Doctoral School on "Life and Humanoid Technologies"

 

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