Dasatinib reverses the multidrug resistance of breast cancer MCF-7 cells to doxorubicin by downregulating P-gp expression via inhibiting the activation of ERK …

T Chen, C Wang, Q Liu, Q Meng, H Sun… - Cancer biology & …, 2015 - Taylor & Francis
Multidrug resistance (MDR) is one of the major obstacles to the efficiency of cancer
chemotherapy, which often results from the overexpression of drug efflux transporters such …

[HTML][HTML] Repurposing tyrosine kinase inhibitors to overcome multidrug resistance in cancer: a focus on transporters and lysosomal sequestration

M Krchniakova, J Skoda, J Neradil, P Chlapek… - International journal of …, 2020 - mdpi.com
Tyrosine kinase inhibitors (TKIs) are being increasingly used to treat various malignancies.
Although they were designed to target aberrant tyrosine kinases, they are also intimately …

Interaction of the efflux transporters ABCB1 and ABCG2 with imatinib, nilotinib, and dasatinib

LN Eadie, TP Hughes, DL White - Clinical Pharmacology & …, 2014 - Wiley Online Library
The efflux transporters adenosine triphosphate (ATP)‐binding cassette (ABC) B1 and
ABCG2 have been demonstrated to interact with the tyrosine kinase inhibitors (TKIs) …

Tyrosine kinase inhibitors as modulators of ATP binding cassette multidrug transporters: substrates, chemosensitizers or inducers of acquired multidrug resistance?

A Brózik, C Hegedüs, Z Erdei, T Hegedűs… - Expert opinion on …, 2011 - Taylor & Francis
Introduction: Anticancer tyrosine kinase inhibitors (TKIs) are small molecule hydrophobic
compounds designed to arrest aberrant signaling pathways in malignant cells. Multidrug …

[HTML][HTML] Therapeutic drug monitoring and individualized medicine of dasatinib: focus on clinical pharmacokinetics and pharmacodynamics

S He, J Bian, Q Shao, Y Zhang, X Hao, X Luo… - Frontiers in …, 2021 - frontiersin.org
Dasatinib is an oral second-generation tyrosine kinase inhibitor known to be used widely in
Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) and Ph+ acute …

[HTML][HTML] Tivantinib, A c-met inhibitor in clinical trials, is susceptible to ABCG2-mediated drug resistance

ZX Wu, Y Yang, QX Teng, JQ Wang, ZN Lei, JQ Wang… - Cancers, 2020 - mdpi.com
Tivantinib, also known as ARQ-197, is a potent non-ATP competitive selective c-Met inhibitor
currently under phase 3 clinical trial evaluation for liver and lung cancers. In this study, we …

The novel BCR-ABL and FLT3 inhibitor ponatinib is a potent inhibitor of the MDR-associated ATP-binding cassette transporter ABCG2

R Sen, K Natarajan, J Bhullar, S Shukla, HB Fang… - Molecular cancer …, 2012 - AACR
Ponatinib is a novel tyrosine kinase inhibitor with potent activity against BCR-ABL with
mutations, including T315I, and also against fms-like tyrosine kinase 3. We tested …

In vitro and in vivo evidence for the importance of breast cancer resistance protein transporters (BCRP/MXR/ABCP/ABCG2)

HEM Schwabedissen, HK Kroemer - Drug Transporters, 2011 - Springer
The breast cancer resistance protein (BCRP/ABCG2) is a member of the G-subfamiliy of the
ATP-binding cassette (ABC)-transporter superfamily. This half-transporter is assumed to …

Dual inhibitors as a new challenge for cancer multidrug resistance treatment

T Stanković, J Dinić, A Podolski-Renić… - Current Medicinal …, 2019 - ingentaconnect.com
Background: Dual-targeting in cancer treatment by a single drug is an unconventional
approach in relation to drug combinations. The rationale for the development of …

[HTML][HTML] Mechanisms of acquired resistance to tyrosine kinase inhibitors

Y Chen, L Fu - Acta Pharmaceutica Sinica B, 2011 - Elsevier
In recent years, structural and functional studies reveal that tyrosine kinases (TKs) act as the
essential components of signal transduction pathways that regulate cancer cell proliferation …