Learning outcomes of the course unit
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.
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.
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.
• Drug and drug target: definition
• Binding properties of proteins
• Receptors as drug target:
• Intracellular receptors
• 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
• Enzyme inhibition in HIV therapy
• Recombinant drugs and systems for their production
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)
Biologia Molecolare della Cellula
3 ed italiana, Zanichelli (6th Edition)
Copeland R. Evaluation of enzyme inhibition in drug discovery, Wiley.
Introduzione alla Chimica Farmaceutica, Ed. EdiSES
The teaching activities will be carried out in the form of in-person and synchronous online lectures (on the Teams platform) unless otherwise indicated by the University) with short classroom exercises aimed at the student's self-assessment. Each lesson will be preceded by a short summary of the previous one. Students will be offered, on a voluntary basis, the possibility to read and discuss with the teacher a review paper on a topic of their choice.
Assessment methods and criteria
The assessment of the achievements will be carried out in an oral exam in the dates established in the official exam schedule. Three questions will be asked on the main topics of the course. The purpose of the exam is to ascertain the knowledge and understanding of the contents illustrated in the lectures. The scoring, on a scale 0-30, will take into account the level of analysis, the ability to critically apply the knowledge, the appropriateness of the scientific language and the autonomy in the discussion. A lower passing grade (18-23 / 30) corresponds to a basic knowledge of the main contents, even if the answer is not given in total autonomy. A higher score (26-27 / 30) will require more detailed knowledge, good scientific vocabulary and partial autonomy in the discussion. The highest scores (28-30 / 30) are awarded for an excellent level of knowledge and communication skills. The “lode” is awarded if the maximum score for all the questions is reached and the discussion is led by the student in full autonomy. If the candidate is completely unable to answer - even in its fundamental points - to one of the three general questions, the exam will be considered insufficient. 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.