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Selective histone deacetylase (HDAC) inhibitors with therapeutic potential for cancer, neurodegenerative diseases, and autoimmune disorders

Summary: Histone deacetylases (HDACs) are a family of proteins that remove acetyl functional groups from histones and other cellular proteins. There are eighteen known HDACs in humans, and they play a critical role in the regulation of processes from gene transcription to protein folding. As a class, HDACs have been implicated in diseases from cancer to autoimmune disorders. HDAC6 is located in the cytoplasm and has a number of different protein substrates including a-tubulin, ubiquitin, and HSP90. Its structure and function are unique among the HDACs making it an attractive drug target, however most HDAC inhibitors are not specific to a single type of HDAC protein and are therefore toxic. This technology describes two small-molecule inhibitors that are selective for HDAC6, and provides structural information for the design of other HDAC6 inhibitors.

Technology Benefits: Fewer side effects when compared with other HDAC inhibitorsReduced cellular toxicitySpecific to HDAC6Patent Information:Patent Pending (WO/2013/052110)Tech Ventures Reference: IR CU12080

Technology Application: Sensitize cancer cells to approved anticancer therapiesTherapy for neurodegenerative diseases including Alzheimer's, Parkinson's, Huntington's and Niemann-Pick type C diseasesTherapy for autoimmune disorders including AIDSResearch tool for understanding HDAC6's role in disease progression

Detailed Technology Description: None

*Abstract: None

*Inquiry: Beth KaudererColumbia Technology VenturesTel: (212) 854-8444Email: TechTransfer@columbia.edu

*IR: CU12080

*Principal Investigator

*Publications: Lee JH, Mahendran A, Yao Y, Ngo L, Venta-Perez G, Choy ML, Kim N, Ham WS, Breslow R, and Marks PA. "Development of a histone deacetylase 6 inhibitor and its biological effects." Proc Natl Acad Sci U S A. 2013 Sep 24;110(39):15704-9.Marks PA and Breslow R. "Dimethyl sulfoxide to vorinostat: development of this histone deacetylase inhibitor as an anticancer drug." Nat Biotechnol. 2007 Jan;25(1):84-90.Marks P, Rifkind RA, Richon VM, Breslow R, Miller T, and Kelly WK. "Histone deacetylases and cancer: causes and therapies." Nat Rev Cancer. 2001 Dec;1(3):194-202.

Country/Region: USA

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