Impact of membrane drug transporters on resistance to small-molecule tyrosine kinase inhibitors

C Neul, E Schaeffeler, A Sparreboom, S Laufer… - Trends in …, 2016 - cell.com
Small-molecule inhibitors of tyrosine kinases (TKIs) are the mainstay of treatment for many
malignancies and represent novel treatment options for other diseases such as idiopathic …

Towards Comprehension of the ABCB1/P-Glycoprotein Role in Chronic Myeloid Leukemia

RC Maia, FC Vasconcelos, PS Souza, VM Rumjanek - Molecules, 2018 - mdpi.com
The introduction of imatinib (IM), a BCR-ABL1 tyrosine kinase inhibitor (TKI), has
represented a significant advance in the first-line treatment of chronic myeloid leukemia …

Wnt/β-catenin pathway regulates ABCB1 transcription in chronic myeloid leukemia

S Corrêa, R Binato, B Du Rocher, MTL Castelo-Branco… - BMC cancer, 2012 - Springer
Background The advanced phases of chronic myeloid leukemia (CML) are known to be
more resistant to therapy. This resistance has been associated with the overexpression of …

[HTML][HTML] Association between imatinib transporters and metabolizing enzymes genotype and response in newly diagnosed chronic myeloid leukemia patients …

S Angelini, S Soverini, G Ravegnini, M Barnett… - …, 2013 - ncbi.nlm.nih.gov
Imatinib has so far been the first-choice treatment in chronic myeloid leukemia with excellent
results. However, only a proportion of patients achieve major molecular response–hence the …

Facilitated Transport of EGFR Inhibitors Plays an Important Role in Their Cellular Uptake

BS Wong, EL Dunnington, R Wu, JI Kim, K Hu… - Analytical …, 2024 - ACS Publications
Epidermal growth factor receptor (EGFR) is a transmembrane protein commonly targeted by
tyrosine kinase inhibitors (TKIs) as a front-line therapy for patients with many cancers …

The hOCT1 SNPs M420del and M408V alter imatinib uptake and M420del modifies clinical outcome in imatinib-treated chronic myeloid leukemia

A Giannoudis, L Wang, AL Jorgensen… - Blood, The Journal …, 2013 - ashpublications.org
Although the prognosis of chronic myeloid leukemia (CML) patients treated with imatinib is
good, many fail to develop an optimal response or lose one. This heterogeneity could be …

OCT1 and imatinib transport in CML: is it clinically relevant?

DB Watkins, TP Hughes, DL White - Leukemia, 2015 - nature.com
Imatinib is a highly effective therapy for chronic phase-chronic myeloid leukaemia (CP-CML)
patients; however, responses to frontline imatinib are variable. The human organic cation …

Chronic myeloid leukemia in the era of tyrosine kinase inhibitors: an evolving paradigm of molecularly targeted therapy

MAM Ali - Molecular diagnosis & therapy, 2016 - Springer
Chronic myeloid leukemia (CML) is a myeloproliferative neoplasm, characterized by the
unrestrained expansion of pluripotent hematopoietic stem cells. CML was the first …

The role of reduced intracellular concentrations of active drugs in the lack of response to anticancer chemotherapy

JJG Marin, MJ Monte, AG Blazquez… - Acta Pharmacologica …, 2014 - nature.com
A major difficulty in the treatment of cancers is the poor response of many tumors to
pharmacological regimens. This situation can be accounted for by the existence of a variety …

Organic Cation Transporter 1 (OCT1) mRNA expression in hepatocellular carcinoma as a biomarker for sorafenib treatment

D Grimm, J Lieb, V Weyer, J Vollmar, F Darstein… - BMC cancer, 2016 - Springer
Background The polyspecific organ cation transporter 1 (OCT1) is one of the most important
active influx pumps for drugs like the kinase inhibitor sorafenib. The aim of this retrospective …