Search Results - "Shreder, Kevin"

Hit-to-lead optimization and kinase selectivity of imidazo[1,2-a]quinoxalin-4-amine derived JNK1 inhibitors by Li, Bei, Cociorva, Oana M., Nomanbhoy, Tyzoon, Weissig, Helge, Li, Qiang, Nakamura, Kai, Liyanage, Marek, Zhang, Melissa C., Shih, Ann Y., Aban, Arwin, Hu, Yi, Cajica, Julia, Pham, Lan, Kozarich, John W., Shreder, Kevin R.

“…As the result of a rhJNK1 HTS, the imidazo[1,2-a]quinoxaline 1 was identified as a 1.6μM rhJNK1 inhibitor. Optimization of this compound lead to AX13587…”
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Quinolone derivatives containing strained spirocycle as orally active glycogen synthase kinase 3β (GSK-3β) inhibitors for type 2 diabetics by Seto, Shigeki, Yumoto, Kazuhiko, Okada, Kyoko, Asahina, Yoshikazu, Iwane, Aya, Iwago, Maki, Terasawa, Reiko, Shreder, Kevin R., Murakami, Koji, Kohno, Yasushi

“…The design, synthesis, and evaluation of 6-6-7 tricyclic quinolones containing the strained spirocycle moiety aiming at the GSK-3β inhibitor were described…”
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High-Resolution Functional Proteomics by Active-Site Peptide Profiling by Okerberg, Eric S., Wu, Jiangyue, Zhang, Baohong, Samii, Babak, Blackford, Kelly, Winn, David T., Shreder, Kevin R., Burbaum, Jonathan J., Patricelli, Matthew P., Stubbe, JoAnne

“…Characterization and functional annotation of the large number of proteins predicted from genome sequencing projects poses a major scientific challenge…”
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Amides of 4-hydroxy-8-methanesulfonylamino-quinoline-2-carboxylic acid as zinc-dependent inhibitors of Lp-PLA by Hu, Yi, Lin, Emme C K, Pham, Lan M, Cajica, Julia, Amantea, Christopher M, Okerberg, Eric, Brown, Heidi E, Fraser, Allister, Du, Lingling, Kohno, Yasushi, Ishiyama, Junichi, Kozarich, John W, Shreder, Kevin R

“…AX10479, the phenyl amide of 4-hydroxy-8-methanesulfonylamino-quinoline-2-carboxylic acid, was identified as a Zn(2+)-dependent, 27nM inhibitor of human plasma…”
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Synthesis and structure–activity relationship of 4-quinolone-3-carboxylic acid based inhibitors of glycogen synthase kinase-3β by Cociorva, Oana M., Li, Bei, Nomanbhoy, Tyzoon, Li, Qiang, Nakamura, Ayako, Nakamura, Kai, Nomura, Masahiro, Okada, Kyoko, Seto, Shigeki, Yumoto, Kazuhiro, Liyanage, Marek, Zhang, Melissa C., Aban, Arwin, Leen, Brandon, Szardenings, Anna Katrin, Rosenblum, Jonathan S., Kozarich, John W., Kohno, Yasushi, Shreder, Kevin R.

“…The synthesis, GSK-3β inhibitory activity, and anti-microbial activity of bicyclic and tricyclic derivatives of the…”
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Amides of xanthurenic acid as zinc-dependent inhibitors of Lp-PLA by Lin, Emme C.K, Hu, Yi, Amantea, Christopher M, Pham, Lan M, Cajica, Julia, Okerberg, Eric, Brown, Heidi E, Fraser, Allister, Du, Lingling, Kohno, Yasushi, Ishiyama, Junichi, Kozarich, John W, Shreder, Kevin R

“…AX10185, the phenyl amide of xanthurenic acid, was found to be a sub-100nM inhibitor of Lp-PLA₂. However, in the presence of EDTA the inhibitory activity of…”
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Synthesis and structure–activity relationship of (1-halo-2-naphthyl) carbamate-based inhibitors of KIAA1363 (NCEH1/AADACL1) by Shreder, Kevin R., Lin, Emme C.K., Wu, Jiangyue, Cajica, Julia, Amantea, Christopher M., Hu, Yi, Okerberg, Eric, Brown, Heidi E., Pham, Lan M., Chung, De Michael, Fraser, Allister S., McGee, Ethel, Rosenblum, Jonathan S., Kozarich, John W.

“…KIAA1363 is a serine hydrolase whose activity has been shown to be positively associated with tumor cell invasiveness. Thus, inhibitors of KIAA1363 represent a…”
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6-Position optimization of tricyclic 4-quinolone-based inhibitors of glycogen synthase kinase-3β: Discovery of nitrile derivatives with picomolar potency by Li, Bei, Cociorva, Oana M., Nomanbhoy, Tyzoon, Li, Qiang, Nakamura, Kai, Nomura, Masahiro, Okada, Kyoko, Yumoto, Kazuhiro, Liyanage, Marek, Zhang, Melissa C., Aban, Arwin, Szardenings, Anna Katrin, Kozarich, John W., Kohno, Yasushi, Shreder, Kevin R.

“…We previously disclosed tricylic, 6-carboxylic acid-bearing 4-quinolones as GSK-3β inhibitors. Herein we discuss the optimization of this series to yield a…”
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Synthesis of AX7593, a Quinazoline-Derived Photoaffinity Probe for EGFR by Shreder, Kevin R, Wong, Melissa S, Nomanbhoy, Tyzoon, Leventhal, Phillip S, Fuller, Stacy R

“…The synthesis of a photoaffinity probe for EGFR is described. O-Alkylation of 4-(meta-azidoanilino)-6-methoxy-7-hydroxy-quinazoline with a protected…”
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Synthesis and optimization of 2-pyridin-3-yl-benzo[ d][1,3]oxazin-4-one based inhibitors of human neutrophil elastase by Shreder, Kevin R., Cajica, Julia, Du, Lingling, Fraser, Allister, Hu, Yi, Kohno, Yasushi, Lin, Emme C.K., Liu, Steve J., Okerberg, Eric, Pham, Lan, Wu, Jiangyue, Kozarich, John W.

“…The synthesis, inhibitory activity, hydrolytic stability, and rat plasma stability of 2-pyridin-3-yl-benzo[ d][1,3]oxazin-4-one based inhibitors of human…”
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Amides of xanthurenic acid as zinc-dependent inhibitors of Lp-PLA2 by Lin, Emme C.K., Hu, Yi, Amantea, Christopher M., Pham, Lan M., Cajica, Julia, Okerberg, Eric, Brown, Heidi E., Fraser, Allister, Du, Lingling, Kohno, Yasushi, Ishiyama, Junichi, Kozarich, John W., Shreder, Kevin R.

“…AX10185, the phenyl amide of xanthurenic acid, was found to be a sub-100nM inhibitor of Lp-PLA2. However, in the presence of EDTA the inhibitory activity of…”
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Protonated Sapphyrins. Highly Effective Phosphate Receptors by Král, Vladimír, Furuta, Hiroyuki, Shreder, Kevin, Lynch, Vincent, Sessler, Jonathan L

“…The phosphate anion chelation properties of several sapphyrin derivatives, namely…”
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Design and Synthesis of AX7574:  A Microcystin-Derived, Fluorescent Probe for Serine/Threonine Phosphatases by Shreder, Kevin R, Liu, Yongsheng, Nomanhboy, Tyzoon, Fuller, Stacy R, Wong, Melissa S, Gai, Wen Zhi, Wu, Jiangyue, Leventhal, Phillip S, Lill, Jennie R, Corral, Sergio

“…The design and synthesis of AX7574, a microcystin-derived probe for serine/threonine phosphatases, is described. A key step in the synthesis was the…”
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Design and synthesis of AX4697, a bisindolylmaleimide exo-affinity probe that labels protein kinase C alpha and beta by Liu, Yongsheng, Wu, Jiangyue, Weissig, Helge, Betancort, Juan M., Gai, Wen Zhi, Leventhal, Phillip S., Patricelli, Matthew P., Samii, Babak, Szardenings, Anna K., Shreder, Kevin R., Kozarich, John W.

“…The synthesis and biochemical characterization of AX4697, bisindolylmaleimide-derived, exo-affinity probe for PKCα and β, is described. The synthesis and…”
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Synthesis and structure–activity relationship of N-alkyl Gly-boro-Pro inhibitors of DPP4, FAP, and DPP7 by Hu, Yi, Ma, Lifu, Wu, Min, Wong, Melissa S., Li, Bei, Corral, Sergio, Yu, Zhizhou, Nomanbhoy, Tyzoon, Alemayehu, Senaiet, Fuller, Stacy R., Rosenblum, Jonathan S., Rozenkrants, Natasha, Minimo, Lauro C., Ripka, William C., Szardenings, Anna K., Kozarich, John W., Shreder, Kevin R.

“…The structure-activity relationship of various N-alkyl Gly-boro-Pro derivatives against three dipeptidyl peptidases (DPP4, FAP, and DPP7) was explored. The…”
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Quenching of Biotinylated Aequorin Bioluminescence by Dye-Labeled Avidin Conjugates:  Application to Homogeneous Bioluminescence Resonance Energy Transfer Assays by Adamczyk, Maciej, Moore, Jeffrey A, Shreder, Kevin

“…Avidin conjugates containing the covalently attached dyes QSY-7 and dabcyl were prepared and shown to quench the bioluminescence of biotinylated aequorin…”
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Synthesis of a constrained enkephalin analog to illustrate a novel route to the piperazinone ring structure by Shreder, Kevin, Zhang, Li, Goodman, Murray

“…The synthesis of a constrained, piperazinone analog of Leu-enkephalin is presented. A key step in this synthesis was the use of the secondary amine, Boc-Tyr(O…”
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Boro-norleucine as a P1 residue for the design of selective and potent DPP7 inhibitors by Shreder, Kevin R., Wong, Melissa S., Corral, Sergio, Yu, Zhizhou, Winn, David T., Wu, Min, Hu, Yi, Nomanbhoy, Tyzoon, Alemayehu, Senaiet, Fuller, Stacy R., Rosenblum, Jonathan S., Kozarich, John W.

“…Dipeptide-based dipeptidyl peptidase inhibitors with C-substituted (alkyl or aminoalkyl) α-amino acids in the P2 position and boro-norleucine (boro-Nle) in the…”
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Region-Selective Labeling of Antibodies as Determined by Electrospray Ionization-Mass Spectrometry (ESI-MS) by Adamczyk, Maciej, Gebler, John, Shreder, Kevin, Wu, Jiang

“…The electrospray ionization-mass spectrometry (ESI-MS) analysis of three sets of monoclonal antibody-acridinium-9-carboxamide conjugates is described. The…”
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Wortmannin, a Widely Used Phosphoinositide 3-Kinase Inhibitor, also Potently Inhibits Mammalian Polo-like Kinase by Liu, Yongsheng, Shreder, Kevin R., Gai, Wenzhi, Corral, Sergio, Ferris, Douglas K., Rosenblum, Jonathan S.

“…Polo-like kinases (PLKs) play critical roles throughout mitosis. Here, we report that wortmannin, which was previously thought to be a highly selective…”
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