tubacin and Neoplasms

Tumor-derived extracellular vesicles (EVs) are emerging as an important mode of intercellular communication, capable of transferring biologically active molecules that facilitate the malignant growth and metastatic process. CD133 (Prominin-1), a stem cell marker implicated in tumor initiation, differentiation and resistance to anti-cancer therapy, is reportedly associated with EVs in various types of cancer. However, little is known about the factors that regulate the release of these CD133

Topics: AC133 Antigen; Anilides; Cell Line, Tumor; Cell-Derived Microparticles; Histone Deacetylase 6; Histone Deacetylase Inhibitors; Humans; Hydroxamic Acids; Neoplasm Proteins; Neoplasms

The FDA-approved drug suberoylanilide hydroxamic acid (SAHA, Vorinostat) was modified to improve its selectivity for a single histone deaetylase (HDAC) isoform. We show that attaching an ethyl group at the C3 position transforms SAHA from nonselective to an HDAC6-selective inhibitor. Theses results indicate that small structural changes in SAHA can significantly influence selectivity, which will lead future anti-cancer design efforts targeting HDAC proteins.

Topics: Antineoplastic Agents; HeLa Cells; Histone Deacetylase Inhibitors; Histone Deacetylases; Humans; Hydroxamic Acids; Neoplasms; Protein Isoforms; Vorinostat

Topics: Anilides; Animals; Anti-Inflammatory Agents, Non-Steroidal; Antineoplastic Agents; Apoptosis; Boronic Acids; Bortezomib; Endoplasmic Reticulum; Histone Deacetylase Inhibitors; Humans; Hydroxamic Acids; Neoplasms; Protease Inhibitors; Proteasome Endopeptidase Complex; Proteasome Inhibitors; Protein Folding; Pyrazines