Search Results - "COPELAND, R. A"

Purification and Cloning of Aggrecanase-1: A Member of the ADAMTS Family of Proteins by Tortorella, M. D., Burn, T. C., Pratta, M. A., Abbaszade, I., Hollis, J. M., Liu, R., Rosenfeld, S. A., Copeland, R. A., Decicco, C. P., Wynn, R., Rockwell, A., Yang, F., Duke, J. L., Solomon, K., George, H., Bruckner, R., Nagase, H., Itoh, Y., Ellis, D. M., Ross, H., Wiswall, B. H., Murphy, K., Hillman, M. C., Hollis, G. F., Newton, R. C., Magolda, R. L., Trzaskos, J. M., Arner, E. C.

“…We purified, cloned, and expressed aggrecanase, a protease that is thought to be responsible for the degradation of cartilage aggrecan in arthritic diseases…”
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A Medium-Throughput Single Cell CRISPR-Cas9 Assay to Assess Gene Essentiality by Grassian, A R, Scales, T M E, Knutson, S K, Kuntz, K W, McCarthy, N J, Lowe, C E, Moore, J D, Copeland, R A, Keilhack, H, Smith, J J, Wickenden, J A, Ribich, S

“…Target selection for oncology is a crucial step in the successful development of therapeutics. Clustered regularly interspaced short palindromic repeats…”
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Targeting genetic alterations in protein methyltransferases for personalized cancer therapeutics by Copeland, R A, Moyer, M P, Richon, V M

“…The human protein methyltransferases (PMTs) constitute a large enzyme class composed of two families, the protein lysine methyltransferases (PKMTs) and the…”
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Mechanism of Selective Inhibition of the Inducible Isoform of Prostaglandin G/H Synthase by Copeland, Robert A., Williams, Jean M., Giannaras, John, Nurnberg, Sherrill, Covington, Maryanne, Pinto, Donald, Pick, Stephen, Trzaskos, James M.

“…Selective inhibition of the inducible isoform of prostaglandin G/H synthase (cyclooxygenase-2; COX2; EC 1.14.99.1) can be achieved with compounds of the…”
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Design and Synthesis of Cyclic Inhibitors of Matrix Metalloproteinases and TNF-α Production by Xue, Chu-Biao, He, Xiaohua, Roderick, John, DeGrado, William F, Cherney, Robert J, Hardman, Karl D, Nelson, David J, Copeland, Robert A, Jaffee, Bruce D, Decicco, Carl P

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Enoyl-ACP Reductase (FabI) of Haemophilus influenzae: Steady-State Kinetic Mechanism and Inhibition by Triclosan and Hexachlorophene by Marcinkeviciene, Jovita, Jiang, Wenjun, Kopcho, Lisa M, Locke, Gregory, Luo, Ying, Copeland, Robert A

“…Steady-state kinetics, equilibrium binding, and primary substrate kinetic isotope effect studies revealed that the reduction of crotonyl-CoA by NADH, catalyzed…”
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SCFβ-TRCP and phosphorylation dependent ubiquitination of IκBα catalyzed by Ubc3 and Ubc4 by STRACK, P, CALIGIURI, M, BENFIELD, P, BRIZUELA, L, ROLFE, M, PELLETIER, M, BOISCLAIR, M, THEODORAS, A, BEER-ROMERO, P, GLASS, S, PARSONS, T, COPELAND, R. A, AUGER, K. R

“…NFκB is an important transcriptional regulator of multiple pro-inflammatory genes. In non-stimulated cells NFκB is anchored in the cytoplasm via the inhibitory…”
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Selective inhibition of bacterial dihydroorotate dehydrogenases by thiadiazolidinediones by Marcinkeviciene, Jovita, Rogers, M.John, Kopcho, Lisa, Jiang, Wenjun, Wang, Kathy, Murphy, Dennis J, Lippy, Jonathan, Link, Steven, Chung, Thomas D.Y, Hobbs, Frank, Haque, Tasir, Trainor, George L, Slee, Andrew, Stern, Andrew M, Copeland, Robert A

“…Dihydroorotate dehydrogenase is a critical enzyme of de novo pyrimidine biosynthesis in prokaryotic and eukaryotic cells. Differences in the primary structure…”
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Macrocyclic Amino Carboxylates as Selective MMP-8 Inhibitors by Cherney, Robert J, Wang, Li, Meyer, Dayton T, Xue, Chu-Baio, Wasserman, Zelda R, Hardman, Karl D, Welch, Patty K, Covington, Maryanne B, Copeland, Robert A, Arner, Elizabeth C, DeGrado, William F, Decicco, Carl P

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Limbal autograft reconstruction after conjunctival squamous cell carcinoma by Copeland, Jr, R A, Char, D H

“…Two patients who had squamous cell carcinoma with extensive limbal and corneal involvement were treated with surgery and cryotherapy. Rarely large areas of the…”
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Identification of a Novel Inhibitor of Mitogen-activated Protein Kinase Kinase by Favata, M F, Horiuchi, K Y, Manos, E J, Daulerio, A J, Stradley, D A, Feeser, W S, Van Dyk, D E, Pitts, W J, Earl, R A, Hobbs, F, Copeland, R A, Magolda, R L, Scherle, P A, Trzaskos, J M

“…The compound U0126 (1,4-diamino-2,3-dicyano-1,4-bis[2-aminophenylthio]butadiene) was identified as an inhibitor of AP-1 transactivation in a cell-based…”
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Conformational Switching at Cytochrome a During Steady-State Turnover of Cytochrome c Oxidase by Copeland, Robert A.

“…As an electron transfer-driven proton pump, cytochrome c oxidase (ferrocytochrome-c:oxygen oxidoreductase, EC 1.9.3.1) must alternate between two conformations…”
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Histidine to alanine mutants of human dihydroorotate dehydrogenase: Identification of a brequinar-resistant mutant enzyme by Davis, June P., Copeland, Robert A.

“…Dihydroorotate dehydrogenase (DHODase) is the rate-limiting enzyme of the mammalian de novo pyrimidine biosynthesis pathway, and is the molecular target of the…”
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Presenilin-1 and -2 Are Molecular Targets for γ-Secretase Inhibitors by Seiffert, Dietmar, Bradley, Jodi D., Rominger, Cynthia M., Rominger, David H., Yang, Fude, Meredith, Jere E., Wang, Qian, Roach, Arthur H., Thompson, Lorin A., Spitz, Susan M., Higaki, Jeffrey N., Prakash, Shimoga R., Combs, Andrew P., Copeland, Robert A., Arneric, Stephen P., Hartig, Paul R., Robertson, David W., Cordell, Barbara, Stern, Andrew M., Olson, Richard E., Zaczek, Robert

“…Presenilins are integral membrane protein involved in the production of amyloid β-protein. Mutations of the presenilin-1 and -2 gene are associated with…”
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Deep-ultraviolet Raman excitation profiles and vibronic scattering mechanisms of phenylalanine, tyrosine, and tryptophan by Fodor, Stephen P. A, Copeland, Robert A, Grygon, Christine A, Spiro, Thomas G

“…Raman cross sections for excitation at wavelengths between 240 and 192 nm have been determined for resonance-enhanced ring modes of phenylalanine (Phe),…”
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Kinetic Effects Due to Nonspecific Substrate-Inhibitor Interactions in Enzymatic Reactions by Copeland, Robert A., Horiuchi, Kurumi Y.

“…Nonspecific protein binding is a commonly encountered problem with synthetic molecules designed as enzyme inhibitors. When the substrate for the enzymatic…”
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Macrocyclic hydroxamate inhibitors of matrix metalloproteinases and TNF-α production by Cherney, Robert J., Wang, Li, Meyer, Dayton T., Xue, Chu-Biao, Arner, Elizabeth C., Copeland, Robert A., Covington, Maryanne B., Hardman, Karl D., Wasserman, Zelda R., Jaffee, Bruce D., Decicco, Carl P.

“…Several macrocyclic, hydroxamate derivatives were synthesized and evaluated as inhibitors of matrix metalloproteinases (MMPs) and tumour necrosis factor-α…”
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Structure-based design and synthesis of a series of hydroxamic acids with a quaternary-hydroxy group in P1 as inhibitors of matrix metalloproteinases by Jacobson, Irina C., Reddy, Prabhakar G., Wasserman, Zelda R., Hardman, Karl D., Covington, Maryanne B., Arner, Elizabeth C., Copeland, Robert A., Decicco, Carl P., Magolda, Ronald L.

“…Examination of the S1 area of the active site of pro-stromelysin has led us to the design of novel and potent inhibitors of matrix metalloproteinases…”
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Heteroatom- and carbon-linked biphenyl analogs of Brequinar as immunosuppressive agents by Batt, Douglas G., Petraitis, Joseph J., Sherk, Susan R., Copeland, Robert A., Dowling, Randine L., Taylor, Tracy L., Jones, Elizabeth A., Magolda, Ronald L., Jaffee, Bruce D.

“…Structure-activity relationships were explored for some analogs of Brequinar having a linking atom between the 2-biphenyl substituent and the quinoline ring…”
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Terphenyl cyclooxygenase-2 (COX-2) inhibitors: Optimization of the central ring and o-biphenyl analogs by Pinto, Donald J.P., Batt, Douglas G., Pitts, William J., Petraitis, Joseph J., Orwat, Michael J., Wang, Shuaige, Jetter, James W., Sherk, Susan R., Houghton, Gregory C., Copeland, Robert A., Covington, Maryanne B., Trzaskos, James M., Magolda, Ronald L.

“…The discovery of terphenyl derivatives as highly selective COX-2 inhibitors resulted from our efforts to overcome poor pharmacokinetics demonstrated by the…”
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