Search Results - "TIPPIN, T. K"
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Synthetic LXR Ligand Inhibits the Development of Atherosclerosis in Mice
Published in Proceedings of the National Academy of Sciences - PNAS (28-05-2002)“…The nuclear receptors LXRα and LXRβ have been implicated in the control of cholesterol and fatty acid metabolism in multiple cell types. Activation of these…”
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Orally active nonpeptide CCK-A agonists
Published in Pharmaceutical biotechnology (1998)Get more information
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6-Azasteroids : potent dual inhibitors of human type 1 and 2 steroid 5α-reductase
Published in Journal of medicinal chemistry (24-12-1993)Get full text
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Identification of a Nonsteroidal Liver X Receptor Agonist through Parallel Array Synthesis of Tertiary Amines
Published in Journal of medicinal chemistry (09-05-2002)“…A potent, selective, orally active LXR agonist was identified from focused libraries of tertiary amines. GW3965 (12) recruits the steroid receptor coactivator…”
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Enhancing paracellular permeability by modulating epithelial tight junctions
Published in Pharmaceutical Science & Technology Today (01-10-2000)“…The intestinal epithelium is a major barrier to the absorption of hydrophilic drugs. The presence of intercellular junctional complexes, particularly the tight…”
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Book Review Journal Article -
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Regulation of cholesterol homeostasis by the liver X receptors in the central nervous system
Published in Molecular endocrinology (Baltimore, Md.) (01-06-2002)“…The nuclear oxysterol receptors liver X receptor-alpha [LXRalpha (NR1H3)] and LXRbeta (NR1H2) coordinately regulate genes involved in cholesterol homeostasis…”
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P-glycoprotein influences the brain concentrations of cetirizine (Zyrtec), a second-generation non-sedating antihistamine
Published in Journal of pharmaceutical sciences (01-10-2003)“…Recent in vitro studies have suggested that P-glycoprotein (Pgp) and passive membrane permeability may influence the brain concentrations of non-sedating…”
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Pharmacokinetic parameters and mechanisms of inhibition of rat type 1 and 2 steroid 5alpha-reductases: determinants for different in vivo activities of GI198745 and finasteride in the rat
Published in Biochemical pharmacology (01-10-2001)“…The interaction of baculovirus expressed rat steroid 5alpha-reductase types 1 and 2 (r5AR1 and r5AR2) with…”
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In vitro absorption and secretory quotients: practical criteria derived from a study of 331 compounds to assess for the impact of P-glycoprotein-mediated efflux on drug candidates
Published in Journal of pharmaceutical sciences (01-10-2004)“…The absorptive (AQ) and secretory (SQ) quotients have been proposed as a novel experimental approach to quantify the modulation of intestinal absorption and…”
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CYP3A induction by n-hydroxyformamide tumor necrosis factor-α converting enzyme/matrix metalloproteinase inhibitors: Use of a pregnane X receptor activation assay and primary hepatocyte culture for assessing induction potential in humans
Published in Drug metabolism and disposition (01-07-2003)Get full text
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Structure-activity relationships for inhibition of type 1 and 2 human 5α-reductase and human adrenal 3β-hydroxy-Δ5-steroid dehydrogenase/3-keto-Δ5-steroid isomerase by 6-azaandrost-4-en-3-ones : optimization of the C17 substituent
Published in Journal of medicinal chemistry (1995)Get full text
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N-Hydroxyformamide peptidomimetics as TACE/Matrix metalloprotease inhibitors: oral activity via P1′ isobutyl substitution
Published in Bioorganic & medicinal chemistry letters (20-08-2001)“…N-Hydroxyformamide-class metalloprotease inhibitors were designed and synthesized, which have potent broad-spectrum activity versus matrix metalloproteases and…”
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