The course aims at providing students with the molecular basis for the
understanding of the interaction between biological macromolecules and ligands, with a focus on drug targets.
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
• Recombinant drugs:
o General principles for recombinant drugs production
o Recombinant drugs produced in E. coli
o Recombinant drugs produced in yeast
o Recombinant drugs produced in CHO
o Recombinant drugs produced in plant cells
o Recombinant drugs produced in transgenic organisms
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.
The topics of the course will be delivered with oral presentations associated with informatics tools and visits to laboratories
Assessment methods and criteria
The exam is either a written "in itinere" test or a final oral test.
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.
The oral test is given together with the test for the Biological Physical Chemistry module during the exam periods.