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Can I read Discovery and Biological Activity of 6BrCaQ as an Inhibitor of the Hsp90 Protein Folding Machinery on EtoBox?
Discovery and Biological Activity of 6BrCaQ as an Inhibitor of the Hsp90 Protein Folding Machinery by Dr. Davide Audisio; Dr. Samir Messaoudi; Lukasz Cegielkowski; Prof. Jean-François Peyrat; Prof. Jean-Daniel Brion; Dr. Délphine Methy-Gonnot; Dr. Christine Radanyi; Dr. Jack-Michel Renoir; Dr. Mouâd Alami is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is Discovery and Biological Activity of 6BrCaQ as an Inhibitor of the Hsp90 Protein Folding Machinery about?
## Abstract Heat shock protein 90 (Hsp90) is a significant target in the development of rational cancer therapy, due to its role at the crossroads of multiple signaling pathways associated with cell proliferation and viability. Here, a novel series of Hsp90 inhibitors containing a quinolein‐2‐one scaffold was synthesized and evaluated in cell proliferation assays. Results from these structure–activity relationships studies enabled identification of the simplified 3‐aminoquinolein‐2‐one analogue **2 b** (6BrCaQ), which manifests micromolar activity against a panel of cancer cell lines. The molecular signature of Hsp90 inhibition was assessed by depletion of standard known Hsp90 client proteins. Finally, processing and activation of caspases 7, 8, and 9, and the subsequent cleavage of PARP by 6BrCaQ, suggest stimulation of apoptosis through both extrinsic and intrinsic pathways.
Who reads Discovery and Biological Activity of 6BrCaQ as an Inhibitor of the Hsp90 Protein Folding Machinery?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Dr. Davide Audisio; Dr. Samir Messaoudi; Lukasz Cegielkowski; Prof. Jean-François Peyrat; Prof. Jean-Daniel Brion; Dr. Délphine Methy-Gonnot; Dr. Christine Radanyi; Dr. Jack-Michel Renoir; Dr. Mouâd Alami
- Publisher
- John Wiley and Sons; Wiley (John Wiley & Sons); Wiley - V C H Verlag GmbbH & Co.; Wiley (ISSN 1860-7179)
- Published
- 2011
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)