Search Results - "Aggen, James"
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Synthesis and Spectrum of the Neoglycoside ACHN-490
Published in Antimicrobial Agents and Chemotherapy (01-11-2010)“…Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley Reddit…”
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2
Discovery of RMC-5552, a Selective Bi-Steric Inhibitor of mTORC1, for the Treatment of mTORC1-Activated Tumors
Published in Journal of medicinal chemistry (12-01-2023)“…Hyperactivation of mTOR kinase by mutations in the PI3K/mTOR pathway or by crosstalk with other mutant cancer drivers, such as RAS, is a feature of many…”
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3
Selective inhibitors of mTORC1 activate 4EBP1 and suppress tumor growth
Published in Nature chemical biology (01-10-2021)“…The clinical benefits of pan-mTOR active-site inhibitors are limited by toxicity and relief of feedback inhibition of receptor expression. To address these…”
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4
ACHN-490, a Neoglycoside with Potent In Vitro Activity against Multidrug-Resistant Klebsiella pneumoniae Isolates
Published in Antimicrobial Agents and Chemotherapy (01-10-2009)“…Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley Reddit…”
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5
Optimization of LpxC Inhibitors for Antibacterial Activity and Cardiovascular Safety
Published in ChemMedChem (20-08-2019)“…UDP‐3‐O‐(R‐3‐hydroxymyristoyl)‐N‐acetylglucosamine deacetylase (LpxC) is a Zn2+ deacetylase that is essential for the survival of most pathogenic Gram‐negative…”
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6
In Vivo Efficacy of the Novel Aminoglycoside ACHN-490 in Murine Infection Models
Published in Antimicrobial Agents and Chemotherapy (01-04-2011)“…Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley Reddit…”
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7
Author Correction: Selective inhibitors of mTORC1 activate 4EBP1 and suppress tumor growth
Published in Nature chemical biology (01-08-2021)Get full text
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8
Compound design guidelines for evading the efflux and permeation barriers of Escherichia coli with the oxazolidinone class of antibacterials: Test case for a general approach to improving whole cell Gram-negative activity
Published in Bioorganic & medicinal chemistry letters (01-12-2017)“…[Display omitted] Previously we reported the results from an effort to improve Gram-negative antibacterial activity in the oxazolidinone class of antibiotics…”
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Author Correction: Selective inhibitors of mTORC1 activate 4EBP1 and suppress tumor growth
Published in Nature chemical biology (01-11-2021)Get full text
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10
Toxicity Modulation, Resistance Enzyme Evasion, and A‑Site X‑ray Structure of Broad-Spectrum Antibacterial Neomycin Analogs
Published in ACS chemical biology (19-09-2014)“…Aminoglycoside antibiotics are pseudosaccharides decorated with ammonium groups that are critical for their potent broad-spectrum antibacterial activity…”
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11
Progress against Escherichia coli with the Oxazolidinone Class of Antibacterials: Test Case for a General Approach To Improving Whole-Cell Gram-Negative Activity
Published in ACS infectious diseases (10-06-2016)“…Novel antibacterials with activity against the Gram-negative bacteria associated with nosocomial infections, including Escherichia coli and other…”
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12
1-(4-Phenylpiperazin-1-yl)-2-(1H-pyrazol-1-yl)ethanones as novel CCR1 antagonists
Published in Bioorganic & medicinal chemistry letters (01-03-2013)“…A novel series of CCR1 antagonists based on the 1-(4-phenylpiperazin-1-yl)-2-(1H-pyrazol-1-yl)ethanone scaffold was identified by screening a compound library…”
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13
Congener-Independent Immunoassay for Microcystins and Nodularins
Published in Environmental science & technology (15-12-2001)“…Cyanobacteria (blue-green algae) (e.g., Microcystis and Nodularia spp.) capable of producing toxic peptides are found in fresh and brackish water worldwide…”
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14
Multivalent design of long-acting β(2)-adrenoceptor agonists incorporating biarylamines
Published in Bioorganic & medicinal chemistry letters (15-06-2014)“…A series of potent β2-adrenoceptor agonists incorporating a biarylamine secondary binding group was identified. The previously reported milveterol (5),…”
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15
Exploring the Positional Attachment of Glycopeptide/β-lactam Heterodimers
Published in Journal of antibiotics (01-10-2008)“…Further investigations towards novel glycopeptide/β-lactam heterodimers are reported. Employing a multivalent approach to drug discovery, vancomycin and…”
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A Multivalent Approach to Drug Discovery for Novel Antibiotics
Published in Journal of antibiotics (01-10-2008)“…The design, synthesis and antibacterial activity of novel glycopeptide/β-lactam heterodimers is reported. Employing a multivalent approach to drug discovery,…”
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17
A Central Strategy for Converting Natural Products into Fluorescent Probes
Published in Chembiochem : a European journal of chemical biology (01-03-2006)“…A centralized method for studying natural product chemical biology begins by designating a single fluorescent dye as a core reporter and develops through the…”
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18
Toward Overcoming Staphylococcus aureus Aminoglycoside Resistance Mechanisms with a Functionally Designed Neomycin Analogue
Published in ACS medicinal chemistry letters (08-12-2011)“…Deoxygenation of the diol groups in rings A and D of neomycin in combination with the introduction of an N1-(l)-HABA group in the 2-deoxystreptamine subunit…”
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Microcystin analogues comprised only of adda and a single additional amino acid retain moderate activity as PP1/PP2A inhibitors
Published in Bioorganic & medicinal chemistry letters (01-09-2003)“…A series of greatly simplified microcystin analogues comprised only of Adda (the β-amino acid common to the microcystins, nodularins, and motuporin,) and a…”
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Total Synthesis of the Serine-Threonine Phosphatase Inhibitor Microcystin-LA
Published in Journal of the American Chemical Society (27-11-1996)“…Reversible protein phosphorylation, which is mediated by kinases and phosphatases, is a major control element of the cell. There is a diverse group of toxic…”
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