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Can I read Design and synthesis of pyridine–pyrazolopyridine-based inhibitors of protein kinase B/Akt on EtoBox?
Design and synthesis of pyridine–pyrazolopyridine-based inhibitors of protein kinase B/Akt by Gui-Dong Zhu; Jianchun Gong; Viraj B. Gandhi; Keith Woods; Yan Luo; Xuesong Liu; Ran Guan; Vered Klinghofer; Eric F. Johnson; Vincent S. Stoll; Mulugeta Mamo; Qun Li; Saul H. Rosenberg; Vincent L. Giranda is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is Design and synthesis of pyridine–pyrazolopyridine-based inhibitors of protein kinase B/Akt about?
Thr-211 is one of three different amino acid residues in the kinase domain of protein kinase B/Akt as compared to protein kinase A (PKA), a closely related analog in the same AGC family. In an attempt to improve the potency and selectivity of our indazole-pyridine series of Akt inhibitors over PKA, efforts have focused on the incorporation of a chemical functionality to interact with the hydroxy group of Thr-211. Several substituents including an oxygen anion, amino, and nitro groups have been introduced at the C-6 position of the indazole scaffold, leading to a significant drop in Akt potency. Incorporation of a nitrogen atom into the phenyl ring at the same position (i.e., 9f) maintained the Akt activity and, in some cases, improved the selectivity over PKA. The structure-activity relationships of the new pyridine-pyrazolopyridine series of Akt inhibitors and their structural features when bound to PKA are also discussed.
Who reads Design and synthesis of pyridine–pyrazolopyridine-based inhibitors of protein kinase B/Akt?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Gui-Dong Zhu; Jianchun Gong; Viraj B. Gandhi; Keith Woods; Yan Luo; Xuesong Liu; Ran Guan; Vered Klinghofer; Eric F. Johnson; Vincent S. Stoll; Mulugeta Mamo; Qun Li; Saul H. Rosenberg; Vincent L. Giranda
- Publisher
- Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)
- Published
- 2007
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)