Search Results - "Ma, Sylvia"

Design and Discovery of N‑(2-Methyl-5′-morpholino-6′-((tetrahydro‑2H‑pyran-4-yl)oxy)-[3,3′-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers by Nishiguchi, Gisele A, Rico, Alice, Tanner, Huw, Aversa, Robert J, Taft, Benjamin R, Subramanian, Sharadha, Setti, Lina, Burger, Matthew T, Wan, Lifeng, Tamez, Victoriano, Smith, Aaron, Lou, Yan, Barsanti, Paul A, Appleton, Brent A, Mamo, Mulugeta, Tandeske, Laura, Dix, Ina, Tellew, John E, Huang, Shenlin, Mathews Griner, Lesley A, Cooke, Vesselina G, Van Abbema, Anne, Merritt, Hanne, Ma, Sylvia, Gampa, Kalyani, Feng, Fei, Yuan, Jing, Wang, Yingyun, Haling, Jacob R, Vaziri, Sepideh, Hekmat-Nejad, Mohammad, Jansen, Johanna M, Polyakov, Valery, Zang, Richard, Sethuraman, Vijay, Amiri, Payman, Singh, Mallika, Lees, Emma, Shao, Wenlin, Stuart, Darrin D, Dillon, Michael P, Ramurthy, Savithri

“…RAS oncogenes have been implicated in >30% of human cancers, all representing high unmet medical need. The exquisite dependency on CRAF kinase in KRAS mutant…”
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Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor by Karpov, Alexei S, Amiri, Payman, Bellamacina, Cornelia, Bellance, Marie-Helene, Breitenstein, Werner, Daniel, Dylan, Denay, Regis, Fabbro, Doriano, Fernandez, Cesar, Galuba, Inga, Guerro-Lagasse, Stephanie, Gutmann, Sascha, Hinh, Linda, Jahnke, Wolfgang, Klopp, Julia, Lai, Albert, Lindvall, Mika K, Ma, Sylvia, Möbitz, Henrik, Pecchi, Sabina, Rummel, Gabriele, Shoemaker, Kevin, Trappe, Joerg, Voliva, Charles, Cowan-Jacob, Sandra W, Marzinzik, Andreas L

“…The discovery of inhibitors targeting novel allosteric kinase sites is very challenging. Such compounds, however, once identified could offer exquisite levels…”
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Inhibition of prenylated KRAS in a lipid environment by Jansen, Johanna M, Wartchow, Charles, Jahnke, Wolfgang, Fong, Susan, Tsang, Tiffany, Pfister, Keith, Zavorotinskaya, Tatiana, Bussiere, Dirksen, Cheng, Jan Marie, Crawford, Kenneth, Dai, Yumin, Dove, Jeffrey, Fang, Eric, Feng, Yun, Florent, Jean-Michel, Fuller, John, Gossert, Alvar D, Hekmat-Nejad, Mohammad, Henry, Chrystèle, Klopp, Julia, Lenahan, William P, Lingel, Andreas, Ma, Sylvia, Meyer, Arndt, Mishina, Yuji, Narberes, Jamie, Pardee, Gwynn, Ramurthy, Savithri, Rieffel, Sebastien, Stuart, Darrin, Subramanian, Sharadha, Tandeske, Laura, Widger, Stephania, Widmer, Armin, Winterhalter, Aurelie, Zaror, Isabel, Hardy, Stephen

“…RAS mutations lead to a constitutively active oncogenic protein that signals through multiple effector pathways. In this chemical biology study, we describe a…”
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Selective Glycogen Synthase Kinase 3 Inhibitors Potentiate Insulin Activation of Glucose Transport and Utilization In Vitro and In Vivo by RING, David B, JOHNSON, Kirk W, WAGMAN, Allan S, HAMMOND, Mary-Ellen Wernette, HARRISON, Stephen D, HENRIKSEN, Erik J, NUSS, John M, GOFF, Dane, KINNICK, Tyson R, MA, Sylvia T, REEDER, John W, SAMUELS, Isa, SLABIAK, Trina

“…Selective Glycogen Synthase Kinase 3 Inhibitors Potentiate Insulin Activation of Glucose Transport and Utilization In Vitro and In Vivo David B. Ring 1 , Kirk…”
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CHIR-124, a Novel Potent Inhibitor of Chk1, Potentiates the Cytotoxicity of Topoisomerase I Poisons In vitro and In vivo by TSE, Archie N, RENDAHL, Katherine G, HIBNER, Barbara, GESNER, Thomas G, SCHWARTZ, Gary K, SHEIKH, Tahir, CHEEMA, Haider, AARDALEN, Kim, EMBRY, Millicent, MA, Sylvia, MOLER, Edward J, ZHI JIE NI, LOPES DE MENEZES, Daniel E

“…Purpose: Chk1 kinase is a critical regulator of both S and G 2 -M phase cell cycle checkpoints in response to DNA damage. This study aimed to evaluate the…”
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Effect of sodium stearoyl-2-lactylate, carboxymethyl cellulose and guar-xanthan gums on muffins enriched with soybean milk powder and amaranth flour by Pérez-Carrillo, Esther, González-Fernández, Ana G., Morales-Garza, Sylvia M.A., Treviño-Garza, Elvira E., Guajardo-Flores, Sara, Serna-Saldívar, Sergio O., Sánchez-Hernández, Diana

“…Soybean milk powder (SMP) and amaranth flour (AF) can improve the nutritional profile of bakery products. Nonetheless, these ingredients can impart undesirable…”
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In Vitro and In Vivo Properties of CUO246, a Novel Bacterial DNA Gyrase/Topoisomerase IV Inhibitor by Blais, Johanne, Dean, Charles R, Lapointe, Guillaume, Leeds, Jennifer A, Ma, Sylvia, Morris, Laura, Moser, Heinz E, Osborne, Colin S, Prosen, Katherine R, Richie, Daryl, Skepper, Colin, Thompson, Katherine, Vo, Jason, Yue, Qin, Rivkin, Alexey

“…CUO246, a novel DNA gyrase/topoisomerase IV inhibitor, is active against a broad range of Gram-positive, fastidious Gram-negative, and atypical bacterial…”
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Two Distinct Mechanisms of Inhibition of LpxA Acyltransferase Essential for Lipopolysaccharide Biosynthesis by Han, Wooseok, Ma, Xiaolei, Balibar, Carl J, Baxter Rath, Christopher M, Benton, Bret, Bermingham, Alun, Casey, Fergal, Chie-Leon, Barbara, Cho, Min-Kyu, Frank, Andreas O, Frommlet, Alexandra, Ho, Chi-Min, Lee, Patrick S, Li, Min, Lingel, Andreas, Ma, Sylvia, Merritt, Hanne, Ornelas, Elizabeth, De Pascale, Gianfranco, Prathapam, Ramadevi, Prosen, Katherine R, Rasper, Dita, Ruzin, Alexey, Sawyer, William S, Shaul, Jacob, Shen, Xiaoyu, Shia, Steven, Steffek, Micah, Subramanian, Sharadha, Vo, Jason, Wang, Feng, Wartchow, Charles, Uehara, Tsuyoshi

“…The lipopolysaccharide biosynthesis pathway is considered an attractive drug target against the rising threat of multi-drug-resistant Gram-negative bacteria…”
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Rationally Designed PI3Kα Mutants to Mimic ATR and Their Use to Understand Binding Specificity of ATR Inhibitors by Lu, Yipin, Knapp, Mark, Crawford, Kenneth, Warne, Robert, Elling, Robert, Yan, Kelly, Doyle, Michael, Pardee, Gwynn, Zhang, Li, Ma, Sylvia, Mamo, Mulugeta, Ornelas, Elizabeth, Pan, Yue, Bussiere, Dirksen, Jansen, Johanna, Zaror, Isabel, Lai, Albert, Barsanti, Paul, Sim, Janet

“…ATR, a protein kinase in the PIKK family, plays a critical role in the cell DNA-damage response and is an attractive anticancer drug target. Several potent and…”
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Topoisomerase Inhibitors Addressing Fluoroquinolone Resistance in Gram-Negative Bacteria by Skepper, Colin K, Armstrong, Duncan, Balibar, Carl J, Bauer, Daniel, Bellamacina, Cornelia, Benton, Bret M, Bussiere, Dirksen, De Pascale, Gianfranco, De Vicente, Javier, Dean, Charles R, Dhumale, Bhavesh, Fisher, L. Mark, Fuller, John, Fulsunder, Mangesh, Holder, Lauren M, Hu, Cheng, Kantariya, Bhavin, Lapointe, Guillaume, Leeds, Jennifer A, Li, Xiaolin, Lu, Peichao, Lvov, Anatoli, Ma, Sylvia, Madhavan, Shravanthi, Malekar, Swapnil, McKenney, David, Mergo, Wosenu, Metzger, Louis, Moser, Heinz E, Mutnick, Daniel, Noeske, Jonas, Osborne, Colin, Patel, Ashish, Patel, Darshit, Patel, Tushar, Prajapati, Krunal, Prosen, Katherine R, Reck, Folkert, Richie, Daryl L, Rico, Alice, Sanderson, Mark R, Satasia, Shailesh, Sawyer, William S, Selvarajah, Jogitha, Shah, Nirav, Shanghavi, Kartik, Shu, Wei, Thompson, Katherine V, Traebert, Martin, Vala, Anand, Vala, Lakhan, Veselkov, Dennis A, Vo, Jason, Wang, Michael, Widya, Marcella, Williams, Sarah L, Xu, Yongjin, Yue, Qin, Zang, Richard, Zhou, Bo, Rivkin, Alexey

“…Since their discovery over 5 decades ago, quinolone antibiotics have found enormous success as broad spectrum agents that exert their activity through dual…”
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Discovery and Optimization of DNA Gyrase and Topoisomerase IV Inhibitors with Potent Activity against Fluoroquinolone-Resistant Gram-Positive Bacteria by Lapointe, Guillaume, Skepper, Colin K, Holder, Lauren M, Armstrong, Duncan, Bellamacina, Cornelia, Blais, Johanne, Bussiere, Dirksen, Bian, Jianwei, Cepura, Cody, Chan, Helen, Dean, Charles R, De Pascale, Gianfranco, Dhumale, Bhavesh, Fisher, L. Mark, Fulsunder, Mangesh, Kantariya, Bhavin, Kim, Julie, King, Sean, Kossy, Lauren, Kulkarni, Upendra, Lakshman, Jay, Leeds, Jennifer A, Ling, Xiaolan, Lvov, Anatoli, Ma, Sylvia, Malekar, Swapnil, McKenney, David, Mergo, Wosenu, Metzger, Louis, Mhaske, Keshav, Moser, Heinz E, Mostafavi, Mina, Namballa, Sunil, Noeske, Jonas, Osborne, Colin, Patel, Ashish, Patel, Darshit, Patel, Tushar, Piechon, Philippe, Polyakov, Valery, Prajapati, Krunal, Prosen, Katherine R, Reck, Folkert, Richie, Daryl L, Sanderson, Mark R, Satasia, Shailesh, Savani, Bhautik, Selvarajah, Jogitha, Sethuraman, Vijay, Shu, Wei, Tashiro, Kyuto, Thompson, Katherine V, Vaarla, Krishniah, Vala, Lakhan, Veselkov, Dennis A, Vo, Jason, Vora, Bhavesh, Wagner, Trixie, Wedel, Laura, Williams, Sarah L, Yendluri, Satya, Yue, Qin, Yifru, Aregahegn, Zhang, Yong, Rivkin, Alexey

“…Herein, we describe the discovery and optimization of a novel series that inhibits bacterial DNA gyrase and topoisomerase IV via binding to, and stabilization…”
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Design and Synthesis of Orally Bioavailable Benzimidazoles as Raf Kinase Inhibitors by Ramurthy, Savithri, Subramanian, Sharadha, Aikawa, Mina, Amiri, Payman, Costales, Abran, Dove, Jeff, Fong, Susan, Jansen, Johanna M, Levine, Barry, Ma, Sylvia, McBride, Christopher M, Michaelian, Jonah, Pick, Teresa, Poon, Daniel J, Girish, Sandhya, Shafer, Cynthia M, Stuart, Darrin, Sung, Leonard, Renhowe, Paul A

“…A series of arylaminobenzimidazoles was designed and synthesized as Raf kinase inhibitors. Exploration of the structure−activity relationship resulted in…”
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Design and synthesis of 5,6-fused heterocyclic amides as Raf kinase inhibitors by Ramurthy, Savithri, Aikawa, Mina, Amiri, Payman, Costales, Abran, Hashash, Ahmad, Jansen, Johanna M., Lin, Song, Ma, Sylvia, Renhowe, Paul A., Shafer, Cynthia M., Subramanian, Sharadha, Sung, Leonard, Verhagen, Joelle

“…Two scaffolds based on 5,6-fused heterocyclic backbones were designed and synthesized as Raf kinase inhibitors. The scaffolds were assessed for in vitro…”
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Report of an EU–US Symposium on Understanding Nutrition-Related Consumer Behavior: Strategies to Promote a Lifetime of Healthy Food Choices by Friedl, Karl E., PhD, Rowe, Sylvia, MA, Bellows, Laura L., PhD, MPH, RD, Johnson, Susan L., PhD, Hetherington, Marion M., DPhil, de Froidmont-Görtz, Isabelle, MSc, Lammens, Veerle, MSc, Hubbard, Van S., MD, PhD

“…Abstract This report summarizes an EU–US Task Force on Biotechnology Research symposium on healthy food choices and nutrition-related purchasing behaviors…”
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4-(Aminoalkylamino)-3-benzimidazole-quinolinones as potent CHK-1 inhibitors by Ni, Zhi-Jie, Barsanti, Paul, Brammeier, Nathan, Diebes, Anthony, Poon, Daniel J., Ng, Simon, Pecchi, Sabina, Pfister, Keith, Renhowe, Paul A., Ramurthy, Savithri, Wagman, Allan S., Bussiere, Dirksen E., Le, Vincent, Zhou, Yasheen, Jansen, Johanna M., Ma, Sylvia, Gesner, Thomas G.

“…CHK-1 is one of the key enzymes regulating checkpoints in cellular growth cycles. Novel 4-(amino-alkylamino)-3-benzimidazole-quinolinones were prepared and…”
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Design and structure–activity relationship of 3-benzimidazol-2-yl-1H-indazoles as inhibitors of receptor tyrosine kinases by McBride, Christopher M., Renhowe, Paul A., Heise, Carla, Jansen, Johanna M., Lapointe, Gena, Ma, Sylvia, Piñeda, Ramon, Vora, Jayesh, Wiesmann, Marion, Shafer, Cynthia M.

“…The synthesis and SAR of 3-benzimidazol-2-yl-1H-indazole analogs developed as inhibitors of receptor tyrosine kinases (RTK) is reported…”
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Discovery of 2-pyrimidyl-5-amidothiophenes as potent inhibitors for AKT: Synthesis and SAR studies by Lin, Xiaodong, Murray, Jeremy M., Rico, Alice C., Wang, Michael X., Chu, Daniel T., Zhou, Yasheen, Rosario, Merci Del, Kaufman, Susan, Ma, Sylvia, Fang, Eric, Crawford, Kenneth, Jefferson, A.B.

“…A series of 2-pyrimidyl-5-amidothiophenes has been synthesized and evaluated for AKT inhibition. Compound 2aa is a potent AKT inhibitor and showed cellular…”
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Distribution and physical properties of BCA200, a Mr 200,000 glycoprotein selectively associated with human breast cancer by RING, D. B, KASSEL, J. A, HSIEH-MA, S. T, BJORN, M. J, TRINGALE, F, EATON, A. M, REID, S. A, FRANKEL, A. E, NADJI, M

“…Of 122 mouse monoclonal antibodies selective for human breast cancer, 13 immunoprecipitated an acidic glycoprotein from SK-Br-3 and ZR-75-30 human breast…”
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3-Benzimidazol-2-yl-1H-indazoles as potent c-ABL inhibitors by MCBRIDE, Christopher M, RENHOWE, Paul A, GESNER, Thomas G, JANSEN, Johanna M, JULIE LIN, MA, Sylvia, ZHOU, Yasheen, SHAFER, Cynthia M

“…The 3-benzimidazol-2-yl-1H-indazole scaffold was developed as an alternate scaffold for our receptor tyrosine kinase (RTK) inhibitor program. In exploring the…”
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Host lung gene expression patterns predict infectious etiology in a mouse model of pneumonia by Evans, Scott E, Tuvim, Michael J, Zhang, Jiexin, Larson, Derek T, García, Cesar D, Martinez-Pro, Sylvia, Coombes, Kevin R, Dickey, Burton F

“…Lower respiratory tract infections continue to exact unacceptable worldwide mortality, often because the infecting pathogen cannot be identified. The…”
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