A major roadblock that contributes to the lack of success in brain cancer therapeutics is that most commonly used anti-cancer drugs are not able to cross the blood-brain barrier (BBB), the brain’s blood vessel system which protects the brain from foreign substances in the bloodstream. Conversely, toxic chemotherapeutics that can enter the brain can be harmful to healthy tissues. Our lab is developing human organoid models to mimic the BBB and brain tumors in culture as platforms for high-throughput screening and testing of brain cancer therapeutics, as well as for studying biological processes and mechanisms. Particularly our team combines the utility of these tools with medicinal chemistry to design and engineer new small molecules that can specifically recognize tumor cells and enable delivery of high therapeutic payload directly to tumor sites without affecting healthy tissues. We aim to facilitate the development of new targeted therapies that are much needed in neuro-oncology to achieve enhancement of treatment efficacy while minimizing toxicity in patients. Additionally, a neuroimaging approach that can discriminate between tumor vs. normal cells would allow surgeons to delineate tumor margin from surrounding brain, as well as enable oncologists to accurately assess tumor progression to improve long-term management and treatment of malignant brain tumors. We are also developing brain tumor-targeting radiotracers for non-invasive imaging and monitoring of brain tumors using positron emission tomography (PET), with the aim to ultimately benefit patient care.