been developed to…”
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Capzimin is a potent and specific inhibitor of proteasome isopeptidase Rpn11 by Li, Jing, Yakushi, Tanya, Parlati, Francesco, Mackinnon, Andrew L, Perez, Christian, Ma, Yuyong, Carter, Kyle P, Colayco, Sharon, Magnuson, Gavin, Brown, Brock, Nguyen, Kevin, Vasile, Stefan, Suyama, Eigo, Smith, Layton H, Sergienko, Eduard, Pinkerton, Anthony B, Chung, Thomas D Y, Palmer, Amy E, Pass, Ian, Hess, Sonja, Cohen, Seth M, Deshaies, Raymond J

“…Two screening approaches converge on capzimin, a first-in-class inhibitor of the Rpn11 protease component of the 19S proteasome. Capzimin stabilizes…”
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Allosteric Inhibition of Ubiquitin-like Modifications by a Class of Inhibitor of SUMO-Activating Enzyme by Li, Yi-Jia, Du, Li, Wang, Jianghai, Vega, Ramir, Lee, Terry D, Miao, Yunan, Aldana-Masangkay, Grace, Samuels, Eric R, Li, Baozong, Ouyang, S Xiaohu, Colayco, Sharon A, Bobkova, Ekaterina V, Divlianska, Daniela B, Sergienko, Eduard, Chung, Thomas D Y, Fakih, Marwan, Chen, Yuan

“…Ubiquitin-like (Ubl) post-translational modifications are potential targets for therapeutics. However, the only known mechanism for inhibiting a Ubl-activating…”
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Dominant-negative mutants of a yeast G-protein beta subunit identify two functional regions involved in pheromone signalling by Leberer, E, Dignard, D, Hougan, L, Thomas, D.Y, Whiteway, M

“…The STE4 gene, which encodes the beta subunit of the mating response G-protein in the yeast Saccharomyces cerevisiae, was subjected to a saturation mutagenesis…”
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Processing of the papain precursor. Purification of the zymogen and characterization of its mechanism of processing by Vernet, T. (National Research Council of Canada, Montreal, Quebec, Canada), Khouri, H.E, Laflamme, P, Tessier, D.C, Musil, R, Gour-Salin, B.J, Storer, A.C, Thomas, D.Y

“…The precursor of the cysteine protease papain has been expressed and secreted as propapain from insect cells infected with a recombinant baculovirus expressing…”
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