Search Results - "Carr, Donna"
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A translational pharmacokinetic/pharmacodynamic model to characterize bacterial kill in the presence of imipenem-relebactam
Published in International journal of infectious diseases (01-12-2019)“…•The impact of relebactam concentration on imipenem susceptibility is described.•The PK/PD driver for relebactam is fAUC/MIC.•A relebactam fAUC/MIC ratio of…”
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Exploring the Pharmacokinetic/Pharmacodynamic Relationship of Relebactam (MK-7655) in Combination with Imipenem in a Hollow-Fiber Infection Model
Published in Antimicrobial agents and chemotherapy (01-05-2018)“…Resistance to antibiotics among bacterial pathogens is rapidly spreading, and therapeutic options against multidrug-resistant bacteria are limited. There is an…”
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Development of a fully automated platform for agar-based measurement of viable bacterial growth
Published in SLAS technology (01-08-2022)“…Dynamic in vitro antibacterial studies provide valuable insight on effective dosing strategies prior to translating to in vivo models. Frequent sampling is…”
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Farnesyl Transferase Inhibitors Block the Farnesylation of CENP-E and CENP-F and Alter the Association of CENP-E with the Microtubules
Published in The Journal of biological chemistry (29-09-2000)“…Human tumor cell lines that are sensitive to the effects of farnesyl transferase inhibitors accumulate in G2 → M (except for cells with an activated Ha-ras…”
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The Farnesyl Transferase Inhibitor SCH 66336 Induces a G2 → M or G1 Pause in Sensitive Human Tumor Cell Lines
Published in Experimental cell research (01-01-2001)“…SCH 66336 is a potent farnesyl transferase inhibitor (FTI) in clinical development. It efficiently prevents the membrane association of H-ras, but not K- or…”
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Characterization of Ha-Ras, N-Ras, Ki-Ras4A, and Ki-Ras4B as in Vitro Substrates for Farnesyl Protein Transferase and Geranylgeranyl Protein Transferase Type I
Published in The Journal of biological chemistry (11-04-1997)“…Ras proteins are small GTP-binding proteins which are critical for cell signaling and proliferation. Four Ras isoforms exist: Ha-Ras, N-Ras, Ki-Ras4A, and…”
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Selective small-molecule inhibition of an RNA structural element
Published in Nature (London) (29-10-2015)“…Riboswitches are non-coding RNA structures located in messenger RNAs that bind endogenous ligands, such as a specific metabolite or ion, to regulate gene…”
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Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors
Published in Cancer discovery (01-07-2013)“…The high frequency of activating RAS or BRAF mutations in cancer provides strong rationale for targeting the mitogen-activated protein kinase (MAPK) pathway…”
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Discovery of Ruzasvir (MK-8408): A Potent, Pan-Genotype HCV NS5A Inhibitor with Optimized Activity against Common Resistance-Associated Polymorphisms
Published in Journal of medicinal chemistry (12-01-2017)“…We describe the research that led to the discovery of compound 40 (ruzasvir, MK-8408), a pan-genotypic HCV nonstructural protein 5A (NS5A) inhibitor with a…”
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Crystal Structures of MEK1 Binary and Ternary Complexes with Nucleotides and Inhibitors
Published in Biochemistry (Easton) (31-03-2009)“…MEK1 is a member of the MAPK signal transduction pathway that responds to growth factors and cytokines. We have determined that the kinase domain spans…”
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Biological Effects and Mechanism of Action of Farnesyl Transferase Inhibitors
Published in Chemical research in toxicology (16-10-2000)Get full text
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The impact of curricular changes on BSCN students' clinical learning outcomes
Published in Nurse education in practice (01-11-2016)“…Ongoing curricular renewal is a necessary phenomenon in nursing education to align learning with ever-changing professional practice demands. The McMaster…”
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Development of MK-8353, an orally administered ERK1/2 inhibitor, in patients with advanced solid tumors
Published in JCI insight (22-02-2018)“…Constitutive activation of ERK1/2 occurs in various cancers, and its reactivation is a well-described resistance mechanism to MAPK inhibitors. ERK inhibitors…”
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In Vitro Antiviral Profile of Ruzasvir, a Potent and Pangenotype Inhibitor of Hepatitis C Virus NS5A
Published in Antimicrobial agents and chemotherapy (01-11-2018)“…Inhibition of NS5A has emerged as an attractive strategy to intervene in hepatitis C virus (HCV) replication. Ruzasvir (formerly MK-8408) was developed as a…”
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Discovery of MK-6169, a Potent Pan-Genotype Hepatitis C Virus NS5A Inhibitor with Optimized Activity against Common Resistance-Associated Substitutions
Published in Journal of medicinal chemistry (10-05-2018)“…We describe the discovery of MK-6169, a potent and pan-genotype hepatitis C virus NS5A inhibitor with optimized activity against common resistance-associated…”
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Discovery of Novel, Dual Mechanism ERK Inhibitors by Affinity Selection Screening of an Inactive Kinase
Published in Journal of medicinal chemistry (13-11-2014)“…An affinity-based mass spectrometry screening technology was used to identify novel binders to both nonphosphorylated and phosphorylated ERK2. Screening of…”
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Discovery of hydroxyaniline amides as selective Extracellular Regulated Kinase (Erk) inhibitors
Published in Bioorganic & medicinal chemistry letters (01-04-2015)“…[Display omitted] Starting from weak μM hits identified through affinity based Automated Ligand Identification System (ALIS) screenings, double digit nM…”
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Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology
Published in Bioorganic & medicinal chemistry letters (15-06-2018)“…[Display omitted] •Discovery of potent, selective and orally bioavailable ERK inhibitor for oncology.•Synthesis of tert 3-(S)thiomethyl pyrrolidine based ERK…”
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MK-8353: Discovery of an Orally Bioavailable Dual Mechanism ERK Inhibitor for Oncology
Published in ACS medicinal chemistry letters (12-07-2018)“…The emergence and evolution of new immunological cancer therapies has sparked a rapidly growing interest in discovering novel pathways to treat cancer. Toward…”
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Affinity Selection–Mass Spectrometry Identifies a Novel Antibacterial RNA Polymerase Inhibitor
Published in ACS chemical biology (19-05-2017)“…The growing prevalence of drug resistant bacteria is a significant global threat to human health. The antibacterial drug rifampin, which functions by…”
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