33282-15-4, Name is 5-(4-Hydroxyphenyl)isoxazole-3-carboxylic acid, belongs to Isoxazoles compound, is a common compound. Safety of 5-(4-Hydroxyphenyl)isoxazole-3-carboxylic acidIn an article, once mentioned the new application about 33282-15-4.
Microplate-based assay for identifying small molecules that bind a specific intersubunit interface within the assembled HIV-1 capsid
Despite the availability of>30 effective drugs for managing HIV-1 infection, no current therapy is curative, and long-term management is challenging owing to the emergence and spread of drug-resistant mutants. Identification of drugs against novel HIV-1 targets would expand the current treatment options and help to control resistance. The highly conserved HIV-1 capsid protein represents an attractive target because of its multiple roles in replication of the virus. However, the low antiviral potencies of the reported HIV-1 capsid-targeting inhibitors render them unattractive for therapeutic development. To facilitate the identification of more-potent HIV-1 capsid inhibitors, we developed a scintillation proximity assay to screen for small molecules that target a biologically active and specific intersubunit interface in the HIV-1 capsid. The assay, which is based on competitive displacement of a known capsid-binding small-molecule inhibitor, exhibited a signal-to-noise ratio of>9 and a Z factor of>0.8. In a pilot screen of a chemical library containing 2,400 druglike compounds, we obtained a hit rate of 1.8%. This assay has properties that are suitable for screening large compound libraries to identify novel HIV-1 capsid ligands with antiviral activity.
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Reference£º
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem