What does ABCG2 do?
The ABCG2 gene belongs to a group of genes called the ATP-binding cassette family; genes in this family provide instructions for making proteins that transport molecules across cell membranes. In the intestines, the ABCG2 protein helps release (secrete) a substance called urate into the urine.
What is ABCG2 transporter?
ABCG2 is a constitutively expressed ATP-binding cassette (ABC) transporter that protects many tissues against xenobiotic molecules. Its activity affects the pharmacokinetics of commonly used drugs and limits the delivery of therapeutics into tumour cells, thus contributing to multidrug resistance.
Where is ABCG2 found?
GENETICS AND GENE REGULATION The human ABCG2 gene is located on chromosome 4, band 4q21-4q22, and extends over 66 kb containing 16 exons and 15 introns. Exons range in size from 60 to 532 bp, with the translational start site in the second exon, the Walker A site in exon 3 and the ABC signature motif in exon 6 [31].
What does ABCB1 gene do?
ABCB1 is an environment susceptible gene that codes for P-glycoprotein (P-gp). P-gp is responsible for multidrug resistance during chemotherapy of breast cancer. Six different non-synonymous Single Nucleotide Polymorphism (nsSNPs) of human ABCB1 gene were found in COSMIC database.
What are BCRP inhibitors?
BCRP inhibitors include, among others, fumitremorgin C (FTC), the FTC analogue Ko143, the acridone carboxamide derivative GF120918, anti-HIV protease inhibitors nelfinavir and ritonavir, the dietary flavonoids chrysin and biochanin A, the tyrosine kinase inhibitors gefitinib and imatinib [5, 16, 36], and herb extracts …
What are inhibitors of ABCG2 pumps?
As an efflux pump exhibiting a broad substrate specificity localized on cellular plasma membrane, ABCG2 excretes a variety of endogenous and exogenous substrates including chemotherapeutic agents, such as mitoxantrone and several tyrosine kinase inhibitors.
What is BCRP substrate?
ABCG2, more commonly referred to as BCRP (Breast Cancer Resistance Protein), is an efflux transporter that serves two major drug transport functions. Firstly, it restricts the distribution of its substrates into organs such as the brain, testes, placenta, and across the gastrointestinal tract (GIT).
What is Bcrp substrate?