NIH Licensing Opportunity: Small Molecule Inhibitor of MYC as a Cancer Therapeutic

NIH Licensing Opportunity:
Small Molecule Inhibitor of MYC as a Cancer Therapeutic 

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One Million Solutions in Health™ has established a one-of-a-kind partnership with the United States’ National Institutes of Health Office of Technology Transfer (NIH-OTT) and the National Cancer Institute Technology Transfer Center (NCI-TTC) to increase awareness and understanding of NIH technologies by potential partners in the life science and healthcare industries.

This provides you with a front-row seat to hear about new technology and science from various scientists at the NIH. This is also your opportunity to participate in our proprietary Signature Square™ process, where end-users can evaluate the technology, ask questions and provide feedback directly to the scientist.

Small Molecule Inhibitor of MYC as a Cancer Therapeutic
Join us for this webinar that will introduce a ground-breaking small molecule that can be used as a potential therapeutic for multiple myeolma, carcinoma of the cervix, colon, breast, lung and stomach.

The proto-oncogene c-Myc is deregulated and overexpressed in ~70% of all cancers. Thus, c-Myc is an attractive therapeutic target, since disrupting c-Myc activity could be used as pan-chemotherapy.

Beyond cancer, Myc is also a positive effector of tissue inflammation, and its function has been implicated in the pathophysiology of heart failure.

Because c-Myc is a transcription factor, a rationally designed small molecule targeting c-Myc is required to exhibit significant specificity. Unfortunatly, several physical characteristics of Myc make it a very difficult protein to target and, to date, there are no approved drugs targeting c-Myc.

The invention being discussed in this webinar is directed to small molecules that stabilize the transcription repressing quadruplex in the c-Myc gene promoter region. The compounds available for licensing target c-Myc at the transcriptional level, and have been shown to inhibit c-Myc expression.

The compounds being discussed are effective in selective killing in a variety of c-Myc-driven cancer cell lines, including leukemia, non-small-cell lung cancer, colon, central nervous system, melanoma, ovarian, renal prostate and breast. Minimal unwanted activity has been observed in 1) peripheral blood mononucleocytes or 2) cancer cell lines that resist inhibition of c-Myc protein expression.

The team’s efforts have been focused on developing these more potent molecules, with an improved ability to decrease c-Myc expression, along with superior bioavailability. Through synthesis of a focused library of analogs, the team has identified inhibitors with improved Kd values for the quadruplex, improved toxicity towards c-Myc-driven cancer cells, and improved efficacy for decreasing c-Myc expression.

By solving an NMR structure of the quadruplex with this small molecule, we have begun to establish a molecular basis for selectivity, as observed in cell-based and biophysical assays, and are working to use this information to design improved inhibitors. Additionally, we show that one compound of interest is orally bioavailable.

Potential therapeutic for multiple myeloma, carcinoma of the cervix, colon, breast, lung and stomach.

This is an opportunity to LICENSE THIS TECHNOLOGY, or participate in further collaborative work to enhance its development.

The Signature Square process is part of our Consortium infrastructure. Current member companies in the Technology Evaluation Consortium and SafeTEC include organizations like AstraZeneca, AbbVie, Amgen and Allergan, along with many others, including scientists, clinicians and investors in organizations around the world who help to evaluate this technology.

This is your opportunity to ask questions and provide feedback directly to the scientists by taking part in this Signature Square program.

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PANELISTS
	SPEAKER: John Schneekloth Jr., Ph.D. Investigator National Cancer Institute Center for Cancer Research (CCR)
	SPEAKER: Beverly Mock, Ph.D. Senior Investigator National Cancer Institute Center for Cancer Research (CCR)
	MODERATOR: Dawn Van Dam Executive Director & CEO One Million Solutions in Health™