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Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling.
- M. Wittwer, A. Zur, +7 authors K. Giacomini
- Chemistry, Medicine
- Journal of medicinal chemistry
- 22 January 2013
The human multidrug and toxin extrusion (MATE) transporter 1 contributes to the tissue distribution and excretion of many drugs. Inhibition of MATE1 may result in potential drug-drug interactions… Expand
Contribution of the organic anion transporter OAT2 to the renal active tubular secretion of creatinine and mechanism for serum creatinine elevations caused by cobicistat
Many xenobiotics including the pharmacoenhancer cobicistat increase serum creatinine by inhibiting its renal active tubular secretion without affecting the glomerular filtration rate. This study… Expand
Cloning and Expression of a 5‐Hydroxytryptamine7 Receptor Positively Coupled to Adenylyl Cyclase
Abstract: A cDNA clone (designated as GP2‐7) encoding a novel 5‐hydroxytryptamine (5‐HT) receptor was isolated from a guinea pig hippocampal library. The receptor shares amino acid homology within… Expand
Cloning, expression and pharmacology of a truncated splice variant of the human 5‐HT7 receptor (h5‐HT7(b))
1 The rat 5‐hydroxytryptamine (5‐HT)7 receptor displays two splice variations, a long form, and a truncated splice isoform, arising from the introduction of a stop codon near the carboxy‐terminus.… Expand
P2X receptors and their role in female idiopathic detrusor instability.
PURPOSE It is clear from previous studies that adenosine triphosphate is released as a contractile co-transmitter with acetylcholine from parasympathetic nerves supplying the mammalian bladder but… Expand
Molecular cloning, genomic characterization and expression of novel human α1A‐adrenoceptor isoforms
We have isolated and characterized from human prostate novel splice variants of the human α1A‐adrenoceptor, several of which generate truncated products and one isoform, α1A‐4, which has the… Expand
Existence of hepatitis C virus NS5B variants naturally resistant to non-nucleoside, but not to nucleoside, polymerase inhibitors among untreated patients.
- S. Le Pogam, A. Seshaadri, +7 authors I. Nájera
- Biology, Medicine
- The Journal of antimicrobial chemotherapy
- 1 June 2008
OBJECTIVES To characterize the effect of hepatitis C virus (HCV) polymerase intrinsic genetic heterogeneity on the inhibitory activity of nucleoside and non-nucleoside HCV polymerase inhibitors. … Expand
Assessment of the relationship between signal intensities and transcript concentration for Affymetrix GeneChip® arrays
BackgroundAffymetrix microarrays have become increasingly popular in gene-expression studies; however, limitations of the technology have not been well established for commercially available arrays.… Expand
RG7128 alone or in combination with pegylated interferon-α2a and ribavirin prevents hepatitis C virus (HCV) Replication and selection of resistant variants in HCV-infected patients.
- S. Le Pogam, A. Seshaadri, +8 authors I. Nájera
- Biology, Medicine
- The Journal of infectious diseases
- 15 November 2010
INTRODUCTION RG7128 (prodrug of PSI-6130) shows potent antiviral efficacy in patients infected with hepatitis C virus (HCV) genotypes 1, 2, or 3, with mean viral load decreases of 2.7 and 5 log(10)… Expand
Cloning, expression and pharmacology of a truncated splice variant of the human 5-HT7 receptor (h5-HT7b).
1. The rat 5-hydroxytryptamine (5-HT)7 receptor displays two splice variations, a long form, and a truncated splice isoform, arising from the introduction of a stop codon near the carboxy-terminus.… Expand