C9550 - CHIMICA DEI RECETTORI E BIOCATALISI

Learning outcomes

Topics in receptor chemistry, pharmacodynamics, pharmacokinetics, neurotransmitters, and strategies for the design of drugs targeting the central nervous system. In addition, the student is able to classify enzymes, explain their mechanisms of action and the stereochemical aspects of biocatalysis, use enzymes for alternative synthetic approaches, and apply their chemical expertise to industrial applications in the pharmaceutical sector. Finally, the student possesses the scientific vocabulary and communication skills necessary to conduct interdisciplinary research and to interact effectively with biologists, biotechnologists, biochemists, and physicians.

Course contents

MODULE 1. RECEPTORS

PREREQUISITES: Organic chemistry, functional groups and their properties and reactivity; chemistry of natural products, carbohydrates, lipids, amino acids, and nucleotides.

Part 1. Drug Discovery and Development.

QSAR, high-throughput screening, virtual screening, computer-assisted drug design, molecular docking, combinatorial chemistry, etc.

Drug development through peptidomimetics.

Part 2. Fundamentals of Medicinal Chemistry.

Pharmacodynamics. Molecule–receptor interactions. Agonism and antagonism. Different types of receptors: ion channels, GPCRs, nuclear receptors, etc. Signal transmission, tolerance, desensitization, and termination of effect.

Pharmacokinetics. ADMET profile of a drug.

Part 3. Communication in the Central Nervous System.

Signal transduction within the cell and nucleus. Neurotransmitter secretion. Biosynthesis, mechanisms of action, and chemical modulation of neurotransmitters.

Opioid system: origin, role in pain transmission, and therapeutic applications. Opiates and endogenous peptides. Strategies applied to the synthesis of analgesics. Receptor studies and structural analysis.

Dopamine and adrenaline systems. Acetylcholine system. GABA system. Hormone-mediated signaling.

Examples of drugs: hormones, antidepressants, neuroleptics (antipsychotics), drugs of abuse, etc.

PRACTICAL SESSIONS.

Synthesis of compounds of pharmaceutical interest.

In silico exercise: design of antihistamine compounds using online resources for virtual screening of pharmacokinetic and pharmacodynamic properties.

MODULE 2. ENZYMATIC CATALYSIS

Introduction to enzymatic catalysis in organic synthesis, historical background, and economic impact.

Classification, structure, and sources of enzymes.

Fundamentals of enzyme kinetics, enzyme specificity, and selectivity. Acid–base mechanisms, covalent catalysis, and catalysis by metalloenzymes.

Use of enzymes in organic synthesis. Advantages and limitations of enzymatic catalysis.

Mechanisms and synthetic applications of selected enzyme classes: hydrolases, proteases, transaminases, oxidoreductases, and lyases.

Use of enzymes in organic solvents and non-conventional media.

Biocatalysis for sustainability and enzyme immobilization techniques.

Discussion of industrial applications in the pharmaceutical, textile, food, biorefinery, and biocatalysis sectors.

Readings/Bibliography

Farmacologia generale e molecolare, Clementi, Fumagalli, UTET

Siliprandi & Tettamanti - Biochimica Medica - Parti I e II - PICCIN

Santagada, Caliendo - Peptidi e peptidomimetici - PICCIN

Intro alla Chimica Fermaceutuca, Patrick, Edises

Faber, Biotransformation in Organic Chemistry

Voet, Voet, Pratt, Fondamenti di Biochimica

Garrett, Grisham, Biochemistry

Gerhartz, W. Enzymes in Industry

Wong, C.H.; Whitesides, G. M: Enzymes in Synthetic Organic Chemistry

Teaching methods

Lecture-based teaching with slide presentations, group exercise: synthesis of CNS (central nervous system) drugs. Practical exercise: design of antihistamine compounds (laptop required).

Assessment methods

The examination is oral and consists of two parts. The first part assesses knowledge related to the Receptor Chemistry module, while the second focuses on topics covered in the Enzyme Chemistry module.

The final grade is determined by the scores obtained in the two parts, weighted equally. For both sections, the oral examination is designed to evaluate the competencies and skills acquired, starting from the theoretical aspects of the course. In addition, students will be asked to solve exercises on the board, discussing procedures, reaction mechanisms, and synthetic pathways.

On average, approximately 25 minutes are devoted to each module.

Grading Scale

Fail (<18): Significant gaps in course content are evident, along with deficiencies in fundamental chemical knowledge, inappropriate use of scientific terminology, and an inability to navigate the topics covered in the course.

Pass (18–23): Barely adequate use of scientific language, limited reasoning and argumentation skills, and only minimal knowledge of the examination topics.

Good (24–27): Good factual knowledge of the subject, together with satisfactory analytical and synthesis skills, and correct use of technical terminology.

Excellent (28–30 cum laude): In addition to strong knowledge, students must demonstrate the ability to elaborate on concepts independently. This requires a clear and comprehensive understanding of the subject matter, strong reasoning skills, broad mastery of the discipline and its technical language, and the ability to solve complex exercises.

Note: A solid background in organic chemistry and biochemistry is required in order to place the course topics in the proper scientific context.

Students with Specific Learning Disorders (SLD) and/or temporary or permanent disabilities: are encouraged to contact the appropriate University Office as early as possible (https://site.unibo.it/studenti-con-disabilita-e-dsa/it/per-gli-studenti ) so that suitable accommodations can be proposed. Requests for accommodations must be submitted to the instructor well in advance (at least 15 days before the examination date). The instructor will evaluate their appropriateness in light of the course learning objectives.

Teaching tools

PowerPoint presentations and course handouts available at Unibo/Gentilucci/Teaching Materials.

Electronic presentations available on AMS Campus.

Office hours

See the website of Luca Gentilucci

See the website of Alessandra Tolomelli