Search Results - "Sonatore, Lisa M"
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A Peptide-Based Fluorescence Resonance Energy Transfer Assay for Bacillus anthracis Lethal Factor Protease
Published in Proceedings of the National Academy of Sciences - PNAS (14-05-2002)“…A fluorescence resonance energy transfer assay has been developed for monitoring Bacillus anthracis lethal factor (LF) protease activity. A fluorogenic 16-mer…”
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The Catalytic Flexibility of tRNAIle-lysidine Synthetase Can Generate Alternative tRNA Substrates for Isoleucyl-tRNA Synthetase
Published in The Journal of biological chemistry (10-04-2009)“…Bacteria decode the isoleucine codon AUA using a tRNA species that is posttranscriptionally modified at the wobble position of the anticodon with a…”
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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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Accelerating the discovery of DGAT1 inhibitors through the application of parallel medicinal chemistry (PMC)
Published in Bioorganic & medicinal chemistry letters (01-06-2019)“…[Display omitted] The parallel medicinal chemistry (PMC) was effectively applied to accelerate the optimization of diacylglycerol O-acyltransferase I (DGAT-1)…”
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Definitive Metabolite Identification Coupled with Automated Ligand Identification System (ALIS) Technology: A Novel Approach to Uncover Structure–Activity Relationships and Guide Drug Design in a Factor IXa Inhibitor Program
Published in Journal of medicinal chemistry (10-03-2016)“…A potent and selective Factor IXa (FIXa) inhibitor was subjected to a series of liver microsomal incubations, which generated a number of metabolites. Using…”
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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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Benzimidazole-based DGAT1 inhibitors with a [3.1.0] bicyclohexane carboxylic acid moiety
Published in Bioorganic & medicinal chemistry letters (15-05-2019)“…Previously disclosed benzimidazole-based DGAT1 inhibitors containing a cyclohexane carboxylic acid moiety suffer from isomerization at the alpha position of…”
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Development of a novel class of potent and selective FIXa inhibitors
Published in Bioorganic & medicinal chemistry letters (01-11-2015)“…[Display omitted] Using structure based drug design (SBDD), a novel class of potent coagulation Factor IXa (FIXa) inhibitors was designed and synthesized. High…”
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Identification of DGAT2 Inhibitors Using Mass Spectrometry
Published in Journal of biomolecular screening (01-02-2016)“…Mass spectrometry offers significant advantages over other detection technologies in the areas of hit finding, hit validation, and medicinal chemistry compound…”
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Development of a novel tricyclic class of potent and selective FIXa inhibitors
Published in Bioorganic & medicinal chemistry letters (15-11-2015)“…[Display omitted] Using structure based drug design, a novel class of potent coagulation factor IXa (FIXa) inhibitors was designed and synthesized. High…”
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Discovery of a Potent and Selective DGAT1 Inhibitor with a Piperidinyl-oxy-cyclohexanecarboxylic Acid Moiety
Published in ACS medicinal chemistry letters (09-10-2014)“…We report the discovery of a novel series of DGAT1 inhibitors in the benzimidazole class with a piperdinyl-oxy-cyclohexanecarboxylic acid moiety. This novel…”
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Potent DGAT1 Inhibitors in the Benzimidazole Class with a Pyridyl-oxy-cyclohexanecarboxylic Acid Moiety
Published in ACS medicinal chemistry letters (08-08-2013)“…We report the design and synthesis of a series of novel DGAT1 inhibitors in the benzimidazole class with a pyridyl-oxy-cyclohexanecarboxylic acid moiety. In…”
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Disubstituted pyrimidines as Lck inhibitors
Published in Bioorganic & medicinal chemistry letters (15-09-2009)“…Compound 4 was found to be a potent inhibitor of Lck activity (IC 50 = 0.1 nM) and cellular IL2 release (IC 50 = 8 nM). We have developed a family of…”
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The Utility of FK506-Binding Protein as a Fusion Partner in Scintillation Proximity Assays: Application to SH2 Domains
Published in Analytical biochemistry (05-09-1996)“…Methodology has been developed which gives a specific measure of the interaction of an SH2 domain with a phosphopeptide ligand using scintillation proximity…”
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