Learning objectives
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)
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 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 as drug target
• Enzyme inhibition and drug discovery:
• Enzymes as drug targets
• Enzymatic catalysis
• Reversible inhibitors
• Irreversible inhibitors
• Tight-binding and slow-binding inhibitors
• NSAIDs
• Enzyme inhibition in HIV therapy
• Recombinant drugs and systems for their production
Bibliography
Selected scientific papers and copy of slides can be downloaded from the Elly
website.
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
Oral lessons integrated with informatic tools and the support of multimedia
Assessment methods and criteria
During the course 2 written tests (pre-appelli) are planned. If the result is positive for both tests, the exam will be passed, with a mark that will be the average of the two marks. Alternatively, an oral exam will be carried out during the regular exam sessions together with the exam of the module Chimica Fisica Biologica.
The written tests (pre-appelli) will be composed of multiple-choice questions and open questions.
If the final mark will be positive (at least 18/30), the mark will be averaged with the mark of the module Chimica Fisica Biologica to determine the final mark of the exam Interazione Farmaco-Biomolecole.
Other information
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