Journal
CHEMICAL COMMUNICATIONS
Volume 53, Issue 26, Pages 3637-3640Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c7cc00667e
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Funding
- National Major Scientific and Technological Special Project for Significant New Drugs Development'' during the Twelfth Five-year Plan from the Chinese Ministry of Science and Technology [2013ZX0950910]
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We report the development of novel Mixed Lineage Kinase Domain-Like protein (MLKL) inhibitors with single nanomolar potency (compound 15 is also named as TC13172). Using the converting biochemistry to chemistry activity-based protein profiling (BTC-ABPP) method, we were able to determine that the inhibitors covalently bind to Cysteine86 (Cys-86) of MLKL. This is the first example of the use of LC-MS/MS to identify the binding site of an MLKL inhibitor. The novel MLKL inhibitors provide powerful tools to study the biological function of MLKL and demonstrate that MLKL should be viewed as a druggable target.
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