Proteins as molecular targets in drug design 1200-1PMTDDL

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.