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Mitochondrial-targeted Hsp90 C-terminal Inhibitors Manifest Anti-Proliferative Activity

Zheng Zhang, Monimoy Banerjee, Rachel E Davis, Brian S J Blagg

Bioorg Med Chem Lett. 2019 Nov 15;29(22):126676.

PMID: 31591016

Abstract:

The development of C-terminal heat shock protein 90 kDa (Hsp90) inhibitors has emerged as a potential treatment for cancer. Similarly, small molecules that target the mitochondria have proven to be efficacious towards cancer, as the reprogramming of mitochondrial function is often associated with oncogenic transformation. Herein, we report the development of triphenylphosphonium (TPP)-conjugated Hsp90 C-terminal inhibitors, their anti-proliferative activity, and accumulation in the mitochondria. In general, TPP-conjugated Hsp90 C-terminal inhibitors were found to manifest increased activity against various cancer cell lines when compared to the parent compounds.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
IAR42414012 Anti-Coronin-1C (C-terminal) Anti-Coronin-1C (C-terminal) Price
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