Search Results - "Ramurthy, Savithri"

Discovery of Potent and Selective RSK Inhibitors as Biological Probes by Jain, Rama, Mathur, Michelle, Lan, Jiong, Costales, Abran, Atallah, Gordana, Ramurthy, Savithri, Subramanian, Sharadha, Setti, Lina, Feucht, Paul, Warne, Bob, Doyle, Laura, Basham, Stephen, Jefferson, Anne B., Lindvall, Mika, Appleton, Brent A., Shafer, Cynthia M.

“…While the p90 ribosomal S6 kinase (RSK) family has been implicated in multiple tumor cell functions, the full understanding of this kinase family has been…”
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Antitumor Properties of RAF709, a Highly Selective and Potent Inhibitor of RAF Kinase Dimers, in Tumors Driven by Mutant RAS or BRAF by Shao, Wenlin, Mishina, Yuji M, Feng, Yun, Caponigro, Giordano, Cooke, Vesselina G, Rivera, Stacy, Wang, Yingyun, Shen, Fang, Korn, Joshua M, Mathews Griner, Lesley A, Nishiguchi, Gisele, Rico, Alice, Tellew, John, Haling, Jacob R, Aversa, Robert, Polyakov, Valery, Zang, Richard, Hekmat-Nejad, Mohammad, Amiri, Payman, Singh, Mallika, Keen, Nicholas, Dillon, Michael P, Lees, Emma, Ramurthy, Savithri, Sellers, William R, Stuart, Darrin D

“…Resistance to the RAF inhibitor vemurafenib arises commonly in melanomas driven by the activated BRAF oncogene. Here, we report antitumor properties of RAF709,…”
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Synthesis, Binding Mode, and Antihyperglycemic Activity of Potent and Selective (5-Imidazol-2-yl-4-phenylpyrimidin-2-yl)[2-(2-pyridylamino)ethyl]amine Inhibitors of Glycogen Synthase Kinase 3 by Wagman, Allan S, Boyce, Rustum S, Brown, Sean P, Fang, Eric, Goff, Dane, Jansen, Johanna M, Le, Vincent P, Levine, Barry H, Ng, Simon C, Ni, Zhi-Jie, Nuss, John M, Pfister, Keith B, Ramurthy, Savithri, Renhowe, Paul A, Ring, David B, Shu, Wei, Subramanian, Sharadha, Zhou, Xiaohui A, Shafer, Cynthia M, Harrison, Stephen D, Johnson, Kirk W, Bussiere, Dirksen E

“…In an effort to identify new antidiabetic agents, we have discovered a novel family of…”
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Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma by Williams, Teresa E, Subramanian, Sharadha, Verhagen, Joelle, McBride, Christopher M, Costales, Abran, Sung, Leonard, Antonios-McCrea, William, McKenna, Maureen, Louie, Alicia K, Ramurthy, Savithri, Levine, Barry, Shafer, Cynthia M, Machajewski, Timothy, Renhowe, Paul A, Appleton, Brent A, Amiri, Payman, Chou, James, Stuart, Darrin, Aardalen, Kimberly, Poon, Daniel

“…Abrogation of errant signaling along the MAPK pathway through the inhibition of B-RAF kinase is a validated approach for the treatment of pathway-dependent…”
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Discovery of HC-7366: An Orally Bioavailable and Efficacious GCN2 Kinase Activator by Thomson, Christopher G., Aicher, Thomas D., Cheng, Weiwei, Du, Hongwen, Dudgeon, Crissy, Li, An-Hu, Li, Baozhong, Lightcap, Eric, Luo, Diheng, Mulvihill, Mark, Pan, Pengwei, Rahemtulla, Benjamin F., Rigby, Alan C., Sherborne, Bradley, Sood, Sanjeev, Surguladze, David, Talbot, Eric P. A., Tameire, Feven, Taylor, Simon, Wang, Yi, Wojnarowicz, Paulina, Xiao, Fenfen, Ramurthy, Savithri

“…A series of activators of GCN2 (general control nonderepressible 2) kinase have been developed, leading to HC-7366, which has entered the clinic as an…”
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Asymmetric Total Synthesis of an Important 3-(Hydroxymethyl)carbacephalosporin by Stocksdale, Mark G, Ramurthy, Savithri, Miller, Marvin J

“…Carbacephalosporins have gained much attention as important antibacterial agents. Recently, 3-(hydroxymethyl)carbacephalosporins have been linked to quinolones…”
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Design and Discovery of N‑(3-(2-(2-Hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide, a Selective, Efficacious, and Well-Tolerated RAF Inhibitor Targeting RAS Mutant Cancers: The Path to the Clinic by Ramurthy, Savithri, Taft, Benjamin R, Aversa, Robert J, Barsanti, Paul A, Burger, Matthew T, Lou, Yan, Nishiguchi, Gisele A, Rico, Alice, Setti, Lina, Smith, Aaron, Subramanian, Sharadha, Tamez, Victoriano, Tanner, Huw, Wan, Lifeng, Hu, Cheng, Appleton, Brent A, Mamo, Mulugeta, Tandeske, Laura, Tellew, John E, Huang, Shenlin, Yue, Qin, Chaudhary, Apurva, Tian, Hung, Iyer, Raman, Hassan, A. Quamrul, Mathews Griner, Lesley A, La Bonte, Laura R, Cooke, Vesselina G, Van Abbema, Anne, Merritt, Hanne, Gampa, Kalyani, Feng, Fei, Yuan, Jing, Mishina, Yuji, Wang, Yingyun, Haling, Jacob R, Vaziri, Sepideh, Hekmat-Nejad, Mohammad, Polyakov, Valery, Zang, Richard, Sethuraman, Vijay, Amiri, Payman, Singh, Mallika, Sellers, William R, Lees, Emma, Shao, Wenlin, Dillon, Michael P, Stuart, Darrin D

“…Direct pharmacological inhibition of RAS has remained elusive, and efforts to target CRAF have been challenging due to the complex nature of RAF signaling,…”
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Discovery and optimization of novel pyridines as highly potent and selective glycogen synthase kinase 3 inhibitors by Ramurthy, Savithri, Pfister, Keith B., Boyce, Rustum S., Brown, Sean P., Costales, Abran Q., Desai, Manoj C., Fang, Eric, Levine, Barry H., Ng, Simon C., Nuss, John M., Ring, David B., Shafer, Cynthia M., Shu, Wei, Subramanian, Sharadha, Wagman, Allan S., Wang, Haixia, Bussiere, Dirksen E.

“…[Display omitted] Glycogen synthase kinase-3 plays an essential role in multiple biochemical pathways in the cell, particularly in regards to energy…”
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Design and synthesis of potent RSK inhibitors by Jain, Rama, Mathur, Michelle, Lan, Jiong, Costales, Abran, Atallah, Gordana, Ramurthy, Savithri, Subramanian, Sharadha, Setti, Lina, Feucht, Paul, Warne, Bob, Doyle, Laura, Basham, Stephen, Jefferson, Anne B., Appleton, Brent A., Lindvall, Mika, Shafer, Cynthia M.

“…[Display omitted] •Picomolar pan-RSK inhibitors developed.•Using modeling, phenol isosteres were evaluated in order to identify a tool compound for in vivo…”
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Structural and Biological Basis of Small Molecule Inhibition of Escherichia coli LpxD Acyltransferase Essential for Lipopolysaccharide Biosynthesis by Ma, Xiaolei, Prathapam, Ramadevi, Wartchow, Charles, Chie-Leon, Barbara, Ho, Chi-Min, De Vicente, Javier, Han, Wooseok, Li, Min, Lu, Yipin, Ramurthy, Savithri, Shia, Steven, Steffek, Micah, Uehara, Tsuyoshi

“…LpxD, acyl-ACP-dependent -acyltransferase, is the third enzyme of lipid A biosynthesis in Gram-negative bacteria. A recent probe-based screen identified…”
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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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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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Abstract DDT01-04: Pharmacological profile and anti-tumor properties of LXH254, a highly selective RAF kinase inhibitor by Stuart, Darrin D., Shao, Wenlin, Mishina, Yuji, Feng, Yun, Caponigro, Giordano, Cooke, Vesselina G., Rivera, Stacey, Shen, Fang, Korn, Joshua, Griner, Lesley A. Mathews, Nishiguchi, Giselle, Taft, Benjamin, Wan, Lifeng, Subramanian, Sharadha, Lou, Yan, Setti, Lina, Burger, Matthew, Tamez, Victor, Rico, Alice, Aversa, Robert, Tellew, John, Haling, Jacob R., Polyakov, Valery, Lambert, Amy, Zang, Richard, Abbema, Ann Van, Hekmat-Nejad, Mohamad, Amiri, Payman, Singh, Mallika, Keen, Nicholas, Dillon, Michael P., Lees, Emma, Sellers, William R., Ramurthy, Savithri

“…Abstract The mitogen-activated protein kinase (MAPK) signaling pathway is frequently activated in human cancers due to genetic alterations that can occur at…”
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Abstract 330: Development of a highly selective BCRAF kinase inhibitor that exhibits antitumor activities in RAS and BRAF mutant tumors with minimal paradoxical activation by Shao, Wenlin, Mishina, Yuji, Feng, Yun, Caponigro, Giordano, Ramurthy, Savithri, Cooke, Vesselina, Griner, Lesley, Nishiguchi, Gisele, Rico, Alice, Taft, Ben, Burger, Matthew, Tanner, Huw, Polyakov, Valery, Appleton, Brent, Tellew, John, Zang, Richard, Hekmat-Nejad, Mohammad, Amiri, Payman, Singh, Mallika, Stuart, Darrin

“…The mitogen-activated protein kinase (MAPK) signaling pathway is frequently activated in human cancers due to genetic alterations that can occur at multiple…”
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Abstract 330: Development of a highly selective B/CRAF kinase inhibitor that exhibits antitumor activities in RAS and BRAF mutant tumors with minimal paradoxical activation by Shao, Wenlin, Mishina, Yuji, Feng, Yun, Caponigro, Giordano, Ramurthy, Savithri, Cooke, Vesselina, Griner, Lesley, Nishiguchi, Gisele, Rico, Alice, Taft, Ben, Burger, Matthew, Tanner, Huw, Polyakov, Valery, Appleton, Brent, Tellew, John, Zang, Richard, Hekmat-Nejad, Mohammad, Amiri, Payman, Singh, Mallika, Stuart, Darrin

“…Abstract The mitogen-activated protein kinase (MAPK) signaling pathway is frequently activated in human cancers due to genetic alterations that can occur at…”
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Abstract A30: Activation of GCN2 by HC-7366 results in significant anti-tumor efficacy as monotherapy and in combination with Venetoclax in AML models by Tameire, Feven, Wojnarowicz, Paulina M., Fujisawa, Sho, Huang, Sharon, Reilly, Owen, Dudgeon, Crissy, Collette, Nicholas, Drees, Jeremy, Bieging-Rolett, Kathryn, Kangas, Takashi O, Zhang, Weiyu, Fumagalli, Maria, Dewji, Iman, Li, Yunfang, Chan, Anissa SH, Qiu, Xiaohong, Harrison, Ben, LaCayo, Ashley, Staschke, Kirk A., Rigby, Alan C., Ramurthy, Savithri, Lightcap, Eric S., Surguladze, David, Bose, Nandita

“…Abstract The integrated stress response (ISR) is an adaptive signaling pathway that cells utilize to respond to a wide range of extrinsic and intrinsic…”
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Abstract 6231: Activation of GCN2 by HC-7366 results in significant antitumor efficacy as monotherapy and in combination with multiple standard of care agents in various solid cancer models by Tameire, Feven, Wojnarowicz, Paulina, Dudgeon, Crissy, Fujisawa, Sho, Huang, Sharon, Reilly, Owen B., Collette, Nicholas, Drees, Jeremy, Bieging-Rolett, Kathryn, Kangas, Takashi O., Zhang, Weiyu, Fumagalli, Maria, Dewji, Iman, Li, Yunfang, Chan, Anissa SH, Qiu, Xiaohong, Harrison, Ben, LaCayo, Ashley, Cordova, Ricardo A., Staschke, Kirk A., Rigby, Alan C., Ramurthy, Savithri, Lightcap, Eric S., Surguladze, David, Bose, Nandita

“…Abstract The integrated stress response (ISR) is an adaptive signaling pathway that cells utilize to respond to a wide range of extrinsic and intrinsic…”
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Peptidomimetics of the immunoglobulin supergene family--a review by Nakanishi, H, Ramurthy, S, Raktabutr, A, Shen, R, Kahn, M

“…An important goal of structural biochemistry is the reduction of complex molecules to small functional units that are amenable to high-resolution structural…”
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2-Amino-7-substituted benzoxazole analogs as potent RSK2 inhibitors by Costales, Abran, Mathur, Michelle, Ramurthy, Savithri, Lan, Jiong, Subramanian, Sharadha, Jain, Rama, Atallah, Gordana, Setti, Lina, Lindvall, Mika, Appleton, Brent A., Ornelas, Elizabeth, Feucht, Paul, Warne, Bob, Doyle, Laura, Basham, Stephen E., Aronchik, Ida, Jefferson, Anne B., Shafer, Cynthia M.

“…2-Amino-7-substituted benzoxazole analogs were identified by HTS as inhibitors of RSK2. Molecular modeling and medicinal chemistry techniques were employed to…”
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Design and synthesis of 6,6-fused heterocyclic amides as raf kinase inhibitors by Ramurthy, Savithri, Costales, Abran, Jansen, Johanna M., Levine, Barry, Renhowe, Paul A., Shafer, Cynthia M., Subramanian, Sharadha

“…Compounds belonging to several scaffolds—quinazolines, quinolines and quinoxalines—were designed and synthesized as Raf kinase inhibitors. Scaffolds were…”
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