Search Results - "Wegerski, Christopher J"
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Design of Development Candidate eFT226, a First in Class Inhibitor of Eukaryotic Initiation Factor 4A RNA Helicase
Published in Journal of medicinal chemistry (11-06-2020)“…Dysregulation of protein translation is a key driver for the pathogenesis of many cancers. Eukaryotic initiation factor 4A (eIF4A), an ATP-dependent DEAD-box…”
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Disposition and metabolism of 2′,2′”-Dithiobisbenzanilide in rodents following intravenous and oral administration and dermal application
Published in Toxicology reports (01-01-2020)“…•2′,2′′′-Dithiobisbenzanilide (DTBBA) is a chemical used as a peptizing agent for rubber.•Humane exposure to DTBBA is possible via oral and dermal…”
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Structure-based Design of Pyridone–Aminal eFT508 Targeting Dysregulated Translation by Selective Mitogen-activated Protein Kinase Interacting Kinases 1 and 2 (MNK1/2) Inhibition
Published in Journal of medicinal chemistry (26-04-2018)“…Dysregulated translation of mRNA plays a major role in tumorigenesis. Mitogen-activated protein kinase interacting kinases (MNK)1/2 are key regulators of mRNA…”
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Targeting Oncogene mRNA Translation in B-Cell Malignancies with eFT226, a Potent and Selective Inhibitor of eIF4A
Published in Molecular cancer therapeutics (01-01-2021)“…The PI3K/AKT/mTOR pathway is often activated in lymphoma through alterations in PI3K, PTEN, and B-cell receptor signaling, leading to dysregulation of eIF4A…”
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Strategic Diastereoselective C1 Functionalization in the Aza-Rocaglamide Scaffold toward Natural Product-Inspired eIF4A Inhibitors
Published in Organic letters (21-08-2020)“…Rocaglates, rocaglamides, and related flavagline natural products exert their remarkable anticancer activity through inhibition of eukaryotic initiation factor…”
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1-Aminomethyl SAR in a novel series of flavagline-inspired eIF4A inhibitors: Effects of amine substitution on cell potency and in vitro PK properties
Published in Bioorganic & medicinal chemistry letters (01-09-2021)“…[Display omitted] Flavaglines such as silvestrol (1) and rocaglamide (2) constitute an interesting class of natural products with promising anticancer…”
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Metabolism and disposition of 2-hydroxy-4-methoxybenzophenone, a sunscreen ingredient, in Harlan Sprague Dawley rats and B6C3F1/N mice; a species and route comparison
Published in Xenobiotica (02-06-2020)“…2-Hydroxy-4-methoxybenzophenone (HMB) is a common ingredient in personal care products and used as an UV stabilizer. In these studies, disposition and…”
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Disposition of β-N-methylamino-l-alanine (L-BMAA), a neurotoxin, in rodents following a single or repeated oral exposure
Published in Toxicology and applied pharmacology (15-01-2018)“…β-N-methylamino-l-alanine (L-BMAA) is produced by cyanobacteria (blue-green algae). Human exposure to L-BMAA occurs via consumption of L-BMAA-contaminated…”
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Using a kinase screen to investigate the constituents of the sponge Stelletta clavosa obtained from diverse habitats
Published in Bioorganic & medicinal chemistry (01-11-2004)“…[Display omitted] Fourteen collections of the marine sponge Stelletta clavosa have been obtained from diverse Indo-Pacific locations in order to conduct a…”
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A Serendipitous Discovery of Isomotuporin-Containing Sponge Populations of Theonella swinhoei
Published in Journal of natural products (Washington, D.C.) (01-01-2007)“…An in-depth LCMS examination of 14 different collections of Indo-Pacific Theonella swinhoei sponges resulted in the discovery of four diastereomeric analogues…”
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Disposition and Metabolism of Cumene in F344 Rats and B6C3F1 Mice
Published in Drug metabolism and disposition (01-03-2011)“…Cumene is a high-production volume chemical that has been shown to be a central nervous system depressant and has been implicated as a long-term exposure…”
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Abstract B33: Targeting PI3K/mTOR signaling with potent, selective and orally-available small-molecule inhibitors of eIF4E
Published in Molecular cancer research (01-10-2020)“…Abstract Aberrant protein translation plays a role in the pathogenesis of multiple solid tumors and hematologic malignancies. The translation initiation factor…”
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Abstract 2698: eFT226, a potent and selective inhibitor of eIF4A, is efficacious in preclinical models of lymphoma
Published in Cancer research (Chicago, Ill.) (01-07-2019)“…Abstract Dysregulated messenger RNA (mRNA) translation drives the pathogenesis of multiple hematological malignancies. In lymphoma this includes the…”
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Abstract 1302: Targeting hormone receptor-dependent cancers with potent, selective and orally-available small molecule inhibitors of eIF4E
Published in Cancer research (Chicago, Ill.) (01-07-2019)“…Abstract The PI3K/mTOR pathway is commonly dysregulated in many hormone receptor-dependent tumors and plays a key role in promoting tumor growth and mediating…”
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Abstract B133: eFT226, a first in class inhibitor of eIF4A1, targets FGFR1/2 and HER2 driven cancers
Published in Molecular cancer therapeutics (01-12-2019)“…Abstract Background: Mutations or amplifications affecting receptor tyrosine kinases (RTKs) activate the RAS/MAPK and PI3K/AKT signaling pathways thereby…”
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Abstract DDT02-05: eFT226: A selective and highly potent inhibitor of eukaryotic initiation factor 4A (eIF4A), a novel approach for the treatment of cancer
Published in Cancer research (Chicago, Ill.) (01-07-2018)“…Abstract eFT226: A Selective and Highly Potent Inhibitor of Eukaryotic Initiation Factor 4A (eIF4A), a Novel Approach for the Treatment of Cancer Siegfried H…”
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Abstract 596: eFT508, a potent and highly selective inhibitor of MNK1/2 regulates immune checkpoint and cytokine expression promoting anti-tumor immunity
Published in Cancer research (Chicago, Ill.) (01-07-2017)“…Abstract Dysregulated translation of messenger RNA (mRNA) plays a role in the pathogenesis of multiple solid tumors and hematological malignancies. MNK1 and…”
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Abstract PR11: eFT508: An oral, potent and highly selective inhibitor of MNK1 and MNK2, promotes anti-tumor immunity as a monotherapy and in combination with immune checkpoint blockade
Published in Cancer research (Chicago, Ill.) (15-03-2017)“…Abstract Purpose: This study was designed to evaluate the potential of eFT508 to selectively regulate key immune signaling pathways and enhance anti-tumor…”
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eFT508, a Potent and Selective Mitogen-Activated Protein Kinase Interacting Kinase (MNK) 1 and 2 Inhibitor, Is Efficacious in Preclinical Models of Diffuse Large B-Cell Lymphoma (DLBCL)
Published in Blood (03-12-2015)“…Dysregulated translation of messenger RNA (mRNA) plays a role in the pathogenesis of multiple solid tumors and hematological malignancies. MNK1 and MNK2…”
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Disposition and Metabolism of Cumene in F344 Rats and B6C3F1 MiceS
Published in Drug metabolism and disposition (01-03-2011)“…Cumene is a high-production volume chemical that has been shown to be a central nervous system depressant and has been implicated as a long-term exposure…”
Get full text
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