The Mark Foundation has announced $3.4 million in ASPIRE Awards to support high risk, high reward approaches to solving complex problems in cancer research. We are proud to support innovative science. Associate Professor of Chemistry, Nutritional Sciences & Toxicology and Molecular Biology has received an ASPIRE award for his project Chemoproteomics-Enabled Covalent Ligand Discovery Platforms for Accessing Novel Druggable Modalities.
Developing drugs that bind to many of the proteins known to play a role in cancer has proven to be an extraordinarily difficult challenge. A team of researchers in Nomura's lab at UC Berkeley have identified candidate drug binding sites for a number of these proteins using novel chemical biology profiling techniques. The team is now building on this knowledge to screen for molecules that can bind these sites and serve as the starting point for the creation of new drugs to treat cancer.
The researchers are focused on making drugs for cancer targets that have traditionally been considered “undruggable”. In general, small molecule drugs target proteins by binding to a pocket or cleft in the protein and changing its function. More than 90% of human proteins, however, do not have an obvious binding pocket. The researchers are using activity-based protein profiling to map hotspots on proteins that can bind to or react with a small molecule. The team has already discovered more than 100,000 such hotspots in more than 20,000 human protein targets – revealing binding sites across almost all human proteins that can form the basis for developing new drugs. Many of these binding sites are on proteins that are known to drive cancer. Nomura is developing ligands against previously undruggable cancer protein targets by screening libraries of drug-like compounds against the newly discovered hotspots and determining if these compounds are likely to function in vivo.
As part of this ASPIRE Award, one of the targets Nomura is focusing on is the transcription factor brachyury, a protein that has been shown to drive the development of chordoma, a rare bone cancer of the spine and skull. The brachyury-targeting aspect of this project was also awarded a Therapeutic Innovation Award jointly with the Chordoma Foundation.
About the Mark Foundation
Established by Alex Knaster in memory of his father, Mark, who succumbed to cancer in 2014, the goal of The Mark Foundation is to reward cutting-edge, innovative scientific ideas that transform patient care and answer the most complex questions about cancer biology.
The Mark Foundation for Cancer Research is dedicated to accelerating cures for cancer by integrating discoveries in biology with innovative technology.
Launched in 2017, The Mark Foundation pursues its mission by funding a global portfolio of groundbreaking research carried out by individual investigators, multi-investigator teams, and inter-institutional collaborations.
Recognizing the obstacles that can prevent scientific advances from improving patient outcomes, The Mark Foundation maintains a nimble, high-impact approach to funding research that encompasses grants for basic and translational cancer research, as well as venture philanthropy investment in companies that bridge the gap between the bench and the bedside.