Search Results - "Carlson, Timothy J"
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Discovery and molecular basis of potent noncovalent inhibitors of fatty acid amide hydrolase (FAAH)
Published in Proceedings of the National Academy of Sciences - PNAS (03-05-2011)“…Fatty acid amide hydrolase (FAAH), an amidase-signature family member, is an integral membrane enzyme that degrades lipid amides including the endogenous…”
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In vitro and in vivo pharmacokinetic characterization of mavacamten, a first-in-class small molecule allosteric modulator of beta cardiac myosin
Published in Xenobiotica (03-06-2019)“…Mavacamten is a small molecule modulator of cardiac myosin designed as an orally administered drug for the treatment of patients with hypertrophic…”
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Activation of cytochrome P450 2C9-mediated metabolism: mechanistic evidence in support of kinetic observations
Published in Archives of biochemistry and biophysics (01-02-2003)“…Studies were designed to investigate the possible mechanisms associated with the kinetic observation of CYP2C9 activation by dapsone and its phase I…”
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Metabolite Profiling and Reaction Phenotyping for the in Vitro Assessment of the Bioactivation of Bromfenac
Published in Chemical research in toxicology (21-01-2020)“…Bromfenac is a nonsteroidal anti-inflammatory drug that was approved and subsequently withdrawn from the market because of reported cases of acute…”
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A three-year clinical evaluation of two dentin bonding agents
Published in The Journal of the American Dental Association (1939) (01-04-2004)“…A new restorative called a "giomer composite" has been introduced. The authors conducted a study to determine retention, anatomical form, caries, staining,…”
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Structure guided design of a series of sphingosine kinase (SphK) inhibitors
Published in Bioorganic & medicinal chemistry letters (15-08-2013)“…Sphingosine-1-phosphate (S1P) signaling plays a vital role in mitogenesis, cell migration and angiogenesis. Sphingosine kinases (SphKs) catalyze a key step in…”
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Discovery of AMG 925, a FLT3 and CDK4 Dual Kinase Inhibitor with Preferential Affinity for the Activated State of FLT3
Published in Journal of medicinal chemistry (24-04-2014)“…We describe the structural optimization of a lead compound 1 that exhibits dual inhibitory activities against FLT3 and CDK4. A series of…”
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An infinitary extension of the Graham--Rothschild Parameter Sets Theorem
Published in Transactions of the American Mathematical Society (01-07-2006)“…The {\it Graham-Rothschild Parameter Sets Theorem} is one of the most powerful results of Ramsey Theory. (The Hales-Jewett Theorem is its most trivial…”
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MS(M), an efficient workflow for metabolite identification using hybrid linear ion trap Orbitrap mass spectrometer
Published in Journal of the American Society for Mass Spectrometry (01-05-2012)“…Identification of drug metabolites can often yield important information regarding clearance mechanism, pharmacologic activity, or toxicity for drug candidate…”
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Identification of potent, noncovalent fatty acid amide hydrolase (FAAH) inhibitors
Published in Bioorganic & medicinal chemistry letters (15-04-2011)“…Starting from a series of ureas that were determined to be mechanism-based inhibitors of FAAH, several spirocyclic ureas and lactams were designed and…”
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Reagent-free LC-MS/MS-based pharmacokinetic quantification of polyhistidine-tagged therapeutic proteins
Published in Bioanalysis (01-02-2017)“…Immobilized metal ion affinity chromatography is widely employed for purifying polyhistidine-tagged recombinant proteins from cell lysates. The technique can…”
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MSM, an Efficient Workflow for Metabolite Identification Using Hybrid Linear Ion Trap Orbitrap Mass Spectrometer
Published in Journal of the American Society for Mass Spectrometry (01-05-2012)“…Identification of drug metabolites can often yield important information regarding clearance mechanism, pharmacologic activity, or toxicity for drug candidate…”
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13
On the conservativity of the axiom of choice over set theory
Published in Archive for mathematical logic (01-11-2011)“…We show that for various set theories T including ZF, T + AC is conservative over T for sentences of the form A(x, y) where A(x, y) is a Δ 0 formula…”
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Normal forms for elementary patterns
Published in The Journal of symbolic logic (01-03-2012)“…A notation for an ordinal using patterns of resemblance is based on choosing an isominimal set of ordinals containing the given ordinal. There are many choices…”
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Development of a robust and sensitive LC–MS/MS method for the determination of adenine in plasma of different species and its application to in vivo studies
Published in Journal of pharmaceutical and biomedical analysis (05-12-2011)“…A simple, robust, and sensitive liquid chromatography–tandem mass spectrometric (LC–MS/MS) method was developed for the measurement of endogenous adenine in…”
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Recent advances in high throughput screening for ADME properties
Published in Combinatorial chemistry & high throughput screening (01-03-2008)“…With the increase in the numbers of molecules synthesized in a typical drug discovery program, as well as the large amount of information utilized in the…”
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Metabolism-guided discovery of a potent and orally bioavailable urea-based calcimimetic for the treatment of secondary hyperparathyroidism
Published in Bioorganic & medicinal chemistry letters (15-12-2013)“…A series of urea based calcimimetics was optimized for potency and oral bioavailability. Crucial to this process was overcoming the poor pharmacokinetic…”
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High Confidence Predictions of Drug−Drug Interactions: Predicting Affinities for Cytochrome P450 2C9 with Multiple Computational Methods
Published in Journal of medicinal chemistry (14-02-2008)“…Four different models are used to predict whether a compound will bind to 2C9 with a Ki value of less than 10 µM. A training set of 276 compounds and a diverse…”
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Clinical evaluation of in-office and at-home bleaching treatments
Published in Operative dentistry (01-03-2003)“…This three-month, single-blind clinical study compared two whitening treatments, at-home with 10% carbamide peroxide and in-office with 35% hydrogen peroxide,…”
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Application of DBS sampling in combination with LC-MS/MS for pharmacokinetic evaluation of a compound with species-specific blood-to-plasma partitioning
Published in Bioanalysis (01-08-2012)“…Dried blood spot (DBS) sampling in combination with LC-MS/MS has been used increasingly in drug discovery for quantitative analysis to support pharmacokinetic…”
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