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HIV Capsid is a Tractable Target for Small Molecule Therapeutic Intervention
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.
Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19
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.
Discovery of a Novel Class of Boron-Based Antibacterials with Activity against Gram-Negative Bacteria
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.
Boron‐based phosphodiesterase inhibitors show novel binding of boron to PDE4 bimetal center
Synthesis and antimitotic/cytotoxic activity of hemiasterlin analogues.
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.
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.
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.
Improved SARS-CoV-2 Mpro inhibitors based on feline antiviral drug GC376: Structural enhancements, increased solubility, and micellar studies
Comprehensive in vitro characterization of PD-L1 small molecule inhibitors
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.
Bioactivation of Flutamide Metabolites by Human Liver Microsomes
- Ping Kang, D. Dalvie, Evan B. Smith, S. Zhou, A. Deese, J. Nieman
- Biology, ChemistryDrug Metabolism and Disposition
- 1 July 2008
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.