AI Article Synopsis
- Hsp90 is an important chaperone overexpressed in many cancers, making it a key target for drug discovery.
- Novobiocin, an antibiotic, has been shown to inhibit Hsp90 and exhibits anti-cancer properties, prompting the development of better compounds.
- A new series of novobiocin analogs were created, tested on breast cancer cell lines, and analyzed for their effects on cell cycle progression, apoptosis, and Hsp90 client protein degradation.
Article Abstract
Hsp90 is an ATP-dependent chaperone known to be overexpressed in many cancers. This way, Hsp90 is an important target for drug discovery. Novobiocin, an aminocoumarin antibiotic, was reported to inhibit Hsp90 targeting C-terminal domain, and showed anti-proliferative properties, leading to the development of new and more active compounds. Consequently, a new set of novobiocin analogs derived from 1,6-naphthyridin-2(1H)-one scaffold was designed, synthesized and evaluated against two breast cancer cell lines. Subsequently, cell cycle progression and apoptosis were conducted on best candidates, finally Western Blot analysis was performed to measure their ability to induce degradation of Hsp90 client proteins.
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| http://dx.doi.org/10.1016/j.ejmech.2016.04.050 | DOI Listing |
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