Redox active or thiol reactive?

Autor: Proj, Matic, Knez, Damijan, Sosič, Izidor, Gobec, Stanislav
Jazyk: angličtina
Rok vydání: 2022
Předmět:
Zdroj: Drug discovery today, vol. 27, no. 6, pp. 1733-1742, 2022.
ISSN: 1359-6446
Popis: Compounds that exhibit assay interference or undesirable mechanisms of bioactivity are routinely encountered in assays at various stages of drug discovery. We observed that assays for the investigation of thiol-reactive and redox-active compounds have not been collected in a comprehensive review. Here, we review these assays and subject them to experimental optimization to improve their reliability. We demonstrate the usefulness of our assay cascade by assaying a library of bioactive compounds, chemical probes, and a set of approved drugs. These high-throughput assays should complement the array of wet-lab and in silico assays during the initial stages of hit discovery campaigns to pursue only hit compounds with tractable mechanisms of action.
Databáze: OpenAIRE