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Can I read 2-(6-Phenyl-1H-indazol-3-yl)-1H-benzo[d]imidazoles: Design and synthesis of a potent and isoform selective PKC-ζ inhibitor on EtoBox?
2-(6-Phenyl-1H-indazol-3-yl)-1H-benzo[d]imidazoles: Design and synthesis of a potent and isoform selective PKC-ζ inhibitor by John I. Trujillo; James R. Kiefer; Wei Huang; Atli Thorarensen; Li Xing; Nicole L. Caspers; Jacqueline E. Day; Karl J. Mathis; Kuniko K. Kretzmer; Beverley A. Reitz; Robin A. Weinberg; Roderick A. Stegeman; Ann Wrightstone; Lori Christine; Robert Compton; Xiong Li is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is 2-(6-Phenyl-1H-indazol-3-yl)-1H-benzo[d]imidazoles: Design and synthesis of a potent and isoform selective PKC-ζ inhibitor about?
The inhibition of PKC-zeta has been proposed to be a potential drug target for immune and inflammatory diseases. A series of 2-(6-phenyl-1H indazol-3-yl)-1H-benzo[d]imidazoles with initial high crossover to CDK-2 has been optimized to afford potent and selective inhibitors of protein kinase c-zeta (PKC-zeta). The determination of the crystal structures of key inhibitor:CDK-2 complexes informed the design and analysis of the series. The most selective and potent analog was identified by variation of the aryl substituent at the 6-position of the indazole template to give a 4-NH(2) derivative. The analog displays good selectivity over other PKC isoforms (alpha, betaII, gamma, delta, epsilon, mu, theta, eta and iota/lambda) and CDK-2, however it displays marginal selectivity against a panel of other kinases (37 profiled).
Who reads 2-(6-Phenyl-1H-indazol-3-yl)-1H-benzo[d]imidazoles: Design and synthesis of a potent and isoform selective PKC-ζ inhibitor?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- John I. Trujillo; James R. Kiefer; Wei Huang; Atli Thorarensen; Li Xing; Nicole L. Caspers; Jacqueline E. Day; Karl J. Mathis; Kuniko K. Kretzmer; Beverley A. Reitz; Robin A. Weinberg; Roderick A. Stegeman; Ann Wrightstone; Lori Christine; Robert Compton; Xiong Li
- Publisher
- Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0960-894X)
- Published
- 2009
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)