Yale, NFCR launch cancer drug research center

Five-year, $750,000 grant to develop new beta-peptide inhibitors.

Jeffrey Bouley

NEW HAVEN, Conn.—A five-year, $750,000 grant from the National Foundation for Cancer Research (NFCR) is allowing for the establishment of an NFCR Center for Anti-Cancer Drug Design and Discovery at Yale University that will work to develop new beta-peptide inhibitors.

Under the leadership of Drs. Alanna Schepartz and William Jorgensen, the cen­ter will work in particular to better under­stand how beta-peptides can be designed to disrupt protein-protein interactions that transmit cell signals. Abnormally behav­ing proteins can send incorrect signals that result in uncontrolled cell growth and division, and the idea is to block transmis­sion of cellular signals that lead to cancer growth.

"[Our] focus is on cancer targets such as the complex between p53 and hDM2—hDM2 amplification is implicated in many soft tissue cancers—and between Myc and Max, as c-Myc overexpression is implicat­ed in Burkitt's lymphoma as well as can­cers of the breast, GI tract, and the pros­tate," says Schepartz.

Unlike the more commonly used small-molecule inhibitors, beta-peptides have a chemical structure very similar to that of their target proteins, allow­ing the drug to bind the target pro­teins more specifically and inhibit them more effectively. Schepartz and Jorgensen report that because beta-peptides are stable within the human body, the center's research has the potential to create a com­pletely new technology platform for more effective and long-lasting anticancer drugs.

 But while the promise is there, Schepartz also notes that signifi­cant work remains.

"At this point, beta-peptides are simply a potential option in cases where inhibition of a protein-protein interaction is needed," she says. "We are working hard to learn how to best design these molecules to balance the often competing goals of affinity, speci­ficity, bioavailability and cost."

In addition to implications for cancer, beta-peptides hold promise for other areas of drug discovery, Schepartz notes.

"We have already reported beta-peptides that block HIV cell fusion through their interactions with gp41," she says. "In theory, these molecules represent the first step towards a cheaper, more tolerable replacement for Fuseon."

Jeffrey Bouley

Subscribe to Newsletter
Subscribe to our eNewsletters

Stay connected with all of the latest from Drug Discovery News.

June 2023 Magazine Issue Front Cover

Latest Issue  

• Volume 19 • Issue 6 • June 2023

June 2023

June 2023 Issue