The aim of the thesis is to review different bioconjugational approaches for the development of new anticancer and antimicrobial agents displaying improved performance in the treatment of cancer and microbial infections, when compared to current treatment approaches. Considering that this technology was originally developed for oncology, we initially focused on the detailed description of the mechanism of action of antibody-drug conjugates for the treatment of cancer. Every component of the conjugates is individually presented and a detailed description of their mechanism of action is provided. The majority of the thesis is focused on the explanation of the complexity of antimicrobial resistance and a detailed presentation of the most recent examples of antibody-antibiotic conjugates for the target elimination of Staphylococcus aureus and Pseudomonas aeruginosa. The main part of the thesis describes the important properties of these important pathogens, the key characteristics of the conjugates, their structural elements and the mechanism of action of each conjugate against bacteria. Furthermore, a detailed insight into steroid bioconjugates is provided. Different examples of the synthesis of certain antibiotic analogues by conjugation of steroids, such as bile acids and other biological molecules, such as polyamines are presented. The main purpose of this thesis is to show how the new bioconjugation approaches allow the use of certain antibiotics or antimicrobial agents, whose application has been restricted due to the toxicity and other undesired properties caused by their antimicrobial activity.
|
