Results 11 to 20 of about 19,287 (163)

OTS964, a TOPK Inhibitor, Is Susceptible to ABCG2-Mediated Drug Resistance

open access: yesFrontiers in Pharmacology, 2021
OTS964 is a potent T-LAK cell-originated protein kinase (TOPK) inhibitor. Herein, we investigated the interaction of OTS964 and multidrug resistance (MDR)-associated ATP-binding cassette sub-family G member 2 (ABCG2).
Yuqi Yang   +8 more
doaj   +1 more source

Ivermectin Interacts With Human ABCG2 [PDF]

open access: yesJournal of Pharmaceutical Sciences, 2011
Ivermectin is an antiparasitic drug frequently administered to humans. It has a limited brain exposure that is attributed to the efflux activity of ABCB1/Abcb1. ABCG2/Abcg2 is also a major transporter present in most pharmacologically important barriers.
Jani, Marton   +6 more
openaire   +4 more sources

The Challenge of Exploiting ABCG2 in the Clinic [PDF]

open access: yesCurrent Pharmaceutical Biotechnology, 2011
ABCG2, or breast cancer resistance protein (BCRP), is an ATP-binding cassette half transporter that has been shown to transport a wide range of substrates including chemotherapeutics, antivirals, antibiotics and flavonoids. Given its wide range of substrates, much work has been dedicated to developing ABCG2 as a clinical target.
Robert W, Robey   +3 more
openaire   +2 more sources

ABCG2 Gene and ABCG2 Protein Expression in Colorectal Cancer—In Silico and Wet Analysis

open access: yesInternational Journal of Molecular Sciences, 2023
ABCG2 (ATP-binding cassette superfamily G member 2) is a cell membrane pump encoded by the ABCG2 gene. ABCG2 can protect cells against compounds initiating and/or intensifying neoplasia and is considered a marker of stem cells responsible for cancer growth, drug resistance and recurrence. Expression of the ABCG2 gene or its protein has been shown to be
Aleksandra Sałagacka-Kubiak   +5 more
openaire   +2 more sources

Dynamic vs static ABCG2 inhibitors to sensitize drug resistant cancer cells. [PDF]

open access: yesPLoS ONE, 2010
Human ABCG2, a member of the ATP-binding cassette transporter superfamily, plays a key role in multidrug resistance and protecting cancer stem cells. ABCG2-knockout had no apparent adverse effect on the development, biochemistry, and life of mice.
Hui Peng   +3 more
doaj   +1 more source

The Inhibitor Ko143 Is Not Specific for ABCG2 [PDF]

open access: yesThe Journal of Pharmacology and Experimental Therapeutics, 2015
Imaging ATP-binding cassette (ABC) transporter activity in vivo with positron emission tomography requires both a substrate and a transporter inhibitor. However, for ABCG2, there is no inhibitor proven to be specific to that transporter alone at the blood-brain barrier.
Lora D, Weidner   +9 more
openaire   +2 more sources

Pharmacokinetics and Pharmacogenetics of Apixaban

open access: yesРациональная фармакотерапия в кардиологии, 2020
Apixaban is oral anticoagulant, it is widely used in prevention of stroke in non-valvular atrial fibrillation and treatment of deep vein thrombosis and pulmonary embolism. Its main mechanism of action is through reversible inhibition of factor Xa.
A. V. Savinova   +4 more
doaj   +1 more source

Molecular evolution of the ATP-binding cassette subfamily G member 2 gene subfamily and its paralogs in birds

open access: yesBMC Evolutionary Biology, 2020
Background ATP-binding cassette (ABC) transporters are involved in the active transportation of various endogenous or exogenous substances. Two ABCG2 gene subfamily members have been identified in birds.
Shengchao Ma   +9 more
doaj   +1 more source

ABCG2 – a transporter for all seasons [PDF]

open access: yesFEBS Letters, 2004
The human ABCG2 (ABCP/MXR/BCRP) protein is a recently recognized ABC half‐transporter, which forms homodimers in the plasma membrane and actively extrudes a wide variety of chemically unrelated compounds from the cells. This protein protects our cells and tissues against various xenobiotics, with a crucial role in the intestine, liver, placenta, and ...
Sarkadi, Balázs   +3 more
openaire   +2 more sources

Transporter-centric view of urate metabolism: From genome-wide association study to pathophysiology

open access: yesJournal of Physical Fitness and Sports Medicine, 2012
While urate is an important anti-oxidant molecule in the body, high plasma levels of urate cause morbidity including urate crystal deposition in joints (gout) and stone formation in the urinary tract. Because urate is an end product of purine metabolism,
Hiroyuki Sakurai
doaj   +1 more source

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