Search Results - "Strobel, Eric D."
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Discovery of LX2761, a Sodium-Dependent Glucose Cotransporter 1 (SGLT1) Inhibitor Restricted to the Intestinal Lumen, for the Treatment of Diabetes
Published in Journal of medicinal chemistry (26-01-2017)“…The increasing number of people afflicted with diabetes throughout the world is a major health issue. Inhibitors of the sodium-dependent glucose cotransporters…”
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LX2761, a Sodium/Glucose Cotransporter 1 Inhibitor Restricted to the Intestine, Improves Glycemic Control in Mice
Published in The Journal of pharmacology and experimental therapeutics (01-07-2017)“…LX2761 is a potent sodium/glucose cotransporter 1 inhibitor restricted to the intestinal lumen after oral administration. Studies presented here evaluated the…”
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Macrocyclic BACE inhibitors: Optimization of a micromolar hit to nanomolar leads
Published in Bioorganic & medicinal chemistry letters (15-05-2010)“…Structural biology allowed the identification of 7 as a potent BACE inhibitor (IC 50 = 5 nM). We have identified macrocyclic inhibitors of the aspartic…”
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Tuning isoform selectivity and bortezomib sensitivity with a new class of alkenyl indene PDI inhibitor
Published in European journal of medicinal chemistry (15-01-2020)“…Protein disulfide isomerase (PDI, PDIA1) is an emerging therapeutic target in oncology. PDI inhibitors have demonstrated a unique propensity to selectively…”
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Potency of a small molecule that targets the molluscum contagiosum virus processivity factor increases when conjugated to a tripeptide
Published in Antiviral research (01-06-2024)“…We recently developed compound FC-7269 for targeting the Molluscum contagiosum virus processivity factor (mD4) and demonstrated its ability to inhibit viral…”
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A small molecule that targets the processivity factor of molluscum contagiosum virus has therapeutic potential
Published in Antiviral research (01-03-2023)“…Molluscum contagiosum (MC) is an infectious disease that occurs only in humans with a tropism that is narrowly restricted to the outermost epidermal layer of…”
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Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation
Published in ACS medicinal chemistry letters (08-01-2015)“…The first allosteric, type III inhibitor of LIM-kinase 2 (LIMK2) is reported. A series of molecules that feature both an N-phenylsulfonamide and tertiary amide…”
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Mutation and structure guided discovery of an antiviral small molecule that mimics an essential C-Terminal tripeptide of the vaccinia D4 processivity factor
Published in Antiviral research (01-02-2019)“…The smallpox virus (variola) remains a bioterrorism threat since a majority of the human population has never been vaccinated. In the event of an outbreak, at…”
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(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: Platelet-Derived Growth Factor Receptor Tyrosine Kinase Inhibitors with Broad Antiproliferative Activity against Tumor Cells
Published in Journal of medicinal chemistry (29-12-2005)“…A series of (6,7-dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines has been optimized to preserve both potent kinase inhibition activity against the…”
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