Wednesday , April 14 2021

Study: High-throughput platform enables activity mapping of emerging cancer drug targets – (Details)

A powerful new biochemical platform is fueling the work of an enzyme family that is promising targets for cancer treatment.

Published today Scientific DevelopmentsThe novel method provides a high-resolution view of how these enzymes, called lysine methyltransferases, selectively select their proteins by chemical tags that alter their function. Because of their central role in all aspects of health and disease, proteins and molecules that interact and interact with them are often the targets of therapeutic development.

Platform, EpiCypher, Inc. co-operation with Van Andel Research Institute Scott Rothbart, Ph.D. Developed by.

Yardımcı This technology helps us identify protein interaction networks for this subtle family of enzymes based on chemical labeling,. Rothbart said. Isi Some inhibitors of these enzymes are currently on the clinical development line for cancer treatment. It is important to identify the spectrum of their activities, to understand exactly how these drugs work, and to select reliable biomarkers to monitor their activity in patients. "

There are about 20,000 genes, ranging from helping human beings to proteins, the molecular workers responsible for carrying out every process in the human body, to assisting in nutrient digestion, and in managing communication between cells.

Once a protein has been created, its function is usually modified by adding small chemical labels that teach cells where to go and when to do their work. There are more than 100 different types of these tags, including the addition of methyl groups to amino acid lysine.

Using new techniques, the team found that more proteins could be labeled with lysis more than previously thought.

He was the first author of our study and a post-doctorate fellow in the laboratory of Rothbart's Institute. U Our study shows that what we know about lysine methylation is just the tip of the iceberg, Ev said Evan Cornett. ”The method we develop will allow us to identify new targets in the full set of lysine methyltransferases in humans and, in doing so, will help us and others determine which cancers and other diseases can benefit from treatments targeting these class enzymes.“

This technology is the latest development from the collaboration between Rothbart's laboratory and EpiCypher. Several National Institutes of Health (NIH) were supported by Small Business Innovation Research (SBIR) awards. SBIR, commonly known as the Seed Fund of America, offers federally funded research grants to small businesses to invest in the American-led exploration. The SBIR program supports small businesses in the biotechnology sector and focuses on strategies with significant potential for successful commercialization in the medical field. SBIR is the key stimulus to academic innovation and to close the gap between basic science and clinical advances.

Arı The beauty of this technology is the amazing simplicity and volume of business compared to current mass spectrometry-based approaches, inin says Martis Cowles, Chief Operating Officer and co-author of EpiCypher. , We are excited to use this technology to help drug developers identify new therapeutic targets and even identify the most appropriate target substrates for high-throughput screening screening. “


Van Andel Research Institute. .

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