Search Results - "Blevitt, Jonathan M."

Phenotyping drug polypharmacology via eicosanoid profiling of blood[S] by Song, Jiao, Liu, Xuejun, Rao, Tadimeti S., Chang, Leon, Meehan, Michael J., Blevitt, Jonathan M., Wu, Jiejun, Dorrestein, Pieter C., Milla, Marcos E.

“…It is widely accepted that small-molecule drugs, despite their selectivity at primary targets, exert pharmacological effects (and safety liabilities) through a…”
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Identification of benzofuran central cores for the inhibition of leukotriene A4 hydrolase by Eccles, Wendy, Blevitt, Jonathan M., Booker, Jamila N., Chrovian, Christa C., Crawford, Shelby, de Leon, Aimee Rose, Deng, Xiaohu, Fourie, Anne M., Grice, Cheryl A., Herman, Krystal, Karlsson, Lars, Kearney, Aaron M., Lee-Dutra, Alice, Liang, Jimmy, Luna, Rosa, Pippel, Dan, Rao, Navin, Riley, Jason P., Santillán, Alejandro, Savall, Brad, Tanis, Virginia M., Xue, Xiaohua, Young, Arlene L.

“…Leukotrienes (LT’s) are known to play a physiological role in inflammatory immune response. Leukotriene A4 hydrolase (LTA4H) is a cystolic enzyme that…”
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A novel B-RAF inhibitor blocks interleukin-8 (IL-8) synthesis in human melanoma xenografts, revealing IL-8 as a potential pharmacodynamic biomarker by Crawford, Shelby, Belajic, Daniel, Wei, Jianmei, Riley, Jason P, Dunford, Paul J, Bembenek, Scott, Fourie, Anne, Edwards, James P, Karlsson, Lars, Brunmark, Anders, Wolin, Ronald L, Blevitt, Jonathan M

“…B-RAF mutations have been identified in the majority of melanoma and a large fraction of colorectal and papillary thyroid carcinoma. Drug discovery efforts…”
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Structural Basis of Small-Molecule Aggregate Induced Inhibition of a Protein–Protein Interaction by Blevitt, Jonathan M, Hack, Michael D, Herman, Krystal L, Jackson, Paul F, Krawczuk, Paul J, Lebsack, Alec D, Liu, Annie X, Mirzadegan, Taraneh, Nelen, Marina I, Patrick, Aaron N, Steinbacher, Stefan, Milla, Marcos E, Lumb, Kevin J

“…A prevalent observation in high-throughput screening and drug discovery programs is the inhibition of protein function by small-molecule compound aggregation…”
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Coupling to Gq Signaling Is Required for Cardioprotection by an Alpha-1A-Adrenergic Receptor Agonist by Myagmar, Bat-Erdene, Ismaili, Taylor, Swigart, Philip M, Raghunathan, Anaha, Baker, Anthony J, Sahdeo, Sunil, Blevitt, Jonathan M, Milla, Marcos E, Simpson, Paul C

“…RATIONALE:Gq signaling in cardiac myocytes is classically considered toxic. Targeting Gq directly to test this is problematic, because cardiac myocytes have…”
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A highly selective, orally bioavailable, vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor has potent activity in vitro and in vivo by LaMontagne, Kenneth R., Butler, Jeannene, Borowski, Virna B., Fuentes-Pesquera, Angel R., Blevitt, Jonathan M., Huang, Shenlin, Li, Ronghua, Connolly, Peter J., Greenberger, Lee M.

“…Angiogenesis is a complex process that relies on a variety of growth factors and signaling pathways to stimulate endothelial cell responses and establish…”
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A highly efficient, high-throughput lipidomics platform for the quantitative detection of eicosanoids in human whole blood by Song, Jiao, Liu, Xuejun, Wu, Jiejun, Meehan, Michael J., Blevitt, Jonathan M., Dorrestein, Pieter C., Milla, Marcos E.

“…We have developed an ultra-performance liquid chromatography–multiple reaction monitoring/mass spectrometry (UPLC–MRM/MS)-based, high-content, high-throughput…”
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A Single Amino Acid Difference between Mouse and Human 5-Lipoxygenase Activating Protein (FLAP) Explains the Speciation and Differential Pharmacology of Novel FLAP Inhibitors by Blevitt, Jonathan M., Hack, Michael D., Herman, Krystal, Chang, Leon, Keith, John M., Mirzadegan, Tara, Rao, Navin L., Lebsack, Alec D., Milla, Marcos E.

“…5-Lipoxygenase activating protein (FLAP) plays a critical role in the metabolism of arachidonic acid to leukotriene A4, the precursor to the potent…”
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Polypharmacology of Small-Molecule Modulators of the 5-Lipoxygenase Activating Protein (FLAP) Observed via a High-throughput Lipidomics Platform by Song, Jiao, Liu, Xuejun, Zhu, Jian, Tootoonchi, Mandana, Keith, John M, Meduna, Steven P, Dvorak, Curt A, Eccles, Wendy, Krawczuk, Paul J, Blevitt, Jonathan M, Wu, Jiejun, Rao, Navin L, Lebsack, Alec D, Milla, Marcos E

“…Leukotrienes (LTs) and related species are proinflammatory lipid mediators derived from arachidonic acid (AA) that have pathological roles in autoimmune and…”
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Identification of benzofuran central cores for the inhibition of leukotriene A(4) hydrolase by Eccles, Wendy, Blevitt, Jonathan M, Booker, Jamila N, Chrovian, Christa C, Crawford, Shelby, de Leon, Aimee Rose, Deng, Xiaohu, Fourie, Anne M, Grice, Cheryl A, Herman, Krystal, Karlsson, Lars, Kearney, Aaron M, Lee-Dutra, Alice, Liang, Jimmy, Luna, Rosa, Pippel, Dan, Rao, Navin, Riley, Jason P, Santillán, Alejandro, Savall, Brad, Tanis, Virginia M, Xue, Xiaohua, Young, Arlene L

“…Leukotrienes (LT's) are known to play a physiological role in inflammatory immune response. Leukotriene A(4) hydrolase (LTA(4)H) is a cystolic enzyme that…”
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Azabenzthiazole inhibitors of leukotriene A4 hydrolase by Tanis, Virginia M., Bacani, Genesis M., Blevitt, Jonathan M., Chrovian, Christa C., Crawford, Shelby, De Leon, Aimee, Fourie, Anne M., Gomez, Laurent, Grice, Cheryl A., Herman, Krystal, Kearney, Aaron M., Landry-Bayle, Adrienne M., Lee-Dutra, Alice, Nelson, Jay, Riley, Jason P., Santillán, Alejandro, Wiener, John J.M., Xue, Xiaohua, Young, Arlene L.

“…Previously, benzthiazole containing LTA4H inhibitors were discovered that were potent (1–3), but were associated with the potential for a hERG liability…”
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2-Aryl benzimidazoles featuring alkyl-linked pendant alcohols and amines as inhibitors of checkpoint kinase Chk2 by Neff, Danielle K., Lee-Dutra, Alice, Blevitt, Jonathan M., Axe, Frank U., Hack, Michael D., Buma, Johnathan C., Rynberg, Raymond, Brunmark, Anders, Karlsson, Lars, Breitenbucher, J. Guy

“…A series of benzimidazole compounds containing pendant alcohol and amine moieties was found to be active against checkpoint kinase Chk2. These compounds were…”
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Dual binding site inhibitors of B-RAF kinase by Wolin, Ronald L., Bembenek, Scott D., Wei, Jianmei, Crawford, Shelby, Lundeen, Katherine, Brunmark, Anders, Karlsson, Lars, Edwards, James P., Blevitt, Jonathan M.

“…Diarylimidazole motifs were designed to interact with both the ATP binding site and the adjacent allosteric region. Computer aided modeling guided the design…”
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Phosphoinositide 3-kinase gamma (PI3Kgamma) inhibitors for the treatment of inflammation and autoimmune disease by Venable, Jennifer D, Ameriks, Michael K, Blevitt, Jonathan M, Thurmond, Robin L, Fung-Leung, Wai-Ping

“…Phosphoinositide 3-kinase gamma (PI3Kgamma) is a lipid kinase in leukocytes that generates phosphatidylinositol 3,4,5-trisphosphate to recruit and activate…”
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Abstract 11086: Isoproterenol Can Act as a Biased Partial Agonist on the Cardiac Myocyte Alpha-1A-Adrenergic Receptors but Does Not Confer Cardioprotection by Myagmar, Bat-erdene, Montgomery, Megan D, Ismaili, Taylor K, Swigart, Philip M, Baker, Anthony J, Sahdeo, Sunil, Blevitt, Jonathan M, Milla, Marcos E, Simpson, Paul C

“…RationaleIsoproterenol (ISO) is used classically as a specific agonist of beta-adrenergic receptors (ARs) in the heart and cardiac myocytes. However, some…”
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Structural analysis of the p62 complex, an assembly of O-linked glycoproteins that localizes near the central gated channel of the nuclear pore complex by Guan, T, Müller, S, Klier, G, Panté, N, Blevitt, J M, Haner, M, Paschal, B, Aebi, U, Gerace, L

“…The p62 complex is an oligomeric assembly of O-linked glycoproteins of the nuclear pore complex that interacts with cytosolic transport factors and is part of…”
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The alpha‐helical rod domain of human lamins A and C contains a chromatin binding site by Glass, C.A., Glass, J.R., Taniura, H., Hasel, K.W., Blevitt, J.M., Gerace, L.

“…We examined regions of human lamins A and C involved in binding to surfaces of mitotic chromosomes. An Escherichia coli expression system was used to produce…”
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O-Linked Glycoproteins of the Nuclear Pore Complex Interact with a Cytosolic Factor Required for Nuclear Protein Import by Sterne-Marr, Rachel, Blevitt, Jonathan M., Gerace, Larry

“…Mediated import of proteins into the nucleus requires cytosolic factors and can be blocked by reagents that bind to O-linked glycoproteins of the nuclear pore…”
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