Search Results - "PIKUL, STANISLAW"

The matrix metalloproteinase inhibitor marimastat inhibits seizures in a model of kainic acid-induced status epilepticus by Pijet, Barbara, Konopka, Anna, Rejmak, Emilia, Stefaniuk, Marzena, Khomiak, Danylo, Bulska, Ewa, Pikul, Stanisław, Kaczmarek, Leszek

“…An intra-hippocampus injection of kainic acid serves as a model of status epilepticus and the subsequent development of temporal lobe epilepsy. Matrix…”
Get full text

Design and Synthesis of Piperazine-Based Matrix Metalloproteinase Inhibitors by Cheng, Menyan, De, Biswanath, Pikul, Stanislaw, Almstead, Neil G, Natchus, Michael G, Anastasio, Melanie V, McPhail, Sara J, Snider, Catherine E, Taiwo, Yetunde O, Chen, Longyin, Dunaway, C. Michelle, Gu, Fei, Dowty, Martin E, Mieling, Glen E, Janusz, Michael J, Wang-Weigand, Sherry

“…A new generation of cyclic matrix metalloproteinase (MMP) inhibitors derived from dl-piperazinecarboxylic acid has been described. The design involves: …”
Get full text

Practical enantioselective Diels-Alder and aldol reactions using a new chiral controller system by Corey, E. J, Imwinkelried, Rene, Pikul, Stanislaw, Xiang, Yi Bin

Get full text

Design, Synthesis, and Biological Evaluation of Potent Thiazine- and Thiazepine-Based Matrix Metalloproteinase Inhibitors by Almstead, Neil G, Bradley, Rimma S, Pikul, Stanislaw, De, Biswanath, Natchus, Michael G, Taiwo, Yetunde O, Gu, Fei, Williams, Lisa E, Hynd, Barbara A, Janusz, Michael J, Dunaway, C. Michelle, Mieling, Glen E

“…The synthesis and enzyme inhibition data for a series of thiazine- and thiazepine-based matrix metalloproteinase (MMP) inhibitors are described. The thiazine-…”
Get full text

Discovery of Potent, Achiral Matrix Metalloproteinase Inhibitors by Pikul, Stanislaw, McDow Dunham, Kelly L, Almstead, Neil G, De, Biswanath, Natchus, Michael G, Anastasio, Melanie V, McPhail, Sara J, Snider, Catherine E, Taiwo, Yetunde O, Rydel, Timothy, Dunaway, C. Michelle, Gu, Fei, Mieling, Glen E

Get full text

Design, Synthesis, and Biological Evaluation of Matrix Metalloproteinase Inhibitors Derived from a Modified Proline Scaffold by Cheng, Menyan, De, Biswanath, Almstead, Neil G, Pikul, Stanislaw, Dowty, Martin E, Dietsch, Charles R, Dunaway, C. Michelle, Gu, Fei, Hsieh, Lily C, Janusz, Michael J, Taiwo, Yetunde O, Natchus, Michael G, Hudlicky, Tomas, Mandel, Martin

“…The synthesis and structure−activity relationship (SAR) studies of a series of proline-based matrix metalloproteinase inhibitors are described. The data reveal…”
Get full text

Arginase 1/2 Inhibitor OATD-02: From Discovery to First-in-man Setup in Cancer Immunotherapy by Borek, Bartlomiej, Nowicka, Julita, Gzik, Anna, Dziegielewski, Marek, Jedrzejczak, Karol, Brzezinska, Joanna, Grzybowski, Marcin, Stanczak, Paulina, Pomper, Paulina, Zagozdzon, Agnieszka, Rejczak, Tomasz, Matyszewski, Krzysztof, Golebiowski, Adam, Olczak, Jacek, Lisiecki, Kamil, Tyszkiewicz, Magdalena, Kania, Magdalena, Piasecka, Sylwia, Cabaj, Anna, Dera, Paulina, Mulewski, Krzysztof, Chrzanowski, Jacek, Kusmirek, Damian, Sobolewska, Elzbieta, Magdycz, Marta, Mucha, Lukasz, Masnyk, Marek, Golab, Jakub, Nowotny, Marcin, Nowak, Elzbieta, Napiorkowska-Gromadzka, Agnieszka, Pikul, Stanislaw, Jazwiec, Radoslaw, Dzwonek, Karolina, Dobrzanski, Pawel, Meyring, Michael, Skowronek, Krzysztof, Iwanowski, Piotr, Zaslona, Zbigniew, Blaszczyk, Roman

“…Pharmacologic inhibition of the controlling immunity pathway enzymes arginases 1 and 2 (ARG1 and ARG2) is a promising strategy for cancer immunotherapy. Here,…”
Get full text

The development of new carboxylic acid-based MMP inhibitors derived from a cyclohexylglycine scaffold by Tullis, Joshua S., Laufersweiler, Matthew J., VanRens, John C., Natchus, Michael G., Bookland, Roger G., Almstead, Neil G., Pikul, Stanislaw, De, Biswanath, Hsieh, Lily C., Janusz, Michael J., Branch, Todd M., Peng, Sean X., Jin, Yingkun Y., Hudlicky, Tomas, Oppong, Kofi

“…A series of carboxylic acids was prepared based on cyclohexylglycine scaffolds and tested for potency as matrix metalloproteinase (MMP) inhibitors. Detailed…”
Get full text

A New Inhibitor of Tubulin Polymerization Kills Multiple Cancer Cell Types and Reveals p21-Mediated Mechanism Determining Cell Death after Mitotic Catastrophe by Zdioruk, Mykola, Want, Andrew, Mietelska-Porowska, Anna, Laskowska-Kaszub, Katarzyna, Wojsiat, Joanna, Klejman, Agata, Użarowska, Ewelina, Koza, Paulina, Olejniczak, Sylwia, Pikul, Stanislaw, Konopka, Witold, Golab, Jakub, Wojda, Urszula

“…Induction of mitotic catastrophe through the disruption of microtubules is an established target in cancer therapy. However, the molecular mechanisms…”
Get full text

Synthetic Process Development of BMS-599793 Including Azaindole Negishi Coupling on Kilogram Scale by Pikul, Stanislaw, Cheng, Hua, Cheng, Allen, Huang, C. D, Ke, Alex, Kuo, LungHuang, Thompson, Andrew, Wilder, Susan

“…A new approach to the synthesis of 1 (DS003, BMS-599793), a small-molecule HIV entry inhibitor, is described. The initial medical chemistry route has been…”
Get full text

Crystal structure of the stromelysin catalytic domain at 2.0 A resolution: inhibitor-induced conformational changes by Chen, L, Rydel, T J, Gu, F, Dunaway, C M, Pikul, S, Dunham, K M, Barnett, B L

“…Matrix metalloproteinases are believed to play an important role in pathological conditions such as osteoarthritis, rheumatoid arthritis and tumor invasion…”
Get full text

Development of New Hydroxamate Matrix Metalloproteinase Inhibitors Derived from Functionalized 4-Aminoprolines by Natchus, Michael G, Bookland, Roger G, De, Biswanath, Almstead, Neil G, Pikul, Stanislaw, Janusz, Michael J, Heitmeyer, Sandra A, Hookfin, Erin B, Hsieh, Lily C, Dowty, Martin E, Dietsch, Charles R, Patel, Vikram S, Garver, Susan M, Gu, Fei, Pokross, Matthew E, Mieling, Glen E, Baker, Timothy R, Foltz, David J, Peng, Sean X, Bornes, David M, Strojnowski, Michael J, Taiwo, Yetunde O

“…A series of hydroxamates was prepared from an aminoproline scaffold and tested for efficacy as matrix metalloproteinase (MMP) inhibitors. Detailed SAR for the…”
Get full text

Potent and Selective Carboxylic Acid-Based Inhibitors of Matrix Metalloproteinases by Pikul, Stanislaw, Ohler, Norman E, Ciszewski, Greg, Laufersweiler, Michael C, Almstead, Neil G, De, Biswanath, Natchus, Michael G, Hsieh, Lily C, Janusz, Michael J, Peng, Sean X, Branch, Todd M, King, Selane L, Taiwo, Yetunde O, Mieling, Glen E

“…A novel series of carboxylic acids containing a substituted piperidine were synthesized and tested for inhibition of selected matrix metalloproteinases…”
Get full text

Gas chromatographic–mass spectrometric analysis of hydroxylamine for monitoring the metabolic hydrolysis of metalloprotease inhibitors in rat and human liver microsomes by Peng, Sean X., Strojnowski, Michael J., Hu, Joanna K., Smith, Bill J., Eichhold, Thomas H., Wehmeyer, Kenneth R., Pikul, Stanislaw, Almstead, Neil G.

“…A gas chromatographic–mass spectrometric (GC–MS) method was developed for the analysis of hydroxylamine (HA) in supernatants obtained from liver microsomes. HA…”
Get full text

Design and Synthesis of Phosphinamide-Based Hydroxamic Acids as Inhibitors of Matrix Metalloproteinases by Pikul, Stanislaw, McDow Dunham, Kelly L, Almstead, Neil G, De, Biswanath, Natchus, Michael G, Anastasio, Melanie V, McPhail, Sara J, Snider, Catherine E, Taiwo, Yetunde O, Chen, Longyin, Dunaway, C. Michelle, Gu, Fei, Mieling, Glen E

“…A new series of hydroxamic acid-based matrix metalloproteinase (MMP) inhibitors containing a unique phosphinamide motif derived from d-amino acid was designed,…”
Get full text

Heterocycle-based MMP Inhibitors with P2′ Substituents by Pikul, Stanislaw, Dunham, Kelly McDow, Almstead, Neil G, De, Biswanath, Natchus, Michael G, Taiwo, Yetunde O, Williams, Lisa E, Hynd, Barbara A, Hsieh, Lily C, Janusz, Michael J, Gu, Fei, Mieling, Glen E

“…Potent and selective inhibition of matrix metalloproteinases was demonstrated for a series of sulfonamide-based hydroxamic acids. The design of the…”
Get full text

Application of LC-NMR and LC-MS to the identification of degradation products of a protease inhibitor in dosage formulations by Peng, Sean X, Borah, Babul, Dobson, Roy L.M, Liu, Y.Diana, Pikul, Stanislaw

“…LC-NMR and LC-MS were applied to the characterization of six degradation products of a protease inhibitor,…”
Get full text

The Next Generation of MMP Inhibitors: Design and Synthesis by DE, BISWANATH, NATCHUS, MICHAEL G., CHENG, MENYAN, PIKUL, STANISLAW, ALMSTEAD, NEIL G., TAIWO, YETUNDE O., SNIDER, CATHERINE E., CHEN, LONGYIN, BARNETT, BOBBY, GU, FEI, DOWTY, MARTIN

“…Since their inception during the eighties, MMP inhibitors (MMPIs) have gone through several cycles of metamorphosis. The design of early MMPIs was based on the…”
Get full text

Crystal structure of the stromelysin catalytic domain at 2.0 Å resolution: inhibitor-induced conformational changes 1 1Edited by R. Huber by Chen, Longyin, Rydel, Timothy J, Gu, Fei, Dunaway, C.Michelle, Pikul, Stanislaw, Dunham, Kelly McDow, Barnett, B.L

Get full text

Zirconium tetrachloride as a convenient catalyst for the glycosylation of sterols with 2,3,4,6,6′-penta- O-acetyl-5-hydroxymethylgalactosyl fluoride by Pikul, Stanislaw, Greg Switzer, A.

“…Zirconium tetrachloride was found to catalyze glycosylation of various sterols with peracetylated 5-hydroxymethylene galactosyl fluoride. Graphic…”
Get full text