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Content archived on 2024-06-16

Combinatorial synthesis of beta-lactones and beta-lactams as potential inhibitors for Cdc25A phosphatase; an interesting target for anti-cancer drugs

Final Activity Report Summary - FJDEKKER04 (Combinatorial synthesis of beta-lactones and beta-lactams as potential inhibitors for Cdc25A phosphatase; an interesting target for anti-cancer drugs.)

The project aimed at the development of a novel methodology to define small molecule modulators of protein function.

Protein structure similarity, in conjunction with natural products, was used as inspiration source for the synthesis of a compound collection and target selection. The applicability of this new methodology was investigated and new small molecule modulators of protein function were identified.

One of these small molecules was used, by the time of the project completion, in a reverse chemical genetics study to evaluate the role of the acyl protein thioesterase 1 enzyme in cell-based studies. The newly identified small molecule enabled the identification of acyl protein thioesterase 1 as a new anti-cancer drug target.