Search Results - "Steffey, Michael E."

Development of a Highly Selective c-Src Kinase Inhibitor by Brandvold, Kristoffer R, Steffey, Michael E, Fox, Christel C, Soellner, Matthew B

“…Generating highly selective probes to interrogate protein kinase function in biological studies remains a challenge, and new strategies are required. Herein,…”
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Calcimimetics with Potent and Selective Activity on the Parathyroid Calcium Receptor by Nemeth, Edward F., Steffey, Michael E., Hammerland, Lance G., Benjamin C. P. Hung, Van Wagenen, Bradford C., DelMar, Eric G., Balandrin, Manuel F.

“…Parathyroid hormone (PTH) secretion is regulated by a cell surface Ca2+receptor that detects small changes in the level of plasma Ca2+. Because this G…”
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Cell Surface Expression of the Melanocortin-4 Receptor Is Dependent on a C-terminal Di-isoleucine Sequence at Codons 316/317 by VanLeeuwen, Donald, Steffey, Michael E., Donahue, Christopher, Ho, Guyu, MacKenzie, Robert G.

“…Loss-of-function mutations in the human melanocortin-4 receptor (MC4R) are associated with obesity. Previous work has implicated a C-terminal di-isoleucine…”
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UM-164: A Potent c-Src/p38 Kinase Inhibitor with In Vivo Activity against Triple-Negative Breast Cancer by Gilani, Rabia A, Phadke, Sameer, Bao, Li Wei, Lachacz, Eric J, Dziubinski, Michele L, Brandvold, Kristoffer R, Steffey, Michael E, Kwarcinski, Frank E, Graveel, Carrie R, Kidwell, Kelley M, Merajver, Sofia D, Soellner, Matthew B

“…c-Src has been shown to play a pivotal role in breast cancer progression, metastasis, and angiogenesis. In the clinic, however, the limited efficacy and high…”
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Retraction: UM-164: A Potent c-Src/p38 Kinase Inhibitor with In Vivo Activity against Triple-Negative Breast Cancer by Gilani, Rabia A, Phadke, Sameer, Bao, Li Wei, Lachacz, Eric J, Dziubinski, Michele L, Brandvold, Kristoffer R, Steffey, Michael E, Kwarcinski, Frank E, Graveel, Carrie R, Kidwell, Kelley M, Merajver, Sofia D, Soellner, Matthew B

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Irreversible Inhibitors of c‑Src Kinase That Target a Nonconserved Cysteine by Kwarcinski, Frank E, Fox, Christel C, Steffey, Michael E, Soellner, Matthew B

“…We have developed the first irreversible inhibitors of wild-type c-Src kinase. We demonstrate that our irreversible inhibitors display improved potency and…”
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Substrate Activity Screening with Kinases: Discovery of Small-Molecule Substrate-Competitive c-Src Inhibitors by Breen, Meghan E., Steffey, Michael E., Lachacz, Eric J., Kwarcinski, Frank E., Fox, Christel C., Soellner, Matthew B.

“…Substrate‐competitive kinase inhibitors represent a promising class of kinase inhibitors, however, there is no methodology to selectively identify this type of…”
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Development of a Chimeric c‑Src Kinase and HDAC Inhibitor by Ko, Kristin S, Steffey, Michael E, Brandvold, Kristoffer R, Soellner, Matthew B

“…On the basis of synergism observed between a selective c-Src kinase inhibitor with an HDAC inhibitor, the development of the first chimeric c-Src kinase and…”
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Exquisitely Specific Bisubstrate Inhibitors of c‑Src Kinase by Brandvold, Kristoffer R, Santos, Shana M, Breen, Meghan E, Lachacz, Eric J, Steffey, Michael E, Soellner, Matthew B

“…We have developed a modular approach to bisubstrate inhibition of protein kinases. We apply our methodology to c-Src and identify a highly selective…”
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Discovery of Bivalent Kinase Inhibitors via Enzyme-Templated Fragment Elaboration by Kwarcinski, Frank E, Steffey, Michael E, Fox, Christel C, Soellner, Matthew B

“…We have employed novel fragment-based screening methodology to discover bivalent kinase inhibitors with improved selectivity. Starting from a low molecular…”
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Substrate Activity Screening with Kinases: Discovery of Small-Molecule Substrate-Competitive c-Src Inhibitors by Breen, Meghan E., Steffey, Michael E., Lachacz, Eric J., Kwarcinski, Frank E., Fox, Christel C., Soellner, Matthew B.

“…Substrate‐competitive kinase inhibitors represent a promising class of kinase inhibitors, however, there is no methodology to selectively identify this type of…”
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Abstract 2643: Human and mouse reconstructed plate-based 3-dimensional culture assays that mimic the tumor microenvironment by Steffey, Michael E., Qu, Ying, Karalewitz, Andrew, Urs, Sumithra, Kirshner, Julia, Wise, Scott

“…In order to predict efficacy and toxicity of compounds advancing in the oncology drug discovery pipeline, and to minimize requirements for multiple animal…”
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The parathyroid calcium receptor: a novel therapeutic target for treating hyperparathyroidism by Nemeth, E F, Steffey, M E, Fox, J

“…Parathyroid cells, C-cells, and certain cells in the kidney express a cell surface calcium (Ca2+) receptor which enables these cells to detect and respond to…”
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Abstract 5536: KB-164, a novel and highly potent Src family kinase inhibitor, reduces cancer cell invasion and abrogates downstream oncogenic pathways in triple negative breast cancer by Gilani, Rabia A., Brandvold, Kristoffer R., Bao, Li Wei, Phadke, Sameer, Steffey, Michael E., Soellner, Matthew B., Merajver, Sofia D.

“…Src is a non-receptor tyrosine kinase, which acts as an integrator of diverse signaling pathways used by cancer cells for cell proliferation, migration and…”
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UM-164: A Potent c-Srcp38 Kinase Inhibitor with In Vivo Activity against Triple-Negative Breast Cancer by Gilani, Rabia A, Phadke, Sameer, Bao, Li Wei, Lachacz, Eric J, Dziubinski, Michele L, Brandvold, Kristoffer R, Steffey, Michael E, Kwarcinski, Frank E, Graveel, Carrie R, Kidwell, Kelley M, Merajver, Sofia D, Soellner, Matthew B

“…Purpose: c-Src has been shown to play a pivotal role in breast cancer progression, metastasis, and angiogenesis. In the clinic, however, the limited efficacy…”
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Substrate Activity Screening for Kinases: Discovery of Small Molecule Substrate-Competitive c-Src Inhibitors by Breen, Meghan E., Steffey, Michael E., Lachacz, Eric J., Kwarcinski, Frank E., Fox, Christel C., Soellner, Matthew B.

“…Substrate-competitive kinase inhibitors represent a promising class of kinase inhibitors, however, there is no methodology to selectively identify this type of…”
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Irreversible inhibitors of c-Src kinase that target a non-conserved cysteine by Kwarcinski, Frank E., Fox, Christel C., Steffey, Michael E., Soellner, Matthew B.

“…We have developed the first irreversible inhibitors of wild-type c-Src kinase. We demonstrate that our irreversible inhibitors display improved potency and…”
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Serine mutations in transmembrane V of the dopamine D1 receptor affect ligand interactions and receptor activation by POLLOCK, N. J, MANELLI, A. M, HUTCHINS, C. W, STEFFEY, M. E, MACKENZIE, R. G, FRAIL, D. E

“…Several serines present in transmembrane domain V are conserved among members of the G-protein-coupled receptor family that bind catecholamines. Two of these…”
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Cloning and characterization of a truncated dopamine D1 receptor from goldfish retina: stimulation of cyclic AMP production and calcium mobilization by Frail, D E, Manelli, A M, Witte, D G, Lin, C W, Steffey, M E, Mackenzie, R G

“…Receptors for dopamine are present on horizontal cells of fish retina that are linked to the activation of adenylate cyclase. In the present study, the…”
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A D1/D2 chimeric dopamine receptor mediates a D1 response to a D2-selective agonist by MacKenzie, Robert G., Steffey, Michael E., Manelli, Arlene M., Pollock, Nancy J., Frail, Donald E.

“…D1 and D2 dopamine receptors are G-protein coupled receptors and have seven transmembrane spanning regions (TM) typical of this receptor superfamily. Although…”
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