Search Results - "Brown, Janice A"
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Discovery of Potent and Orally Bioavailable Macrocyclic Peptide–Peptoid Hybrid CXCR7 Modulators
Published in Journal of medicinal chemistry (14-12-2017)“…The chemokine receptor CXCR7 is an attractive target for a variety of diseases. While several small-molecule modulators of CXCR7 have been reported, peptidic…”
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Discovery and Preclinical Characterization of 6‑Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]‑1H‑indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy
Published in Journal of medicinal chemistry (08-09-2016)“…Adenosine monophosphate-activated protein kinase (AMPK) is a protein kinase involved in maintaining energy homeostasis within cells. On the basis of human…”
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Discovery and evaluation of non-basic small molecule modulators of the atypical chemokine receptor CXCR7
Published in Bioorganic & medicinal chemistry letters (15-10-2021)“…[Display omitted] The atypical chemokine receptor C–X–C chemokine receptor type 7 (CXCR7) is an attractive therapeutic target for a variety of cardiac and…”
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Acyl Glucuronide Metabolites of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1 H-indole-3-carboxylic Acid (PF-06409577) and Related Indole-3-carboxylic Acid Derivatives are Direct Activators of Adenosine Monophosphate-Activated Protein Kinase (AMPK)
Published in Journal of medicinal chemistry (23-08-2018)“…Studies on indole-3-carboxylic acid derivatives as direct activators of human adenosine monophosphate-activated protein kinase (AMPK) α1β1γ1 isoform have…”
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Determination of Unbound Partition Coefficient and in Vitro-in Vivo Extrapolation for SLC13A Transporter-Mediated Uptake
Published in Drug metabolism and disposition (01-10-2016)“…Unbound partition coefficient (Kpuu) is important to an understanding of the asymmetric free drug distribution of a compound between cells and medium in vitro,…”
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Discovery of a Novel Small-Molecule Modulator of C–X–C Chemokine Receptor Type 7 as a Treatment for Cardiac Fibrosis
Published in Journal of medicinal chemistry (26-04-2018)“…C–X–C chemokine receptor type 7 (CXCR7) is involved in cardiac and immune pathophysiology. We report the discovery of a novel 1,4-diazepine CXCR7 modulator,…”
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Discovery of Diphenylacetamides as CXCR7 Inhibitors with Novel β-Arrestin Antagonist Activity
Published in ACS medicinal chemistry letters (11-06-2020)“…The atypical chemokine receptor CXCR7 has been studied in various disease settings including immunological diseases and heart disease. Efforts to elucidate the…”
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Discovery of Orally Bioavailable Selective Inhibitors of the Sodium-Phosphate Cotransporter NaPi2a (SLC34A1)
Published in ACS medicinal chemistry letters (10-05-2018)“…Sodium-phosphate cotransporter 2a, or NaPi2a (SLC34A1), is a solute-carrier (SLC) transporter located in the kidney proximal tubule that reabsorbs…”
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Zoniporide: a potent and highly selective inhibitor of human Na +/H + exchanger-1
Published in European journal of pharmacology (06-09-2002)“…We evaluated the in vitro pharmacological profile of a novel, potent and highly selective Na +/H + exchanger-1 (NHE-1) inhibitor,…”
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N-Benzylimidazole carboxamides as potent, orally active stearoylCoA desaturase-1 inhibitors
Published in Bioorganic & medicinal chemistry letters (15-03-2011)“…A potent, small molecule inhibitor with a favorable pharmacokinetic profile to allow for sustained SCD inhibition in vivo was identified. Biological evaluation…”
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Design, synthesis, and pharmacology of fluorescently labeled analogs of serotonin: application to screening of the 5-HT2C receptor
Published in Journal of biomolecular screening (01-04-2009)“…Novel fluorescent derivatives of serotonin have been synthesized and used as tracers for the development of a 5-HT2C fluorescence polarization assay. Serotonin…”
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Orally active and brain permeable proline amides as highly selective 5HT2c agonists for the treatment of obesity
Published in Bioorganic & medicinal chemistry letters (01-04-2010)“…Brain-penetrable proline amides were developed as 5HT2c agonists with more than 1000-fold binding selectivity against 5HT2b receptor. After medicinal chemistry…”
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Development of a high-throughput screening-amenable assay for human poly(ADP-ribose) polymerase inhibitors
Published in Journal of pharmacological and toxicological methods (01-05-2002)“…Introduction: Poly(ADP-ribose) polymerase (PARP) plays a pivotal role in the repair of DNA strand breaks. However, excessive activation of PARP causes a rapid…”
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Discovery of zoniporide: A potent and selective sodium–hydrogen exchanger type 1 (NHE-1) inhibitor with high aqueous solubility
Published in Bioorganic & medicinal chemistry letters (26-03-2001)“…Zoniporide (CP-597,396) is a potent and selective inhibitor of NHE-1, which exhibits high aqueous solubility and acceptable pharmacokinetics for intravenous…”
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Acyl Glucuronide Metabolites of 6‑Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]‑1H‑indole-3-carboxylic Acid (PF-06409577) and Related Indole-3-carboxylic Acid Derivatives are Direct Activators of Adenosine Monophosphate-Activated Protein Kinase (AMPK)
Published in Journal of medicinal chemistry (23-08-2018)“…Studies on indole-3-carboxylic acid derivatives as direct activators of human adenosine monophosphate-activated protein kinase (AMPK) α1β1γ1 isoform have…”
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Optimization of Metabolic and Renal Clearance in a Series of Indole Acid Direct Activators of 5′-Adenosine Monophosphate-Activated Protein Kinase (AMPK)
Published in Journal of medicinal chemistry (22-03-2018)“…Optimization of the pharmacokinetic (PK) properties of a series of activators of adenosine monophosphate-activated protein kinase (AMPK) is described…”
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Discovery and Preclinical Characterization of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1 H -indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy
Published in Journal of medicinal chemistry (08-09-2016)Get full text
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Prevention of transmitted infections in a pet therapy program: An exemplar
Published in American journal of infection control (01-07-2016)“…Highlights • Guidelines have been recently published by the Society for Healthcare Epidemiology of America on the safe oversite and management of animals in…”
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