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Study of the binding interaction of tyrosine kinase inhibitors with serum albumin
Rodová, Marie ; Indra, Radek (advisor) ; Heidingsfeld, Olga (referee)
Sunitinib and vandetanib are anti-cancer medications prescribed for medullary thyroid cancer (in the case of vandetanib) and for renal cell carcinoma, gastrointestinal stromal tumor, and pancreatic cancer (in the case of sunitinib). They belong to the group of tyrosine kinase inhibitors and act by exhibiting anti-angiogenic effects and by inhibiting tumor cell proliferation and survival through VEGFR. Additionally, vandetanib also inhibits tumor cell survival via EGFR and RET. In the presented thesis, we investigated the binding interaction between serum albumin and the TKIs vandetanib and sunitinib using BSA, HSA, and blood plasma. We examined the differences in interaction between the TKIs and various serum albumins, including pure BSA, pure HSA, and blood plasma, as well as the nature and location of the binding interaction. Additionally, we studied the influence of other ligands on this interaction and the photosensitivity of sunitinib itself. Utilizing spectroscopic techniques, including UV-VIS absorption and fluorescence quenching, we have determined the Stern-Volmer and binding constants, as well as the thermodynamic parameters, for the binding interactions of sunitinib and vandetanib with BSA and HSA. Our results indicate that complex formation occurs between BSA and sunitinib, BSA and...
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Binding of low-molecular weight ligands to serum albumin
Buša, Michal ; Hudeček, Jiří (advisor) ; Vaněk, Ondřej (referee)
In this Thesis, we studied the possibilities of an enlargement of the existing practical task in the Advanced practical course in biochemistry I, dealing with interaction of a dye (bromophenol blue) with serum albumin. Experimental protocol was proposed and tested, allowing the inclusion of Scatchard plot (in addition to the previously used Job plot). As part of the Thesis, the new protocol for students is presented, which may help them to understand the most used approaches for studying the stoichiometry of protein-ligand complexes. In Czech.
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