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New Treatments for Cancer and Metabolic Diseases: Vitamin D Receptor-Coregulator Inhibitors
Milwaukee Regional Technology Transfer Group United States flag United States
Abstract ID:
Dr. Alexander Arnold has discovered small molecules that can disrupt the interaction between the vitamin D receptor (VDR) and coregulator proteins that modulate VDR-mediated gene transcription.
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Dr. Alexander Arnold has discovered small
molecules that can disrupt the interaction between the vitamin D receptor (VDR)
and coregulator proteins that modulate VDR-mediated gene transcription.  VDR is a transcription factor, which is
activated by the binding of calcitriol and other active metabolites of vitamin
D.  Small molecules with the ability to
inhibit interactions between the VDR and coregulators have the potential for
treating metabolic disorders such as chronic renal failure, skin diseases,
cancer, autoimmune disease, and heart disease. 



 



The current problem with treatment of
metabolic disorders such as chronic renal failure, in which patients are
treated with calcitriol or synthetic vitamin D analogs, is a high risk of producing
elevated calcium in the blood (hypercalcemia). 
This can lead to psychosis, bone pain, calcification of soft tissue, and
in severe cases, coma and cardiac arrest. The application of VDR-coregulator
inhibitors is advantageous due to coregulator-specific regulation of VDR target
genes.   One of the most important genes
regulated by VDR is the 24-hydroxylase gene (CYP24A1), which is overexpressed
in many cancers.  Many new anti-cancer
therapies are based on vitamin D analogs, but similar to the treatment of
metabolic disorders, these compounds lead to hypercalcemia and excessive excretion
of calcium in the urine of patients which can lead to impairment of renal
function.  Dr. Arnold's group has
identified small molecules that act as irreversible antagonists to disrupt the
interactions between VDR and coregulators and regulate the expression of CYP24A1.  The lead compounds also inhibited growth of
the prostate cancer cell line DU145, which effect was reversed by higher
concentration of calcitriol, supporting the fact that growth inhibition by coregulator
binding inhibitors is mediated by VDR.   This
technology shows great promise as a drug for both cancer and metabolic
disease. 



 



 



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This technology is part of an active and ongoing research program and is seeking partners for development of the final product. It is available for developmental research support/licensing under either exclusive or non-exclusive terms.

FEATURED
Last Updated Jul 2013
Technology Type THERAPEUTIC
Phase of Development EARLY STAGE
UNIVERSITY

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