Search Results - "Chung, Thomas D. Y"

Identification of the GPR55 Antagonist Binding Site Using a Novel Set of High-Potency GPR55 Selective Ligands by Kotsikorou, Evangelia, Sharir, Haleli, Shore, Derek M, Hurst, Dow P, Lynch, Diane L, Madrigal, Karla E, Heynen-Genel, Susanne, Milan, Loribelle B, Chung, Thomas D. Y, Seltzman, Herbert H, Bai, Yushi, Caron, Marc G, Barak, Larry S, Croatt, Mitchell P, Abood, Mary E, Reggio, Patricia H

“…GPR55 is a class A G protein-coupled receptor (GPCR) that has been implicated in inflammatory pain, neuropathic pain, metabolic disorder, bone development, and…”
Get full text

Identification of the GPR55 Agonist Binding Site Using a Novel Set of High-Potency GPR55 Selective Ligands by Kotsikorou, Evangelia, Madrigal, Karla E, Hurst, Dow P, Sharir, Haleli, Lynch, Diane L, Heynen-Genel, Susanne, Milan, Loribelle B, Chung, Thomas D. Y, Seltzman, Herbert H, Bai, Yushi, Caron, Marc G, Barak, Larry, Abood, Mary E, Reggio, Patricia H

“…Marijuana is the most widely abused illegal drug, and its spectrum of effects suggests that several receptors are responsible for the activity. Two cannabinoid…”
Get full text

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…”
Get full text

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…”
Get full text

An Optimized Dihydrodibenzothiazepine Lead Compound (SBI-0797750) as a Potent and Selective Inhibitor of Plasmodium falciparum and P. vivax Glucose 6-Phosphate Dehydrogenase 6-Phosphogluconolactonase by Berneburg, Isabell, Peddibhotla, Satyamaheshwar, Heimsch, Kim C, Haeussler, Kristina, Maloney, Patrick, Gosalia, Palak, Preuss, Janina, Rahbari, Mahsa, Skorokhod, Oleksii, Valente, Elena, Ulliers, Daniela, Simula, Luigi Felice, Buchholz, Kathrin, Hedrick, Michael P, Hershberger, Paul, Chung, Thomas D Y, Jackson, Michael R, Schwarzer, Evelin, Rahlfs, Stefan, Bode, Lars, Becker, Katja, Pinkerton, Anthony B

“…In , the first two and rate-limiting enzymes of the pentose phosphate pathway, glucose 6-phosphate dehydrogenase (G6PD) and the 6-phosphogluconolactonase, are…”
Get full text

Discovery of Orally Bioavailable Purine-Based Inhibitors of the Low-Molecular-Weight Protein Tyrosine Phosphatase by Stanford, Stephanie M, Diaz, Michael A, Ardecky, Robert J, Zou, Jiwen, Roosild, Tarmo, Holmes, Zachary J, Nguyen, Tiffany P, Hedrick, Michael P, Rodiles, Socorro, Guan, April, Grotegut, Stefan, Santelli, Eugenio, Chung, Thomas D. Y, Jackson, Michael R, Bottini, Nunzio, Pinkerton, Anthony B

“…Obesity-associated insulin resistance plays a central role in the pathogenesis of type 2 diabetes. A promising approach to decrease insulin resistance in…”
Get full text

Discovery of β‑Arrestin Biased, Orally Bioavailable, and CNS Penetrant Neurotensin Receptor 1 (NTR1) Allosteric Modulators by Pinkerton, Anthony B, Peddibhotla, Satyamaheshwar, Yamamoto, Fusayo, Slosky, Lauren M, Bai, Yushi, Maloney, Patrick, Hershberger, Paul, Hedrick, Michael P, Falter, Bekhi, Ardecky, Robert J, Smith, Layton H, Chung, Thomas D. Y, Jackson, Michael R, Caron, Marc G, Barak, Lawrence S

“…Neurotensin receptor 1 (NTR1) is a G protein coupled receptor that is widely expressed throughout the central nervous system where it acts as a neuromodulator…”
Get full text

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…”
Get full text

Diabetes reversal by inhibition of the low-molecular-weight tyrosine phosphatase by Stanford, Stephanie M, Aleshin, Alexander E, Zhang, Vida, Ardecky, Robert J, Hedrick, Michael P, Zou, Jiwen, Ganji, Santhi R, Bliss, Matthew R, Yamamoto, Fusayo, Bobkov, Andrey A, Kiselar, Janna, Liu, Yingge, Cadwell, Gregory W, Khare, Shilpi, Yu, Jinghua, Barquilla, Antonio, Chung, Thomas D Y, Mustelin, Tomas, Schenk, Simon, Bankston, Laurie A, Liddington, Robert C, Pinkerton, Anthony B, Bottini, Nunzio

“…The generation of low-molecular-weight protein tyrosine phosphatase (LMPTP) knockout mice combined with the identification of a small-molecule uncompetitive…”
Get full text

Both HIV-Infected and Uninfected Cells Express TRAILshort, Which Confers TRAIL Resistance upon Bystander Cells within the Microenvironment by Nie, Zilin, Aboulnasr, Fatma, Natesampillai, Sekar, Burke, Stephen P, Krogman, Ashton, Bren, Gary D, Chung, Thomas D Y, Anderson, Jeff R, Smart, Michele K, Katzmann, David J, Rajagopalan, Govindarajan, Cummins, Nathan W, Badley, Andrew D

“…TNF-related apoptosis-inducing ligand (TRAIL) was initially described to induce apoptosis of tumor cells and/or virally infected cells, although sparing normal…”
Get full text

Identification and characterization of small molecule inhibitors of the ubiquitin ligases Siah1/2 in melanoma and prostate cancer cells by Feng, Yongmei, Sessions, E. Hampton, Zhang, Fan, Ban, Fuqiang, Placencio-Hickok, Veronica, Ma, Chen-Ting, Zeng, Fu-Yue, Pass, Ian, Terry, David B., Cadwell, Gregory, Bankston, Laurie A., Liddington, Robert C., Chung, Thomas D.Y., Pinkerton, Anthony B., Sergienko, Eduard, Gleave, Martin, Bhowmick, Neil A., Jackson, Michael R., Cherkasov, Artem, Ronai, Ze'ev A.

“…Inhibition of ubiquitin ligases with small molecule remains a very challenging task, given the lack of catalytic activity of the target and the requirement of…”
Get full text

Discovery of Small Molecule Kappa Opioid Receptor Agonist and Antagonist Chemotypes through a HTS and Hit Refinement Strategy by Frankowski, Kevin J, Hedrick, Michael P, Gosalia, Palak, Li, Kelin, Shi, Shenghua, Whipple, David, Ghosh, Partha, Prisinzano, Thomas E, Schoenen, Frank J, Su, Ying, Vasile, S, Sergienko, Eduard, Gray, Wilson, Hariharan, Santosh, Milan, Loribelle, Heynen-Genel, Susanne, Mangravita-Novo, Arianna, Vicchiarelli, Michael, Smith, Layton H, Streicher, John M, Caron, Marc G, Barak, Lawrence S, Bohn, Laura M, Chung, Thomas D. Y, Aubé, Jeffrey

“…Herein we present the outcome of a high throughput screening (HTS) campaign-based strategy for the rapid identification and optimization of selective and…”
Get full text

Inhibition of Hematopoietic Protein Tyrosine Phosphatase Augments and Prolongs ERK1/2 and p38 Activation by Sergienko, Eduard, Xu, Jian, Liu, Wallace H, Dahl, Russell, Critton, David A, Su, Ying, Brown, Brock T, Chan, Xochella, Yang, Li, Bobkova, Ekaterina V, Vasile, Stefan, Yuan, Hongbin, Rascon, Justin, Colayco, Sharon, Sidique, Shyama, Cosford, Nicholas D. P, Chung, Thomas D. Y, Mustelin, Tomas, Page, Rebecca, Lombroso, Paul J, Tautz, Lutz

“…The hematopoietic protein tyrosine phosphatase (HePTP) is implicated in the development of blood cancers through its ability to negatively regulate the…”
Get full text

Discovery of Sulfonamidebenzamides as Selective Apoptotic CHOP Pathway Activators of the Unfolded Protein Response by Flaherty, Daniel P, Miller, Justin R, Garshott, Danielle M, Hedrick, Michael, Gosalia, Palak, Li, Yujie, Milewski, Monika, Sugarman, Eliot, Vasile, Stefan, Salaniwal, Sumeet, Su, Ying, Smith, Layton H, Chung, Thomas D. Y, Pinkerton, Anthony B, Aubé, Jeffrey, Callaghan, Michael U, Golden, Jennifer E, Fribley, Andrew M, Kaufman, Randal J

“…Cellular proteins that fail to fold properly result in inactive or disfunctional proteins that can have toxic functions. The unfolded protein response (UPR) is…”
Get full text

Imidazole-derived agonists for the neurotensin 1 receptor by Hershberger, Paul M, Hedrick, Michael P, Peddibhotla, Satyamaheshwar, Mangravita-Novo, Arianna, Gosalia, Palak, Li, Yujie, Gray, Wilson, Vicchiarelli, Michael, Smith, Layton H, Chung, Thomas D Y, Thomas, James B, Caron, Marc G, Pinkerton, Anthony B, Barak, Lawrence S, Roth, Gregory P

“…A scaffold-hop program seeking full agonists of the neurotensin-1 (NTR1) receptor identified the probe molecule ML301 (1) and associated analogs, including its…”
Get full text

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…”
Get full text

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…”
Get full text

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…”
Get more information

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,…”
Get more information

Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes by Schreiber, Stuart L., Kotz, Joanne D., Li, Min, Aubé, Jeffrey, Austin, Christopher P., Reed, John C., Rosen, Hugh, White, E. Lucile, Sklar, Larry A., Lindsley, Craig W., Alexander, Benjamin R., Bittker, Joshua A., Clemons, Paul A., de Souza, Andrea, Foley, Michael A., Palmer, Michelle, Shamji, Alykhan F., Wawer, Mathias J., McManus, Owen, Wu, Meng, Zou, Beiyan, Yu, Haibo, Golden, Jennifer E., Schoenen, Frank J., Simeonov, Anton, Jadhav, Ajit, Jackson, Michael R., Pinkerton, Anthony B., Chung, Thomas D.Y., Griffin, Patrick R., Cravatt, Benjamin F., Hodder, Peter S., Roush, William R., Roberts, Edward, Chung, Dong-Hoon, Jonsson, Colleen B., Noah, James W., Severson, William E., Ananthan, Subramaniam, Edwards, Bruce, Oprea, Tudor I., Conn, P. Jeffrey, Hopkins, Corey R., Wood, Michael R., Stauffer, Shaun R., Emmitte, Kyle A., Brady, Linda S., Driscoll, Jamie, Li, Ingrid Y., Loomis, Carson R., Margolis, Ronald N., Michelotti, Enrique, Perry, Mary E., Pillai, Ajay, Yao, Yong

“…Small-molecule probes can illuminate biological processes and aid in the assessment of emerging therapeutic targets by perturbing biological systems in a…”
Get full text