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Renal Selective Unsaturated Englerin Analogues

Researchers at the National Cancer Institute (NCI) have developed a number of analogs of the natural product englerin A, an inhibitor of renal cancer cell growth. Englerin A is thought to exert its anticancer effects by activating protein kinase C (PKC) theta, and exert cytotoxic effects through activation of transient receptor potential cation (TRPC) channels. The invention englerin analogues provide promising treatment strategies for various cancers, diabetes, and HIV, and other diseases associated with the PKC theta and/or TRPC ion channel proteins. Researchers at the NCI seek licensing and/or co-development research collaborations for englerin A analogue compounds.

Compounds that Interfere with the Androgen Receptor Complex

NCI researchers have identified novel compounds that inhibit FKBP52-mediated activation of the androgen receptor protein (AR), a major target for anti-prostate cancer therapeutic development. As FKBP52 is implicated in the regulation of other hormone receptors, anti-FKBP52 may be applicable in the treatment of hormone-dependent diseases such as diabetes or even used as contraceptives. NCI seeks partners to license or co-develop this technology.

Aryl Hydantoin Heterocycle Compounds that Target the Androgen Receptor for Prostate Cancer Treatment

Researchers at the National Cancer Institute (NCI) have developed aryl hydantoin heterocycles that target the androgen receptor (AR). NCI seeks research co-development partners and/or licensees to develop these compounds as therapeutics for prostate cancer. As these compounds consist of both AR agonists and antagonists, they may also be effective therapeutics for androgen dysfunctional disorders, such as androgen deficiency disorders or hyperandrogenism.