Targeting Oncogenic Proteoforms Using Tyrosine-Reactive Chemistry

2021 Emerging Leader Award

Ku-Lung (Ken) Hsu, PhD, University of Virginia

Ku-Lung (Ken) Hsu, PhD

Dr. Hsu is developing a chemical technology that can selectively enrich, quantify, and pharmacologically target different molecular forms of oncogenic proteins based on their tyrosine phosphorylation (pTyr) state. This research is needed to complement large-scale patient sequencing initiatives — to understand and identify driver mutations that have biological and clinical importance. In this project, Dr. Hsu’s team is combining innovative chemical biology and proteomics approaches, including a covalent chemical probe platform developed in his lab known as SuTEx that is specific for tyrosines, to detect and selectively perturb low abundance pTyr sites on oncogenic proteins. This work aims to establish tyrosine mutational hotspots as a new target for development of cancer drugs and gain fundamental understanding of pTyr dysfunction in cancer signaling.

Dr. Hsu earned his PhD in Chemistry and Biochemistry from the University of Texas at Austin and completed his postdoctoral training at The Scripps Research Institute.


Grams RJ, Hsu KL. Reactive chemistry for covalent probe and therapeutic development. Trends Pharmacol Sci. 2022.

Ciancone AM, Hosseinibarkooie S, Bai DL, Borne AL, Ferris HA, Hsu KL. Global profiling identifies a stress-responsive tyrosine site on EDC3 regulating biomolecular condensate formation. Cell Chem Biol. 2022.