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Target intelligence / Profile preview
LIM kinase 1 (LIMK1)
- Target
- LIMK1
- Molecular classification
- Enzyme, Protein Kinase, Serine/threonine kinase, Tyrosine kinase, Dual-specificity kinase, LIM Kinase subfamily
01
Overview
LIM kinase 1 (LIMK1) is a serine/threonine and tyrosine dual-specificity protein kinase that plays a critical role in regulating the actin cytoskeleton. By phosphorylating and inactivating ADF/cofilin family members, LIMK1 promotes F-actin stabilization, influencing cell shape, motility, and division. It is highly expressed in the brain and involved in neuronal development and synaptic maturation. LIMK1 is activated downstream of Rho GTPases, particularly by PAKs and ROCK, and its dysregulation is implicated in Williams syndrome and various cancers. Overexpression in cancer contributes to increased invasiveness and metastasis. Targeting LIMK1 is being explored as a potential therapeutic strategy, particularly in oncology.
02
Mechanism of action
Inhibition of LIMK1 leads to decreased phosphorylation of ADF/cofilins, promoting actin filament destabilization.
03
Biological functions
Actin cytoskeleton regulationCell shape regulationCell motilityCell divisionIntracellular transportSignal transductionNeuronal developmentSynaptic maturation
04
Disease associations
Williams syndromeCancerCardiovascular disorders
05
Safety considerations
Inhibition may affect normal actin dynamics in non-cancerous cells.Potential for off-target effects due to kinase family similarities.
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