Description
Tubacin is a histone deacetylase 6 (HDAC6) inhibitor that prevents α-tubulin deacetylation and displays anticancer activity. In cellular models of multiple myeloma and acute lymphoblastic leukemia, inhibition of HDAC6 inhibits cell motility and induces accumulation of ubiquitinated proteins, inducing apoptosis. Tubacin’s inhibitory action on HDAC also downregulates EGFR levels in a mutant renal epithelial cell line, indicating potential benefit as a treatment for polycystic kidney disease.
References
Liu W, Fan LX, Zhou X, et al. HDAC6 regulates epidermal growth factor receptor (EGFR) endocytic trafficking and degradation in renal epithelial cells. PLoS One. 2012;7(11):e49418. d PMID: 23152903.
Aldana-Masangkay GI, Rodriguez-Gonzalez A, Lin T, et al. Tubacin suppresses proliferation and induces apoptosis of acute lymphoblastic leukemia cells. Leuk Lymphoma. 2011 Aug;52(8):1544-55. PMID: 21699378.
Hideshima T, Bradner JE, Wong J, et al. Small-molecule inhibition of proteasome and aggresome function induces synergistic antitumor activity in multiple myeloma. Proc Natl Acad Sci U S A. 2005 Jun 14;102(24):8567-72. PMID: 15937109.
Haggarty SJ, Koeller KM, Wong JC, et al. Domain-selective small-molecule inhibitor of histone deacetylase 6 (HDAC6)-mediated tubulin deacetylation. Proc Natl Acad Sci U S A. 2003 Apr 15;100(8):4389-94. PMID: 12677000.
