Learning objectives
1. Knowledge and understanding. At the end of the course, the student is expected to be able to:
- know the biological function and the general properties of drug targets (enzymes, receptors, transmembrane transport proteins, protein carriers, DNA)
-Know the mechanisms of drug-taget interaction described in the course
2. Applying knowledge and understanding. At the end of the course, the student is expected to be able to:
- interpret simple plots representing experimental data
- reconstruct a general mechanism of protein-drug interaction from the reading of a short text of scientific literature
3. Communication skills. At the end of the course, the student is expected to be able to:
- communicate the topics in a clear, concise and effective way, using the technical terminology
- describe the structure of proteins
- describe in details the structures of the proteins encountered in the course
4. Learning skills. At the end of the course, the student is expected to be able to make connections between the topics covered in this course and other courses (particularly in the fields of Biochemistry and Physiology) and to extrapolate pieces of information on protein-ligand interaction from the reading of scientific literature.
Prerequisites
Students should have a basic knowledge of Biochemistry, especially on the structure-activity relationship of proteins and on the mechanism of action of enzymes.
Course unit content
Definition of drug and drug target.
Binding properties of proteins.
Receptors as drug target.
Membrane transporters and ionic channels as drug target.
Enzymes as drug target.
Treatment of HIV and NSAIDs as examples of the therapeutic use of enzyme inhibitors.
Recombinant drugs.
Full programme
• Drug and drug target: definition
• Binding properties of proteins
• Receptors as drug target:
• Intracellular receptors
• GPCRs
• Receptor tyrosine kinases
• Tyr kinase-associated receptors
• Receptor guanylyl cyclases
• Membrane transporters and ionic channels as drug target
• Enzyme inhibition and drug discovery:
• Enzymes as drug targets
• Enzymatic catalysis
• Reversible inhibitors
• Irreversible inhibitors
• NSAIDs
• Enzyme inhibition in HIV therapy
• Recombinant drugs and systems for their production
Bibliography
The teaching material will be made available on a weekly basis and loaded on the Elly platform. The teaching material includes all the slides.
David L. Nelson, Michael M. Cox
I PRINCIPI DI BIOCHIMICA DI LEHNINGER 7 ed, ZANICHELLI. (7th Edition)
Lodish H.
Biologia Molecolare della Cellula
3 ed italiana, Zanichelli (6th Edition)
Copeland R. Evaluation of enzyme inhibition in drug discovery, Wiley.
Patrick G.L.
Introduzione alla Chimica Farmaceutica, Ed. EdiSES
Teaching methods
Lezioni orali integrate con ausili informatici e multimediali.
Assessment methods and criteria
Two written exams (preappelli) will be held, one during the course and one at the end. If both exams are passed, the module will be considered successfully completed. As an alternative, during the exam period the students will take the oral exam together with the Biological Physical Chemistry module. Students diagnosed with specific learning disorders (DSA), certified in accordance with law No. 170/2010, will be able to take the exams in the forms required by law.
Other information
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