72964 - Research and Development of Drugs and Small Molecules

Academic Year 2021/2022

Learning outcomes

Al termine del corso lo studente possiede le conoscenze chimico-farmaceutiche di base sugli approcci e le metodologie utilizzate correntemente nell'industria farmaceutica nella scoperta e sviluppo di nuovi farmaci, così come gli approcci innovativi per i farmaci in sperimentazione. In particolare lo studente è in grado di conoscere gli aspetti peculiari riguardanti la progettazione e il meccanismo d'azione a livello molecolare di farmaci aventi struttura di “piccole molecole”.

Course contents

Drug discovery process in the post-genomic era.

Biological macromolecules as drug targets: proteins, (enzymes, structural and carrier proteins, ion pumps, ion channels, membrane and intracellular receptors), nucleic acids, lipids, carbohydrates.

Ion channel receptor superfamily: classification and models. The nicotinic receptor (LGIC): channel structural and functional organization; development of competitive and non-competitive agonists for the treatment of neurological disorders. Vanilloid receptors: channel structural and functional organization; development of agonist and antagonists for the treatment of pain.

GPCR superfamily: classification and models. The muscarinic receptor: structural organization and functional domains; development of allosteric/bitopic modulators for the treatment of Alzheimer's disease.

Intracellular receptor superfamily: classification and models. The estrogen receptor: structural organization of the ligand binding pocket (LBP) and receptor conformational states; development of agonists, antagonists and SERMs.

Tyrosine kinase receptor superfamily : classification and models. The epidermal growth factor receptor: ATP binding site topology. Development of catalytic site inhibitors: from competitive to covalent inhibitors. Paradigm shift from selective to multi-target ligands. Smart chemotherapy: small molecules vs antibodies.



Slides and lecture notes, selected references will be provided during the class

Teaching methods

Lectures in class (Tutor Presentation and Tutor Guided Group Discussion),

Assessment methods

A comprehensive final viva voce examination, meant to assess the skills acquired during the course, is given.

Teaching tools

Videoprojector, PC

Office hours

See the website of Maria Laura Bolognesi


Good health and well-being

This teaching activity contributes to the achievement of the Sustainable Development Goals of the UN 2030 Agenda.