Selectively Targeted Histone Deacetylase Inhibitors

Inhibitors of histone deacetylases (HDAC) are regarded as an important approach to cancer chemotherapy, since they disrupt the aberrant cellular metabolism that occurs in many tumor types. The HDAC inhibitors currently in clinical trials and typified by compounds such as trichostatin (TSA) and MS-275, are effective antitumor agents, but also produce significant toxicity to cells and whole animals. JHU researchers have designed and synthesized 16 compounds which are hybrids including structural aspects of polyamines (normal constituent of human cells with a high affinity for DNA) and known HDAC inhibitors. One of these analogues, compound 19, is 79% as effective as TSA as a HDAC inhibitor, and yet has a greater activity on processes controlled by HDAC in cells, including re-expression of P21, a tumor suppressor factor that is deficient in many tumors. In addition, compound 19 is significantly less toxic to cells than either TSA or MS-275. Based on our results, it is apparent that compound 19 and its analogues represent an important series of HDAC inhibitors with novel structures. Description (Set) Proposed Use (Set) These compounds could be developed as treatments for various forms of cancer.

Inventor(s): Casero, Robert A.

Type of Offer: Licensing



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