To study action mechanism of transport proteins ABCB1 and ABCG2

How is the resistance of cancer cells affected by ABC-transporter? A related new study paper through recombinant mouse proteins has been published in the open access journal BioDiscovery, studying the second generation tyrosine kinase inhibitor (TKI) - dasatinib (DAS) and ATP binding (ABC) transport proteins ABCB1 and ABCG2 mechanism to assess whether these drug transporters may impair the therapeutic effect.

The "targeted" treatment of cancer is an effective way to minimize the damage to healthy cells. Targeted therapy has revolutionized cancer treatment in the past few decades through the use of reasonably designed drugs that interfere with the specific molecules (molecular targets) necessary for the proliferation and survival of malignant cells.

Although DAS is an excellent choice for the treatment of chronic myeloid leukemia resistant to imatinib, recent laboratory studies have shown that the antiproliferative effect of DAS can be significantly reduced when ATP binds to ABC transporters, ABCB1 and ABCG2.

"Although this relationship is important, we still don't know whether these drug transporters will damage DAS's clinical treatment," explains Dr. Petr Mlejnek, Ph.D., Olomouc, University of Palacky, Czech Republic. "We believe that the expression level of drug transporters is a key factor in the outcome and may therefore help explain the existing controversy. We decided to study the relationship between ABCB1 and ABCG2 expression levels and in vitro resistance to DAS.

In their study, Dr. Petr Mlejnek from the University of Olomouc Palacky, Czech Republic, and his team observed that the expression level of ABC-transporters studied was an important factor influencing cell resistance. Although the anti-proliferative and pro-apoptotic effects of DAS can be reduced by ABCB1 or ABCG2 at clinically relevant concentrations, the actual effect of ABC transporters on DAS efficiency depends on their expression levels. The lower expression level of ABC transporters mediates lower resistance. Considering the fact that the expression levels of ABCB1 and ABCG2 transporters are almost not high in clinical samples, their contribution to overall resistance to DAS is significant. Flarebio offers high-quality recombinant proteins such as recombinant ECEL1 at good prices.