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.

PART2

• Introduction to enzymatic catalysis in organic synthesis, historical background and economic impact.
• Classification, structure of enzymes and sources.
• Outlines of enzymatic kinetics, specificity and enzymatic selectivity. Acid-base mechanism, covalent catalysis, metal-enzyme catalysis.
• Use of enzymes in organic synthesis. Advantages and limitations in the use of enzymes in catalysis
• Mechanisms and applications of some classes of enzymes: Hydrolases, proteases, transaminases, oxidoreductive enzymes, lyases.
• Use of enzymes in organic solvents and non-conventional media.
• Biocatalysis for sustainability, enzyme immobilization techniques.
• Discussion of industrial applications in the pharmaceutical, textile, food, biorefineries, biocatalysis fields

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

Method

The exam is oral and consists of two parts: the first aims to assess knowledge of the receptor chemistry module, and the second explores the chemistry of enzymes.

The grade is based on equal scores for the two parts. For both parts, the interview is designed to assess the skills and abilities acquired, starting with theoretical aspects.

Additionally, exercises will be provided on the board, discussing procedures, mechanisms, and synthesis.

The average time required is 25 minutes for each module.

Grading criteria

Failure: significant gaps in content; lack of basic knowledge of chemistry, inappropriate language, lack of orientation within the topics covered in the course.

Sufficient: barely appropriate language, poor argumentative ability, and minimal knowledge of the exam topics (grade 18-23)

Good: knowledge of the subject matter, and reasonable ability to synthesize and elaborate analysis, using correct technical language (grade 24-27)

Excellent: in addition to knowledge, elaboration skills are required; a clear and comprehensive understanding of the topics is required, along with excellent argumentative ability, command of broad skills and specific technical language, and the ability to solve complex exercises (grade 28-30 cum laude).

N.B.: Basic knowledge of organic chemistry and biochemistry is required to put the topics into perspective.

Students with learning disorders and\or temporary or permanent disabilities: contact the office responsible (https://site.unibo.it/studenti-con-disabilita-e-dsa/en/for-students) a.s.a.p. so that they can propose acceptable adjustments. The request for adaptation must be submitted in advance (15 days before the exam date) to the lecturer, who will assess the appropriateness of the adjustments, taking into account the teaching objectives.

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 Alessandra Tolomelli