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Target intelligence / Profile preview
Myosin Light-Chain Kinase (MLCK)
- Target
- MLCK
- Molecular classification
- Enzyme, Protein Kinase, Serine/Threonine-specific protein kinase
01
Overview
Myosin light-chain kinase (MLCK), also known as MYLK, is a serine/threonine-specific protein kinase that phosphorylates the regulatory light chain of myosin II. This phosphorylation event is crucial for the regulation of actin-myosin interactions and thus plays a central role in muscle contraction, cell motility, and various cellular processes. Abnormal expression or regulation of MLCK has been implicated in multiple diseases, including inflammatory diseases, respiratory diseases, cardiovascular diseases, and cancer progression/metastasis. Several isoforms exist with tissue-specific expression patterns.
- Other names
- MYLKmylkMYLK1MYLK2
02
Mechanism of action
Phosphorylates serine residue 19 on myosin regulatory light chains (RLCs), enabling myosin crossbridges to bind actin filaments and initiating contraction.
03
Biological functions
Smooth muscle contractionCell divisionCell migrationCell-matrix adhesionRegulation of actin-myosin interactionsRegulation of vascular tone
04
Disease associations
Inflammatory diseasesPancreatitisInflammatory bowel diseaseRespiratory diseasesAsthmaAirway hyperreactivityCardiovascular diseasesHypertensionVascular leakage syndromesCancerCancer progressionCancer metastasisCardiomyopathiesMuscular disorders
05
Safety considerations
Potential for off-target effects due to widespread expressionComplex regulation requiring careful consideration of downstream effectsInhibition can disrupt cellular processes beyond muscle contractionUpregulation involved in tumor cell migration and metastasis
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