Search

Your search keyword '"Cook, Andrew S."' showing total 23 results
Start Over Author "Cook, Andrew S." Search Limiters Full Text
23 results on '"Cook, Andrew S."'

1. EZH2 Inhibitor Efficacy in Non-Hodgkin’s Lymphoma Does Not Require Suppression of H3K27 Monomethylation

Author

Bradley, William D., Arora, Shilpi, Busby, Jennifer, Balasubramanian, Srividya, Gehling, Victor S., Nasveschuk, Christopher G., Vaswani, Rishi G., Yuan, Chih-Chi, Hatton, Charlie, Zhao, Feng, Williamson, Kaylyn E., Iyer, Priyadarshini, Méndez, Jacqui, Campbell, Robert, Cantone, Nico, Garapaty-Rao, Shivani, Audia, James E., Cook, Andrew S., Dakin, Les A., Albrecht, Brian K., Harmange, Jean-Christophe, Daniels, Danette L., Cummings, Richard T., Bryant, Barbara M., Normant, Emmanuel, and Trojer, Patrick

Published
2014
Full Text
View/download PDF

3. Porphyrazinediols: synthesis, characterization, and complexation to group IVB metallocenes

Author

Bellec, Nathalie, Montalban, Antonio Garrido, Williams, D. Bradley G., Cook, Andrew S., Anderson, Mairin E., Feng, Xidong, Barrett, Anthony G.M., and Hoffman, Brian M.

Subjects
Organic compounds -- Synthesis, Organometallic compounds -- Analysis, Organometallic chemistry -- Research, Ligands -- Analysis, Biological sciences, Chemistry
Abstract

Research describes the synthesis of porphyrazinediols, their conversion into solitaire complexes, and chemical oxidation of the polydentate noninnocent macrocycles. Results demonstrate that porphyrazinediols are a novel class of redox-active ligands whose diol chelating group is directly attached at the beta-positions of the macrocycle.

Published
2000

4. Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B-Cell Lymphomas

Author

Vaswani, Rishi G., Gehling, Victor S., Dakin, Les A., Cook, Andrew S., Nasveschuk, Christopher G., Duplessis, Martin, Iyer, Priyadarshini, Balasubramanian, Srividya, Zhao, Feng, Good, Andrew C., Campbell, Robert, Lee, Christina, Cantone, Nico, Cummings, Richard T., Normant, Emmanuel, Bellon, Steven F., Albrecht, Brian K., Harmange, Jean-Christophe, Trojer, Patrick, Audia, James E., Zhang, Ying, Justin, Neil, Chen, Shuyang, Wilson, Jon R., and Gamblin, Steven J.

Subjects
Models, Molecular, Indoles, Lymphoma, B-Cell, Clinical Trials, Phase I as Topic, Dose-Response Relationship, Drug, Molecular Structure, Antineoplastic Agents, macromolecular substances, Histone-Lysine N-Methyltransferase, Neoplasms, Experimental, Article, Rats, Structure-Activity Relationship, Dogs, Piperidines, Histone Methyltransferases, Animals, Humans, Drug Screening Assays, Antitumor, Enzyme Inhibitors, Cell Proliferation
Abstract

Polycomb repressive complex 2 (PRC2) has been shown to play a major role in transcriptional silencing in part by installing methylation marks on lysine 27 of histone 3. Dysregulation of PRC2 function correlates with certain malignancies and poor prognosis. EZH2 is the catalytic engine of the PRC2 complex and thus represents a key candidate oncology target for pharmacological intervention. Here we report the optimization of our indole-based EZH2 inhibitor series that led to the identification of CPI-1205, a highly potent (biochemical IC50 = 0.002 μM, cellular EC50 = 0.032 μM) and selective inhibitor of EZH2. This compound demonstrates robust antitumor effects in a Karpas-422 xenograft model when dosed at 160 mg/kg BID and is currently in Phase I clinical trials. Additionally, we disclose the co-crystal structure of our inhibitor series bound to the human PRC2 complex.

Published
2016

6. Book reviews

Author

Grim, Ronald E., primary, Woodward, David, additional, Karrow, Robert W., additional, Glazer, George D., additional, Mokre, Jan, additional, Avdoyan, Levon, additional, Edson, Evelyn, additional, Goodrich, Thomas D., additional, Richard, Hélène, additional, Steven, Michael D., additional, McCorkle, Barbara B., additional, McDermott, Paul D., additional, Akerman, James R., additional, Mullan, Anthony Páez, additional, Rebert, Paula, additional, Cook, Andrew S., additional, Prince, Hugh, additional, Molen van Ee, Patricia, additional, Engstrom, Kathryn L., additional, Warner, Deborah Jean, additional, and Andrews, J. H., additional

Published
2001
Full Text
View/download PDF

7. Reviews

Author

Ferguson, Paul, primary, Woodward, David, additional, Gruber, Mayer I., additional, Ruggles, Richard I., additional, Swift, Katherine, additional, Harvey, P.D.A., additional, Sporrong, Ulf, additional, Bennett, J.A., additional, Baigent, Elizabeth, additional, Pedley, Mary, additional, Oliver, Richard, additional, Bremner, R.W., additional, Andrews, J.H., additional, Bevilacqua, Mario, additional, Cook, Andrew S., additional, and Herbert, Francis, additional

Published
1994
Full Text
View/download PDF

9. Reviews

Author

Ferguson, Paul, primary, Cook, Andrew S., additional, Pastoureau, Mireille, additional, O'Brien, C. I. M., additional, Royle, Stephen A., additional, Burden, Eugene, additional, Bravo‐Dobrée, Michael, additional, Simms, Anngret, additional, Bennett, J. A., additional, Pelletier, Monique, additional, Puig, Esther Carnice, additional, Hameleers, Marc, additional, Gallez, Paul, additional, and Astengo, Corradino, additional

Published
1991
Full Text
View/download PDF

10. Reviews

Author

Ferguson, Paul, primary, Meurer, Peter H., additional, Koeman, C., additional, Elliot, James D., additional, Dilke, O. A. W., additional, Pedley, Mary Sponberg, additional, Mumford, Ian, additional, Bosse, David, additional, Scharfe, Wolfgang, additional, Godlewska, Anne, additional, Delano‐Smith, Catherine, additional, Davis, John F., additional, Smyth, W. J., additional, Hopkins, Daniel, additional, Andrews, J. H., additional, Swift, Katherine, additional, Moore, John N., additional, Haworth, Richard, additional, Clutton, Elizabeth, additional, Tyner, Judith A., additional, Bremner, R. W., additional, Herries Davies, Gordon L., additional, Bendall, A. Sarah, additional, and Cook, Andrew S., additional

Published
1990
Full Text
View/download PDF

11. Variation in the biologic and biochemical characteristics of human menopausal gonadotropin**Presented at the Forty-Third Annual Meeting of The American Fertility Society, September 28 to 30, 1987, Reno, Nevada, and awarded the Associate Member’s Forum Prize Paper.††Supported in part by the Wesley Medical Research Institutes and the Women’s Research Institute, Wichita, Kansas.

Author

Cook, Andrew S., Webster, Bobby W., Terranova, Paul F., and Keel, Brooks A.

Abstract

Lot differences in the biopotency of human menopausal gonadotropin (hMG) were evaluated and the potential biochemical basis was investigated. The in vivo biopotency of hMG was assessed by a unique bioassay that evaluates the number of ova shed in the cyclic hamster in response to hMG administration. Significant variation in hMG lots was observed using this assay. When subjected to chromatofocusing, hMG displayed five immunoreactive follicle-stimulating hormone (FSH) isohormones and nine luteinizing hormone (LH) isohormones. The relative distribution of FSH, but not LH isohormones, was slightly but significantly different between the lots tested. These data indicate that significant differences exist in the ability of commercially available hMG to stimulate follicular development and ovulation. The biochemical basis for these differences in in vivo biopotency remains to be elucidated.

Published
1988
Full Text
View/download PDF

18. Reviews

Author

Hodson, Yolande, primary, Pelletier, Monique, additional, Beckingham, C.F., additional, Shirley, Rodney W., additional, Fairclough, Roger H., additional, Simms, Anngret, additional, Hyde, Ralph, additional, Johnson, Hildegard Binder, additional, Koeman, C., additional, Stone, Jeffrey C., additional, Ravenhill, William, additional, Robinson, A. H. W., additional, Babicz, J., additional, Desreumaux, Roger, additional, Valerio, Vladimiro, additional, Persi, Peris, additional, Dilke, O. A. W., additional, Cook, Andrew S., additional, Cross, David A, additional, and Danforth, Susan, additional

Published
1983
Full Text
View/download PDF

19. Reviews

Author

Barber, Peter, primary, Pastoureau, Mireille, additional, Koeman, C., additional, Kupčík, Ivan, additional, and Cook, Andrew S., additional

Published
1988
Full Text
View/download PDF

20. Reviews

Author

Cook, Andrew S., primary, Martin, G. H., additional, Cook, Karen S., additional, Sargent, John, additional, Mumford, Ian, additional, Lenman, Bruce P., additional, and Clark, Peter K., additional

Published
1989
Full Text
View/download PDF

21. Reviews

Author

Mead, W. R., primary, Harvey, P. D. A., additional, Tyacke, Sarah, additional, Smith, Catherine Delano, additional, Herries Davies, Gordon L., additional, Sebert, L. M., additional, Wallis, Helen, additional, Fairclough, Roger H., additional, Ravenhill, William, additional, Andrews, J. H., additional, Danckaert, Lisette, additional, Kretschmer, Ingrid, additional, Mikos, Michael J., additional, Kupčík, Ivan, additional, Szykula, Krystyna, additional, Unno, Kazutaka, additional, Stone, Jeffrey C., additional, Killen, James E., additional, Cumming, William P., additional, Lewis, G. Malcolm, additional, Pearson, Karen Severud, additional, and Cook, Andrew S., additional

Published
1985
Full Text
View/download PDF

Catalog

Books, media, physical & digital resources
See catalog results