ATP-binding cassette superfamily G member 2 (ABCG2) is a translocation protein encoded by the ABCG2 gene on human Chromosome 4q22.1. Creative Biolabs provides all-sided analysis services about the ABCG2 gene and the protein encoded by it. We also offer a series of customized services for ABCG2 analysis. Our first-class service can provide you with satisfactory advanced analytical services.
Being a member of the superfamily of ATP-binding cassette (ABC) transporters, ABCG2 can actively pump drugs and other compounds to maintain osmotic balance inside and outside the cell by utilizing the binding and hydrolysis of ATP as an energy source. Compared to other transporters,
As Fig.1 shown, ABCG2 is characterized as a half-transporter, hypothetically comprising a transmembrane domain (TMD) with 6 α-helices that spawns the membrane bilayer and a nucleotide-binding domain (NBD) where ATP binds and hydrolyzes. Moreover, the activity of ABCG2 affects the pharmacokinetics of many drugs and limits the delivery of therapeutics into tumor cells, which further contributes to multidrug resistance.
Fig.1 ABCG2 topological membrane configuration.1
As mentioned above, various cytotoxic agents are substrates for ABCG2, and the efflux of those drugs by ABCG2 leads to resistance to these agents. Further in vitro studies have confirmed that the potency of many cancer drugs is inversely correlated with the expression level of ABCG2.
High expression of ABCG2 would result in the intracellular accumulation of these drugs. Hence, much research has focused on inhibiting the activity of ABCG2 to obtain a better tumor treatment effect. More recently, some new poor substrates have also been used for circumventing ABCG2-mediated resistance, and there are already drugs approved by the FDA for the treatment of drug-dependent cancer patients.
Photodynamic therapy (PDT) in cancers refers to targeting tumor tissue through tumor-selective photosensitizers and then generating reactive oxygen species under the irradiation of specific wavelengths of light to kill cancer cells. PDT has been approved for the treatment of certain cancers such as esophageal cancer and non-small cell lung cancer. However, lots of PDT agents are also substrates of ABCG2. High ABCG2 expression will also decrease the intracellular accumulation and in vitro potency of the investigational PDT agents.
The up-regulation of many ABC transporter in drug-resistant cells has been reported during radiation therapy. It was first noticed that efflux pump-mediated regulation of GSH may play a role in radiation resistance in 2007. Since then, more studies have confirmed that ABCG2 is strongly associated with cell resistance during radiotherapy.
Since ABCG2 plays an important role in the intracellular and extracellular transport of biomolecules, Creative Biolabs provides comprehensive ABCG2 expression level detection service, drug pharmacokinetics-related assay, and cell resistance analysis services for global clients. We also provide customized analysis services for ABCG2 to meet your specific needs.
With years of deep cultivation in the biological field, Creative Biolabs is a first-class analysis service provider in the industry. Our rich service experience and first-class biotechnology platforms provide you with a variety of customized services. Creative Biolabs is a great partner for your drug development and academic research. If you are interested in our services, please do not hesitate to contact us for more information.
Reference
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