Proteins as molecular targets in drug design

During the lecture, the main types of proteins important for pharmacology will be discussed. On the example of GPCR receptors, the drug design process will be presented, taking into account the relationship between the structure of the compound and its activity, as well as data from the clinical phase.

A lecture introduces basic information on the main types of proteins which are molecular targets of currently used drugs, with particular emphasis on transmembrane proteins. Among enzymes i.a. kinases and proteases will be presented, among receptors - GPCR receptors and nuclear receptors, among transport proteins - SLC transporters. Additionally, proteins constituting new molecular targets will be presented, e.g. adhesive proteins. The next part of the lecture will be dedicated to biochemical processes corresponding to these proteins. The concept of a signaling and metabolic pathway will be introduced on the example of drugs modulating the activation of GPCR receptors and on the example of antibiotics. The last part of the lecture will be dedicated to the drug design process, taking into account e.g. virtual screening based on either ligand or receptor structure, ADMETox, drug repositioning, drug adverse reactions and pharmacogenomics. The relationship between the chemical structure of the proposed drug and its activity will be also discussed, as well as selectivity and specificity of drugs targeting GPCR receptors.

1. An Introduction to Medicinal Chemistry, P. Graham, Oxford University Press, 1995.

2. Biochemistry, L. Stryer, Springer Berlin, 2017

3. Medical Genetics, Lynn B. Jorde & John C. Carey & Michael J. Bamshad, Elsevier, 2019.

4. Additional literature provided during the lecture.

Students will be able to describe basic types of proteins – targets of modern drugs and describe the corresponding biochemical processes in a basic way. Students will be able to describe the drug design process on selected example and to interpret associated clinical data. Students will be able to explain basic terms related to drug design.

A written exam with at least 60 % is required to pass. It will cover issues discussed during the lecture. Class attendance is required with two possible absences.