Search Results - "EVENOU, PIERRE"
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The potent protein kinase C-selective inhibitor AEB071 (sotrastaurin) represents a new class of immunosuppressive agents affecting early T-cell activation
Published in The Journal of pharmacology and experimental therapeutics (01-09-2009)“…There is a pressing need for immunosuppressants with an improved safety profile. The search for novel approaches to blocking T-cell activation led to the…”
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Discovery of 3-(1H-Indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione (AEB071), a Potent and Selective Inhibitor of Protein Kinase C Isotypes
Published in Journal of medicinal chemistry (22-10-2009)“…A series of novel maleimide-based inhibitors of protein kinase C (PKC) were designed, synthesized, and evaluated. AEB071 (1) was found to be a potent,…”
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A Streaming Distance Transform Algorithm for Neighborhood-Sequence Distances
Published in Image processing on line (01-09-2014)“…We describe an algorithm that computes a “translated” 2D Neighborhood-Sequence Distance Transform (DT) using a look up table approach. It requires a single…”
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Rational Design, Synthesis, and X-ray Structure of Selective Noncovalent Thrombin Inhibitors
Published in Journal of medicinal chemistry (10-09-1998)“…We have designed, synthesized, and tested in vitro a novel class of noncovalent thrombin inhibitors. The main feature of these inhibitors is a 6,5-fused…”
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Structure–Activity Relationship and Pharmacokinetic Studies of Sotrastaurin (AEB071), a Promising Novel Medicine for Prevention of Graft Rejection and Treatment of Psoriasis
Published in Journal of medicinal chemistry (08-09-2011)“…Protein kinase C (PKC) isotypes have emerged as key targets for the blockade of early T-cell activation. Herein, we report on the structure–activity…”
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128-LB: Insulin Glargine 300 U/mL (Gla-300) vs. First-Generation Basal Insulins (BI) in Insulin-Naïve Type 2 Diabetes (T2D) Patients (Pts) With and Without Cardiovascular Disease (CVD): Outcomes of the Randomized Pragmatic Real-Life Clinical Trial ACHIEVE Control
Published in Diabetes (New York, N.Y.) (01-06-2019)“…ACHIEVE Control demonstrated superiority of Gla-300 vs. standard of care (SOC) BIs (glargine 100 U/mL and detemir), with a significantly greater proportion of…”
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Bridging β‐Cyclodextrin Prevents Self‐Inclusion, Promotes Supramolecular Polymerization, and Promotes Cooperative Interaction with Nucleic Acids
Published in Angewandte Chemie International Edition (25-06-2018)“…A bridge to assemble: Cyclodextrins bridged with an ammonium linker bearing a hydrophobic substituent can efficiently form supramolecular polymers and avoid…”
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1038-P: Insulin Glargine 300 U/ml (Gla-300) vs. First-Generation Standard-of-Care Basal Insulin Analogs (SOC-BI) in Insulin-Naïve Patients with Type 2 Diabetes (T2D): Impact of Renal Function on the Outcomes of the Randomized Pragmatic Real-Life Achieve Control S
Published in Diabetes (New York, N.Y.) (01-06-2020)“…In the 12-month ACHIEVE Control study, significantly more insulin-naive patients with T2D treated with Gla-300 vs. SOC-BI (glargine 100 U/mL or detemir)…”
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2,6-Naphthyridines as potent and selective inhibitors of the novel protein kinase C isozymes
Published in Bioorganic & medicinal chemistry letters (15-12-2011)“…Compound 11 potently inhibits the novel PKC isozymes δ, ε, η, θ, with IC 50 values of 20, 5, 5 and 77 nM, respectively, and displays a 11–180-fold selectivity…”
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Target attainment in insulin-naive patients at high risk for hypoglycemia: Results from ACHIEVE Control
Published in Journal of diabetes and its complications (01-04-2021)“…To better understand outcomes in people with type 2 diabetes at high risk of hypoglycemia, we conducted post hoc analyses in subgroups of participants from the…”
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Medial axis lookup table and test neighborhood computation for 3D chamfer norms
Published in Pattern recognition (01-10-2009)“…Chamfer distances are discrete distances based on the propagation of local distances, or weights, defined in a mask. The medial axis, i.e. the centers of…”
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Minimal-delay distance transform for neighborhood-sequence distances in 2D and 3D
Published in Computer vision and image understanding (01-04-2013)“…► New class of discrete distances that includes neighborhood-sequences distances and chamfer distances. ► Application to neighborhood-sequence distance…”
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Post Hoc Analysis Evaluating the Impact of Antihyperglycemic Background Therapies on Attainment of A1C Targets Without Hypoglycemia in the ACHIEVE Control Pragmatic, Real-Life Study
Published in Diabetes spectrum (01-11-2021)“…ACHIEVE Control, a prospective, open-label, randomized, pragmatic, real-life study in insulin-naive people with type 2 diabetes (A1C 8.0-11.0%), demonstrated…”
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Discovery of Novel (Imidazo[1,2-a]pyrazin-6-yl)ureas as Antiproliferative Agents Targeting P53 in Non-small Cell Lung Cancer Cell Lines
Published in Anticancer research (01-04-2016)“…A series of (imidazo[1,2-a]pyrazin-6-yl)ureas were synthesized through 6-aminoimidazo[1,2-a]pyrazine as a key intermediate…”
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Bridging β‐Cyclodextrin Prevents Self‐Inclusion, Promotes Supramolecular Polymerization, and Promotes Cooperative Interaction with Nucleic Acids
Published in Angewandte Chemie (25-06-2018)“…Cyclodextrine, die von einem Ammoniumlinker mit hydrophoben Substituenten überbrückt sind, können effizient supramolekulare Polymere bilden und den…”
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Bridging β‐Cyclodextrin Prevents Self‐Inclusion, Promotes Supramolecular Polymerization, and Promotes Cooperative Interaction with Nucleic Acids
Published in Angewandte Chemie (01-06-2018)“…Cyclodextrine, die von einem Ammoniumlinker mit hydrophoben Substituenten überbrückt sind, können effizient supramolekulare Polymere bilden und den…”
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Indolyl-naphthyl-maleimides as potent and selective inhibitors of protein kinase C-α/β
Published in Bioorganic & medicinal chemistry letters (15-02-2017)“…[Display omitted] The indolyl-naphthyl maleimide 7 is a potent inhibitor of the classical PKC isotypes α,β and shows excellent selectivity over the novel PKC…”
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Binding of a Bolton-Hunter substituted homostatine analog to affinity-immobilized human renin
Published in Biochemical pharmacology (15-08-1990)“…The binding of a Bolton-Hunter reagent substituted homostatine analog, SDZ 213-776, to human renin was investigated at pH 6.5 and 7.4. At both pH values, SDZ…”
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