Drug Discovery Core

Research in Drug Discovery at the University of Wisconsin focuses on areas related to medicinal chemistry, such as small molecule development, natural products isolation and characterization, organic synthesis, and rational drug design. In collaboration with the Pharmaceutical Sciences Drug Action and Drug Delivery Cores, these new chemical entities can be subsequently evaluated via high throughput screening toward lead generation or specifically utilized to probe novel biological phenomenon toward in-depth mechanistic studies. Thus, the UW–Madison Pharmaceutical Sciences Drug Discovery Core presents our graduate students and post-doctoral trainees with intensive training in modern organic chemistry coupled with a distinctive exposure to the modern applications of small molecules within biology and medicine.

• Laboratories in the drug discovery core are supported by multiple campus facilities and centers that provide state of the art instrumentation and analytical capabilities, computational resources, and other research support. A prime example of this is the Lachman Institute for Pharmaceutical Development within the School of Pharmacy that houses the Analytical Instrumentation Center, the Medicinal Chemistry Center, the Small Molecule Screening Facility, the Wisconsin Center for Nanobiosystems, and the Zeeh Pharmaceutical Experiment Station.
• Students within the UW–Madison Pharmaceutical Sciences Drug Discovery Core are eligible for a number of diverse traineeships including the Chemistry-Biology Interface and the Biotechnology Training Programs.
• Students within the UW–Madison Pharmaceutical Sciences Drug Discovery Core have been awarded prestigious fellowships such as NSF-GRFP and AFPE pre-doctoral fellowships. They have participated in the Delta program to hone their teaching and mentoring skills to prepare for careers in academia.
• Through internships and networking opportunities with alumni and other leaders in industry and academia, our trainees can learn additional skills and create connections that make them highly competitive for jobs in their chosen career paths.

Drug Discovery faculty research interests:

• Marine natural products chemistry; antibiotic drug discovery; structure determination of novel natural products using NMR and mass spectrometry; and metabolomics studies of marine invertebrate associated microorganisms. (Bugni)
• Synthetic methodology, medicinal chemistry and drug discovery. Optimization of structure-activity and structure-property relationships. Exploratory pharmacological mining of novel chemical scaffolds. Emphasis on development of anticancer and anti-infective agents. (Golden)
• Radiochemistry applications in biomedical research; Targeted radionuclide therapy–theranostics; Radio-immunooncology; Neutron capture therapy. (Hernandez)
• Mechanism and function of protein post-translational modifications using a variety of interdisciplinary approaches, such as chemical biology, enzymology, biochemistry, mass spectrometry, X-ray crystallography, cell biology, and genetics. (Jiang)
• The role of uncultured symbionts in natural product biosynthesis within marine invertebrates; marine natural product chemistry; drug discovery; next-generation sequencing; metagenomics; bioinformatics; biosynthesis. (Kwan)
• Biochemistry of RNA modifying enzymes; bioorganic chemistry of RNA; nucleotide based rational drug design. (Lauhon)
• Analytical neurochemistry; neuropeptides; proteomics and peptidomics; glycomics and glycoproteomics; biomarker discovery in neurodegenerative diseases; quantitative system biology; metabolomics; microseparations; imaging mass spectrometry and its application to drug delivery and biodistribution; biological mass spectrometry. (Li)
• Di- and tri-block copolymers in drug delivery and imaging; 19F-MRI; nanotechnologies in cancer therapy; immunotherapies; molecular recognition of RNA. (Mecozzi)
• Antimicrobial resistance and pharmacodynamics; antimicrobial effects on host-pathogen interactions (Rose)
• In vitro and preclinical model systems to investigate the role of the growth hormone/IGF-I axis in prostate carcinogenesis. Mouse-based studies of preclinical efficiency. (Swanson)
• Medicinal chemistry and bioassay development. Develop small molecule and protein-based therapeutics to selectively modulate disease-causing proteins. Design and synthesize ligands for carbohydrate binding proteins. Develop cell-based and biochemical assays to evaluate the pharmacological properties of novel therapeutics and to study their mechanism of action in-vitro and in-vivo. (Tang)
• Design and development of tumor targeted molecular agents for imaging, radiotherapy, and immunotherapy oncology applications. (Weichert)
• Synaptic plasticity in substance use and major depressive disorders; Development of antibodies against cannabinoids, opioids, sedative-hypnotics, and classical psychedelics; Immunologic biomarkers of drug use; Implementation of novel psychiatric treatments, including vaccine-based approaches and medication-assisted psychotherapy. (Wenthur)