Interactions of Drugs with their Molecular Targets 1200-2BLOK4-BIOW6
In this lecture the structures of various kinds of complexes with ligands as well as the mechanisms of drug action on the molecular level will be shown. Currently, the large number of 3D structures of these complexes allows for detailed analyses of interactions in complexes drug-target. Described structures will be presented in dynamic view to show their thermal motions and especially a dynamic mutual induced fit of ligand and receptor or enzyme in their binding sites.
The following essential groups of drugs will be described based on selected examples: antibacterial (penicillins, cephalosporins, blocking DNA or RNA (ribosome) of bacteria), antiviral (acting on particular enzymes of viruses: protease, neuraminidase, reverse transcriptase, etc.), anticancer (blocking of DNA, blocking of topoisomerases in complexes with DNA, blocking of microtubule growth, blocking of kinases, proteasome, etc.), anti-inflammatory (acting on enzymes i.a. COX1/2, effects of drug selectivity), drugs for reproductive medicine, drugs acting on GPCRs (G-protein-coupled receptors) (agonists/antagonists and other ligand types, biased ligands and functional selectivity).
Some other aspects of drug actions will be also illustrated: reasons of drug resistance to antibiotics, the structure and action of viruses, weak points of viruses – how one can block the virus, synthesis of proinflammatory factors from arachidonic acid, transduction of signals through the cell surface by GPCRs, strategies of drug actions on neurons(synapses), drugs and poisons, and other issues.
- Total student workload: 1.5 * 30 = 45 hours.
- Class participation: 15 hours
- Preparing for classes and exam: 20 hours
- Consultations with lecturer: 10 hours
Main fields of studies for MISMaP
Type of course
Mode
Prerequisites (description)
Course coordinators
Learning outcomes
Knowledge: The graduate knows and understands
(K_W01) Has extensive knowledge of the place of chemistry in the system of natural sciences and its importance for the human development.
(K_W05) Possesses in-depth knowledge and skills in the selected chemical specialization, enabling the use of methods and concepts appropriate for this specialization and enabling independent research.
(K_W10) Has a good understanding of current developments in chemistry and the latest scientific discoveries in a given chemical specialization.
Skills: The graduate is able to
(K_U08) Possesses advanced knowledge and skills enabling the use of professional literature, databases, and other sources of information, and the ability to assess the reliability of obtained information.
(K_U11) Is able to discuss the place of chemistry in the system of natural sciences and its importance for the development of our civilization.
Assessment criteria
Requirements related to participation in class - none.
Permitted number of justified absences - 50%.
Written exam with 50% of closed questions and 50% of open questions -
the same for correction test.
Required minimum 50% of correct answers to pass.
Practical placement
N/A
Additional information
Additional information (registration calendar, class conductors, localization and schedules of classes), might be available in the USOSweb system: