- Docente: Maria Laura Bolognesi
- Credits: 5
- SSD: CHIM/08
- Language: Italian
- Teaching Mode: Traditional lectures
- Campus: Bologna
- Corso: Single cycle degree programme (LMCU) in Chemistry and Pharmaceutical Technologies (cod. 8412)
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; design of competitive and non-competitive agonists for the treatment of neurological disorders. Vanilloid receptors: channel structural and functional organization; design of agonist and antagonists for the treatment of pain.
GPCR superfamily : classification and models. The muscarinic receptor: structural organization and functional domains; design 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; design of agonists, antagonists and SERMs.
Tyrosine kinase receptor superfamily : classification and models. The epidermal growth factor receptor: ATP binding site topology. Design of catalytic site inhibitors: from competitive to covalent inhibitors. Paradigm shift from selective to multi target ligands. Smart chemotherapy: small molecules vs antibodies.
Readings/Bibliography
Lecture notes, selected references will be provided during the class
Teaching methods
Lectures in class
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