Search Results - "Hurley, Christopher A."
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A restricted role for TYK2 catalytic activity in human cytokine responses revealed by novel TYK2-selective inhibitors
Published in The Journal of immunology (1950) (01-09-2013)“…TYK2 is a JAK family protein tyrosine kinase activated in response to multiple cytokines, including type I IFNs, IL-6, IL-10, IL-12, and IL-23. Extensive…”
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Discovery of Potent and Selective Pyrazolopyrimidine Janus Kinase 2 Inhibitors
Published in Journal of medicinal chemistry (26-11-2012)“…The discovery of somatic Jak2 mutations in patients with chronic myeloproliferative neoplasms has led to significant interest in discovering selective Jak2…”
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Discovery of a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling
Published in Bioorganic & medicinal chemistry letters (15-06-2019)“…[Display omitted] Disruption of interleukin-13 (IL-13) signaling with large molecule antibody therapies has shown promise in diseases of allergic inflammation…”
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Identification of Imidazo-Pyrrolopyridines as Novel and Potent JAK1 Inhibitors
Published in Journal of medicinal chemistry (28-06-2012)“…A therapeutic rationale is proposed for the treatment of inflammatory diseases, such as rheumatoid arthritis (RA), by specific targeting of the JAK1 pathway…”
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Identification of C‑2 Hydroxyethyl Imidazopyrrolopyridines as Potent JAK1 Inhibitors with Favorable Physicochemical Properties and High Selectivity over JAK2
Published in Journal of medicinal chemistry (13-06-2013)“…Herein we report on the structure-based discovery of a C-2 hydroxyethyl moiety which provided consistently high levels of selectivity for JAK1 over JAK2 to the…”
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2-Amino-[1,2,4]triazolo[1,5-a]pyridines as JAK2 inhibitors
Published in Bioorganic & medicinal chemistry letters (01-09-2013)“…The advancement of a series of ligand efficient 2-amino-[1,2,4]triazolo[1,5-a]pyridines, initially identified from high-throughput screening, to a JAK2…”
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Discovery and Optimization of C-2 Methyl Imidazopyrrolopyridines as Potent and Orally Bioavailable JAK1 Inhibitors with Selectivity over JAK2
Published in Journal of medicinal chemistry (12-07-2012)“…Herein we report the discovery of the C-2 methyl substituted imidazopyrrolopyridine series and its optimization to provide potent and orally bioavailable JAK1…”
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Novel triazolo-pyrrolopyridines as inhibitors of Janus kinase 1
Published in Bioorganic & medicinal chemistry letters (15-06-2013)“…The identification of a novel fused triazolo-pyrrolopyridine scaffold, optimized derivatives of which display nanomolar inhibition of Janus kinase 1, is…”
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Structure-based discovery of C-2 substituted imidazo-pyrrolopyridine JAK1 inhibitors with improved selectivity over JAK2
Published in Bioorganic & medicinal chemistry letters (15-12-2012)“…Herein we describe our successful efforts in obtaining C-2 substituted imidazo-pyrrolopyridines with improved JAK1 selectivity relative to JAK2 by targeting an…”
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10
Azepines and Piperidines with Dual Norepinephrine Dopamine Uptake Inhibition and Antidepressant Activity
Published in ACS medicinal chemistry letters (10-01-2013)“…Herein, we describe the discovery of inhibitors of norepinephrine (NET) and dopamine (DAT) transporters with reduced activity relative to serotonin…”
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Biophysical Characterization of an Integrin-Targeted Lipopolyplex Gene Delivery Vector
Published in Biochemistry (Easton) (13-11-2007)“…Nonviral gene delivery vectors now show good therapeutic potential: however, detailed characterization of the composition and macromolecular organization of…”
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Mono- and dicationic short PEG and methylene dioxyalkylglycerols for use in synthetic gene delivery systems
Published in Organic & biomolecular chemistry (01-01-2008)“…A range of monocationic and dicationic dioxyalkylglycerol cytofectins have been synthesised possessing methylene and short n-ethylene glycol spacers. The…”
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Mannose-pepstatin conjugates as targeted inhibitors of antigen processing
Published in Organic & biomolecular chemistry (01-01-2006)“…The molecular details of antigen processing, including the identity of the enzymes involved, their intracellular location and their substrate specificity, are…”
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Asymmetric Synthesis of Dialkyloxy-3-alkylammonium Cationic Lipids
Published in Journal of organic chemistry (06-02-2004)“…The cationic diether-linked cytofectin DOTMA (available commercially as a mixture, Lipofectin comprised of DOTMA:DOPE, 1:1) and analogues including DIMRIE and…”
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The Off-Label Use of POM Wonderful: Using Section 43(a) to Eliminate Misleading Off-Label Drug Promotion
Published in Washington and Lee law review (01-01-2018)“…On his way home from the hospital with his newborn son, a hit-and-run accident left Jeremy Lew with a severely injured spine. Lew underwent surgery, during…”
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Analysis and Optimization of the Cationic Lipid Component of a Lipid/Peptide Vector Formulation for Enhanced Transfection In Vitro and In Vivo
Published in Journal of liposome research (2006)“…We have previously described a lipopolyplex formulation comprising a mixture of a cationic peptide with an integrin-targeting motif (K16GACRRETAWACG) and…”
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