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HIV Capsid is a Tractable Target for Small Molecule Therapeutic Intervention
TLDR
It is shown that amino acid substitutions in the N-terminal domain of HIV-1 CA are sufficient to confer resistance to this class of compounds, identifying CA as the target in infected cells and revealing HIV CA as a tractable drug target for HIV therapy.
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Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19
TLDR
Preclinical experiments reveal 4 (PF-00835231) as a potent inhibitor of CoV-2 3CLpro with suitable pharmaceutical properties to warrant further development as an intravenous treatment for COVID-19.
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Discovery of a Novel Class of Boron-Based Antibacterials with Activity against Gram-Negative Bacteria
TLDR
A new boron-based antibiotic class, the aminomethylbenzoxaboroles, which inhibit bacterial leucyl-tRNA synthetase and have activity against Gram-negative bacteria by largely evading the main efflux mechanisms in Escherichia coli and Pseudomonas aeruginosa is developed.
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Boron‐based phosphodiesterase inhibitors show novel binding of boron to PDE4 bimetal center
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Synthesis and antimitotic/cytotoxic activity of hemiasterlin analogues.
TLDR
The antimitotic sponge tripeptide hemiasterlin and a number of structural analogues have been synthesized and evaluated in cell-based assays in order to explore the SAR for this promising anticancer drug lead.
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HTI-286, a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo.
TLDR
The data suggest that HTI-286 has excellent preclinical properties that may translate into superior clinical activity, as well as provide a useful synthetic reagent to probe the drug contact sites of peptide-like molecules that interact with tubulin.
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Improved SARS-CoV-2 Mpro inhibitors based on feline antiviral drug GC376: Structural enhancements, increased solubility, and micellar studies
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Comprehensive in vitro characterization of PD-L1 small molecule inhibitors
TLDR
This work reports the rigorous and systematic in vitro characterization of a selected set of potent PD-1/PD-L1 macrocyclic peptide and small-molecule inhibitors from Bristol-Myers Squibb (BMS) and a peptidomimetic small- molecule inhibitor from Aurigene (Aurigene-1) using a series of biochemical and cell-based assays.
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Bioactivation of Flutamide Metabolites by Human Liver Microsomes
TLDR
In vitro studies in human liver microsomes were conducted to probe the cytochrome P450 (P450)-mediated bioactivation of flutamide metabolites and identify the possible reactive species using reduced glutathione (GSH) as a trapping agent.
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Solvent and in situ catalyst preparation impacts upon Noyori reductions of aryl-chloromethyl ketones: application to syntheses of chiral 2-amino-1-aryl-ethanols
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