diplomsko delo
Tjaša Drožina (Author), Črtomir Podlipnik (Mentor)

Abstract

Tirozin kinaze (TK) imajo ključno vlogo pri številnih bioloških procesih, kot so celična rast, diferenciacija, migracija, metabolizem in apoptoza. Nepravilnosti v delovanju tirozin kinaz so prisotne pri rakavih obolenjih, kar kaže na njihovo pomembno vlogo tudi pri procesu angiogeneze. Signalne poti fosfotransferaz lahko inhibiramo s pomočjo majhnih molekul zaviralcev. Slednji delujejo na različne načine, med drugim lahko tekmujejo z molekulo ATP za vezavo na ATP-vezavno mesto in s tem preprečujejo fosforilacijo tirozinskih aminokislinskih ostankov. Poznamo receptorske in nereceptorske inhibitorje tirozin kinaz, ki jih lahko klasificiramo glede na to, katero družino TK inhibirajo. Zaviralci so lahko specifični in inhibirajo le eno ali nekaj vrst tirozin kinaz. Takšni primeri so dasatinib, ki zavira ABL, geftinib, znan kot inhibitor kinaze EGFR ter sunitinib, ki je zaviralec VEGFR. Inhibitorji lahko preprečujejo tudi delovanje več vrst tirozin kinaz hkrati, takšen primer je stavrosporin. Slednji način inhibicije je sicer učinkovitejši, vseeno pa je pomembna čim boljša selektivnost, saj se s tem zmanjšajo možni neželeni učinki zdravljenja.

Keywords

encimi;proteinske kinaze;tirozin kinaze;zaviralci tirozin kinaz;angiogeneza;selektivnost;zdravljenje raka;molekulsko modeliranje;diplomska dela;

Data

Language: Slovenian
Year of publishing:
Typology: 2.11 - Undergraduate Thesis
Organization: UL FKKT - Faculty of Chemistry and Chemical Technology
Publisher: [T. Drožina]
UDC: 577.15(043.2)
COBISS: 14593027 Link will open in a new window
Views: 782
Downloads: 229
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Other data

Secondary language: English
Secondary title: Molecule models of tyrosine kinase inhibitors
Secondary abstract: Tyrosine kinases play a key role in a diverse biological processes such as cell growth, differentiation, migration, metabolism and apoptosis. However, dysregulation of tyrosine kinases has been found in a different types of cancer, and have been shown to correlate with angiogenesis. One way to block phosphotransferases pathways is inhibition with small molecule inhibitors. They operate by various mechanisms, one of them is to compete with ATP for the ATP binding site and reduce phosphorylation of tyrosine residues. We know receptor and nonreceptor inhibitors, which can be classified according to their acting target, for example ABL TKIs (dasatinib), EGFR TKIs (gefitinib), VEGFR TKIs (sunitinib)... Many tyrosine kinase inhibitors, such as staurosporine, target a number of different kinases, which are involved in several signaling pathways. They are deffinitely more effective, but more important is to develop inhibitors with high selectivity and minimize posible treatment toxicities.
Secondary keywords: tyrosine kinase;tyrosine kinase inhibitors;angiogenesis;selectivity;cancer therapy;
Type (COBISS): Bachelor thesis/paper
Study programme: 1000373
Embargo end date (OpenAIRE): 1970-01-01
Thesis comment: Univ. v Ljubljani, Fak. za kemijo in kemijsko tehnologijo, UNI Kemija
Pages: 31 str.
ID: 11643850