Detecting and better understanding important cellular processes is largely based on our ability to design synthetic agents that can selectively target, sense, or regulate the function of biomolecules in their native environment. The field of bioorganic chemistry addresses these challenges by combining principles of synthetic organic chemistry and biochemistry in order to realize biomimetics with unique properties. These synthetic systems, which can be based on small molecules, peptides, oligonucleotides and their combinations, can be applied in drug development, biomolecule labeling, disease diagnosis, and cellular imaging.
This course will provide an overview of some of the most important synthetic methods and analytical tools used for targeting and sensing a wide range of biomolecules such as proteins, carbohydrates, and DNA, by using a rational design approach.
Research topics covered in this course:
- General introduction, inhibitors of protein-protein interactions, antibody-based therapy, targeting hot spots, and designing synthetic inhibitors.
- Peptide synthesis, protecting group chemistry, and designing modified peptides
- Techniques for following biomolecule interactions, binding curves, mimicking protein secondary structures, and peptido mimetics as inhibitors of protein-protein interactions
- Covalent protein labeling and designing synthetic protein tags
- Designing fluorescent probes for sensing anions, metal ions, phosphates, and proteins. Utilizing fluorescence resonance energy transfer, photoinduced electron transfer and intenral charge transfer processes, as well as excimer formation, and indicator displacement assays.
- Labeling proteins in their native environment using genetically targeted fluorescent molecules, photo-crosslinking, site-selective chemical reactions, and applications in cellular imaging.
- Oligonucleotide synthesis, DNA and RNA structures, and designing modified oligonucleotides for biosensing and therapy.
- DNA and RNA aptamers, G-quadruplex structures, DNA hairpin structures, and controlling DNA melting temperature and stability.
- Oligonucleotide-based biosensors, aptamer biosensors, and molecular beacons.
- Introduction to glycobiology, carbohydrate structures, and modified carbohydrates.