Search Results - "Lee, Tobie D."

Efficient gene disruption in diverse strains of Toxoplasma gondii using CRISPR/CAS9 by Shen, Bang, Brown, Kevin M, Lee, Tobie D, Sibley, L David

“…Toxoplasma gondii has become a model for studying the phylum Apicomplexa, in part due to the availability of excellent genetic tools. Although reverse genetic…”
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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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Characterization and tissue localization of zebrafish homologs of the human ABCB1 multidrug transporter by Robey, Robert W., Robinson, Andrea N., Ali-Rahmani, Fatima, Huff, Lyn M., Lusvarghi, Sabrina, Vahedi, Shahrooz, Hotz, Jordan M., Warner, Andrew C., Butcher, Donna, Matta, Jennifer, Edmondson, Elijah F., Lee, Tobie D., Roth, Jacob S., Lee, Olivia W., Shen, Min, Tanner, Kandice, Hall, Matthew D., Ambudkar, Suresh V., Gottesman, Michael M.

“…Capillary endothelial cells of the human blood–brain barrier (BBB) express high levels of P-glycoprotein (P-gp, encoded by ABCB1 ) and ABCG2 (encoded by ABCG2…”
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Say No to DMSO: Dimethylsulfoxide Inactivates Cisplatin, Carboplatin, and Other Platinum Complexes by HALL, Matthew D, TELMA, Katherine A, CHANG, Ki-Eun, LEE, Tobie D, MADIGAN, James P, LLOYD, John R, GOLDLUST, Ian S, HOESCHELE, James D, GOTTESMAN, Michael M

“…The platinum drugs cisplatin, carboplatin, and oxaliplatin are highly utilized in the clinic and as a consequence are extensively studied in the laboratory…”
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Pan-cancer proteogenomics expands the landscape of therapeutic targets by Savage, Sara R, Yi, Xinpei, Lei, Jonathan T, Wen, Bo, Zhao, Hongwei, Liao, Yuxing, Jaehnig, Eric J, Somes, Lauren K, Shafer, Paul W, Lee, Tobie D, Fu, Zile, Dou, Yongchao, Shi, Zhiao, Gao, Daming, Hoyos, Valentina, Gao, Qiang, Zhang, Bing

“…Fewer than 200 proteins are targeted by cancer drugs approved by the Food and Drug Administration (FDA). We integrate Clinical Proteomic Tumor Analysis…”
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Structural Characterization of Degrader-Induced Ternary Complexes Using Hydrogen–Deuterium Exchange Mass Spectrometry and Computational Modeling: Implications for Structure-Based Design by Eron, Scott J, Huang, Hongwei, Agafonov, Roman V, Fitzgerald, Mark E, Patel, Joe, Michael, Ryan E, Lee, Tobie D, Hart, Ashley A, Shaulsky, Jodi, Nasveschuk, Christopher G, Phillips, Andrew J, Fisher, Stewart L, Good, Andrew

“…The field of targeted protein degradation (TPD) has grown exponentially over the past decade with the goal of developing therapies that mark proteins for…”
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A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein by Lee, Tobie D, Lee, Olivia W, Brimacombe, Kyle R, Chen, Lu, Guha, Rajarshi, Lusvarghi, Sabrina, Tebase, Bethilehem G, Klumpp-Thomas, Carleen, Robey, Robert W, Ambudkar, Suresh V, Shen, Min, Gottesman, Michael M, Hall, Matthew D

“…The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs…”
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Functional analysis of rhomboid proteases during Toxoplasma invasion by Shen, Bang, Buguliskis, Jeffrey S, Lee, Tobie D, Sibley, L David

“…Host cell invasion by Toxoplasma gondii and other apicomplexan parasites requires transmembrane adhesins that mediate binding to receptors on the substrate and…”
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Discovery and Optimization of 2H‑1λ2‑Pyridin-2-one Inhibitors of Mutant Isocitrate Dehydrogenase 1 for the Treatment of Cancer by Rohde, Jason M, Karavadhi, Surendra, Pragani, Rajan, Liu, Li, Fang, Yuhong, Zhang, Weihe, McIver, Andrew, Zheng, Hongchao, Liu, Qingyang, Davis, Mindy I, Urban, Daniel J, Lee, Tobie D, Cheff, Dorian M, Hollingshead, Melinda, Henderson, Mark J, Martinez, Natalia J, Brimacombe, Kyle R, Yasgar, Adam, Zhao, Wei, Klumpp-Thomas, Carleen, Michael, Sam, Covey, Joseph, Moore, William J, Stott, Gordon M, Li, Zhuyin, Simeonov, Anton, Jadhav, Ajit, Frye, Stephen, Hall, Matthew D, Shen, Min, Wang, Xiaodong, Patnaik, Samarjit, Boxer, Matthew B

“…Neomorphic mutations in isocitrate dehydrogenase 1 (IDH1) are oncogenic for a number of malignancies, primarily low-grade gliomas and acute myeloid leukemia…”
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Pyrazole-Based Lactate Dehydrogenase Inhibitors with Optimized Cell Activity and Pharmacokinetic Properties by Rai, Ganesha, Urban, Daniel J, Mott, Bryan T, Hu, Xin, Yang, Shyh-Ming, Benavides, Gloria A, Johnson, Michelle S, Squadrito, Giuseppe L, Brimacombe, Kyle R, Lee, Tobie D, Cheff, Dorian M, Zhu, Hu, Henderson, Mark J, Pohida, Katherine, Sulikowski, Gary A, Dranow, David M, Kabir, Md, Shah, Pranav, Padilha, Elias, Tao, Dingyin, Fang, Yuhong, Christov, Plamen P, Kim, Kwangho, Jana, Somnath, Muttil, Pavan, Anderson, Tamara, Kunda, Nitesh K, Hathaway, Helen J, Kusewitt, Donna F, Oshima, Nobu, Cherukuri, Murali, Davies, Douglas R, Norenberg, Jeffrey P, Sklar, Larry A, Moore, William J, Dang, Chi V, Stott, Gordon M, Neckers, Leonard, Flint, Andrew J, Darley-Usmar, Victor M, Simeonov, Anton, Waterson, Alex G, Jadhav, Ajit, Hall, Matthew D, Maloney, David J

“…Lactate dehydrogenase (LDH) catalyzes the conversion of pyruvate to lactate, with concomitant oxidation of reduced nicotinamide adenine dinucleotide as the…”
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Discovery and optimization of piperazine-1-thiourea-based human phosphoglycerate dehydrogenase inhibitors by Rohde, Jason M., Brimacombe, Kyle R., Liu, Li, Pacold, Michael E., Yasgar, Adam, Cheff, Dorian M., Lee, Tobie D., Rai, Ganesha, Baljinnyam, Bolormaa, Li, Zhuyin, Simeonov, Anton, Hall, Matthew D., Shen, Min, Sabatini, David M., Boxer, Matthew B.

“…[Display omitted] Proliferating cells, including cancer cells, obtain serine both exogenously and via the metabolism of glucose. By catalyzing the first,…”
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Assessing inhibitors of mutant isocitrate dehydrogenase using a suite of pre-clinical discovery assays by Urban, Daniel J., Martinez, Natalia J., Davis, Mindy I., Brimacombe, Kyle R., Cheff, Dorian M., Lee, Tobie D., Henderson, Mark J., Titus, Steven A., Pragani, Rajan, Rohde, Jason M., Liu, Li, Fang, Yuhong, Karavadhi, Surendra, Shah, Pranav, Lee, Olivia W., Wang, Amy, McIver, Andrew, Zheng, Hongchao, Wang, Xiaodong, Xu, Xin, Jadhav, Ajit, Simeonov, Anton, Shen, Min, Boxer, Matthew B., Hall, Matthew D.

“…Isocitrate dehydrogenase 1 and 2 (IDH1 and IDH2) are key metabolic enzymes that are mutated in a variety of cancers to confer a gain-of-function activity…”
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Discovery and Optimization of 2 H -1λ 2 -Pyridin-2-one Inhibitors of Mutant Isocitrate Dehydrogenase 1 for the Treatment of Cancer by Rohde, Jason M, Karavadhi, Surendra, Pragani, Rajan, Liu, Li, Fang, Yuhong, Zhang, Weihe, McIver, Andrew, Zheng, Hongchao, Liu, Qingyang, Davis, Mindy I, Urban, Daniel J, Lee, Tobie D, Cheff, Dorian M, Hollingshead, Melinda, Henderson, Mark J, Martinez, Natalia J, Brimacombe, Kyle R, Yasgar, Adam, Zhao, Wei, Klumpp-Thomas, Carleen, Michael, Sam, Covey, Joseph, Moore, William J, Stott, Gordon M, Li, Zhuyin, Simeonov, Anton, Jadhav, Ajit, Frye, Stephen, Hall, Matthew D, Shen, Min, Wang, Xiaodong, Patnaik, Samarjit, Boxer, Matthew B

“…Neomorphic mutations in isocitrate dehydrogenase 1 (IDH1) are oncogenic for a number of malignancies, primarily low-grade gliomas and acute myeloid leukemia…”
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Optimization of ether and aniline based inhibitors of lactate dehydrogenase by Christov, Plamen P., Kim, Kwangho, Jana, Somnath, Romaine, Ian M., Rai, Ganesha, Mott, Bryan T., Allweil, Alexander A., Lamers, Alexander, Brimacombe, Kyle R., Urban, Daniel J., Lee, Tobie D., Hu, Xin, Lukacs, Christine M., Davies, Douglas R., Jadhav, Ajit, Hall, Matthew D., Green, Neal, Moore, William J., Stott, Gordon M., Flint, Andrew J., Maloney, David J., Sulikowski, Gary A., Waterson, Alex G.

“…[Display omitted] Lactate dehydrogenase (LDH) is a critical enzyme in the glycolytic metabolism pathway that is used by many tumor cells. Inhibitors of LDH may…”
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Conditional lethality profiling reveals anticancer mechanisms of action and drug-nutrient interactions by Flickinger, Kyle M, Wilson, Kelli M, Rossiter, Nicholas J, Hunger, Andrea L, Vishwasrao, Paresh V, Lee, Tobie D, Mellado Fritz, Carlos A, Richards, Rebecca M, Hall, Matthew D, Cantor, Jason R

“…Chemical screens across hundreds of cell lines have shown that the drug sensitivities of human cancers can vary by genotype or lineage. However, most drug…”
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SULT1A1-dependent sulfonation of alkylators is a lineage-dependent vulnerability of liver cancers by Shi, Lei, Shen, William, Davis, Mindy I, Kong, Ke, Vu, Phuong, Saha, Supriya K, Adil, Ramzi, Kreuzer, Johannes, Egan, Regina, Lee, Tobie D, Greninger, Patricia, Shrimp, Jonathan H, Zhao, Wei, Wei, Ting-Yu, Zhou, Mi, Eccleston, Jason, Sussman, Jonathan, Manocha, Ujjawal, Weerasekara, Vajira, Kondo, Hiroshi, Vijay, Vindhya, Wu, Meng-Ju, Kearney, Sara E, Ho, Jeffrey, McClanaghan, Joseph, Murchie, Ellen, Crowther, Giovanna S, Patnaik, Samarjit, Boxer, Matthew B, Shen, Min, Ting, David T, Kim, William Y, Stanger, Ben Z, Deshpande, Vikram, Ferrone, Cristina R, Benes, Cyril H, Haas, Wilhelm, Hall, Matthew D, Bardeesy, Nabeel

“…Adult liver malignancies, including intrahepatic cholangiocarcinoma and hepatocellular carcinoma, are the second leading cause of cancer-related deaths…”
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Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening by Lee, Olivia W, Austin, Shelley, Gamma, Madison, Cheff, Dorian M, Lee, Tobie D, Wilson, Kelli M, Johnson, Joseph, Travers, Jameson, Braisted, John C, Guha, Rajarshi, Klumpp-Thomas, Carleen, Shen, Min, Hall, Matthew D

“…Cell-based phenotypic screening is a commonly used approach to discover biological pathways, novel drug targets, chemical probes, and high-quality hit-to-lead…”
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Keeping It Clean: The Cell Culture Quality Control Experience at the National Center for Advancing Translational Sciences by Roth, Jacob S, Lee, Tobie D, Cheff, Dorian M, Gosztyla, Maya L, Asawa, Rosita R, Danchik, Carina, Michael, Sam, Simeonov, Anton, Klumpp-Thomas, Carleen, Wilson, Kelli M, Hall, Matthew D

“…Quality control monitoring of cell lines utilized in biomedical research is of utmost importance and is critical for the reproducibility of data. Two key…”
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Dynamic Imaging of LDH Inhibition in Tumors Reveals Rapid In Vivo Metabolic Rewiring and Vulnerability to Combination Therapy by Oshima, Nobu, Ishida, Ryo, Kishimoto, Shun, Beebe, Kristin, Brender, Jeffrey R., Yamamoto, Kazutoshi, Urban, Daniel, Rai, Ganesha, Johnson, Michelle S., Benavides, Gloria, Squadrito, Giuseppe L., Crooks, Dan, Jackson, Joseph, Joshi, Abhinav, Mott, Bryan T., Shrimp, Jonathan H., Moses, Michael A., Lee, Min-Jung, Yuno, Akira, Lee, Tobie D., Hu, Xin, Anderson, Tamara, Kusewitt, Donna, Hathaway, Helen H., Jadhav, Ajit, Picard, Didier, Trepel, Jane B., Mitchell, James B., Stott, Gordon M., Moore, William, Simeonov, Anton, Sklar, Larry A., Norenberg, Jeffrey P., Linehan, W. Marston, Maloney, David J., Dang, Chi V., Waterson, Alex G., Hall, Matthew, Darley-Usmar, Victor M., Krishna, Murali C., Neckers, Leonard M.

“…The reliance of many cancers on aerobic glycolysis has stimulated efforts to develop lactate dehydrogenase (LDH) inhibitors. However, despite significant…”
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Abstract LB-066: A high-throughput screen of an annotated small molecule library identifies substrates of P-glycoprotein by Lee, Tobie D., Lee, Olivia W., Brimacombe, Kyle R., Shen, Min, Chen, Lu, Guha, Rajarshi, Tebase, Bethelihem, Robey, Robert W., Ambudkar, Suresh V., Gottesman, Michael M., Hall, Matthew D.

“…Abstract A major difficulty in treating cancer is the development of cellular resistance to chemotherapeutics, a phenomenon known as multidrug resistance…”
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