Calendar of Courses -- 2010
| PhD Course in Drug Discovery - 2010 | ||||||
| Venue = D3 Meeting Room, Floor 1 | ||||||
| N. | Lecturers | Course Title | Dates | Timetable | Hours | Credits |
| 1 | Angelo Reggiani | Introduction to course | June 7 | 11am - 1pm | 2 | 4 |
| • What is a drug? | ||||||
| ↘ Origin of active principles | ||||||
| ↘ Why new drugs: the unmet medical need concept | ||||||
| ↘ Definitions | ||||||
| • Drug discovery process | ||||||
| ↘ Evolution of the process | ||||||
| ↘ Drug discovery and drug development phases | ||||||
| 2-3-4 | Angelo Reggiani - Glauco Tarozzo - Rosalia Bertorelli - Gianpiero Garau | Target identification and validation | ||||
| • From disease to gene to target | ||||||
| ↘ Source of new targets | ||||||
| ↘ Criteria for target selection | June 9 | 11am - 1pm | 2 | |||
| ↘ Management of taget portfolio | June 14 | 11am - 1pm | 2 | |||
| ↘ Target Validation studies | June 16 | 11am - 1pm | 2 | |||
| - Localization and expression | ||||||
| - Molecular and cellular function | ||||||
| - Role in the disease | ||||||
| 5-6 | Angelo Reggiani - Glauco Tarozzo | Hit identifications | ||||
| • Biomolecular screening | ||||||
| ↘ Assay development | ||||||
| ↘ Creation of recombination systems | ||||||
| - Cloning and expression in host cells | ||||||
| ↘ Choice of the assay/s | June 21 | 11am - 1pm | 2 | |||
| - Cell-based vs cell free | June 23 | 11am - 1pm | 2 | |||
| - Binding assay vs functional assays (2nd messenger) | ||||||
| - Enzymatic inhibition | ||||||
| ↘ HTS | ||||||
| - Assay miniaturization | ||||||
| - Data analysis | ||||||
| - Hit selection | ||||||
| 7-8 | Gianpiero Garau - Claudio Dalvit | Hit identifications | 3 | |||
| • Knowledge-based approach | ||||||
| ↘ Ligand-based approach | June 28 | 11am - 1pm | 2 | |||
| ↘ Structure-based drug design | June30 | 11am - 1pm | 2 | |||
| - X-ray cristallography in structure-based drug design | ||||||
| - Molecular docking | ||||||
| - Fragment elaboration | ||||||
| 9 | Tiziano Bandiera | Hit identifications | July 5 | 11am - 1pm | 2 | 3 |
| Tiziano Bandiera | • Compund collections | |||||
| ↘ Corporate compound collections | ||||||
| ↘ targeted and Diversity Libraries | ||||||
| Tiziano Bandiera | • Natural sources | |||||
| ↘ Active principles derived from natural sources (plants, marine life forms) | ||||||
| ↘ Extraction and characterization | ||||||
| ↘ Example (α-conotoxins, chelerythrine, etc.) | ||||||
| 10 | Tiziano Bandiera | Hit to lead and Lead Optimizations | July 7 | 11am - 1pm | 2 | |
| Renata Riva | • Medicinal Chemistry | |||||
| ↘ Synthesis of drugs | ||||||
| - Synthesis strategies | ||||||
| - Synthetic methodologies | ||||||
| - Computer-aided synthesis planning | ||||||
| 11 | Fabio Bertozzi | ↘ Chiral drug | July 12 | 11am - 1pm | 2 | |
| - Why Chiral drug? | ||||||
| - Active and inactive enantiomers | ||||||
| - Resolution of racemates | ||||||
| 12 | Rita Scarpelli | ↘ Bioisosterism | July 14 | 11am - 1pm | 2 | |
| - The concept of bioisoster | ||||||
| - Use of bioisosters in medicinal chemistry | ||||||
| 13 | Tiziano Bandiera | ↘ Improving drug-likeness | July 19 | 11am - 1pm | 2 | |
| - The concept of drug-likeness | ||||||
| - ADME profiling | ||||||
| - Strategies to improve drug-likeness | ||||||
| 14 | Andrea Cavalli | Hit to lead and Lead Optimizations | July 21 | 11am - 1pm | 2 | 3 |
| • Computational drug design | ||||||
| ↘ Ligand-based drug design | ||||||
| - The concept of pharmacophore | ||||||
| 15 | ↘ Structure-acitivity relationships (SARs) | September 6 | 11am - 1pm | 2 | ||
| - QSAR and 3D QSAR (CoMFA) | ||||||
| - Probing Hydrophilic interactions (H-bond and ionic) | ||||||
| - Probing hydrophobic interactions (aromatic stacking and van der Waals) | ||||||
| 16 | ↘ Structure-based drug design | September 8 | 11am - 1pm | 2 | ||
| - Application of X-ray crystallography to te identification and optimization | ||||||
| of lead compounds | ||||||
| 17-18 | Angelo Reggiani - Roberto Motterlini - Rosalia Bertorelli | Hit to lead and Lead Optimizations | 3 | |||
| • Pharmacology | ||||||
| ↘ Principles of pharmacology (concentration-response, potency, efficacy, | ||||||
| agonists, antagonists, etc.) | ||||||
| ↘ The Screening Cascade | September 13 | 11am - 1pm | 2 | |||
| - Primary and secondary assays | September 15 | 11am - 1pm | 2 | |||
| ↘ Efficacy vs disease animal models | ||||||
| ↘ Target biomarkers identification | ||||||
| ↘ ADME | ||||||
| ↘ Toxicology | ||||||
| 19 | Angelo Reggiani / Invited speakers | Development process | 2 | 3 | ||
| ↘ Chemical development | September 20 | 11am - 1pm | ||||
| ↘ Pharmaceutical Development | ||||||
| ↘ Clinical development | ||||||
| ↘ Post marketign surveillance | ||||||
| 20 | Invited speakers | Patent | 2 | |||
| ↘ Intellectual property | September 22 | 11am - 1pm | ||||
| ↘ What can be patented? | ||||||
| ↘ protection and lifetime of a patent | ||||||