scholarly journals ADMET evaluation in drug discovery. 20. Prediction of breast cancer resistance protein inhibition through machine learning

2020 ◽  
Vol 12 (1) ◽  
Author(s):  
Dejun Jiang ◽  
Tailong Lei ◽  
Zhe Wang ◽  
Chao Shen ◽  
Dongsheng Cao ◽  
...  
2020 ◽  
Vol 21 ◽  
Author(s):  
Sonali Mehendale-Munj

: Breast Cancer Resistance Protein (BCRP) is an efflux transporter responsible for causing multidrug re-sistance(MDR). It is known to expel many potent antineoplastic drugs, owing to its efflux function. Efflux of chemothera-peutics because of BCRP develops resistance to manydrugs, leading to failure in cancer treatment. BCRP plays an important role in physiology by protecting the organism from xenobiotics and other toxins. It is a half-transporter affiliated to theATP-binding cassette (ABC) superfamily of transporters, encoded by the gene ABCG2 and functions in response to adenosine triphosphate (ATP). Regulation of BCRP expression is critically controlled at molecular levels which help in maintaining the balance of xenobiotics and nutrients inside the body. Expression of BCRP can be found in brain, liver, lung cancers and acute myeloid leukemia (AML). Moreover, it is also expressed at high levels in stem cells and many cell lines. This frequent expression of BCRP has an impact on the treatment procedures and if not scrutinized may lead to failure of many cancer therapies.


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