Didattica / Classes 2024-2025

8 hours -Lectures will be helded in the second half of JUNE 2025

Description

This interactive course offers participants hands-on experience in the fascinating world of structural biology. Through theoretical and laboratory sessions, students will explore advanced techniques of protein expression, purification, characterization, and crystallization, as well as data analysis. The main focus will be on obtaining detailed molecular structures from crystals, providing a comprehensive overview of the methods used in modern structural biology. Additionally, the course will introduce key concepts of inorganic chemistry, highlighting the role of metal ions in biological systems, metalloenzymes, and the application of inorganic compounds in structural studies. Students will gain insights into how coordination chemistry and metal-based drugs influence protein function and stability. This course will provide students with fundamental practical and theoretical skills to address challenges and explore opportunities in biological research, medicinal chemistry, and bioinorganic chemistry.

Description
This cycle of lessons will be principally focused on the modulation of γ-aminobutyric acid type A receptors
(GABA A Rs) via the small molecule-protein interaction on the benzodiazepine (BZDs) allosteric binding site.
γ-Aminobutyric acid (GABA) is the major inhibitory neurotransmitter within the central nervous system and
GABA A Rs are responsible for the point-to-point transfer of information across the synapse, but they are also
located extrasynaptically, where they exert a more modulatory and tonic inhibitory effect. The so-called
classical BZDs, such as Diazepam, are non-selective positive allosteric modulators of GABA A Rs that
potentiate the effects of GABA through the different receptor subtypes with equivalent affinity and
efficacy. Starting from this point, this course will explore the design, synthesis and clinical development of
novel GABA A Rs subunit-selective agents which could be used in place of BZDs to treat anxiety disorders,
cognitive disfunctions and other neurological disorders. In addition, a discussion on the use of organic
chemistry to address in vivo-related issues will be given. The course will also give an overview regarding
other allosteric sites of interest present in the different GABA A Rs (e.g. neurosteroids binding site) and will
compare this approach with other targets on different GABA receptors (i.e. GABA B Rs).

n. hours: 12 (6 lessons, 2 h each)
Possible dates (to be confirmed)

12-13/06/25
19-20/06/25
26-27/06/25

Lectures will be helded in the second half of APRIL 2025

COURSE TIMETABLE