- 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)
Also valid for Single cycle degree programme (LMCU) in Chemistry and Pharmaceutical Technologies (cod. 8412)
Second cycle degree programme (LM) in Pharmaceutical Biotechnology (cod. 8519)
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
Slides and 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