NanoDSF Screening for Anti-tubulin Agents Uncovers New Structure-Activity Insights.

ABSTRACT: Microtubule targeting agents (MTAs) constitute a vital category of tubulin-binding compounds deployed across anticancer therapies. Despite the array of MTA drugs developed by pharmaceutical entities, the quest for novel efficacious molecules continues unabated. We unveil an innovative in vitro MTA screening methodology employing nano-differential scanning fluorimetry (nanoDSF), presenting distinct advantages over known assays. This novel approach not only assesses compound-tubulin binding but also quantitatively analyzes its impact on tubulin polymerization, facilitating structure-activity relationship discovery. The proposed nanoDSF assay was rigorously validated using the Prestwick Chemical Library, which encompasses 1520 approved compounds, successfully identifying all previously known

SUBMITTER: Baksheeva V 

PROVIDER: S-EPMC12406199 | biostudies-literature | 2025 Aug

REPOSITORIES: biostudies-literature