Search

Your search keyword '"Eckardt, Annette J."' showing total 10 results
Start Over Author "Eckardt, Annette J."
10 results on '"Eckardt, Annette J."'

5. A Novel, Potent Dual Inhibitor of the Leukocyte Proteases Cathepsin G and Chymase

Author

de Garavilla, Lawrence, primary, Greco, Michael N., additional, Sukumar, Narayanasami, additional, Chen, Zhi-Wei, additional, Pineda, Agustin O., additional, Mathews, F. Scott, additional, Di Cera, Enrico, additional, Giardino, Edward C., additional, Wells, Grace I., additional, Haertlein, Barbara J., additional, Kauffman, Jack A., additional, Corcoran, Thomas W., additional, Derian, Claudia K., additional, Eckardt, Annette J., additional, Damiano, Bruce P., additional, Andrade-Gordon, Patricia, additional, and Maryanoff, Bruce E., additional

Published
2005
Full Text
View/download PDF

6. Novel Indolylindazolylmaleimides as Inhibitors of Protein Kinase C-β: Synthesis, Biological Activity, and Cardiovascular Safety

Author

Zhang, Han-Cheng, primary, Derian, Claudia K., additional, McComsey, David F., additional, White, Kimberly B., additional, Ye, Hong, additional, Hecker, Leonard R., additional, Li, Jian, additional, Addo, Michael F., additional, Croll, Diane, additional, Eckardt, Annette J., additional, Smith, Charles E., additional, Li, Quan, additional, Cheung, Wai-Man, additional, Conway, Bruce R., additional, Emanuel, Stuart, additional, Demarest, Keith T., additional, Andrade-Gordon, Patricia, additional, Damiano, Bruce P., additional, and Maryanoff, Bruce E., additional

Published
2004
Full Text
View/download PDF

7. Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3

Author

Zhang, Han-Cheng, primary, White, Kimberly B., additional, Ye, Hong, additional, McComsey, David F., additional, Derian, Claudia K., additional, Addo, Michael F., additional, Andrade-Gordon, Patricia, additional, Eckardt, Annette J., additional, Conway, Bruce R., additional, Westover, Lori, additional, Xu, Jun Z., additional, Look, Richard, additional, Demarest, Keith T., additional, Emanuel, Stuart, additional, and Maryanoff, Bruce E., additional

Published
2003
Full Text
View/download PDF

10. Novel indolylindazolylmaleimides as inhibitors of protein kinase C-beta: synthesis, biological activity, and cardiovascular safety.

Author

Zhang HC, Derian CK, McComsey DF, White KB, Ye H, Hecker LR, Li J, Addo MF, Croll D, Eckardt AJ, Smith CE, Li Q, Cheung WM, Conway BR, Emanuel S, Demarest KT, Andrade-Gordon P, Damiano BP, and Maryanoff BE

Subjects
Animals, Cell Line, ERG1 Potassium Channel, Ether-A-Go-Go Potassium Channels, Glycogen Synthase Kinase 3 antagonists & inhibitors, Glycogen Synthase Kinase 3 chemistry, Glycogen Synthase Kinase 3 beta, Guinea Pigs, Humans, Indazoles pharmacology, Indazoles toxicity, Indoles pharmacology, Indoles toxicity, Interleukin-8 metabolism, Isoenzymes antagonists & inhibitors, Isoenzymes chemistry, Long QT Syndrome chemically induced, Maleimides pharmacology, Maleimides toxicity, Models, Molecular, Patch-Clamp Techniques, Potassium Channel Blockers chemical synthesis, Potassium Channel Blockers chemistry, Potassium Channel Blockers pharmacology, Potassium Channels, Voltage-Gated drug effects, Potassium Channels, Voltage-Gated metabolism, Protein Kinase C chemistry, Protein Kinase C beta, Structure-Activity Relationship, Indazoles chemical synthesis, Indoles chemical synthesis, Maleimides chemical synthesis, Protein Kinase C antagonists & inhibitors
Abstract

Novel indolylindazolylmaleimides were synthesized and examined for kinase inhibition. We identified low-nanomolar inhibitors of PKC-beta with good to excellent selectivity vs other PKC isozymes and GSK-3beta. In a cell-based functional assay, 8f and 8i effectively blocked IL-8 release induced by PKC-betaII (IC(50) = 20-25 nM). In cardiovascular safety assessment, representative lead compounds bound to the hERG channel with high affinity, potently inhibited ion current in a patch-clamp experiment, and caused a dose-dependent increase of QT(c) in guinea pigs.

Published
2005
Full Text
View/download PDF

Catalog

Books, media, physical & digital resources
See catalog results