“These substances represent an entirely new class of potential drugs,” study leader Gregory Verdine, Ph.D., told the 241st National Meeting & Exposition of the American Chemical Society, being held here this week. “They herald a new era in the drug-discovery world.”
Verdine cited estimates that conventional medicines, most of which belong to a family termed “small molecules,” cannot have any effect on 80-90 percent of the proteins in the body known to be key players in disease. Throwing up their hands in frustration, scientists had even begun to term these prime targets for battling disease as “untouchables” and “undruggable.”
The new substances are not small molecules, but “stapled peptides,” named because they consist of protein fragments termed peptides outfitted with chemical braces or “staples.” The stapling gives peptides a stronger, more stable architecture and the ability to work in ways useful in fighting disease.
“Our new stapled peptides can overcome the shortcomings of drugs of the past and target proteins in the body that were once thought to be undruggable,” Verdine said. “They are a genuinely new frontier in medicine.”
In one advance, Verdine and colleagues at Harvard University described development of the first stapled peptides that target colon cancer and asthma attacks. The colon cancer stapled peptides inhibit activity of a protein called beta-catenin that, when present in a hyperactive form, causes cells to grow in an aggressive and uncontrolled way. That protein normally helps keep certain cells, including those lining the colon, in good health. But the abnormal protein has been directly linked with an increased risk of colon cancer and other types of cancer, including those of the skin, brain, and ovaries.
When added to human colon cancer cells growing in laboratory cultures, the stapled peptides reduced the activity of beta-catenin by 50 percent. In patients, that level of reduction could be sufficient to have a beneficial impact on the disease, Verdine suggested.
Verdine also reported development of the first stapled cytokines, which show promise for fighting asthma. Cytokines are hormone-like proteins secreted by cells of the immune system and other body systems that help orchestrate the exchange of signals between cells. The stapled cytokines moderate the activity of a cytokine called interleukin-13, which asthma patients produce in abnormally large amounts that contribute to asthma attacks.
Current asthma drugs, he noted, tend to treat the underlying symptoms of asthma, particularly inflammation. By contrast, stapled cytokines could treat the underlying causes of the disease. Verdine’s team is collaborating with a pharmaceutical firm on efforts to further develop the stapled peptides.
The American Chemical Society is a non-profit organization chartered by the U.S. Congress. With more than 163,000 members, ACS is the world’s largest scientific society and a global leader in providing access to chemistry-related research through its multiple databases, peer-reviewed journals and scientific conferences. Its main offices are in Washington, D.C., and Columbus, Ohio.
Michael Bernstein | Newswise Science News
At last, butterflies get a bigger, better evolutionary tree
16.02.2018 | Florida Museum of Natural History
New treatment strategies for chronic kidney disease from the animal kingdom
16.02.2018 | Veterinärmedizinische Universität Wien
Breakthrough provides a new concept of the design of molecular motors, sensors and electricity generators at nanoscale
Researchers from the Institute of Organic Chemistry and Biochemistry of the CAS (IOCB Prague), Institute of Physics of the CAS (IP CAS) and Palacký University...
For photographers and scientists, lenses are lifesavers. They reflect and refract light, making possible the imaging systems that drive discovery through the microscope and preserve history through cameras.
But today's glass-based lenses are bulky and resist miniaturization. Next-generation technologies, such as ultrathin cameras or tiny microscopes, require...
Scientists from the University of Zurich have succeeded for the first time in tracking individual stem cells and their neuronal progeny over months within the intact adult brain. This study sheds light on how new neurons are produced throughout life.
The generation of new nerve cells was once thought to taper off at the end of embryonic development. However, recent research has shown that the adult brain...
Theoretical physicists propose to use negative interference to control heat flow in quantum devices. Study published in Physical Review Letters
Quantum computer parts are sensitive and need to be cooled to very low temperatures. Their tiny size makes them particularly susceptible to a temperature...
Let’s say the armrest is broken in your vintage car. As things stand, you would need a lot of luck and persistence to find the right spare part. But in the world of Industrie 4.0 and production with batch sizes of one, you can simply scan the armrest and print it out. This is made possible by the first ever 3D scanner capable of working autonomously and in real time. The autonomous scanning system will be on display at the Hannover Messe Preview on February 6 and at the Hannover Messe proper from April 23 to 27, 2018 (Hall 6, Booth A30).
Part of the charm of vintage cars is that they stopped making them long ago, so it is special when you do see one out on the roads. If something breaks or...
15.02.2018 | Event News
13.02.2018 | Event News
12.02.2018 | Event News
16.02.2018 | Information Technology
16.02.2018 | Health and Medicine
16.02.2018 | Physics and Astronomy