Search Results - "Rago, Brian"
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Development of a high-throughput ultra performance liquid chromatography–mass spectrometry assay to profile 18 eicosanoids as exploratory biomarkers for atherosclerotic diseases
Published in Journal of chromatography. B, Analytical technologies in the biomedical and life sciences (01-10-2013)“…•Development and optimization of a fast UPLC–MS/MS method to quantify 18 eicosanoids in plasma samples.•Application of this assay to profile essential…”
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Dose‐Dependent Inhibition of OATP1B by Rifampicin in Healthy Volunteers: Comprehensive Evaluation of Candidate Biomarkers and OATP1B Probe Drugs
Published in Clinical pharmacology and therapeutics (01-04-2020)“…To address the most appropriate endogenous biomarker for drug–drug interaction risk assessment, eight healthy subjects received an organic anion transporting…”
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Biodistribution and Targeting of Anti-5T4 Antibody-Drug Conjugate Using Fluorescence Molecular Tomography
Published in Molecular cancer therapeutics (01-10-2016)“…Understanding a drug's whole-body biodistribution and tumor targeting can provide important information regarding efficacy, safety, and dosing parameters…”
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A multiplex HRMS assay for quantifying selected human plasma bile acids as candidate OATP biomarkers
Published in Bioanalysis (01-05-2018)“…Selected bile acids (BAs) in plasma have been proposed as endogenous probes for assessing drug-drug interactions involving hepatic drug transporters such as…”
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Preclinical Development of an anti-5T4 Antibody–Drug Conjugate: Pharmacokinetics in Mice, Rats, and NHP and Tumor/Tissue Distribution in Mice
Published in Bioconjugate chemistry (18-11-2015)“…The pharmacokinetics of an antibody (huA1)–drug (auristatin microtubule disrupting MMAF) conjugate, targeting 5T4-expressing cells, were characterized during…”
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Natural Product Bis-Intercalator Depsipeptides as a New Class of Payloads for Antibody–Drug Conjugates
Published in Bioconjugate chemistry (16-01-2019)“…A potent class of DNA-damaging agents, natural product bis-intercalator depsipeptides (NPBIDs), was evaluated as ultrapotent payloads for use in antibody–drug…”
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Characterization of bile acid sulfate conjugates as substrates of human organic anion-transporting polypeptides
Published in Drug metabolism and pharmacokinetics (01-01-2018)Get full text
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Modulation of NMDA receptor function by inhibition of d-amino acid oxidase in rodent brain
Published in Neuropharmacology (01-10-2011)“…Observations that N-Methyl- d-Aspartate (NMDA) antagonists produce symptoms in humans that are similar to those seen in schizophrenia have led to the current…”
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Structure-Based Design of Irreversible Human KAT II Inhibitors: Discovery of New Potency-Enhancing Interactions
Published in ACS medicinal chemistry letters (10-01-2013)“…A series of aryl hydroxamates recently have been disclosed as irreversible inhibitors of kynurenine amino transferase II (KAT II), an enzyme that may play a…”
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Effect of chitosan glutamate, carbomer 974P, and EDTA on the in vitro Caco-2 permeability and oral pharmacokinetic profile of acyclovir in rats
Published in Drug development and industrial pharmacy (01-09-2009)“…Background: Chitosan glutamate and polyacrylic acid (e.g., carbomer 974P) are known to modulate the tight junctions in the intestinal wall and increase…”
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Where Did the Linker-Payload Go? A Quantitative Investigation on the Destination of the Released Linker-Payload from an Antibody-Drug Conjugate with a Maleimide Linker in Plasma
Published in Analytical chemistry (Washington) (03-05-2016)“…The reactive thiol of cysteine is often used for coupling maleimide-containing linker-payloads to antibodies resulting in the generation of antibody drug…”
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Outsource-ability of high-resolution MS-based DMPK assays
Published in Bioanalysis (01-08-2016)Get full text
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A novel hydrophilic interaction chromatography assay characterization of 4-pyridoxic acid, an emergent renal organic anion transporter 1/3 transporter biomarker
Published in Bioanalysis (01-09-2021)“…4-pyridoxic acid (PDA) has been proposed as an endogenous biomarker for renal organic anion transporter 1/3 (OAT1/3) inhibition. Clinical data are needed to…”
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Identification of Glycochenodeoxycholate 3‐O‐Glucuronide and Glycodeoxycholate 3‐O‐Glucuronide as Highly Sensitive and Specific OATP1B1 Biomarkers
Published in Clinical pharmacology and therapeutics (01-03-2021)“…The aim of this study was to investigate the sensitivity and specificity of endogenous glycochenodeoxycholate and glycodeoxycholate 3‐O‐glucuronides (GCDCA‐3G…”
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In vivo biotransformations of antibody-drug conjugates
Published in Bioanalysis (01-01-2015)“…The selective delivery of potent pharmacologically active compounds to target tissue or cells by antibody-drug conjugates makes this immuno-conjugate a…”
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Quantitative Conjugated Payload Measurement Using Enzymatic Release of Antibody–Drug Conjugate with Cleavable Linker
Published in Bioconjugate chemistry (15-02-2017)“…As antibody-drug conjugate (ADC) design is evolving with novel payload, linker, and conjugation chemistry, the need for sensitive and precise quantitative…”
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Characterization of Bile Acid Sulfate Conjugates as Substrates of Human Organic Anion Transporting Polypeptides
Published in Molecular pharmaceutics (05-06-2023)“…Drug interactions involving the inhibition of hepatic organic anion transporting polypeptides (OATPs) 1B1 and OATP1B3 are considered important. Therefore, we…”
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Natural Product Splicing Inhibitors: A New Class of Antibody–Drug Conjugate (ADC) Payloads
Published in Bioconjugate chemistry (17-08-2016)“…There is a considerable ongoing work to identify new cytotoxic payloads that are appropriate for antibody-based delivery, acting via mechanisms beyond DNA…”
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Site Selection: a Case Study in the Identification of Optimal Cysteine Engineered Antibody Drug Conjugates
Published in The AAPS journal (01-07-2017)“…As the antibody drug conjugate (ADC) community continues to shift towards site-specific conjugation technology, there is a growing need to understand how the…”
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