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The Effect Of Oatp2b1-Mediated Statin Transport On Beta Cell Dysfunction, Jihoon Kwon
The Effect Of Oatp2b1-Mediated Statin Transport On Beta Cell Dysfunction, Jihoon Kwon
Electronic Thesis and Dissertation Repository
Statins are a class of cholesterol-lowering drugs which work by inhibiting the mevalonate pathway. Statin treatment has been linked to an increase in the risk of new-onset diabetes mellitus, and previous studies have suggested impairment in insulin secretion following statin treatment. Recent work from our laboratory confirmed the expression of organic anion transporting polypeptide 2B1 (OATP2B1), an important statin uptake transporter, in human pancreatic beta cells. Our study examined the role of OATP2B1 in statin-associated beta cell toxicity using INS-1 cells as a beta cell model. We showed that OATP2B1 augments cellular accumulation of rosuvastatin and atorvastatin, but not pravastatin. …
Quantitative Estimation Of P-Glycorptein-Mediated Drug Transport By Mechanistically Modeled Intrinsic Clearance, Alex D. Morgan
Quantitative Estimation Of P-Glycorptein-Mediated Drug Transport By Mechanistically Modeled Intrinsic Clearance, Alex D. Morgan
Electronic Thesis and Dissertation Repository
P-glycoprotein (P-gp/ABCB1) is an important efflux drug transporter affecting the disposition of 50% of marketed drugs. Cell monolayer permeability assays are the gold standard for assessing P-gp-drug interactions in vitro, but inter-laboratory assay differences produce heterogeneous results. We compared the validity and sensitivity of traditional assay metrics of efflux transport (unidirectional apparent permeability and efflux ratio) with a modeled clearance metric, CLP-gp and hypothesized that CLP-gp would be superior. Cell monolayers heterologously transfected with ABCB1, and 1,25(OH)2D3-modulated ABCB1 in cells served as experimental models. P-gp expression was quantified by western …