Differential Effects of the Oncogenic BRAF Inhibitor PLX4032 (Vemurafenib) and its Progenitor PLX4720 on ABCB1 Function [PDF]
PURPOSE: The clinically approved oncogenic BRAF inhibitor PLX4032 (vemurafenib) was shown to be a substrate of the ATP-binding cassette (ABC) transporter ABCB1. Here, we compared PLX4032 and its structurally closely related precursor compound PLX4720 for
Martin Michaelis +7 more
doaj +2 more sources
Multidrug resistance (MDR) mediated by ATP binding cassette subfamily B member 1 (ABCB1) is significantly hindering effective cancer chemotherapy. However, currently, no ABCB1-inhibitory drugs have been approved to treat MDR cancer clinically, mainly due
Xu Wu, Stella, Chunyuan Zhang
exaly +3 more sources
Erdafitinib Antagonizes ABCB1-Mediated Multidrug Resistance in Cancer Cells
ABCB1 overexpression is known to contribute to multidrug resistance (MDR) in cancers. Therefore, it is critical to find effective drugs to target ABCB1 and overcome MDR.
Weiguo Feng, Zhuo-Xun Wu, Jing-Quan Wang
exaly +3 more sources
Multidrug resistance (MDR) has been extensively reported in colorectal cancer patients, which remains a major cause of chemotherapy failure. One of the critical mechanisms of MDR in colorectal cancer is the reduced intracellular drug level led by the ...
Zi-Ning Lei, Zhuo-Xun Wu, Zhe-Sheng Chen
exaly +2 more sources
H89 Reverses Multidrug Resistance in Colorectal Cancer by Inhibiting the ATPase Activity of ABCB1 [PDF]
Background: Multidrug resistance (MDR) remains a major obstacle in cancer chemotherapy, and overexpression of ABCB1 plays a critical role in the pathogenesis of MDR.
Wei-Jing Liu +9 more
doaj +2 more sources
Importance of Ethnicity, CYP2B6 and ABCB1 Genotype for Efavirenz Pharmacokinetics and Treatment Outcomes: A Parallel-group Prospective Cohort Study in two sub-Saharan Africa Populations. [PDF]
We evaluated the importance of ethnicity and pharmacogenetic variations in determining efavirenz pharmacokinetics, auto-induction and immunological outcomes in two African populations. ART naïve HIV patients from Ethiopia (n = 285) and Tanzania (n = 209)
A Habtewold +48 more
core +22 more sources
Lack of Association between C1236T, G2677T/A and C3435T Variants of the ABCB1 Gene and Imatinib Response in Iranian Chronic Myeloid Leukemia Patients [PDF]
Imatinib introduction caused to improve the clinical outcomes of chronic myeloid leukemia (CML) patients. Despite the significant effects of Imatinib, pharmacogenetic variables induced treatment resistant is also observed.
Maedeh Khosravi +7 more
doaj +1 more source
Minimally invasive differential diagnosis of melanocytic intraocular neoplasms
Purpose: to analyze the mutation frequency of the GNAQ/GNA11 gene in circulating tumor DNA and genotypes of the polymorphic marker C3435T of the ABCB1 gene in a large sample of patients with intraocular melanocytic neoplasms (IMN).Material and methods ...
A. Yu. Tsygankov +4 more
doaj +1 more source
Deregulation of the apoptotic process underlies the pathogenesis of many cancers, including leukemia, but is also very important for the success of chemotherapy treatment.
Pravdic Zlatko +6 more
doaj +1 more source
ABCB1 polymorphism in clopidogrel-treated Montenegrin patients
Clopidogrel is an antiplatelet drug that displays significant interindividual variability in treatment response. Its bioavailability depends on the function of P-glycoprotein (P-gp), which is coded by a highly polymorphic ABCB1 gene.
Mugosa Snezana +4 more
doaj +1 more source

