Search Results - "Milligan, James A"
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Systemic pan-AMPK activator MK-8722 improves glucose homeostasis but induces cardiac hypertrophy
Published in Science (American Association for the Advancement of Science) (04-08-2017)“…5′-Adenosine monophosphate–activated protein kinase (AMPK) is a master regulator of energy homeostasis in eukaryotes. Despite three decades of investigation,…”
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Highly selective and potent agonists of sphingosine-1-phosphate 1 (S1P 1) receptor
Published in Bioorganic & medicinal chemistry letters (15-07-2006)“…Novel series of sphingosine-1-phosphate (S1P) receptor agonists were developed through a systematic SAR aimed to achieve high selectivity for a single member…”
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Synthesis, stereochemical determination and biochemical characterization of the enantiomeric phosphate esters of the novel immunosuppressive agent FTY720
Published in Bioorganic & medicinal chemistry (15-09-2004)“…[Display omitted] The novel immunosuppressive agent FTY720 (1) is phosphorylated in vivo in a variety of species yielding an active metabolite that is an…”
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Discovery of N‑[Bis(4-methoxyphenyl)methyl]-4-hydroxy-2-(pyridazin-3-yl)pyrimidine-5-carboxamide (MK-8617), an Orally Active Pan-Inhibitor of Hypoxia-Inducible Factor Prolyl Hydroxylase 1–3 (HIF PHD1–3) for the Treatment of Anemia
Published in Journal of medicinal chemistry (22-12-2016)“…The discovery of novel 4-hydroxy-2-(heterocyclic)pyrimidine-5-carboxamide inhibitors of hypoxia-inducible factor (HIF) prolyl hydroxylases (PHD) is described…”
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1,3,8-Triazaspiro[4.5]decane-2,4-diones as Efficacious Pan-Inhibitors of Hypoxia-Inducible Factor Prolyl Hydroxylase 1–3 (HIF PHD1–3) for the Treatment of Anemia
Published in Journal of medicinal chemistry (12-04-2012)“…The discovery of 1,3,8-triazaspiro[4.5]decane-2,4-diones (spirohydantoins) as a structural class of pan-inhibitors of the prolyl hydroxylase (PHD) family of…”
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Utilizing Low-Volume Aqueous Acoustic Transfer with the Echo 525 to Enable Miniaturization of qRT-PCR Assay
Published in Journal of Laboratory Automation (01-02-2016)“…Quantitative reverse transcription PCR (qRT-PCR) is a valuable tool for characterizing the effects of inhibitors on viral replication. The amplification of…”
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Discovery of Potent 3,5-Diphenyl-1,2,4-oxadiazole Sphingosine-1-phosphate-1 (S1P1) Receptor Agonists with Exceptional Selectivity against S1P2 and S1P3
Published in Journal of medicinal chemistry (06-10-2005)“…A class of 3,5-diphenyl-1,2,4-oxadiazole based compounds have been identified as potent sphingosine-1-phosphate-1 (S1P1) receptor agonists with minimal…”
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A Rational Utilization of High-Throughput Screening Affords Selective, Orally Bioavailable 1-Benzyl-3-carboxyazetidine Sphingosine-1-phosphate-1 Receptor Agonists
Published in Journal of medicinal chemistry (30-12-2004)“…Moderately potent, selective S1P1 receptor agonists identified from high-throughput screening have been adapted into lipophilic tails for a class of orally…”
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SAR studies of 3-arylpropionic acids as potent and selective agonists of sphingosine-1-phosphate receptor-1 (S1P 1) with enhanced pharmacokinetic properties
Published in Bioorganic & medicinal chemistry letters (01-02-2007)“…Structure–activity relationship (SAR) studies of 3-arylpropionic acids—a class of novel S1P 1 selective agonists—by introducing substitution to the propionic…”
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Discovery of 3-arylpropionic acids as potent agonists of sphingosine-1-phosphate receptor-1 (S1P 1) with high selectivity against all other known S1P receptor subtypes
Published in Bioorganic & medicinal chemistry letters (15-07-2006)“…A series of 3-arylpropionic acids were synthesized as potent and orally bioavailable S1P 1 receptor agonists that were highly selective against other S1P…”
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2-Aryl(pyrrolidin-4-yl)acetic acids are potent agonists of sphingosine-1-phosphate (S1P) receptors
Published in Bioorganic & medicinal chemistry letters (01-07-2006)“…A series of 2-aryl(pyrrolidine-4-yl)acetic acids (e.g., 22g) were synthesized and evaluated as S1P receptor agonists and were found to lower peripheral…”
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2,5-Disubstituted pyrrolidine carboxylates as potent, orally active sphingosine-1-phosphate (S1P) receptor agonists
Published in Bioorganic & medicinal chemistry letters (01-06-2006)“…A series of 2-aryl(pyrrolidine-5-yl)acetic acids (e.g., 21) were synthesized and evaluated as S1P receptor agonists. Compounds 15– 21 were identified with good…”
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Design and synthesis of conformationally constrained 3-( N-alkylamino)propylphosphonic acids as potent agonists of sphingosine-1-phosphate (S1P) receptors
Published in Bioorganic & medicinal chemistry letters (04-10-2004)“…A series of conformationally constrained analogs of 3 were synthesized and evaluated as S1P receptor agonists. Several novel scaffolds were identified as…”
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Assessment of blood pressure in cats presented with urethral obstruction
Published in Journal of veterinary emergency and critical care (San Antonio, Tex. : 2000) (01-03-2007)“…Objective: To determine the arterial blood pressure at presentation in male cats with acute urethral obstruction, and to determine whether there was any…”
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