Forum for Science, Industry and Business

Sponsored by:     3M 
Search our Site:

 

New techniques for stapling peptides could spur development of drugs for cancer

09.02.2011
Researchers at the University at Buffalo have devised two new ways of "stapling" peptide helices to prevent these medically important molecules from losing their shape and degrading in the presence of enzymes.

The discovery could help speed the development of peptide-based drugs against diseases including cancer. UB scientists say the methods they pioneered are simpler than existing techniques, one of which employs an expensive ruthenium catalyst to connect chemical side chains that protrude from the main body of helical peptides.

"There's a lot of potential here. Our chemistry is unique," said Qing Lin, the UB assistant professor of chemistry who led the research. "There are not that many new drug targets out there today, which partly explains the declining number of FDA-approved new drugs in recent years. So there's a need to come up with new technologies that can overcome this barrier. To this end, stapled peptides could open a whole host of new targets for therapies."

Stapled peptides work as treatments against disease by binding tightly to target proteins within cells, thus disrupting specific protein-protein interactions that regulate many biological processes, including response to stress, signaling within cells, and cell death.

In their native state, peptides -- short strings of amino acids -- shift between different shapes, including a helix, sheet and random coil. Stapling the peptides' side chains encourages the peptides to adopt and stay in a helix, which enables them to enter cells more easily. The helical conformation also makes it more difficult for enzymes to break the peptides down, Lin said.

The two processes Lin's team developed for stapling peptides are efficient, producing stapled peptides in high yields, said Timothy Dee, a commercialization manager for UB's Office of Science, Technology Transfer and Economic Outreach (STOR). Through STOR, UB is applying for patents to cover both stapling methods.

"Photoclick stapling," the first approach, involves synthesizing peptides that have alkenes in one side chain and tetrazoles in another. Under ultraviolet light, the two side chains form chemical bonds with one another.

A paper on photoclick stapling appeared online in Bioorganic and Medicinal Chemistry Letters in January and will appear later this year in the journal's print edition. Researchers first published on the subject in 2009 in Chemical Communications.

The second stapling technique Lin and his colleagues devised requires the synthesis of peptides carrying a pair of amino acids called cysteines that contain sulfur in their side chains. When scientists expose these peptides to a chemical that reacts selectively with the sulfur atoms, the chemical forms a "staple" that connects the two cysteine side chains.

Experts believe stapled peptides could treat a wide variety of health problems, including cancer and inflammatory, metabolic and infectious diseases. As evidence of the technology's promise, a company formed in 2005 to commercialize a ruthenium-based stapling method developed at Harvard University has reportedly raised about $60 million in venture capital and landed a deal with pharmaceutical giant Roche that could be worth more than $1 billion over time.

"The field is large enough for multiple players," Lin said. "Stapling is a technology that many people believe will create a new class of drug therapies, hitting new targets that other therapies can't. Our chemistry is distinct from what's already out there."

Lin and his group are particularly interested in developing anti-cancer therapeutics that increase the efficacy of chemotherapy by instructing cancer cells to self-destruct through "programmed cell death," a process called apoptosis.

The University at Buffalo is a premier research-intensive public university, a flagship institution in the State University of New York system and its largest and most comprehensive campus. UB's more than 28,000 students pursue their academic interests through more than 300 undergraduate, graduate and professional degree programs. Founded in 1846, the University at Buffalo is a member of the Association of American Universities.

Charlotte Hsu | EurekAlert!
Further information:
http://www.buffalo.edu

More articles from Life Sciences:

nachricht Researchers identify potentially druggable mutant p53 proteins that promote cancer growth
09.12.2016 | Cold Spring Harbor Laboratory

nachricht Plant-based substance boosts eyelash growth
09.12.2016 | Fraunhofer-Institut für Angewandte Polymerforschung IAP

All articles from Life Sciences >>>

The most recent press releases about innovation >>>

Die letzten 5 Focus-News des innovations-reports im Überblick:

Im Focus: Electron highway inside crystal

Physicists of the University of Würzburg have made an astonishing discovery in a specific type of topological insulators. The effect is due to the structure of the materials used. The researchers have now published their work in the journal Science.

Topological insulators are currently the hot topic in physics according to the newspaper Neue Zürcher Zeitung. Only a few weeks ago, their importance was...

Im Focus: Significantly more productivity in USP lasers

In recent years, lasers with ultrashort pulses (USP) down to the femtosecond range have become established on an industrial scale. They could advance some applications with the much-lauded “cold ablation” – if that meant they would then achieve more throughput. A new generation of process engineering that will address this issue in particular will be discussed at the “4th UKP Workshop – Ultrafast Laser Technology” in April 2017.

Even back in the 1990s, scientists were comparing materials processing with nanosecond, picosecond and femtosesecond pulses. The result was surprising:...

Im Focus: Shape matters when light meets atom

Mapping the interaction of a single atom with a single photon may inform design of quantum devices

Have you ever wondered how you see the world? Vision is about photons of light, which are packets of energy, interacting with the atoms or molecules in what...

Im Focus: Novel silicon etching technique crafts 3-D gradient refractive index micro-optics

A multi-institutional research collaboration has created a novel approach for fabricating three-dimensional micro-optics through the shape-defined formation of porous silicon (PSi), with broad impacts in integrated optoelectronics, imaging, and photovoltaics.

Working with colleagues at Stanford and The Dow Chemical Company, researchers at the University of Illinois at Urbana-Champaign fabricated 3-D birefringent...

Im Focus: Quantum Particles Form Droplets

In experiments with magnetic atoms conducted at extremely low temperatures, scientists have demonstrated a unique phase of matter: The atoms form a new type of quantum liquid or quantum droplet state. These so called quantum droplets may preserve their form in absence of external confinement because of quantum effects. The joint team of experimental physicists from Innsbruck and theoretical physicists from Hannover report on their findings in the journal Physical Review X.

“Our Quantum droplets are in the gas phase but they still drop like a rock,” explains experimental physicist Francesca Ferlaino when talking about the...

All Focus news of the innovation-report >>>

Anzeige

Anzeige

Event News

ICTM Conference 2017: Production technology for turbomachine manufacturing of the future

16.11.2016 | Event News

Innovation Day Laser Technology – Laser Additive Manufacturing

01.11.2016 | Event News

#IC2S2: When Social Science meets Computer Science - GESIS will host the IC2S2 conference 2017

14.10.2016 | Event News

 
Latest News

Researchers identify potentially druggable mutant p53 proteins that promote cancer growth

09.12.2016 | Life Sciences

Scientists produce a new roadmap for guiding development & conservation in the Amazon

09.12.2016 | Ecology, The Environment and Conservation

Satellites, airport visibility readings shed light on troops' exposure to air pollution

09.12.2016 | Health and Medicine

VideoLinks
B2B-VideoLinks
More VideoLinks >>>