B2916 - Analytical Methodologies for Drug Discovery

Learning outcomes

The course aims to provide the industrial pharmacist with an overview of the main (bio)analytical techniques for the evaluation of the recognition mechanisms between active molecules and molecular targets, providing the tools for a rational prioritization of active molecules in the discovery and development of new drugs, including emerging therapeutic classes. At the end of the course, which also includes single-place laboratory exercises, the student: - knows the main analytical techniques used for the study of drug-molecular target interaction; - is able to determine the thermodynamic and kinetic parameters that regulate the formation of a drug-molecular target complex (proteins, nucleic acids); - will be able to plan experimental investigations for the structural characterization and for the definition of molecular recognition mechanisms to support the design and development of new drugs.

Course contents

1. Introduction to analytical approaches for the study of drug-molecular target biorecognition phenomena and for the definition of binding parameters.
2. Highly automated screening techniques based on immobilized targets:
• Bioreactors. Applications in the drug discovery process: selection and optimization of active molecules.
• Surface plasmon resonance (SPR) optical biosensors. Pharmaceutical and biopharmaceutical applications to support emerging therapeutic strategies: antibodies, aptamers, small molecules interacting with nucleic acids.
3. MicroScale Thermophoresis (MST). Applications in the pharmaceutical and biopharmaceutical fields.
4. Circular dichroism (CD). Approaches to study protein misfolding as a target for new therapeutic strategies.
5. Mass spectrometry-based methods for characterizing the molecular target and binding of covalent and non-covalent ligands.

Exercises in the computer room with dedicated software.
• Use of mass spectrometry for the identification and characterization of proteins, for the characterization of structural changes in proteins, for the monitoring of enzymatic activity.

• Use of the optical biosensor and circular dichroism to study the phenomena of molecular recognition.

Readings/Bibliography

Useful texts for consulatation only: V. Cavrini, V. Andrisano. Principi Analisi farmaceutica. Società editrice Esculapio ed. 2013.

Scientific publications available through the Virtual Learning Environment [https://virtuale.unibo.it/] platform. 

Teaching methods

Frontal lectures and laboratories in the computer room.

In consideration of the type of activity and the teaching methods adopted, the attendance of this training activity requires the prior attendance of all students to the training Modules 1 and 2 on safety in the study places [https://elearning-sicurezza.unibo.it/], in e-learning mode.

Assessment methods

The learning assessment test consists of oral interviews on the topics covered during the course.

Teaching tools

Slides, scientific publications and other teaching material made available through the Virtual Learning Environment [https://virtuale.unibo.it/] platform.

Office hours

See the website of Marina Naldi