Accumulation of antiviral nucleotides in renal proximal tubules is controlled by their basolateral uptake via the human renal organic anion transporters type 1 (hOAT1) and 3 (hOAT3) and apical efflux via the multidrug resistance protein 4 (MRP4). GS-9148 is a novel ribose-modified nucleotide human immunodeficiency virus (HIV) reverse transcriptase inhibitor, and its oral prodrug GS-9131 is curr...

GS-9131 is a phosphonoamidate prodrug of the novel ribose-modified phosphonate nucleotide analog GS-9148 that demonstrates potent anti-human immunodeficiency virus type 1 (HIV-1) activity and an excellent resistance profile in vitro. Prodrug moieties were optimized for the efficient delivery of GS-9148 and its active diphosphate (DP) metabolite to lymphoid cells following oral administration. T...

AIMS The aim of the present study was to investigate whether agents which enhance force of contraction via increasing intracellular Na+, i.e. cAMP-independently, remain effective in failing human myocardium. METHODS Cumulative concentration-response curves with (+/-)BDF 9148 (0.01-10 mumol l-1), a Na(+)-channel activator, and ouabain (0.01-0.1 mumol l-1), a Na+/K(+)-ATPase inhibitor, were per...

GS-9148 [(5-(6-amino-purin-9-yl)-4-fluoro-2,5-dihydro-furan-2-yloxymethyl)phosphonic acid] is a novel ribose-modified human immunodeficiency virus type 1 (HIV-1) nucleotide reverse transcriptase (RT) inhibitor (NRTI) selected from a series of nucleoside phosphonate analogs for its favorable in vitro biological properties including (i) a low potential for mitochondrial toxicity, (ii) a minimal c...

GS-9148 is an investigational phosphonate nucleotide analogue inhibitor of reverse transcriptase (RT) (NtRTI) of human immunodeficiency virus type 1 (HIV-1). This compound is an adenosine derivative with a 2',3'-dihydrofuran ring structure that contains a 2'-fluoro group. The resistance profile of GS-9148 is unique in that the inhibitor can select for the very rare Q151L mutation in HIV-1 RT as...

1. BDF 9148 is a newly synthesized congener of DPI 201-106 in which the piperazidinyl moiety has been replaced by an azetidine-3-oxy-moiety. The inotropic effect of both drugs was studied as well as their influence on the action potential, by use of standard microelectrode techniques. 2. BDF 9148 increased the contractile force of guinea-pig atria and papillary muscles. The EC50 was 1.32 X 10(-...

MicroRNA-146a Inhibits Glioma Development by Targeting Notch1 1 2 Running title: miR-146a restricts gliomagenesis 3 4 Jie Mei, Robert Bachoo, and Chun-Li Zhang 5 6 Department of Molecular Biology, Department of Neurology, University of Texas 7 Southwestern Medical Center, Dallas, TX 75390-9148 8 9 10

CONTEXT Adolescent drinking is a major public health concern. The federal government does not restrict alcohol advertising to adolescents, but relies on the alcohol industry for self-regulation. OBJECTIVES To investigate recent alcohol advertising in magazines and to determine whether advertising frequency is associated with adolescent readership. DESIGN, SETTING, AND SUBJECTS All alcohol a...

We isolated a clone containing rat c-jun gene from a rat liver and is highly conserved when compared with that of human cgenomic DNA-X charon 4A library by plaque hybridization with jun gene (4). Nucleotide numbers are given with the initiation P-labeled human c-jun cDNA (1) and determined the site of transcription as +1 . nucleotide sequence. The rat gene encodes a protein whose deduced amino ...

Exact relations between Tk , the kth temporal moments of the nucleation flux, and the derivative of its Laplace transform ~LT! are established and applied to available asymptotic expressions for the LT, generalizing earlier results by Shneidman and Weinberg @J. Chem. Phys. 95, 9148 ~1991!; 97, 3629 ~1992!# on the time-lag T0 . For any k>2 the moments Tk are expressed through simple algebraic co...