Ivermectin Interacts With Human ABCG2 [PDF]
Journal 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
core +6 more sources
Functional relevance of the multi-drug transporter abcg2 on teriflunomide therapy in an animal model of multiple sclerosis [PDF]
Journal of Neuroinflammation, 2020 Background The multi-drug resistance transporter ABCG2, a member of the ATP-binding cassette (ABC) transporter family, mediates the efflux of different immunotherapeutics used in multiple sclerosis (MS), e.g., teriflunomide (teri), cladribine, and ...
Lisa Thiele née Schrewe +14 more
doaj +3 more sources
Investigating the Effect of Lapatinib on the Performance of Sonodynamic Therapy Against Prostate Cancer via Inhibition of the ABCG2 Efflux System [PDF]
Pharmacol Res PerspectABSTRACT Sonodynamic therapy (SDT) is an emerging site specific and minimally‐invasive modality for cancer treatment. Its efficacy heavily relies on the accumulation and retention of systemically‐administered sensitizing agents within tumor cells.
Wang Y, Masood H, Nomikou N.
europepmc +2 more sources
Design of Inhibitors of BCRP/ABCG2
Future Medicinal Chemistry, 2015 BCRP/ABCG2, a second member of ABC transporter subclass G, has been shown to be overexpressed in several solid tumors, acute myelogenous leukemia and chronic myeloid leukemia. A variety of chemically unrelated anticancer drugs have been found to be transported by ABCG2 leading to their lower intracellular accumulation and hence causing chemoresistance.
Kapil, Juvale, Michael, Wiese
openaire +3 more sources
A Human ABCG2 SNP Variant, P269S (rs34678167, c.805C>T), Increases Cellular Resistance to Mitoxantrone and SN-38 Without Detectable Differences in ABCG2 Abundance in Total and Biotinylated Protein Fractions [PDF]
BiomoleculesABCG2 (BCRP/MXR) is an ATP-binding cassette transporter that plays a role in cellular resistance to various anticancer agents. While several non-synonymous single-nucleotide polymorphisms (SNPs) in the ABCG2 gene have been functionally characterized, the
Shiori Sato +4 more
doaj +2 more sources
Pharmacogenomics of dolutegravir: A scoping review of evidence, gaps and clinical implications. [PDF]
Br J Clin PharmacolDolutegravir underpins modern first‐ and second‐line HIV treatment regimens; however, interindividual variability in its disposition and tolerability presents challenges for optimal use. This scoping review mapped current evidence on the pharmacogenomics of dolutegravir, focusing on pharmacokinetics and pharmacodynamics, and methodological limitations ...
Kiguba R, Ssesanga M, Pirmohamed M.
europepmc +2 more sources
Dorsomorphin attenuates ABCG2-mediated multidrug resistance in colorectal cancer [PDF]
Frontiers in PharmacologyColorectal cancer is a common malignant tumor with high mortality, for which chemotherapy resistance is one of the main reasons. The high expression of ABCG2 in the cancer cells and expulsion of anticancer drugs directly cause multidrug resistance (MDR).
Xiao-Peng Li +12 more
doaj +2 more sources
ABCG2 is a potential prognostic marker of overall survival in patients with clear cell renal cell carcinoma [PDF]
BMC Cancer, 2017 Background ATP-binding cassette sub-family G member 2 (ABCG2) is a semi-transport protein that plays a major role in multidrug resistance. We aimed to evaluate the prognostic significance of ABCG2 expression in patients with clear cell renal cell ...
Haofei Wang +9 more
doaj +2 more sources
Reversal of ABCG2-mediated drug resistance by tinodasertib (ETC-206) [PDF]
Frontiers in PharmacologyIntroductionMultidrug resistance (MDR) in cancer therapy, frequently driven by overexpression of ATP-binding cassette (ABC) transporters—particularly ABCG2—continues to undermine the efficacy of chemotherapeutic regimens.
Haigan Yang +10 more
doaj +2 more sources
Reversal of ABCG2-mediated MDR by VEGFR3 inhibitor (S)-SAR131675 [PDF]
Frontiers in PharmacologyMultidrug resistance (MDR) remains a major challenge in cancer treatment, as it is a significant factor contributing to chemotherapy failure and cancer recurrence.
Xiang Chen +9 more
doaj +2 more sources