Activity-Based Dicyanoisophorone Derivatives: Fluorogenic Toolbox Enables Direct Visualization and Monitoring of Esterase Activity in Tumor Models.

ABSTRACT: The visualization and spatiotemporal monitoring of endogenous esterase activity are crucial for clinical diagnostics and treatment of liver diseases. Our research adopts a novel substrate hydrolysis-enzymatic activity (SHEA) approach using dicyanoisophorone-based fluorogenic ester substrates DCIP-R (R = R1-R6) to evaluate esterase preferences on diverse substrate libraries. Esterase-mediated hydrolysis yielded fluorescent DCIP-OH with a nanomolar detection limit in vitro. These probes effectively monitor ester hydrolysis kinetics with a turnover number of 4.73 s^-1 and catalytic efficiency (k_cat/K_m) of 10⁶ M^-1 s^-1 (DCIP-R1). Comparative studies utilizing two-photon imaging have indica

SUBMITTER: Kavyashree P 

PROVIDER: S-EPMC11561878 | biostudies-literature | 2024 Nov

REPOSITORIES: biostudies-literature