Molecular Target Synopsis
Domains and Structures
Drugs and Clinical Candidates
Ligand Efficiency Plot
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
Germline Genetics

ROCK1 (Q13464) - Overview - Molecular Target Synopsis


ROCK1, Rho-associated protein kinase 1
Enzyme Classification
UniProt Q13464

Also Known as ROCK1_HUMAN, ROCK1

Protein kinase which is a key regulator of actin cytoskeleton and cell polarity. Involved in regulation of smooth muscle contraction, actin cytoskeleton organization, stress fiber and focal adhesion formation, neurite retraction, cell adhesion and motility via phosphorylation of DAPK3, GFAP, LIMK1, LIMK2, MYL9/MLC2, PFN1 and PPP1R12A. Phosphorylates FHOD1 and acts synergistically with it to promote SRC-dependent non-apoptotic plasma membrane blebbing. Phosphorylates JIP3 and regulates the recruitment of JNK to JIP3 upon UVB-induced stress. Acts as a suppressor of inflammatory cell migration by regulating PTEN phosphorylation and stability. Acts as a negative regulator of VEGF-induced angiogenic endothelial cell activation. Required for centrosome positioning and centrosome-dependent exit from mitosis. Plays a role in terminal erythroid differentiation. May regulate closure of the eyelids and ventral body wall by inducing the assembly of actomyosin bundles. Promotes keratinocyte terminal differentiation. Involved in osteoblast compaction through the fibronectin fibrillogenesis cell-mediated matrix assembly process, essential for osteoblast mineralization. Homodimer. Interacts with RHOB, RHOC, MYLC2B and PTEN. Interacts with ITGB1BP1 (via N-terminus and PTB domain) (By similarity). Interacts with RHOA (activated by GTP), CHORDC1, DAPK3, GEM, JIP3, RHOE, PPP1R12A, PFN1, LIMK1, LIMK2 and TSG101. Interacts with FHOD1 in a Src-dependent manner.

Inspect Structure
See all 3D Structures for ROCK1

Isoforms / Transcripts (Protein Coding)

Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform

Sub-cellular localization

UniProt: ROCK1 is active in the following subcellular-locations: bleb, cell membrane, cell projection, centriole, centrosome, cytoplasm, cytoskeleton, golgi apparatus membrane, lamellipodium, microtubule organizing center, ruffle.
GO terms: ROCK1 is active in the following subcellular-locations: bleb, centriole, cytoplasm, cytoplasmic stress granule, cytoskeleton, cytosol, extracellular region, Golgi membrane, lamellipodium, plasma membrane, ruffle, secretory granule lumen.

GO terms

Gene Copy Number Variation

In COSMIC - Cell Lines Project ROCK1 has gain in 1 cell-lines, loss in 1 cell-lines and no signal in 956 cell-lines. (see details)

Gene Expression

In NCI60, the highest expressing cell lines are: HL_60, HS578T, SK_OV_3

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: SNU-398, NCI-H209, WSU-FSCCL

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: NHLF, HSMM, MCF-7

(see details)

RNA Interference

ROCK1 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: BXPC3, H23. (see details)

3D Structures

For ROCK1 there are:
27 structures (80 chains) solved
23 are solved in complex with at least one small molecule ligand

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry

ROCK1 has been screened with 2193 compounds (3163 bioactivities), 689 compounds have bioactivities that show binding affinity of <= 500nM (869 bioactivities). (see details)