Search Results - "Caspers, Nicole L."

Structural Basis for AMPK Activation: Natural and Synthetic Ligands Regulate Kinase Activity from Opposite Poles by Different Molecular Mechanisms by Calabrese, Matthew F., Rajamohan, Francis, Harris, Melissa S., Caspers, Nicole L., Magyar, Rachelle, Withka, Jane M., Wang, Hong, Borzilleri, Kris A., Sahasrabudhe, Parag V., Hoth, Lise R., Geoghegan, Kieran F., Han, Seungil, Brown, Janice, Subashi, Timothy A., Reyes, Allan R., Frisbie, Richard K., Ward, Jessica, Miller, Russell A., Landro, James A., Londregan, Allyn T., Carpino, Philip A., Cabral, Shawn, Smith, Aaron C., Conn, Edward L., Cameron, Kimberly O., Qiu, Xiayang, Kurumbail, Ravi G.

“…AMP-activated protein kinase (AMPK) is a principal metabolic regulator affecting growth and response to cellular stress. Comprised of catalytic and regulatory…”
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Discovery and Preclinical Characterization of 6‑Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]‑1H‑indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy by Cameron, Kimberly O, Kung, Daniel W, Kalgutkar, Amit S, Kurumbail, Ravi G, Miller, Russell, Salatto, Christopher T, Ward, Jessica, Withka, Jane M, Bhattacharya, Samit K, Boehm, Markus, Borzilleri, Kris A, Brown, Janice A, Calabrese, Matthew, Caspers, Nicole L, Cokorinos, Emily, Conn, Edward L, Dowling, Matthew S, Edmonds, David J, Eng, Heather, Fernando, Dilinie P, Frisbie, Richard, Hepworth, David, Landro, James, Mao, Yuxia, Rajamohan, Francis, Reyes, Allan R, Rose, Colin R, Ryder, Tim, Shavnya, Andre, Smith, Aaron C, Tu, Meihua, Wolford, Angela C, Xiao, Jun

“…Adenosine monophosphate-activated protein kinase (AMPK) is a protein kinase involved in maintaining energy homeostasis within cells. On the basis of human…”
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Probing the enzyme kinetics, allosteric modulation and activation of α1- and α2-subunit-containing AMP-activated protein kinase (AMPK) heterotrimeric complexes by pharmacological and physiological activators by Rajamohan, Francis, Reyes, Allan R, Frisbie, Richard K, Hoth, Lise R, Sahasrabudhe, Parag, Magyar, Rachelle, Landro, James A, Withka, Jane M, Caspers, Nicole L, Calabrese, Matthew F, Ward, Jessica, Kurumbail, Ravi G

“…AMP-activated protein kinase (AMPK) is a serine/threonine protein kinase that serves as a pleotropic regulator of whole body energy homoeostasis. AMPK exists…”
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Selectively targeting an inactive conformation of interleukin-2-inducible T-cell kinase by allosteric inhibitors by Han, Seungil, Czerwinski, Robert M, Caspers, Nicole L, Limburg, David C, Ding, WeiDong, Wang, Hong, Ohren, Jeffrey F, Rajamohan, Francis, McLellan, Thomas J, Unwalla, Ray, Choi, Chulho, Parikh, Mihir D, Seth, Nilufer, Edmonds, Jason, Phillips, Chris, Shakya, Subarna, Li, Xin, Spaulding, Vikki, Hughes, Samantha, Cook, Andrew, Robinson, Colin, Mathias, John P, Navratilova, Iva, Medley, Quintus G, Anderson, David R, Kurumbail, Ravi G, Aulabaugh, Ann

“…ITK (interleukin-2-inducible T-cell kinase) is a critical component of signal transduction in T-cells and has a well-validated role in their proliferation,…”
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Optimization of Metabolic and Renal Clearance in a Series of Indole Acid Direct Activators of 5′-Adenosine Monophosphate-Activated Protein Kinase (AMPK) by Edmonds, David J, Kung, Daniel W, Kalgutkar, Amit S, Filipski, Kevin J, Ebner, David C, Cabral, Shawn, Smith, Aaron C, Aspnes, Gary E, Bhattacharya, Samit K, Borzilleri, Kris A, Brown, Janice A, Calabrese, Matthew F, Caspers, Nicole L, Cokorinos, Emily C, Conn, Edward L, Dowling, Matthew S, Eng, Heather, Feng, Bo, Fernando, Dilinie P, Genung, Nathan E, Herr, Michael, Kurumbail, Ravi G, Lavergne, Sophie Y, Lee, Esther C.-Y, Li, Qifang, Mathialagan, Sumathy, Miller, Russell A, Panteleev, Jane, Polivkova, Jana, Rajamohan, Francis, Reyes, Allan R, Salatto, Christopher T, Shavnya, Andre, Thuma, Benjamin A, Tu, Meihua, Ward, Jessica, Withka, Jane M, Xiao, Jun, Cameron, Kimberly O

“…Optimization of the pharmacokinetic (PK) properties of a series of activators of adenosine monophosphate-activated protein kinase (AMPK) is described…”
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Thermodynamic and Structure Guided Design of Statin Based Inhibitors of 3-Hydroxy-3-Methylglutaryl Coenzyme A Reductase by Sarver, Ronald W, Bills, Elizabeth, Bolton, Gary, Bratton, Larry D, Caspers, Nicole L, Dunbar, James B, Harris, Melissa S, Hutchings, Richard H, Kennedy, Robert M, Larsen, Scott D, Pavlovsky, Alexander, Pfefferkorn, Jeffrey A, Bainbridge, Graeme

“…Clinical studies have demonstrated that statins, 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMGR) inhibitors, are effective at lowering mortality levels…”
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2-(6-Phenyl-1H-indazol-3-yl)-1H-benzo[d]imidazoles: design and synthesis of a potent and isoform selective PKC-zeta inhibitor by Trujillo, John I, Kiefer, James R, Huang, Wei, Thorarensen, Atli, Xing, Li, Caspers, Nicole L, Day, Jacqueline E, Mathis, Karl J, Kretzmer, Kuniko K, Reitz, Beverley A, Weinberg, Robin A, Stegeman, Roderick A, Wrightstone, Ann, Christine, Lori, Compton, Robert, Li, Xiong

“…The inhibition of PKC-zeta has been proposed to be a potential drug target for immune and inflammatory diseases. A series of 2-(6-phenyl-1H…”
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Development of a high-throughput crystal structure-determination platform for JAK1 using a novel metal-chelator soaking system by Caspers, Nicole L., Han, Seungil, Rajamohan, Francis, Hoth, Lise R., Geoghegan, Kieran F., Subashi, Timothy A., Vazquez, Michael L., Kaila, Neelu, Cronin, Ciarán N., Johnson, Eric, Kurumbail, Ravi G.

“…Crystals of phosphorylated JAK1 kinase domain were initially generated in complex with nucleotide (ADP) and magnesium. The tightly bound Mg2+‐ADP at the…”
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Discovery and Preclinical Characterization of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1 H -indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy by Cameron, Kimberly O., Kung, Daniel W., Kalgutkar, Amit S., Kurumbail, Ravi G., Miller, Russell, Salatto, Christopher T., Ward, Jessica, Withka, Jane M., Bhattacharya, Samit K., Boehm, Markus, Borzilleri, Kris A., Brown, Janice A., Calabrese, Matthew, Caspers, Nicole L., Cokorinos, Emily, Conn, Edward L., Dowling, Matthew S., Edmonds, David J., Eng, Heather, Fernando, Dilinie P., Frisbie, Richard, Hepworth, David, Landro, James, Mao, Yuxia, Rajamohan, Francis, Reyes, Allan R., Rose, Colin R., Ryder, Tim, Shavnya, Andre, Smith, Aaron C., Tu, Meihua, Wolford, Angela C., Xiao, Jun

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2-(6-Phenyl-1H-indazol-3-yl)-1H-benzo[d]imidazoles: Design and synthesis of a potent and isoform selective PKC-[zeta] inhibitor by Trujillo, John I., Kiefer, James R., Huang, Wei, Thorarensen, Atli, Xing, Li, Caspers, Nicole L., Day, Jacqueline E., Mathis, Karl J., Kretzmer, Kuniko K., Reitz, Beverley A., Weinberg, Robin A., Stegeman, Roderick A., Wrightstone, Ann, Christine, Lori, Compton, Robert, Li, Xiong

“…The inhibition of PKC-{zeta} has been proposed to be a potential drug target for immune and inflammatory diseases. A series of 2-(6-phenyl-1H…”
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2-(6-Phenyl-1H-indazol-3-yl)-1H-benzo[d]imidazoles: Design and synthesis of a potent and isoform selective PKC- direct sum inhibitor by Trujillo, John I, Kiefer, James R, Huang, Wei, Thorarensen, Atli, Xing, Li, Caspers, Nicole L, Day, Jacqueline E, Mathis, Karl J, Kretzmer, Kuniko K, Reitz, Beverley A, Weinberg, Robin A, Stegeman, Roderick A, Wrightstone, Ann, Christine, Lori, Compton, Robert, Li, Xiong

“…The inhibition of PKC- direct sum has been proposed to be a potential drug target for immune and inflammatory diseases. A series of 2-(6-phenyl-1H…”
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2-(6-Phenyl-1 H-indazol-3-yl)-1 H-benzo[ d]imidazoles: Design and synthesis of a potent and isoform selective PKC-ζ inhibitor by Trujillo, John I., Kiefer, James R., Huang, Wei, Thorarensen, Atli, Xing, Li, Caspers, Nicole L., Day, Jacqueline E., Mathis, Karl J., Kretzmer, Kuniko K., Reitz, Beverley A., Weinberg, Robin A., Stegeman, Roderick A., Wrightstone, Ann, Christine, Lori, Compton, Robert, Li, Xiong

“…The design and synthesis of a potent and isoform selective PKCw-ζ ( 9, IC 50 = 5.2 nM, 10- to 20,000-fold selective over other PKC isoforms, 200-fold selective…”
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2-(6-Phenyl-lH-indazol-3-yl)-lH-benzo[d]imidazoles : Design and synthesis of a potent and isoform selective PKC-ζ inhibitor by TRUJILLO, John I, KIEFER, James R, WEINBERG, Robin A, STEGEMAN, Roderick A, WRIGHTSTONE, Ann, CHRISTINE, Lori, COMPTON, Robert, XIONG LI, WEI HUANG, THORARENSEN, Atli, LI XING, CASPERS, Nicole L, DAY, Jacqueline E, MATHIS, Karl J, KRETZMER, Kuniko K, REITZ, Beverley A

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