Chemical Biology of compounds with biological interest
| Title | Χημική Βιολογία Ενώσεων Φαρμακευτικού Ενδιαφέροντος / Chemical Biology of compounds with biological interest |
| Code | ΠΜΣΦΧ-004 |
| Faculty | Health Sciences |
| School | Pharmacy |
| Cycle / Level | 2nd / Postgraduate |
| Teaching Period | Winter/Spring |
| Coordinator | Eleni Pontiki |
| Common | No |
| Status | Active |
| Course ID | 600017255 |
Programme of Study: Master's Degree in the Medical Chemistry in Drug Development
Registered students: 0
| Orientation | Attendance Type | Semester | Year | ECTS |
|---|---|---|---|---|
| KORMOS | Compulsory Course | 2 | 1 | 10 |
| Academic Year | 2024 – 2025 |
| Class Period | Spring |
| Faculty Instructors | |
| Class ID | 600272102
|
Course Type 2021
Specialization / Direction
Mode of Delivery
- Face to face
Digital Course Content
- e-Study Guide https://qa.auth.gr/en/class/1/600272102
- At the Website of the School:
- eLearning:
Language of Instruction
- Greek (Instruction, Examination)
Learning Outcomes
The aim of this course is to help students understand oxygen toxicity, generation and activity of free radicals, as well as the critical evaluation of the above in the design and development of molecules capable to protect the organism from radical attack.Another outcome is the knowledge of cannabinoids and their receptors, as well as their agonists and antagonistsandtheir possible applications in contemporary diseases. Upon completion of this course, the student will learn how to design targeted radiopharmaceuticals specific for the detection or radiotherapy of various diseases such as cancer, neurological disorders and Alzheimer disease. Finally, the main principles of Quantitative-Activity Relationships (QSARs) would be analyzed. QSARs studies on histone deacetylase inhibitors (HDACs) and histamine H4 receptor antagonists would be determined in order to correlate the biological activity with the physicochemical properties of the studied novel derivatives.
General Competences
- Apply knowledge in practice
- Retrieve, analyse and synthesise data and information, with the use of necessary technologies
- Work autonomously
- Be critical and self-critical
- Advance free, creative and causative thinking
Course Content (Syllabus)
1. Eleni Rekka
- Chemistry and biological significance of oxygen and oxygen free radicals: Introduction, oxygen toxicity, free radicals, metals, protection of organisms with macromolecules or small molecules. Repairing mechanisms of oxidative stress, lipid peroxidation, protein, sugars, DNA oxidation, free radicals, pathological disorders, drugs, dietary and environmental factors.
- HydrogenSulfide:Biosynthesisandactivity, Therapeutically applications of hydrogensulfide, compounds donors of hydrogen sulfide.
- G-protein coupled receptors: Structure, properties, examples.
- Cannabinoids and their receptors. Cannabinoid receptor agonists and antagonists, as well as possible applications in pathophysiological desorders.
2. Dionysia Papagiannopoulou
1) Development of radiotracers for the non invasive measurement of enzyme activity (e.g. of kinases) as well as the degree of expression of membrane receptors (e.g. G-coupled transmembrane receptors) related to pathological conditions with emphasis in cancer and neurological disorders (dopaminergic neurons and Parkinsonian syndrome). 2) Development of radiotracers for the non invasive detection of beta-amyloid plaques in the brain (Alzheimer’s disease). 3) Biocompatible cycloaddition reactions (“click”) and application in the development of radiolabeled monoclonal antibodies for radioimmunodiagnosis and radioimmunotherapy via the pretargeting approach.
3. Eleni Pontiki
Quantitative Structure Activity Relationships on a) Histone Deacetylase Inhibitors (HDACs) enzymes implicated in cancer and b) H4 receptor antagonists, a receptor implicated with chemotactic reactions and inflammatory and allergic reactions. From the QSAR studies the biological activity is correlated with the physicochemical properties in order to understand the mechanism of action of the studied compounds and design novel derivatives with improved biological activity.
Keywords
free radicals, ΝΟ, receptors of G-protein and cannabinoids, radiotracers, click reactions, QSAR, H4 and HDAC antagonists
Educational Material Types
- Notes
- Slide presentations
Use of Information and Communication Technologies
Use of ICT
- Use of ICT in Course Teaching
- Use of ICT in Communication with Students
Course Organization
| Activities | Workload | ECTS | Individual | Teamwork | Erasmus |
|---|---|---|---|---|---|
| Lectures | 175 | 7 | |||
| Written assigments | 50 | 2 | |||
| Exams | 25 | 1 | |||
| Total | 250 | 10 |
Student Assessment
Description
Eleni Rekka: Written examination at the end of the semester. The written examination process is based on questions that students are asked to answer based on both the knowledge they have gained from teaching and study, as well as the critical thinking and the ability to combine knowledge and information. The examination time is 3 hours. The examinations at the end of the semester are done on the dates, times and places announced by the Department.
Dionysia Papagiannopoulou: Student assessment will be conducted either via written exams or via oral and written presentation of an essay/ assignment at the end of the semester.
Eleni Pontiki: Student assessment will be conducted either via written exams or an assignment. The students are working a project by themselves, searching the literature, and finding data (derivatives and their biological results) analyzing them using several computational techniques and driving equations correlating structure with activity. They discuss the results and they try to explain them.
Student Assessment methods
- Written Exam with Extended Answer Questions (Formative, Summative)
- Written Assignment (Formative, Summative)
Bibliography
Course Bibliography (Eudoxus)
1) Σημειώσεις Δ. Παπαγιαννοπούλου και επιλεγμένα άρθρα ανασκόπησης.
2) J Biomol Struct Dyn, Med Res Rev
Last Update
21-01-2022
