Identification of functionally variant MDR1 alleles among European Americans and African Americans

RB Kim, BF Leake, EF Choo… - Clinical …, 2001 - Wiley Online Library
MDR1 (P‐glycoprotein) is an important factor in the disposition of many drugs, and the
involved processes often exhibit considerable interindividual variability that may be genetically …

The drug transporter P-glycoprotein limits oral absorption and brain entry of HIV-1 protease inhibitors.

RB Kim, MF Fromm, C Wandel, B Leake… - The Journal of …, 1998 - Am Soc Clin Investig
Currently available HIV-1 protease inhibitors are potent agents in the therapy of HIV-1
infection. However, limited oral absorption and variable tissue distribution, both of which are …

[HTML][HTML] Polymorphisms in OATP-C: identification of multiple allelic variants associated with altered transport activity among European-and African-Americans

RG Tirona, BF Leake, G Merino, RB Kim - Journal of Biological Chemistry, 2001 - ASBMB
The human organic anion transporting polypeptide-C (OATP-C) (gene SLC21A6) is a liver-specific
transporter importantly involved in the hepatocellular uptake of a variety of …

Fruit juices inhibit organic anion transporting polypeptide–mediated drug uptake to decrease the oral availability of fexofenadine

GK Dresser, DG Bailey, BF Leake… - Clinical …, 2002 - Wiley Online Library
Objectives Our objective was to examine the effect of different fruits and their constituents on
P‐glycoprotein and organic anion transporting polypeptide (OATP) activities in vitro and on …

OATP and P-glycoprotein transporters mediate the cellular uptake and excretion of fexofenadine

M Cvetkovic, B Leake, MF Fromm, GR Wilkinson… - Drug metabolism and …, 1999 - ASPET
Fexofenadine, a nonsedating antihistamine, does not undergo significant metabolic
biotransformation. Accordingly, it was hypothesized that uptake and efflux transporters could be …

Drug and bile acid transporters in rosuvastatin hepatic uptake: function, expression, and pharmacogenetics

RH Ho, RG Tirona, BF Leake, H Glaeser, W Lee… - Gastroenterology, 2006 - Elsevier
Background & Aims The 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase
inhibitors, or statins, target liver HMG-CoA and are of proven benefit in the prevention of …

The orphan nuclear receptor HNF4α determines PXR-and CAR-mediated xenobiotic induction of CYP3A4

RG Tirona, W Lee, BF Leake, LB Lan, CB Cline… - Nature medicine, 2003 - nature.com
The drug metabolizing enzyme cytochrome P450 3A4 (CYP3A4) is thought to be involved in
the metabolism of nearly 50% of all the drugs currently prescribed. Alteration in the activity …

Interrelationship between substrates and inhibitors of human CYP3A and P-glycoprotein

RB Kirn, C Wandel, B Leake, M Cvetkovic… - Pharmaceutical …, 1999 - Springer
Purpose. CYP3A and P-gp both function to reduce the intracellular concentration of drug
substrates, one by metabolism and the other by transmembrane efflux. Moreover, it has been …

Pharmacological inhibition of P-glycoprotein transport enhances the distribution of HIV-1 protease inhibitors into brain and testes

EF Choo, B Leake, C Wandel, H Imamura… - Drug Metabolism and …, 2000 - ASPET
HIV protease inhibitors have proven remarkably effective in treating HIV-1 infection. However,
some tissues such as the brain and testes (sanctuary sites) are possibly protected from …

[HTML][HTML] Polymorphisms in human organic anion-transporting polypeptide 1A2 (OATP1A2): implications for altered drug disposition and central nervous system drug …

…, GW Moeckel, G Gervasini, BF Leake… - Journal of Biological …, 2005 - ASBMB
Organic anion-transporting polypeptide 1A2 (OATP1A2) is a drug uptake transporter known
for broad substrate specificity, including many drugs in clinical use. Therefore, genetic …