Single-plate kinome screening in live-cells to enable highly cost-efficient kinase inhibitor profiling.

SLAS Discov

Institute for Pharmaceutical Chemistry, Johann Wolfgang Goethe-University, Frankfurt am Main, Germany; Structural Genomics Consortium (SGC), Buchmann Institute for Life Sciences, Frankfurt am Main, Germany; German Cancer Consortium (DKTK)/German Cancer Research Center (DKFZ), DTKT Site Frankfurt-Mainz, Heidelberg, Germany.

Published: January 2025

Cancer research, cancer treatment, and the field of chemical biology are examples which heavily rely on the discovery of selective kinase inhibitors. While determining on-target potency is often feasible for most laboratories, the equally critical but frequently neglected selectivity screening remains less accessible to the broader scientific community. This limitation can stem from various factors, such as the unavailability of a large number of purified kinases or the costs associated with commercial screening systems. To address these challenges and enable a wider range of scientists, this protocol leverages a commercial kinome selectivity screen to facilitate a low-cost, two-day, single-plate selectivity screen against 192 kinases.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.slasd.2025.100214DOI Listing

Publication Analysis

Top Keywords

selectivity screen
8
single-plate kinome
4
kinome screening
4
screening live-cells
4
live-cells enable
4
enable highly
4
highly cost-efficient
4
cost-efficient kinase
4
kinase inhibitor
4
inhibitor profiling
4

Similar Publications

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!