Search Results - "MAY, Earl"

Type IIA topoisomerase inhibition by a new class of antibacterial agents by Giordano, Ilaria, Spitzfaden, Claus E, Jones, Emma, Theobald, Andrew J, Gorrec, Fabrice, Jones, Jo, Hann, Michael M, May, Earl W, Saunders, Martin R, Fosberry, Andrew, Chan, Pan F, Eggleston, Drake S, Hibbs, Martin, Brown, Kristin Koretke, Lewis, Ceri J, Bax, Benjamin D, Singh, Onkar, Pearson, Neil D, Wohlkonig, Alexandre, Hennessy, Alan, Gentry, Daniel R, Huang, Jianzhong, Shen, Carol, Gwynn, Michael N, Shillings, Anthony

“…Despite the success of genomics in identifying new essential bacterial genes, there is a lack of sustainable leads in antibacterial drug discovery to address…”
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Demystifying Functional Parameters for Irreversible Enzyme Inhibitors by Heppner, David E, Ogboo, Blessing C, Urul, Daniel A, May, Earl W, Schaefer, Erik M, Murkin, Andrew S, Gehringer, Matthias

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Pitfalls and Considerations in Determining the Potency and Mutant Selectivity of Covalent Epidermal Growth Factor Receptor Inhibitors by Hoyt, Kristopher W, Urul, Daniel A, Ogboo, Blessing C, Wittlinger, Florian, Laufer, Stefan A, Schaefer, Erik M, May, Earl W, Heppner, David E

“…Enzyme inhibitors that form covalent bonds with their targets are being increasingly pursued in drug development. Assessing their biochemical activity relies…”
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Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448) by Heppner, David E., Wittlinger, Florian, Beyett, Tyler S., Shaurova, Tatiana, Urul, Daniel A., Buckley, Brian, Pham, Calvin D., Schaeffner, Ilse K., Yang, Bo, Ogboo, Blessing C., May, Earl W., Schaefer, Erik M., Eck, Michael J., Laufer, Stefan A., Hershberger, Pamela A.

“…Lazertinib (YH25448) is a novel third-generation tyrosine kinase inhibitor (TKI) developed as a treatment for EGFR mutant non-small cell lung cancer. To better…”
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Reversible linkage of two distinct small molecule inhibitors of Myc generates a dimeric inhibitor with improved potency that is active in myc over-expressing cancer cell lines by Wanner, Jutta, Romashko, Darlene, Werner, Douglas S, May, Earl W, Peng, Yue, Schulz, Ryan, Foreman, Kenneth W, Russo, Suzanne, Arnold, Lee D, Pingle, Maneesh, Bergstrom, Donald E, Barany, Francis, Thomson, Stuart

“…We describe the successful application of a novel approach for generating dimeric Myc inhibitors by modifying and reversibly linking two previously described…”
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Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885 by KING, Alastair J, PATRICK, Denis R, HUGGER, Erin, LIFU WANG, KARRETH, Florian, LOUGHEED, Julie C, LEE, Jae, CHAU, David, STOUT, Thomas J, MAY, Earl W, ROMINGER, Cynthia M, SCHABER, Michael D, BATORSKY, Roberta S, LUSONG LUO, LAKDAWALA, Ami S, ADAMS, Jerry L, CONTRACTOR, Rooja G, SMALLEY, Keiran S. M, HERLYN, Meenhard, MORRISSEY, Michael M, TUVESON, David A, HUANG, Pearl S, HO, Maureen L, DO, Hieu T, SHU YUN ZHANG, KUMAR, Rakesh, RUSNAK, David W, TAKLE, Andrew K, WILSON, David M

“…Oncogenic BRAF alleles are both necessary and sufficient for cellular transformation, suggesting that chemical inhibition of the activated mutant protein…”
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Interaction between chloride and both macro- and micronutrients in annual canarygrass by Earl May, William, MacGregor, Michael

“…Annual canarygrass (Phalaris canariensis L.) has a larger response to chloride (Cl−) fertilizer than other cereal crops. This unexpected response prompted…”
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Linking ATP and allosteric sites to achieve superadditive binding with bivalent EGFR kinase inhibitors by Wittlinger, Florian, Ogboo, Blessing C., Shevchenko, Ekaterina, Damghani, Tahereh, Pham, Calvin D., Schaeffner, Ilse K., Oligny, Brandon T., Chitnis, Surbhi P., Beyett, Tyler S., Rasch, Alexander, Buckley, Brian, Urul, Daniel A., Shaurova, Tatiana, May, Earl W., Schaefer, Erik M., Eck, Michael J., Hershberger, Pamela A., Poso, Antti, Laufer, Stefan A., Heppner, David E.

“…Bivalent molecules consisting of groups connected through bridging linkers often exhibit strong target binding and unique biological effects. However,…”
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Discovery of Novel Insulin-Like Growth Factor‑1 Receptor Inhibitors with Unique Time-Dependent Binding Kinetics by Jin, Meizhong, Petronella, Brenda A, Cooke, Andy, Kadalbajoo, Mridula, Siu, Kam W, Kleinberg, Andrew, May, Earl W, Gokhale, Prafulla C, Schulz, Ryan, Kahler, Jennifer, Bittner, Mark A, Foreman, Kenneth, Pachter, Jonathan A, Wild, Robert, Epstein, David, Mulvihill, Mark J

“…This letter describes a series of small molecule inhibitors of IGF-1R with unique time-dependent binding kinetics and slow off-rates. Structure–activity and…”
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An intrinsic ATPase activity of phospho-MEK-1 uncoupled from downstream ERK phosphorylation by Rominger, Cynthia M., Schaber, Michael D., Yang, Jingsong, Gontarek, Richard R., Weaver, Kurt L., Broderick, Timothy, Carter, Luke, Copeland, Robert A., May, Earl W.

“…We have developed a highly sensitive assay of MEK-mediated ATP hydrolysis by coupling the formation of ADP to NADH oxidation through the enzymes pyruvate…”
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Unexpected Structural Diversity in DNA Recombination: The Restriction Endonuclease Connection by Hickman, Alison Burgess, Li, Ying, Mathew, Shiny Varghese, May, Earl W, Craig, Nancy L, Dyda, Fred

“…Transposition requires a coordinated series of DNA breakage and joining reactions. The Tn7 transposase contains two proteins: TnsA, which carries out DNA…”
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Fluorescence Polarization Method To Characterize Macrolide-Ribosome Interactions by KANG YAN, HUNT, Eric, BERGE, John, MAY, Earl, COPELAND, Robert A, GONTAREK, Richard R

“…Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley Reddit…”
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Discovery of an Orally Efficacious Imidazo[5,1-f][1,2,4]triazine Dual Inhibitor of IGF-1R and IR by Jin, Meizhong, Gokhale, Prafulla C, Cooke, Andy, Foreman, Kenneth, Buck, Elizabeth, May, Earl W, Feng, Lixin, Bittner, Mark A, Kadalbajoo, Mridula, Landfair, Darla, Siu, Kam W, Stolz, Kathryn M, Werner, Douglas S, Laufer, Radoslaw S, Li, An-Hu, Dong, Hanqing, Steinig, Arno G, Kleinberg, Andrew, Yao, Yan, Pachter, Jonathan A, Wild, Robert, Mulvihill, Mark J

“…This report describes the investigation of a series of 5,7-disubstituted imidazo[5,1-f][1,2,4]triazine inhibitors of insulin-like growth factor-1 receptor…”
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Switching from Cut-and-Paste to Replicative Tn7 Transposition by May, Earl W., Craig, Nancy L.

“…The bacterial transposon Tn7 usually moves through a cut-and-paste mechanism where-by the transposon is excised from a donor site and joined to a target site…”
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Pitfalls and Considerations in Determining the Potency and Mutant Selectivity of Covalent Epidermal Growth Factor Receptor Inhibitors: Miniperspective by Hoyt, Kristopher W., Urul, Daniel A., Ogboo, Blessing C., Wittlinger, Florian, Laufer, Stefan A., Schaefer, Erik M., May, Earl W., Heppner, David E.

“…Enzyme inhibitors that form covalent bonds with their targets are being increasingly pursued in drug development. Assessing their biochemical activity relies…”
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Abstract 1426: Sox-based sensor phosphopeptides for continuous, homogeneous and quantitative monitoring of protein phosphatase activity by Cornell-Kennon, Susan, Schaefer, Erik, May, Earl, Hakar, Matthew

“…Introduction: The aberrant activation of oncogenic signaling pathways can drive tumorigenesis and malignant transformation, where deregulation of the activity…”
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Abstract 1666: A novel sox-based continuous and homogeneous assay for the discovery of inhibitors of inactive and active AKT by Cornell-Kennon, Susan, Urul, Daniel, Hakar, Matthew, McMahon, Hayley, Huynh, Khanh, May, Earl, Schaefer, Erik

“…Introduction: The activity of protein kinases plays a critical role in the aberrant activation of oncogenic signaling pathways which can drive tumorigenesis…”
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Abstract 2061: A proven activity-based workflow for the identification and characterization of time-dependent kinase inhibitors using a continuous assay format by May, Earl, Urul, Daniel, Huynh, Khanh, Cornell-Kennon, Susan, Nemmara, Venkatesh, Lu, Zhibing, Hoare, Samuel, Lyles, Michelle, Schaefer, Erik

“…Time-dependent inhibitors (TDIs) of enzyme targets offer distinct advantages for the development of potent and selective compounds with favorable…”
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Abstract 1676: A continuous kinetic assay to quantitate specific protein kinase activity in unfractionated cell lysates by Nemmara, Venkatesh, Cornell-Kennon, Susan, Lu, Zhibing, Pikul, Gabriela, Belisle, Zacchary, Hakar, Matthew, Chin, Jefferson, Schaefer, Erik, May, Earl

“…Protein kinases form a network of signaling pathways and are modified by multiple post-translational modifications, including phosphorylation, which regulate…”
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Abstract A06: Biophysical and biochemical characterization of KRAS G12C inhibition through the SMARTTM platform by Zhou, Minyun, Yuzhakov, Alexander, Benod, Cindy C, Xue, Linlong, Silver, Alec D, Iyer, Ganesh, Townson, Sharon A., Jin, Meizhong, Perl, Nicholas R., Kohlmann, Anna, Mann, Alan S., Akcay, Gizem, May, Earl W.

“…RAS proteins are small GTPases involved in cell proliferation, survival, and differentiation, and are mutationally activated in about a third of all human…”
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