At the end of the course the students should demonstrate the understanding of the molecular basis of drug interaction with their biological targets. In detail, the student should be able to:
1) describe the biological function and mechanism of action of the main drug targets (KNOWLEDGE AND UNDERSTANDING)
2) describe from a molecular point of view how drug-target interaction can interfere with the biological function of the target and thus modify the biological state of the cell (KNOWLEDGE AND UNDERSTANDING)
3) identify correlations in the mechanism of action of different drug targets and establish connections between the mode of action of different ligands / inhibitors / agonists / antagonists (APPLYING KNOWLEDGE AND UNDERSTANDING)
4) explain the topics the course effectively with a language that uses appropriate scientific terminology (COMMUNICATION AND LEARNING SKILLS)
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 contents summary
Definition of drug and drug target.
Binding properties of proteins.
Enzymes as drug target.
Treatment of HIV and NSAIDs as examples of the therapeutic use of enzyme inhibitors.
Receptors as drug targets.
• Drug and drug target: definition
• Binding properties of proteins
• Enzymatic catalysis
• Intracellular receptors
• Receptor tyrosine kinases
• Tyr kinase-associated receptors
• Receptor guanylyl cyclases
• Enzyme inhibition and rug discovery:
o Enzymes as drug targets
o Reversible inhibitors
o Irreversible inhibitors
o Tight-binding and slow-binding inhibitors
o Enzyme inhibition in HIV therapy
• Overview of recombinant drugs
Selected scientific papers and copy of slides can be downloaded from the Elly
David L. Nelson, Michael M. Cox
I PRINCIPI DI BIOCHIMICA DI LEHNINGER 5 ed, ZANICHELLI.
Copeland R. Evaluation of enzyme inhibition in drug discovery, Wiley.
Oral lessons integrated with informatic tools and the support of multimedia
Assessment methods and criteria
The exam is either a written "in itinere" test or a final oral exam.
The written test will take place during the teaching semester and will consist of two tests, dealing with the first and second part of the programm, respectively. The teaching module final mark is the average of the marks of the two tests.
During the exam period the students can take the oral exam together with the Biological Physical Chemistry module.