Target intelligence / Profile preview

Rho-associated protein kinase

Molecular classification
Enzyme, AGC serine/threonine kinases
01

Overview

Rho-associated protein kinase (ROCK) is a serine/threonine-specific protein kinase that acts as a major downstream effector of the small GTPase RhoA. It plays a central role in regulating cytoskeletal dynamics, cell shape, motility, contraction, polarity, division, and gene expression. Dysregulation or overactivation of the Rho/ROCK pathway has been implicated in various diseases such as hypertension, glaucoma, and neurodegeneration. There are two main isoforms in mammals: ROCK1 and ROCK2.

Other names
RockP160ROCKROKα/βCoiled-coil-containing protein kinase
02

Mechanism of action

Pharmacological inhibition of ROCK, targeting either the ATP binding site or allosteric sites on one/both isoforms.

03

Biological functions

Smooth muscle contractionActin cytoskeleton organizationCell migration/motilityCell morphology/polarityCytokinesis/cell divisionNeurite retractionRegulation of vascular toneWound healingNeuronal development/regeneration
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Disease associations

Vasospasm/hypertensionPulmonary hypertensionGlaucomaNerve injury/neurodegenerationAtherosclerosis/inflammatory vascular disease
05

Interacting drugs

ROCK inhibitors

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