Proteomics

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Novel proteolysis targeting chimera (PROTAC) selectively targeting Leucine Zipper-bearing Kinase (LZK) limits oncogenic potential of head and neck cancers.

ABSTRACT: Head and neck squamous cell carcinomas (HNSCC) are aggressive epithelial tumors with a low and unchanged 50% 5-year survival rate. MAP3K13 gene encoding Leucine Zipper-bearing Kinase (LZK) is often amplified in HNSCC patients and can be an oncogenic driver for tumorigenesis. In order to reduce catalytic and non-catalytic functions of LZK we synthetized novel, potent and selective degrader of LZK protein using proteolysis targeting chimera technology. We confirmed efficiency and specificity of our PROTAC by Liquid chromatography-mass spectrometry analysis.

INSTRUMENT(S):

ORGANISM(S): Homo Sapiens (human)

TISSUE(S): Head And Neck Squamous Cell Carcinoma Cell

SUBMITTER: Remigiusz Serwa  

LAB HEAD: John Brognard

PROVIDER: PXD054481 | Pride | 2026-02-16

REPOSITORIES: Pride

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Publications

The worldwide annual frequency and lethality of head and neck squamous cell carcinoma (HNSCC) is not improving, and thus, new therapeutic approaches are needed. Approximately 70% of HNSCC cases have either amplification or overexpression of <i>MAP3K13</i>, which encodes the kinase LZK. Here, we found that LZK is a therapeutic target in HNSCC and that small-molecule inhibition of its catalytic function decreased the viability of HNSCC cells with amplified <i>MAP3K13</i>. Inhibition of LZK suppres  ...[more]

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