66647 - Medicinal Chemistry and Proteomics

Learning outcomes

At the end of the course, the student knows the basic concepts of medicinal chemistry and knows how to use technologies for proteomics in drug design. In particular, the student acquires knowledge of the fundamental concepts related to the chemical-molecular study of drugs (molecular action mechanisms and structure-activity relationships of drugs), and has theoretical and applicative knowledge of analytical techniques for structural, chemical and stereochemical characterization of drugs of synthetic and biotechnological origin (methodological and application bases of the analysis of the drug isolated or interacting with the molecular target).

Course contents

Module: Medicinal chemistry (3 CFU)

The medicine: basic concepts, and approaches to drug discovery.

Process of action of a drug and phases of the process of action.

Molecular basis of the action of drugs: molecular target and drug-target interactions.

Pharmacokinetic phase: absorption, distribution, metabolism, elimination of a drug.

Drugs and biotechnology: penicillins, artemisinin.

Biotechnological drugs.

Module: Technologies for the proteomics (3 CFU)

Analytical methodologies in functional proteomic studies: a) polarized light spectroscopy, study of the biomolecular recognition mechanism, functional conformational transitions of monomeric and oligomeric proteins; b) mass spectrometry in functional proteomics; c) optical biosensor; characterization of the protein/protein interaction and of higher order structures; d) affinity chromatography; immobilization of soluble proteins, enzymes, and membrane receptors; e) hyphenated techniques, HPLC/MS/MS, HPALC/ HPLC/MS/MS, HPLC/CD, HPLC/MS /optical biosensor; specific applications to ligand fishing, post-translational modification, enzyme inhibitor screening and modulation of protein/protein interaction.

Readings/Bibliography

1. Didactic materials in Virtuale

2. Articles provided by the teacher

3. V. Cavrini, V. Andrisano. Principi Analisi farmaceutica. Società editrice Esculapio ed. 2013

Teaching methods

Lectures

Assessment methods

The exam will assess the knowledge of the basic concepts of the pharmaceutical disciplines, with particular regard to the molecular basis of drug action and the analytical techniques used in proteomics investigations. The two modules will be assessed separately and the final score will be calculated as the average score of the modules.

Teaching tools

Online contents and web access tools.

Office hours

See the website of Michela Rosini

See the website of Marina Naldi