66223 - Receptor Chemistry and Biocatalysis

Learning outcomes

At the end of the course, the student has skills on the issue of receptors, pharmacodynamics, pharmacokinetics, neurotransmitters, and strategies for drug design of the central nervous system. Moreover, he can classify the enzymes and clarify the mechanisms of action and the stereochemical aspects of biocatalysis, and is able to use enzymes for synthesis alternatives and transfer their skills chemicals for industrial applications in the pharmaceutical sector. Finally, he can learn a language that allows him to carry out interdisciplinary research and dialogue with biologists, biotechnologists, biochemists, physicians

Course contents

PREREQUISITES: organiche chemistry, including biomolecules (lipids, sugars, peptides, nucleotides, proteins...

PART 1

Drug discovery and development: QSAR, high throughput, virtual screening, computer-assisted, etc

Cell-cell communication. Signal transduction. Transmitter secretion. Biosynthesis, action mechanism, chemical interference of neurotransmitters- dopamine, adrenaline, acetilcoline, serotonine, GABA, glutammate, hormons, etc.

Ligand -receptor interaction. Agonism/antagonism. Different receptor families: channel, GPCR, etc. Tolerance, desensitization, etc. Opioid system: genesis, pain sedation. Synthesis of analgesics, pharmacokinetics and pharmacodynamics,.

Adhesion: integrins, integrin antagonists.

Biologically active peptides. From peptides to peptidomimetics.

Main classes of neuroactive drugs, antidepressants, neurolectics, drugs of abuse, etc.

Practice: from structure to biological activity and return.

Exercises: synthesis of compounds of pharmaceutical interest.

PART 2

Enzymes as catalysts in organic synthesis. Structure, classification and source of enzymes.

Enzymatic specificity and selectivity. Enzymatic catalysis: acid-base mechanism, covalent mechanism and metallo-enzymes. Advantages and disadvantages in applications of biocatalysis in synthetic processes. C-C bond formation with enzymes. Hydrolases, proteases and nitrilases. Oxoreductive enzymes: dehydrogenases and mono- and dioxygenases.

Immobilization techniques. Synthesis of drugs with biocatalysis. Enzymes for a sustainable chemistry. Enzymes in organic solvents. Importance of enzymes in industry.

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

presentation of power point slides , group work

Assessment methods

The exam is oral and consists of two parts, the first aimed at testing the knowledge of the chemistry of the receptors, the second investigates the chemistry of enzymes. The score is made up of the scores of the two parts in equal proportions. For both, the query begins with an exercise carried out on the blackboard to discuss procedures and syntheses. The second part is the theoretical discussion correlated to the exercize. The basic knowledge of organic chemistry is important to place the arguments in the right perspective. On average, the time required is 40 minutes for both arguments. Upon request, the student can carry out a written examination.

Teaching tools

power-point presentation,available at Unibo/Gentilucci/materiale didattico

Electronic presentations on AMS Campus

Office hours

See the website of Luca Gentilucci

See the website of Daria Giacomini