Organogold compounds as “smart” residue specific chemical modifiers: towards new generation Gold-PROTACs (B03)

Project: Research

Project Details

Description

To achieve novel pharmacophores and chemical probes relevant to the ubiquitin-proteasome system (UPS), the design of covalent amino acid (e.g. cysteine) modifiers is of paramount importance. We propose here a medicinal inorganic chemistry approach, using organogold compounds able to ‘catalyze’ bio-orthogonal C-S and C-Se bond-forming reactions under physiological conditions. An integrated investigational approach including chemoprotemoic/protemic, spectroscopic and computational methods, as well as in vitro pharmacological and imaging assays, will be used to elucidate the reactivity of the organogold compounds with target proteins relevant to the network, and their mechanisms of anticancer action focusing on NSCLC and MM. Moreover, the bioactive organogold moiety will enable its integration into a novel Gold-PROTAC construct enabling the selective degradation of specific UPS proteins and beyond.

StatusActive
Effective start/end date1/01/24 → …

Fingerprint

Explore the research topics touched on by this project. These labels are generated based on the underlying awards/grants. Together they form a unique fingerprint.