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

总结

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.

技术优势

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

技术应用

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

详细技术说明

None

*Abstract

None

*Inquiry

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

*IR

CU12080

*Principal Investigation

*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.

国家/地区

美国