Multifunctional activity-based chemical probes for sirtuins.

ABSTRACT: The sirtuin family of NAD⁺-dependent protein deacylases has gained significant attention during the last two decades, owing to their unique enzymatic activities as well as their critical roles in a broad array of cellular events. Innovative chemical probes are heavily pursued for the functional annotation and pharmacological perturbation of this group of "eraser" enzymes. We have developed several series of activity-based chemical probes (ABPs) to interrogate the functional state of active sirtuins in complex biological samples. They feature a simple Ala-Ala-Lys tripeptide backbone with a thioacyl "warhead", a photoaffinity group (benzophenone or diazirine), and a bioorthogonal group (terminal alkyne or azido) for conjugation to reporters. When applied in a comparative fashion,

SUBMITTER: Sharma C 

PROVIDER: S-EPMC10103746 | biostudies-literature | 2023 Apr

REPOSITORIES: biostudies-literature