Kinetolab

Published a study about Activation-Free Sulfonyl Fluoride Probes for Fragment Screening

In Molecules journal was published the research about synthesis and characterization of a small sulfonyl fluoride library for tagging tractable targets at nucleophilic residues. Based on the results, it was propose that coupling diverse fragments to this warhead would result in a library of sulfonyl fluoride bits (SuFBits), available for screening against protein targets. After in-depth characterization at the surrogate level, SuFBits was successfully applied in labelling of the KRasG12D oncogene mutant, where also was confirmed the functional consequences of the covalent binding. The study was performed by KINETO Lab and collaborative labs in the frame of KRAS Consortium.

The publication can be accessed under the following link.