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Combinatorial Chemistry
Description: The course introduces the use of combinatorial chemistry for drug discovery. It covers the requirements for performing combinatorial chemistry, the design and synthesis of combinatorial libraries, and molecular diversity analysis as applied to antibodies, peptides, nucleic acids, and small molecules.
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COURSE OUTLINE
INTRODUCTION
1. Course Information
2. Interface Tour
3. Course Overview
COMBICHEM OVERVIEW
4. Objectives
5. Medicinal Chemistry
6. Combinatorial Chemistry
7. High-Throughput Screening
8. HTS Assays
9. uHTS Requirements
10. Progress Check
DIVERSITY ANALYSIS
11. Objectives
12. Selection and Diversity
13. Peptide Libraries
14. DNA Shuffling
15. Strategic Options
16. Molecular Diversity
17. Synthesis Strategies
18. Phage Display
19. Progress Check
LIBRARY DESIGN
20. Objectives
21. Drug Pharmacophores
22. Library Design
23. Lead Optimization
24. Applications
25. Progress Check
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COURSE OBJECTIVES
Students completing this course should be able
to:
- Define the two technologies that now allow the creation of large combinatorial libraries of compounds
- List the three functions that combinatorial chemistry brings to synthetic medicinal chemistry
- Describe the difference between the three different types of assays with which combinatorial libraries are usually tested
- Specify two of the features of an assay that allow it to be amenable to high-throughput screening
- Explain the advantages of HTRF-based assays
- Describe the three principal requirements needed to scale an assay to the level of uHTS
- Define the difference between a diverse library and a focused or biased library
- Calculate the number of combinations of molecules capable of being created from an n-mer peptide library
- List three classes of proteins that have been "improved" using DNA shuffling
- Specify the strategic options available in the creation of a combinatorial library
- Describe how molecular diversity can be obtained in protein, peptide, nucleic-acid or small-molecule libraries
- Define and explain the two major strategies for synthesizing small-molecule libraries
- List the nine steps involved in creating antibodies via phage display
- Understand the key features of a drug pharmacophore
- List some of the parameters involved in designing combinatorial drug libraries
- Define the two major parameters in drug optimization that can benefit from drug design
- Give two examples of drugs that can now be synthesized by solid-phase combinatorial synthesis
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SeerPharma has partnered with GeneEd to now distribute courses in Major Therapeutic Areas, Clinical Research, and Biotechnology & Genetics.
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