Residues contributing to drug transport by ABCG2 are localised to multiple drug-binding pockets
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چکیده
منابع مشابه
BINDING OF THE ANTITUMOR DRUG ADRIAMYCIN TO DNA-HISTONE COMPLEXES
Isotherms of the binding of the anthracycIine antibiotic, adriamycin (adriblastin), to DNA histone complexes was studied by means of spectroscopic analysis. The results indicated that: (a) binding of adriamycin to histones reduced the interaction of histones with DNA, (b) binding of the drug to DNA did not change the binding affinity of histone to DNA and, (c) in the explored binding range...
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The inhibition of essential enzymes in microbial pathogens offers a route to treatment of infectious diseases. However, although the biology of the organism dictates a need for a particular enzyme activity, this does not necessarily mean that the enzyme is a good drug target. The chemistry of the active site (size, shape and properties) determines the likelihood of finding a molecule with the r...
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isotherms of the binding of the anthracyciine antibiotic, adriamycin (adriblastin), to dna histone complexes was studied by means of spectroscopic analysis. the results indicated that: (a) binding of adriamycin to histones reduced the interaction of histones with dna, (b) binding of the drug to dna did not change the binding affinity of histone to dna and, (c) in the explored binding range of r
متن کاملIdentification of residues in ABCG2 affecting protein trafficking and drug transport, using co-evolutionary analysis of ABCG sequences
ABCG2 is an ABC (ATP-binding cassette) transporter with a physiological role in urate transport in the kidney and is also implicated in multi-drug efflux from a number of organs in the body. The trafficking of the protein and the mechanism by which it recognizes and transports diverse drugs are important areas of research. In the current study, we have made a series of single amino acid mutatio...
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Resistance to etoposide has been associated with the overexpression of P-glycoprotein and MRP1 in human tumor cells. However, the role of BCRP in resistance to etoposide has not been clearly established, especially the significance of arginine 482 mutations in drug transport (cellular uptake and efflux). Different levels of resistance to etoposide...
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ژورنال
عنوان ژورنال: Biochemical Journal
سال: 2018
ISSN: 0264-6021,1470-8728
DOI: 10.1042/bcj20170923