Search Results - "Ripka, William C."

Discovery and SAR of a Novel Selective and Orally Bioavailable Nonpeptide Classical Competitive Inhibitor Class of Protein-Tyrosine Phosphatase 1B by Andersen, Henrik Sune, Olsen, Ole H, Iversen, Lars F, Sørensen, Anette L. P, Mortensen, Steen B, Christensen, Michael S, Branner, Sven, Hansen, Thomas K, Lau, Jesper F, Jeppesen, Lone, Moran, Edmond J, Su, Jing, Bakir, Farid, Judge, Luke, Shahbaz, Manou, Collins, Tassie, Vo, Todd, Newman, Michael J, Ripka, William C, Møller, Niels Peter H

“…Reversible phosphorylation and dephosphorylation of key proteins on tyrosine residues are important parts of intracellular signaling triggered by hormones and…”
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Inhibition of Fructose-1,6-bisphosphatase by a New Class of Allosteric Effectors by Choe, Jun-Young, Nelson, Scott W., Arienti, Kristen L., Axe, Frank U., Collins, Tassie L., Jones, Todd K., Kimmich, Rachel D.A., Newman, Michael J., Norvell, Karl, Ripka, William C., Romano, Suzanne J., Short, Kevin M., Slee, Deborah H., Fromm, Herbert J., Honzatko, Richard B.

“…A highly constrained pseudo-tetrapeptide (OC252-324) further defines a new allosteric binding site located near the center of fructose-1,6-bisphosphatase. In a…”
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High-throughput purification of compound libraries by Ripka, William C, Barker, Geoffrey, Krakover, Jonathan

“…Synthesis of combinatorial libraries by parallel synthesis, followed by high- throughput biological screening, is the new paradigm for drug discovery. Purity…”
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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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Development of Potent Non-Carbohydrate Imidazole-Based Small Molecule Selectin Inhibitors with Antiinflammatory Activity by Slee, Deborah H, Romano, Suzanne J, Yu, Jinghua, Nguyen, Truc N, John, Judy K, Raheja, Neil K, Axe, Frank U, Jones, Todd K, Ripka, William C

“…A novel series of non-carbohydrate imidazole-based selectin inhibitors has been discovered via high-throughput screening using a P-selectin ELISA-based assay…”
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New thrombin inhibitors in cardiovascular disease by Ripka, William C

“…Thrombin is a multifunctional serine protease that plays a primary role in the pathogenic pathway of thrombosis as a consequence of its actions on the two…”
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Design, Synthesis, and Evolution of a Novel, Selective, and Orally Bioavailable Class of Thrombin Inhibitors:  P1-Argininal Derivatives Incorporating P3-P4 Lactam Sulfonamide Moieties by Semple, J. Edward, Rowley, David C, Brunck, Terence K, Ha-Uong, Theresa, Minami, Nathaniel K, Owens, Timothy D, Tamura, Susan Y, Goldman, Erick A, Siev, Daniel V, Ardecky, Robert J, Carpenter, Stephen H, Ge, Yu, Richard, Brigitte M, Nolan, Thomas G, Håkanson, Kjell, Tulinsky, Al, Nutt, Ruth F, Ripka, William C

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Rational design, synthesis, and serine protease inhibitory activity of novel P1-argininoyl heterocycles by TAMURA, S. Y, SHAMBLIN, B. M, BRUNCK, T. K, RIPKA, W. C

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Potent and Selective Thrombin Inhibitors Incorporating the Constrained Arginine Mimic l-3-Piperidyl(N-guanidino)alanine at P1 by Levy, Odile E, Semple, J. Edward, Lim, Michael L, Reiner, John, Rote, William E, Dempsey, Erin, Richard, Brigitte M, Zhang, Erli, Tulinsky, Al, Ripka, William C, Nutt, Ruth F

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Tapping into three dimensions by Ripka, William C

“…The new journal, "Journal of Computer-Aided Molecular Design," brings together reports of research directed towards all of the applications implied by its…”
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Decyanation of tertiary nitriles by alkyllithium reagents observed during the synthesis of imidazoles pendant to a quaternary carbon center by Gregory, George B, Johnson, Alexander L, Ripka, William C

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Study of the shape of the binding site of bovine opsin using 10-substituted retinal isomers by Asato, Alfred E, Denny, Marlene, Matsumoto, Hiroyuki, Mirzadegan, Taraneh, Ripka, William C, Crescitelli, Frederick, Liu, Robert S. H

“…The 9-cis, 11-cis, 13-cis, and all-trans isomers of 10-fluoro-, 10-chloro-, 10-methyl-, and 10-ethylretinals have been prepared and characterized. Results of…”
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Synthesis and biological activity of P2–P4 azapeptidomimetic P1-argininal and P1-ketoargininamide derivatives: a novel class of serine protease inhibitors by Semple, J.Edward, Rowley, David C., Brunck, Terence K., Ripka, William C.

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Dependence of hyperconjugative spin-spin coupling upon electron demand by Ripka, William C, Applequist, Douglas E

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Synthesis and biological activity of P 2–P 4 azapeptidomimetic P 1-argininal and P 1-ketoargininamide derivatives: a novel class of serine protease inhibitors by Semple, J.Edward, Rowley, David C., Brunck, Terence K., Ripka, William C.

“…Molecular modeling and topographic considerations of the thrombin-specific sequences Boc-Asp-Pro-Arg-TS or Ac-d-Phe-Pro-Arg-TS (TS = transition state analog…”
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Rational design, synthesis, and serine protease inhibitory activity of a novel P1-argininal derivative featuring a conformationally constrained P2-P3 bicyclic lactam moiety by TAMURA, S. Y, GOLDMAN, E. A, BRUNCK, T. K, RIPKA, W. C, SEMPLE, J. E

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Rational design and synthesis of a novel, selective class of thrombin inhibitors: P1-argininal derivatives incorporating P3P4 quaternary lactam dipeptide surrogates by Semple, J.Edward, Minami, Nathaniel K., Tamura, Susan Y., Brunck, Terence K., Nutt, Ruth F., Ripka, William C.

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Rational design, synthesis, and serine protease inhibitory activity of a novel P 1-argininal derivative featuring a conformationally constrained P 2–P 3 bicyclic lactam moiety by Tamura, Susan Y., Goldman, Erick A., Brunck, Terence K., Ripka, William C., Edward Semple, J.

“…Based on molecular modeling and judicious combination of the salient topographic features of the recently discovered P 3-lactam derivative 1 with the P…”
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Potent and Selective Thrombin Inhibitors Incorporating the Constrained Arginine Mimic l -3-Piperidyl( N -guanidino)alanine at P 1 by Levy, Odile E., Semple, J. Edward, Lim, Michael L., Reiner, John, Rote, William E., Dempsey, Erin, Richard, Brigitte M., Zhang, Erli, Tulinsky, Al, Ripka, William C., Nutt, Ruth F.

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RATIONAL DESIGN, SYNTHESIS, AND SERINE PROTEASE INHIBITORY ACTIVITY OF NOVEL P 1-ARGININOYL HETEROCYCLES by Tamura, Susan Y, Shamblin, Brian M, Brunck, Terence K, Ripka, William C

“…Peptidomimetic derivatives featuring a P 1-argininoyl heterocycle were designed. The preparation of two key building blocks containing benzoxazole or…”
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