Search Results - "Harrity, Thomas W."
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11β-hydroxysteroid dehydrogenase type 1 gene knockout attenuates atherosclerosis and in vivo foam cell formation in hyperlipidemic apoE⁻/⁻ mice
Published in PloS one (01-02-2013)“…Chronic glucocorticoid excess has been linked to increased atherosclerosis and general cardiovascular risk in humans. The enzyme 11β-hydroxysteroid…”
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PK/PD Disconnect Observed with a Reversible Endothelial Lipase Inhibitor
Published in ACS medicinal chemistry letters (12-07-2018)“…Screening of a small set of nonselective lipase inhibitors against endothelial lipase (EL) identified a potent and reversible inhibitor,…”
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The Ability of Statins to Inhibit Bone Resorption Is Directly Related to Their Inhibitory Effect on HMG‐CoA Reductase Activity
Published in Journal of bone and mineral research (01-01-2003)“…Statins, which are inhibitors of 3‐hydroxy‐3‐glutaryl‐coenzyme A (HMG‐CoA) reductase, decrease the hepatic biosynthesis of cholesterol by blocking the…”
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5-Carboxamido-1,3,2-dioxaphosphorinanes, potent inhibitors of MTP
Published in Bioorganic & medicinal chemistry letters (18-10-2004)“…[Display omitted] 5-Carboxamido-1,3,2-dioxaphosphorinanes have been identified as potent inhibitors of microsomal triglyceride-transfer protein. The…”
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A Novel Series of Highly Potent Benzimidazole-Based Microsomal Triglyceride Transfer Protein Inhibitors
Published in Journal of medicinal chemistry (15-03-2001)“…A series of benzimidazole-based analogues of the potent MTP inhibitor BMS-201038 were discovered. Incorporation of an unsubstituted benzimidazole moiety in…”
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Microsomal triglyceride transfer protein inhibitors: discovery and synthesis of alkyl phosphonates as potent MTP inhibitors and cholesterol lowering agents
Published in Bioorganic & medicinal chemistry letters (07-04-2003)“…A series of newly synthesized phosphonate esters were evaluated for their effects on microsomal triglyceride transfer protein activity (MTP). The most potent…”
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Orally Active Squalene Synthase Inhibitors: Bis((acyloxy)alkyl) Prodrugs of the α-Phosphonosulfonic Acid Moiety
Published in Journal of medicinal chemistry (02-02-1996)Get full text
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1,1-Bisphosphonate Squalene Synthase Inhibitors: Interplay Between the Isoprenoid Subunit and the Diphosphate Surrogate
Published in Journal of medicinal chemistry (01-07-1995)“…Inhibitors of squalene synthase have the potential to be superior cholesterol-lowering agents. We previously disclosed that lipophilic 1,1-bisphosphonates I…”
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11[beta]-Hydroxysteroid Dehydrogenase Type 1 Gene Knockout Attenuates Atherosclerosis and In Vivo Foam Cell Formation in Hyperlipidemic apoE.sup.-/- Mice
Published in PloS one (01-02-2013)“…Background Chronic glucocorticoid excess has been linked to increased atherosclerosis and general cardiovascular risk in humans. The enzyme…”
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An MTP Inhibitor that Normalizes Atherogenic Lipoprotein Levels in WHHL Rabbits
Published in Science (American Association for the Advancement of Science) (23-10-1998)“…Patients with abetalipoproteinemia, a disease caused by defects in the microsomal triglyceride transfer protein (MTP), do not produce apolipoprotein…”
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An Inhibitor of the Microsomal Triglyceride Transfer Protein Inhibits apoB Secretion from HepG2 Cells
Published in Proceedings of the National Academy of Sciences - PNAS (15-10-1996)“…The microsomal triglyceride (TG) transfer protein is a heterodimeric lipid transfer protein that catalyzes the transport of triglyceride, cholesteryl ester,…”
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Anti-C Effects of Two Anti-Inflammatory (AI) Agents, Niflumic and Flufenamic Acids
Published in The Journal of immunology (1950) (01-07-1973)“…Abstract Two anthranilic acid type AI agents, niflumic acid (Nif) and its benzene analog, flufenamic acid (Flu), were examined for anti-C activity in vitro…”
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Lipophilic 1,1-bisphosphonates are potent squalene synthase inhibitors and orally active cholesterol lowering agents in vivo
Published in The Journal of biological chemistry (25-11-1993)“…Squalene synthase catalyzes the reductive dimerization of two molecules of farnesyl diphosphate to form squalene at the final branchpoint of the cholesterol…”
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α-Phosphonosulfonic Acids: Potent and Selective Inhibitors of Squalene Synthase
Published in Journal of medicinal chemistry (02-02-1996)Get full text
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Selective inhibition of urokinase by substituted phenylguanidines: quantitative structure-activity relationship analyses
Published in Journal of medicinal chemistry (01-11-1990)Get full text
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Phosphorus-containing inhibitors of HMG-CoA reductase. 2. Synthesis and biological activities of a series of substituted pyridines containing a hydroxyphosphinyl moiety
Published in Journal of medicinal chemistry (01-09-1991)“…A series of 2,3,4,(5),6-substituted pyridines containing a hydroxyphosphinyl functionally have been prepared and were evaluated for their ability to inhibit…”
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Anti-complement effects of two anti-inflammatory agents. Niflumic and flufenamic acids
Published in Biochemical pharmacology (15-11-1974)Get more information
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