| Summary: | Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmacology and Toxicology Candidate: Mgr. Daniela Číhalová Supervisor: Prof. PharmDr. František Štaud, PhD. Consultant: PharmDr. Martina Čečková, PhD. Title of doctoral thesis: Interactions of cyclin-dependent kinase inhibitors with ABC efflux transporters in vitro: impact on multidrug resistance in cancer therapy Cyclin-dependent kinases play an important role in cell cycle regulation and their enhanced activity can lead to the development of various malignancies. Therefore, these kinases have become a rational target for inhibition in cancer therapy and many compounds from the group of cyclin-dependent kinase inhibitors (CDKIs) are being evaluated in clinical trials. ABC efflux transporters are expressed in physiological tissues, where they influence the absorption, distribution and elimination of their substrates including drugs and determine their pharmacokinetic properties. On the other hand, overexpression of ABC transporters in cancer cells can contribute to the development of multidrug resistance (MDR) against structurally and functionally diverse compounds. Three members of the ABC transporter family play the most prominent role in the development of MDR: ABCB1 (P-glycoprotein), ABCG2 (breast cancer...
|
|---|
