Search Results - "Artis, Dean R."

Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF -mutant melanoma by Marimuthu, Adhirai, D'Andrea, Kurt, Lin, Paul S, Puzanov, Igor, Chapman, Paul B, Zhang, Jiazhong, Tsai, James, Ibrahim, Prabha N, Cho, Hanna, West, Brian L, Nathanson, Katherine L, Zhang, Kam Y. J, Zhang, Ying, Nolop, Keith, Schlessinger, Joseph, Grippo, Joseph, Shellooe, Rafe, Zhang, Chao, Flaherty, Keith T, Tsang, Garson, Powell, Ben, Kim, Kevin B, Wong, Bernice, Stumm, Michael, Ribas, Antoni, Spevak, Wayne, Higgins, Brian, Sosman, Jeffrey A, Artis, Dean R, Habets, Gaston, Hirth, Peter, Burton, Elizabeth A, Iyer, Raman, Su, Fei, Koehler, Astrid, Lee, Richard J, Bollag, Gideon, Nguyen, Hoa, McArthur, Grant A, Xu, Xiaowei

“…B-RAF is the most frequently mutated protein kinase in human cancers. The finding that oncogenic mutations in BRAF are common in melanoma, followed by the…”
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Design and pharmacology of a highly specific dual FMS and KIT kinase inhibitor by Zhang, Chao, Ibrahim, Prabha N., Zhang, Jiazhong, Burton, Elizabeth A., Habets, Gaston, Zhang, Ying, Powell, Ben, West, Brian L., Matusow, Bernice, Tsang, Garson, Shellooe, Rafe, Carias, Heidi, Nguyen, Hoa, Marimuthu, Adhirai, Zhang, Kam Y. J., Oh, Angela, Bremer, Ryan, Hurt, Clarence R., Artis, Dean R., Wu, Guoxian, Nespi, Marika, Spevak, Wayne, Lin, Paul, Nolop, Keith, Hirth, Peter, Tesch, Greg H., Bollag, Gideon

“…Inflammation and cancer, two therapeutic areas historically addressed by separate drug discovery efforts, are now coupled in treatment approaches by a growing…”
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Scaffold-based discovery of indeglitazar, a PPAR pan-active anti-diabetic agent by Artis, Dean R, Lin, Jack J, Zhang, Chao, Wang, Weiru, Mehra, Upasana, Perreault, Mylene, Erbe, David, Krupka, Heike I, England, Bruce P, Arnold, James, Plotnikov, Alexander N, Marimuthu, Adhirai, Nguyen, Hoa, Will, Sarah, Signaevsky, Maxime, Kral, John, Cantwell, John, Settachatgull, Calvin, Yan, Douglas S, Fong, Daniel, Oh, Angela, Shi, Shenghua, Womack, Patrick, Powell, Benjamin, Habets, Gaston, West, Brian L, Zhang, Kam Y.J, Milburn, Michael V, Vlasuk, George P, Hirth, K. Peter, Nolop, Keith, Bollag, Gideon, Ibrahim, Prabha N, Tobin, James F

“…In a search for more effective anti-diabetic treatment, we used a process coupling low-affinity biochemical screening with high-throughput co-crystallography…”
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Crystal Structures of Proto-oncogene Kinase Pim1: A Target of Aberrant Somatic Hypermutations in Diffuse Large Cell Lymphoma by Kumar, Abhinav, Mandiyan, Valsan, Suzuki, Yoshihisa, Zhang, Chao, Rice, Julie, Tsai, James, Artis, Dean R., Ibrahim, Prabha, Bremer, Ryan

“…Pim1, a serine/threonine kinase, is involved in several biological functions including cell survival, proliferation, and differentiation. While pim1 has been…”
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Comprehensive and Quantitative Mapping of Energy Landscapes for Protein-Protein Interactions by Rapid Combinatorial Scanning by Pál, Gábor, Kouadio, Jean-Louis K., Artis, Dean R., Kossiakoff, Anthony A., Sidhu, Sachdev S.

“…A novel, quantitative saturation (QS) scanning strategy was developed to obtain a comprehensive data base of the structural and functional effects of all…”
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A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design by Zhang, Kam Y J, Card, Graeme L, Blasdel, Landy, England, Bruce P, Zhang, Chao, Suzuki, Yoshihisa, Gillette, Sam, Fong, Daniel, Ibrahim, Prabha N, Artis, Dean R, Bollag, Gideon, Milburn, Michael V, Kim, Sung-Hou, Schlessinger, Joseph

“…Cyclic nucleotide phosphodiesterases (PDEs) comprise a large family of enzymes that regulate a variety of cellular processes. We describe a family of potent…”
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Design and synthesis of thiophene dihydroisoquinolines as novel BACE1 inhibitors by Xu, Ying-zi, Yuan, Shendong, Bowers, Simeon, Hom, Roy K., Chan, Wayman, Sham, Hing L., Zhu, Yong L., Beroza, Paul, Pan, Hu, Brecht, Eric, Yao, Nanhua, Lougheed, Julie, Yan, Jiangli, Tam, Danny, Ren, Zhao, Ruslim, Lany, Bova, Michael P., Artis, Dean R.

“…Utilizing a structure based design approach, combined with extensive medicinal chemistry execution, highly selective, potent and novel BACE1 inhibitor 8 (BACE1…”
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Design and synthesis of highly selective, orally active Polo-like kinase-2 (Plk-2) inhibitors by Bowers, Simeon, Truong, Anh P., Ye, Michael, Aubele, Danielle L., Sealy, Jennifer M., Neitz, R. Jeffrey, Hom, Roy K., Chan, Wayman, Dappen, Michael S., Galemmo, Robert A., Konradi, Andrei W., Sham, Hing L., Zhu, Yong L., Beroza, Paul, Tonn, George, Zhang, Heather, Hoffman, Jennifer, Motter, Ruth, Fauss, Donald, Tanaka, Pearl, Bova, Michael P., Ren, Zhao, Tam, Danny, Ruslim, Lany, Baker, Jeanne, Pandya, Deepal, Diep, Linnea, Fitzgerald, Kent, Artis, Dean R., Anderson, John P., Bergeron, Marcelle

“…Polo-like kinase-2 (Plk-2) is a potential therapeutic target for Parkinson’s disease and this Letter describes the SAR of a series of dihydropteridinone based…”
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Design and synthesis of a novel, orally active, brain penetrant, tri-substituted thiophene based JNK inhibitor by Bowers, Simeon, Truong, Anh P., Neitz, R. Jeffrey, Neitzel, Martin, Probst, Gary D., Hom, Roy K., Peterson, Brian, Galemmo, Robert A., Konradi, Andrei W., Sham, Hing L., Tóth, Gergley, Pan, Hu, Yao, Nanhua, Artis, Dean R., Brigham, Elizabeth F., Quinn, Kevin P., Sauer, John-Michael, Powell, Kyle, Ruslim, Lany, Ren, Zhao, Bard, Frédérique, Yednock, Ted A., Griswold-Prenner, Irene

“…The SAR of a series of tri-substituted thiophene JNK3 inhibitors is described. By optimizing both the N-aryl acetamide region of the inhibitor and the…”
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Including Explicit Water Molecules as Part of the Protein Structure in MM/PBSA Calculations by Zhu, Yong-Liang, Beroza, Paul, Artis, Dean R

“…Water is the natural medium of molecules in the cell and plays an important role in protein structure, function and interaction with small molecule ligands…”
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Discovery of a Selective Inhibitor of Oncogenic B-Raf Kinase with Potent Antimelanoma Activity by Tsai, James, Lee, John T., Wang, Weiru, Zhang, Jiazhong, Cho, Hanna, Mamo, Shumeye, Bremer, Ryan, Gillette, Sam, Kong, Jun, Haass, Nikolas K., Sproesser, Katrin, Li, Ling, Smalley, Keiran S. M., Fong, Daniel, Zhu, Yong-Liang, Marimuthu, Adhirai, Nguyen, Hoa, Lam, Billy, Liu, Jennifer, Cheung, Ivana, Rice, Julie, Suzuki, Yoshihisa, Luu, Catherine, Settachatgul, Calvin, Shellooe, Rafe, Cantwell, John, Kim, Sung-Hou, Schlessinger, Joseph, Zhang, Kam Y. J., West, Brian L., Powell, Ben, Habets, Gaston, Zhang, Chao, Ibrahim, Prabha N., Hirth, Peter, Artis, Dean R., Herlyn, Meenhard, Bollag, Gideon

“…$BRAF^{V600E}$ is the most frequent oncogenic protein kinase mutation known. Furthermore, inhibitors targeting "active" protein kinases have demonstrated…”
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A Selective, Slow Binding Inhibitor of Factor VIIa Binds to a Nonstandard Active Site Conformation and Attenuates Thrombus Formation in Vivo by Olivero, Alan G., Eigenbrot, Charles, Goldsmith, Richard, Robarge, Kirk, Artis, Dean R., Flygare, John, Rawson, Thomas, Sutherlin, Daniel P., Kadkhodayan, Saloumeh, Beresini, Maureen, Elliott, Linda O., DeGuzman, Geralyn G., Banner, David W., Ultsch, Mark, Marzec, Ulla, Hanson, Stephen R., Refino, Canio, Bunting, Stuart, Kirchhofer, Daniel

“…The serine protease factor VIIa (FVIIa) in complex with its cellular cofactor tissue factor (TF) initiates the blood coagulation reactions. TF·FVIIa is also…”
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Conformations of Thioamide-Containing Dipeptides:  A Computational Study by Artis, Dean R, Lipton, Mark A

“…Four model dipeptides, Ac-ψ[CSNH]-Gly-NHMe, Ac-Gly-ψ[CSNH]-NHMe, Ac-ψ[CSNH]-Ala-NHMe, and Ac-Ala-ψ[CSNH]-NHMe, each containing a thioamide bond, were studied…”
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Structural Basis for the Activity of Drugs that Inhibit Phosphodiesterases by Card, Graeme L., England, Bruce P., Suzuki, Yoshihisa, Fong, Daniel, Powell, Ben, Lee, Byunghun, Luu, Catherine, Tabrizizad, Maryam, Gillette, Sam, Ibrahim, Prabha N., Artis, Dean R., Bollag, Gideon, Milburn, Michael V., Kim, Sung-Hou, Schlessinger, Joseph, Zhang, Kam Y.J.

“…Phosphodiesterases (PDEs) comprise a large family of enzymes that catalyze the hydrolysis of cAMP or cGMP and are implicated in various diseases. We describe…”
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Oxidative Radical Cyclization of (.omega.-Iodoalkyl)indoles and Pyrroles. Synthesis of (-)-Monomorine and Three Diastereomers by Artis, Dean R, Cho, In-Seop, Jaime-Figueroa, Saul, Muchowski, Joseph M

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Thermodynamic and kinetic characterization of hydroxyethylamine β-secretase-1 inhibitors by Mondal, Kalyani, Regnstrom, Karin, Morishige, Winse, Barbour, Robin, Probst, Gary, Xu, Ying-Zi, Artis, Dean R., Yao, Nanhua, Beroza, Paul, Bova, Michael P.

“…•Kinetic and thermodynamic characterization of 10 hydroxyethylamine BACE-1 inhibitors.•Equilibrium binding of inhibitors was enthalpy driven for…”
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Selective and Brain-Permeable Polo-like Kinase-2 (Plk-2) Inhibitors That Reduce [alpha]-Synuclein Phosphorylation in Rat Brain by Aubele, Danielle L, Hom, Roy K, Adler, Marc, Galemmo, Robert A, Bowers, Simeon, Truong, Anh P, Pan, Hu, Beroza, Paul, Neitz, R Jeffrey, Yao, Nanhua, Lin, May, Tonn, George, Zhang, Heather, Bova, Michael P, Ren, Zhao, Tam, Danny, Ruslim, Lany, Baker, Jeanne, Diep, Linnea, Fitzgerald, Kent, Hoffman, Jennifer, Motter, Ruth, Fauss, Donald, Tanaka, Pearl, Dappen, Michael, Jagodzinski, Jacek, Chan, Wayman, Konradi, Andrei W, Latimer, Lee, Zhu, Yong L, Sham, Hing L, Anderson, John P, Bergeron, Marcelle, Artis, Dean R

“…Polo-like kinase-2 (Plk-2) has been implicated as the dominant kinase involved in the phosphorylation of [alpha]-synuclein in Lewy bodies, which are one of the…”
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Selective and Brain-Permeable Polo-like Kinase-2 (Plk-2) Inhibitors That Reduce α-Synuclein Phosphorylation in Rat Brain by Aubele, Danielle L., Hom, Roy K., Adler, Marc, Galemmo Jr, Robert A., Bowers, Simeon, Truong, Anh P., Pan, Hu, Beroza, Paul, Neitz, R. Jeffrey, Yao, Nanhua, Lin, May, Tonn, George, Zhang, Heather, Bova, Michael P., Ren, Zhao, Tam, Danny, Ruslim, Lany, Baker, Jeanne, Diep, Linnea, Fitzgerald, Kent, Hoffman, Jennifer, Motter, Ruth, Fauss, Donald, Tanaka, Pearl, Dappen, Michael, Jagodzinski, Jacek, Chan, Wayman, Konradi, Andrei W., Latimer, Lee, Zhu, Yong L., Sham, Hing L., Anderson, John P., Bergeron, Marcelle, Artis, Dean R.

“…Polo‐like kinase‐2 (Plk‐2) has been implicated as the dominant kinase involved in the phosphorylation of α‐synuclein in Lewy bodies, which are one of the…”
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Label free fragment screening using surface plasmon resonance as a tool for fragment finding - analyzing parkin, a difficult CNS target by Regnström, Karin, Yan, Jiangli, Nguyen, Lan, Callaway, Kari, Yang, Yanli, Diep, Linnea, Xing, Weimei, Adhikari, Anirban, Beroza, Paul, Hom, Roy K, Riley, Brigit, Rudolph, Don, Jobling, Michael F, Baker, Jeanne, Johnston, Jennifer, Konradi, Andrei, Bova, Michael P, Artis, Dean R, Artis, Rick D

“…Surface Plasmon Resonance (SPR) is rarely used as a primary High-throughput Screening (HTS) tool in fragment-based approaches. With SPR instruments becoming…”
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Correction: Label Free Fragment Screening Using Surface Plasmon Resonance as a Tool for Fragment Finding РAnalyzing Parkin, a Difficult CNS Target by Regnstr̦m, Karin, Yan, Jiangli, Nguyen, Lan, Callaway, Kari, Yang, Yanli, Diep, Linnea, Xing, Weimei, Adhikari, Anirban, Beroza, Paul, Hom, Roy K., Riley, Brigit, Rudolph, Don, Jobling, Michael F., Baker, Jeanne, Johnston, Jennifer, Konradi, Andrei, Bova, Michael P., Artis, Dean R.

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