RECEPTOR CHEMISTRY
cod. 1004495

Academic year 2024/25
5° year of course - First semester
Professor
Marco PIERONI
Academic discipline
Chimica farmaceutica (CHIM/08)
Field
Discipline chimiche, farmaceutiche e tecnologiche
Type of training activity
Characterising
40 hours
of face-to-face activities
5 credits
hub: PARMA
course unit
in ITALIAN

Integrated course unit module: FOOD CHEMISTRY - RECEPTOR CHEMISTRY

Learning objectives

AT the end of the course, the student should be able to:

Knowledge and understanding: To be acquainted with the chemical and the physico-chemical bases that regulate the operation of receptors; to understand the mechanisms through which small molecules activate or block nuclear or membrane receptors

Applying knowledge and understanding: The student must show to be able to synthesize their knowledge, their ability to analyze and understand the structure-activity relationships for classes of drugs through devising and sustaining critical arguments in the field of medicinal chemistry, proving to be able to have a professional approach to discipline

In addition, the teaching aims to achieve autonomy of judgment and Communicative Abilities.

Making judgments: Students will be able during the lessons, to interact with the themes suggested by the teacher and, even with the help of the recommended texts and teaching materials, be able to make independent judgments

Communication skills: The student must be able to clearly and critically present the results of their individual calculations, demonstrating knowledge of research topics carried out during the program

Learning skills: to be acquainted with a method of study and analysis that is tailored on the student and efficient, in order to extend the field of knowledge to different disciplines and in order to make his preparation suitable to higher-learning experiences.

Prerequisites

Organic Chemistry , Medicinal Chemistry , Biochemistry , Physiology , Pharmacology

Course unit content

1) Structure of receptors
- Binding receptor/molecule of interest
- inhibition of receptors
- In-depth analysis of peculiar classes of receptors
2) Nuclear receptors
- classification
- structure
- molecular basis for transcriptional activity
- definition of a steroid hormone
- nomenclature and chemical structure of steroid hormones
- biosynthesis of steroid hormones
- mechanism of action of steroid hormones

3) Corticosteroids
-biosynthesis
-metabolism
-metabolic syndrome
-pharmacokinetic
-SAR of corticosteroids
-Synthesis of cortisone
4) Female sex hormones
-Biosynthesis
-Mechanism of action
-Contraceptive pill
-Marker degradation
-Synthesis of progesterone
5) Male sex hormones
-Biosynthesis
-Mechanism of action -Anabolic steroids
-Doping
-SAR of androgens
-Synthesis of Testosterone
-Reverse anorexia
6) Hyperlipoproteinemia and cardiovascular disease
- the cholesterol and other blood lipids
- cholesterol biosynthesis
- lipoproteins
- hyperlipoproteinemias
- synthesis of Ezetimibe
7) HMG - CoA reductase inhibitors ( statins )
-Stucture
-SAR of statins
-Synthesis of Fluvastatin
8) Medicines to treat diabetes
- type 1 diabetes
- type 2 diabetes
9) Oral hypoglycemic
-Structure and mechanism of action
-Sybthesis of Rosiglitazone
10) Bile acids
-Biosynthesis
-Structure and SAR
-Therapeutic activity
-Obeticholic acid/Synthesis

Full programme

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Bibliography

Gragam L. Patrick ,
Pharmaceutical Chemicals,
III edition Edises

Teaching methods

The course will be conducted through lectures. Each lesson is a teaching module unit , in which , for each topic , are given to the student the foundation for acquiring knowledge and understanding , and to apply the knowledge and understanding to the problem treated in the unit of learning module

Assessment methods and criteria

The final evaluation will be based on a written exam.
The final exam will be made of multiple aswer questions, to be selecetd by the students. To each answer will be applied a score, that can be also negative if the answer is not correct. In some cases, students will be asked to draw and/or describe the mechanism of some reactions.
the exam is passed when the final score is equal or more than 18/30

Other information

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